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搜索结果：“EGFR”

“EGFR”的搜索结果

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Regorafenib (BAY 73-4506)

Catalog No. A10250
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VEGFR 抑制剂

Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。了解更多

Product Citations (9)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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Vandetanib (ZD6474)

Catalog No. A10963
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VEGFR 抑制剂

Vandetanib (ZD6474)是一种VEGFR和EGFR拮抗剂，是一种酪氨酸激酶抑制剂，对于HUVEC增殖，PC-9细胞和酪氨酸激酶活性，IC50为60、90、40 nM。了解更多

Product Citations (9)

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Shinya Kitamura, .et al. Vandetanib inhibits cell growth in EGFR-expressing cutaneous squamous cell carcinoma, Biochem Biophys Res Commun, 2020, Aug 13 PMID: 32800552
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Rintaro Sogawa, .et al. Development of a competitive enzyme-linked immunosorbent assay for therapeutic drug monitoring of afatinib, JPA, 2018, in Press PMID: 30740257
- Park K, .et al. Vascular endothelial growth factor receptor 1 (VEGFR1) tyrosine kinase signaling facilitates granulation tissue formation with recruitment of VEGFR1+ cells from bone marrow, Anat Sci Int, 2018, Jun;93(3):372-383 PMID: 29256114
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Park K, .et al. Vascular endothelial growth factor receptor-1 (VEGFR-1) signaling enhances angiogenesis in a surgical sponge model, Biomed Pharmacother, 2016, Mar;78:140-149 PMID: 26898435
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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。了解更多

Product Citations (12)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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Axitinib

Catalog No. A10103
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VEGFR 抑制剂

Axitinib是一种小分子酪氨酸激酶抑制剂，可抑制多种靶标，包括VEGFR-1，VEGFR-2，VEGFR-3，血小板衍生生长因子受体（PDGFR）和cKIT（CD117）。了解更多

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- Youcef M. Rustum, .et al. Non-Coding Micro RNAs and Hypoxia-Inducible Factors Are Selenium Targets for Development of a Mechanism-Based Combination Strategy in Clear-Cell Renal Cell Carcinoma-Bench-to-Bedside Therapy, Int J Mol Sci, 2018, Nov; 19(11): 3378 PMID: 30380599
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XL184 free base (Cabozantinib)

Catalog No. A10996
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VEGFR 抑制剂

XL184 free base (Cabozantinib)是设计用来抑制多种受体酪氨酸激酶（特别是MET和VEGFR2）的小分子。了解更多

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- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Canertinib (CI-1033)

Catalog No. A10211
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HER2/ErbB2 抑制剂

Canertinib (CI-1033)是一种不可逆的酪氨酸激酶抑制剂，对EGFR（IC50 0.8 nM），HER-2（IC50 19 nM）和ErbB-4（IC50 7 nM）具有活性。了解更多

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- Fukuda N, .et al. Rapid Evaluation of Tyrosine Kinase Activity of Membrane Integrated Human Epidermal Growth Factor Receptor Using the Yeast Gγ Recruitment System, ACS Synth Biol., 2015, 4(4):421-9 PMID: 25006755
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Dovitinib (TKI-258)

Catalog No. A11411
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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Foretinib (GSK1363089, XL880)

Catalog No. A10998
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c-MET 抑制剂

Foretinib (GSK1363089,XL880)是c-Met和VEGFR-2的多激酶抑制剂，可抑制增殖，诱导Anoikis并损害卵巢癌转移。了解更多

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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Hayato Ogura, .et al. TKI-addicted ROS1-rearranged cells are destined to survival or death by the intensity of ROS1 kinase activity, Sci Rep, 2017, 7: 5519 PMID: 28717217
- Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
- Ryohei Katayama, .et al. Cabozantinib overcomes crizotinib resistance in ROS1 fusion positive cancer, Clin Cancer Res. , 2015, Jan 1; 21(1): 166–174. PMID: 25351743
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PCI-32765 (Ibrutinib)

Catalog No. A11020
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Bruton tyrosine kinase 抑制剂

PCI-32765 (Ibrutinib)是Bruton酪氨酸激酶（BTK）的口服生物利用小分子抑制剂，具有潜在的抗肿瘤活性。对Bmx，CSK，FGR，BRK及HCK适度有效，对EGFR，Yes，ErbB2，JAK3等作用效果较弱。了解更多

