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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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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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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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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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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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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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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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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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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)

Bulk Inquiry Free Sample
- 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