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- Simonowski A, .et al. Differential use of BTK and PLC in FcεRI- and KIT-mediated mast cell activation: A marginal role of BTK upon KIT activation, Biochim Biophys Acta Mol Cell Res, 2019, Dec 11;1867(4):118622 PMID: 31837347
- Carolin N. Zorn, .et al. Stimulus strength determines the BTK-dependence of the SHIP1-deficient phenotype in IgE/antigen-triggered mast cells, Sci Rep, 2018, 8: 15467 PMID: 30341350
- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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AP24534 (Ponatinib)

Catalog No. A10080
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BCR-ABL 抑制剂

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Cediranib (AZD2171)

Catalog No. A10185
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VEGFR 抑制剂

Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍和1000倍以上。了解更多

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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RAF265 (CHIR-265)

Catalog No. A10773
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RAF/VEGFR 抑制剂

RAF265 (CHIR-265)是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，可控制或正常化VEGFR-2，同时抑制B-raf和c-Raf突变以预防癌症。了解更多

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Tivozanib (AV-951)

Catalog No. A10101
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VEGFR 抑制剂

Tivozanib (AV-951)是一种口服VEGF受体酪氨酸激酶抑制剂，旨在抑制所有三种VEGF受体。了解更多

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Majid Momeny, .et al. Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells, Sci Rep, 2017, 7: 45954 PMID: 28383032
- Majid Momeny, .et al. Blockade of vascular endothelial growth factor receptors by tivozanib has potential anti-tumour effects on human glioblastoma cells, Sci Rep, 2017, 7: 44075 PMID: 28287096
- Nicholas A. Manieri, .et al. Mucosally transplanted mesenchymal stem cells stimulate intestinal healing by promoting angiogenesis, J Clin Invest, 2015, Sep 1; 125(9): 3606-3618 PMID: 26280574
- Usui T, .et al. Brain-derived neurotrophic factor promotes angiogenic tube formation through generation of oxidative stress in human vascular endothelial cells., Acta Physiol (Oxf), 2014, 211, 385-394 PMID: 24612679
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Danusertib (PHA-739358)

Catalog No. A10715
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Aurora 抑制剂

Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力对Lck，VEGFR2/3，c-Kit，CDK2等有效。了解更多

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- Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.
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Bibf1120 (Nintedanib)

Catalog No. A10137
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VEGFR 抑制剂

Bibf1120 (Nintedanib)是一种新型的三联血管激酶抑制剂，可同时抑制三种生长因子受体：VEGFR，PDGF和FGFR。了解更多

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Chun-Jung Chang, .et al. Overcoming interferon (IFN)-γ resistance ameliorates transforming growth factor (TGF)-β-mediated lung fibroblast-to-myofibroblast transition and bleomycin-induced pulmonary fibrosis, Biochem Pharmacol, 2021, Jan;183:114356 PMID: 33285108
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MGCD-265 (Glesatinib)

Catalog No. A10587
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c-Met 抑制剂

MGCD-265 (Glesatinib)是一种多靶酪氨酸激酶抑制剂，可与多种RTK（包括c-Met受体（HGFR）结合并抑制其磷酸化。Tek/Tie-2受体；VEGFR类型1、2和3；和MST1R。了解更多

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PD173074

Catalog No. A10703
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FGFR1/VEGFR2 抑制剂

PD173074是有效的，细胞可渗透的和ATP竞争性的FGFR和VEGFR抑制剂。了解更多

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- Cheryl Q.E. Lee, .et al. What Is Trophoblast? A Combination of Criteria Define Human First-Trimester Trophoblast, Stem Cell Reports, 2016, Feb 9; 6(2): 257-272 PMID: 26862703
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TSU-68 (Orantinib, SU6668)

Catalog No. A10953
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PDFGRβ 抑制剂

TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2；不抑制EGFR。了解更多

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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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Brivanib (BMS-540215)

Catalog No. A10254
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VEGFR-2 抑制剂

Brivanib (BMS-540215)是一种VEGFR-2抑制剂，IC50为25 nM，Ki为26 nM。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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Brivanib alaninate (BMS-582664)

Catalog No. A10162
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VEGFR 抑制剂

Brivanib alaninate (BMS-582664)是VEGFR和FGFR信号转导的双重酪氨酸激酶抑制剂。了解更多

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BMS-794833

Catalog No. A10154
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c-Met 抑制剂

BMS-794833是Met和VEGFR-2的有效ATP竞争性抑制剂，IC50为1.7和15 nM。了解更多

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AMG-458

Catalog No. A11055
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c-Met 抑制剂

AMG-458是一种有效的c-Met抑制剂，IC50值为60nM，对VEGFR2具有选择性。了解更多

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Linifanib (ABT-869)

Catalog No. A10025
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VEGFR/PDGFR 抑制剂

Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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Vatalanib (PTK787) 2HCl

Catalog No. A10967
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VEGFR 抑制剂

Vatalanib (PTK787) 2HCl是一种小分子蛋白激酶抑制剂，可抑制抑制所有已知VEGF受体以及血小板衍生的生长因子受体β和c-kit的血管生成，但对VEGFR-2的选择性最高。了解更多

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Dasatinib (BMS-354825)

Catalog No. A10290
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Abl-Src 抑制剂

Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL，Src，c-Kit，ephrin受体和其他几种酪氨酸激酶，但不是erbB激酶，例如EGFR或Her2。了解更多

Product Citations (10)

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- Chihiro Motozono, .et al. The SARS-CoV-2 Omicron BA.1 spike G446S mutation potentiates antiviral T-cell recognition, Nat Commun, 2022, Sep 21;13(1):5440 PMID: 36130929
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- David E J Klawon, .et al. Altered selection on a single self-ligand promotes susceptibility to organ-specific T cell infiltration, J Exp Med, 2021, Jun 7;218(6) PMID: 33914024
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Sano T, .et al. Gliding Basal Cell Migration of the Urothelium during Wound Healing, Am J Pathol, 2018, Nov;188(11):2564-2573 PMID: 30121259
- Ines Peschel, .et al. FLT3 and FLT3-ITD phosphorylate and inactivate the cyclin-dependent kinase inhibitor p27Kip1 in acute myeloid leukemia, Haematologica, 2017, Aug; 102(8): 1378-1389 PMID: 28522571
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- John D. Leonard, .et al. Identification of natural regulatory T cell epitopes reveals convergence on a dominant autoantigen, Immunity, 2017, Jul 18; 47(1): 107-117.e8 PMID: 28709804
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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ENMD-2076

Catalog No. A10352
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Aurora A / FLT3 抑制剂

ENMD-2076具有针对Aurora A和Flt3的选择性活性，IC50为14 nM和1.86 nM，对Aurora A的选择性是Aurora B的25倍，对VEGFR2/KDR和VEGFR3，FGFR1和FGFR2和PDGFRα的作用较小。阶段2。了解更多

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Taxifolin

Catalog No. A10893
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VEGFR-2 抑制剂

Taxifolin以很大的结合能值结合在VEGFR-2激酶的ATP结合位点上，并起I型竞争性抑制剂的作用。了解更多

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- Keji Yu, .et al. A role for ascorbate conjugates of (+)-catechin in proanthocyanidin polymerization, Nat Commun, 2022, Jun 14;13(1):3425 PMID: 35701431
- Shinji Kondo, .et al. Antidiabetic Effect of Taxifolin in Cultured L6 Myotubes and Type 2 Diabetic Model KK-Ay/Ta Mice with Hyperglycemia and Hyperuricemia, Curr Issues Mol Biol, 2021, Sep 26;43(3):1293-1306 PMID: 34698101
- Shin-ichi Adachi, .et al. Anti-hyperuricemic effect of taxifolin in cultured hepatocytes and model mice, Cytotechnology, 2017, Apr; 69(2): 329-336 PMID: 28101741
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ARQ 197 (Tivantinib)

Catalog No. A11087
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c-Met 抑制剂

ARQ-197是c-Met受体酪氨酸激酶的选择性抑制剂, 在无细胞试验中Ki为0.355 μM，对Ron几乎没有作用活性，对EGFR， InsR， PDGFRα和FGFR1/4没有抑制作用。了解更多

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- Wang L, .et al. Bispecific Aptamer Induced Artificial Protein-Pairing: A Strategy for Selective Inhibition of Receptor Function, J Am Chem Soc, 2019, Aug 14;141(32):12673-12681 PMID: 31381313
- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
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Mubritinib (TAK 165)

Catalog No. A10612
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HER2/ErbB2 抑制剂

Mubritinib (TAK 165)是一种有效的EGFR和p34cdc2抑制剂，IC50分别为6 nM和0.2 ?M。Mubritinib（TAK 165）也抑制p33cdk2和p33cdk5。了解更多

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Raf265 derivative

Catalog No. A10774
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RAF/VEGFR 抑制剂

Raf265 derivative是Raf265的衍生物，Raf265是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，IC50为5至10μM。了解更多

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Telatinib (BAY 57-9352)

Catalog No. A10903
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VEGFR-2 抑制剂

Telatinib (BAY 57-9352)是一种口服的血管内皮生长因子受体2和3（VEGFR2/3）和血小板衍生的生长因子受体β酪氨酸激酶的小分子抑制剂，IC50分别为6 nM/4 nM，1 nM和15 nM。了解更多

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Apatinib (YN968D1)

Catalog No. A11407
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VEGFR 抑制剂

Apatinib (YN968D1)是一种酪氨酸激酶抑制剂，可选择性抑制血管内皮生长因子受体2（VEGFR2，也称为KDR），后者可抑制VEGF介导的内皮细胞迁移和增殖，从而阻止肿瘤组织中新血管的形成。了解更多

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- Wonjin Park, .et al. Human plasminogen-derived N-acetyl-Arg-Leu-Tyr-Glu antagonizes VEGFR-2 to prevent blood-retinal barrier breakdown in diabetic mice, Biomed Pharmacother, 2021, Feb;134:111110 PMID: 33338749
- Majid Momeny, .et al. Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells, Sci Rep, 2017, 7: 45954 PMID: 28383032
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PP121

Catalog No. A11207
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PI3K 抑制剂

PP121是一种作用于PDGFR，Hck，mTOR，VEGFR2，Src和Abl的多靶点抑制剂，IC50分别为2 nM，8 nM，10 nM，12 nM，14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。了解更多

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Motesanib Diphosphate (AMG-706)

Catalog No. A10608
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VEGFR 抑制剂

Motesanib也称为AMG-706，是一种有效的ATP竞争性的VEGFR1/2/3抑制剂，IC50分别为2 nM/3 nM/6 nM；对Kit具有相似的抑制活性，对VEGFR选择性比PDGFR和Ret高10倍。了解更多

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OSI-930

Catalog No. A10679
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c-Kit/VEGFR 抑制剂

OSI-930是Kit，KDR，Flt，CSF-1R，c-Raf和Lck的有效抑制剂，IC50分别为80 nM，9 nM，8 nM，15 nM，41 nM和22 nM。了解更多

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Pazopanib HCl (GW786034)

Catalog No. A10699
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VEGFR/PDGFR/FGFR 抑制剂

Pazopanib HCl (GW786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Hideharu Yamada, .et al. lncRNA HAR1B has potential to be a predictive marker for pazopanib therapy in patients with sarcoma, Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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PHA-680632

Catalog No. A10714
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Aurora 抑制剂

PHA-680632是Aurora A，Aurora B和Aurora C的有效抑制剂，IC50分别为27 nM，135 nM和120 nM。对于FGFR1，FLT3，LCK，PLK1，STLK2和VEGFR2/3，它的IC50高10到200倍。了解更多

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Sunitinib Malate

Catalog No. A10880
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RTK inhibitor

Sunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，也会抑制c-Kit的活性。用于治疗肾细胞癌（RCC）和伊马替尼耐药的胃肠道间质瘤（GIST）。了解更多

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- Rachel K Toth, .et al. Stabilization of PIM Kinases in Hypoxia Is Mediated by the Deubiquitinase USP28, Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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Dovitinib Dilactic acid (TKI258 Dilactic acid)

Catalog No. A10198
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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INCB28060

Catalog No. A11132
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c-MET 抑制剂

INCB28060 (Capmatinib )是一种新型的，ATP竞争性c-MET抑制剂，无细胞试验中IC50为0.13 nM，对RONβ，EGFR和HER-3无活性。了解更多

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- Wei Deying,etc. CAF-derived HGF promotes cell proliferation and drug resistance by up-regulating the c-Met/PI3K/Akt and GRP78 signalling in ovarian cancer cells. Biosci Rep. 2017 Apr 30; 37(2): BSR20160470.
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CYC116 (CYC-116)

Catalog No. A10248
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Aurora Kinase 抑制剂

CYC116 (CYC-116)是一种有效的Aurora A/B抑制剂，Ki为8.0 nM/9.2 nM，对VEGFR2(Ki为44 nM)作用稍弱。了解更多

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E7080 (Lenvatinib)

Catalog No. A10340
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VEGFR 抑制剂

E7080 (Lenvatinib)是一种多激酶抑制剂，可同时抑制VEGFR2和VEGFR3激酶。了解更多

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- Mai Nakahara, .et al. Effect of Lenvatinib treatment on the cell cycle and microRNA profile in hepatocellular carcinoma cells, Biomed Rep, 2022, Aug 3;17(4):78 PMID: 36158319
- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Keisuke Enomoto, .et al. Synergistic Effects of Lenvatinib (E7080) and MEK Inhibitors against Anaplastic Thyroid Cancer in Preclinical Models, Cancers (Basel), 2021, Feb 18;13(4):862 PMID: 33670725
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Tomoko Ogawa-Morita, .et al. Validation of a Liquid Chromatography-Tandem Mass Spectrometric Assay for Quantitative Analysis of Lenvatinib in Human Plasma, Int J Anal Chem, 2017, 2017: 2341876 PMID: 28680445
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Ki8751

Catalog No. A10502
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VEGFR-2 抑制剂

ki8751是一种细胞可渗透的喹啉氧基苯基脲化合物，在基于细胞和无细胞的检测中起Flk-1 (VEGFR-2)选择性抑制剂的作用。了解更多

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- Kohei Ashina, .et al. VEGF-induced blood flow increase causes vascular hyper-permeability in vivo, Biochem Biophys Res Commun, 2015, Aug 21;464(2):590-5 PMID: 26163262
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KRN 633

Catalog No. A10504
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VEGFR 抑制剂

KRN 633是一种细胞可渗透、可逆、ATP竞争性VEGFR激酶抑制剂，仅在较高浓度下(IC50 = 0.97 μM和4.33 μM)抑制PDGFR-α和C-Kit，对其他17种激酶无活性(IC50 ≥ 10 μM)。了解更多

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Lapatinib (free base)

Catalog No. A11752
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Lapatinib (free base)是一种双重酪氨酸激酶抑制剂，是一种有效的EGFR和ErbB2抑制剂，在无细胞试验中IC50分别为10.2和9.8 nM。可阻断HER2生长受体途径。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
- Tetsuya Saita, .et al. Preparation of Antibodies and Development of an Enzyme-Linked Immunosorbent Assay for the Tyrosine Kinase Inhibitors Lapatinib and Nilotinib., Biol Pharm Bull. , 2015, 38(10):1652-7 PMID: 26424026
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NVP-BAG956

Catalog No. A11511
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PI3K/PDK-1 抑制剂

NVP-BAG956是一种强效、可逆和ATP竞争性PI3-K/PDK1双激酶抑制剂，对VEGFR 1(IC50 = 2.56 μM)的效力大大降低，对其他15种激酶(IC50 > 10 uM)的活性很小或没有活性。了解更多

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Pazopanib (GW-786034)

Catalog No. A11518
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VEGFR 抑制剂

Pazopanib (GW-786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。了解更多

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- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Buflomedil HCl

Catalog No. A11737
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VEGFR 拮抗剂

Buflomedil HCl是一种用于治疗外周血管疾病的血管活性剂。了解更多

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ZM 323881 hydrochloride

Catalog No. A11954
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VEGFR 抑制剂

ZM 323881 hydrochloride是一种有效且选择性的人血管内皮生长因子受体2（VEGFR2/KDR）激酶活性抑制剂。了解更多

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ZM 306416

Catalog No. A11955
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VEGFR 抑制剂

ZM 306416 hydrochloride是一种VEGF受体酪氨酸激酶抑制剂，可抑制KDR（IC50 = 100 nM）和Flt（IC50 = 2 uM）酪氨酸激酶。了解更多

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