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搜索结果：“EGFR”

“EGFR”的搜索结果

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PF299804 (Dacomitinib, PF299)

Catalog No. A11051
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EGFR 抑制剂

PF299804是一种有效的，可口服的酪氨酸激酶人表皮生长因子受体（HER）1（EGFR），HER2和HER4不可逆抑制剂。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
- 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
- Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
- 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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AG-490

Catalog No. A10047
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EGFR 抑制剂

AG 490是EGF受体酪氨酸激酶的选择性抑制剂 (EGFR和ErbB2的IC50值分别为2和13.5μM)。也抑制对Lck，Lyn，Btk，Syk和Src无活性的JAK2。了解更多

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- Matozaki M, .et al. Involvement of Stat3 phosphorylation in mild heat shock-induced thermotolerance, Exp Cell Res, 2019, Feb 15. pii: S0014-4827(18)31030-9 PMID: 30776355
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Gefitinib (Iressa)

Catalog No. A10422
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EGFR 抑制剂

Gefitinib (Iressa)是一种EGFR抑制剂，可阻断靶细胞中表皮生长因子受体(EGFR)的信号传导。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
- Mansi Srivastava, .et al. Inhibition of the TIRAP-c-Jun interaction as a therapeutic strategy for AP1-mediated inflammatory responses, Int Immunopharmacol, 2019, 71: 188-197 PMID: 30909134
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BIBW2992 (Afatinib)

Catalog No. A10141
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EGFR 抑制剂

BIBW2992 (Afatinib)是酪氨酸激酶抑制剂（TKI），它不可逆地抑制人表皮生长因子受体2（Her2）和表皮生长因子受体（EGFR）激酶。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
- Van Sebille YZ, .et al. Use of zebrafish to model chemotherapy and targeted therapy gastrointestinal toxicity, Exp Biol Med (Maywood), 2019, Jun 11:1535370219855334 PMID: 31184924
- 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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AG-17

Catalog No. A11949
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EGFR 抑制剂

AG-17是人表皮样癌细胞系A431中EGFR激酶的抑制剂，IC50值为460 μM，作用于PDGFR更有效，IC50值为0.5μM。了解更多

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AST-6

Catalog No. A10062
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EGFR 抑制剂

AST-6是表皮生长因子受体1和2的新型不可逆抑制剂，可在体内外抑制肿瘤生长。了解更多

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TAK-285

Catalog No. A11236
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HER2/EGFR 抑制剂

TAK-285是一种研究性的HER2/EGFR抑制剂，可在具有完整血脑屏障 (BBB) 的大鼠中穿透CNS。TAK-285对HER2和EGFR激酶具有抑制活性，HER2和EGFR的IC50值分别为17 nmol/L (95％CI 12-24)和23 nmol/L (95％CI 18-30)。了解更多

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Daphnetin

Catalog No. A10286
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EGFR, PKA,PKC 抑制剂

Daphnetin是一种香豆素类似物，可作为几种蛋白激酶的抑制剂。它在体外抑制EGFR激酶（IC50 = 7.67 ?M），PKA（IC50 = 9.33 ?M）和PKC（IC50 = 25 ?M）。蜂胶对EGFR激酶的抑制作用与ATP竞争，对肽底物没有竞争性。还可以用作有效的抗氧化剂和抗疟疾剂。了解更多

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OSI-906

Catalog No. A11053
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IGF-1R 抑制剂

OSI-906是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。了解更多

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- Masao Kakoki, .et al. Cyanocobalamin prevents cardiomyopathy in type 1 diabetes by modulating oxidative stress and DNMT-SOCS1/3-IGF-1 signaling, Communications Biology, 2021, 4:775
- Nakamura T, .et al. Naturally Occurring Hair Growth Peptide: Water-Soluble Chicken Egg Yolk Peptides Stimulate Hair Growth Through Induction of Vascular Endothelial Growth Factor Production, J Med Food, 2018, Jul;21(7):701-708 PMID: 29583066
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Takata N, .et al. IGF-2/IGF-1R signaling has distinct effects on Sox1, Irx3, and Six3 expressions during ES cell derived-neuroectoderm development in vitro, In Vitro Cell Dev Biol Anim., 2016, May;52(5):607-15 PMID: 26956358
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AEE788

Catalog No. A10043
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EGFR 抑制剂

AEE788是一种口服生物可用的多受体酪氨酸激酶抑制剂，可抑制EGFR，HER2和VEGF2酪氨酸激酶的磷酸化。了解更多

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BMS 599626 (AC480)

Catalog No. A11209
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EGFR 抑制剂

BMS 599626 (AC480)是一种选择性的，高效效的HER1，HER2和HER4酪氨酸激酶抑制剂（IC50分别为22、32和190 nM），具有潜在的抗肿瘤活性。了解更多

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WZ3146

Catalog No. A10990
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EGFR 抑制剂

WZ3146是EGFR受体激酶突变体的抑制剂，该突变体在活性位点网守残基（T790M）中带有突变，并且对野生型EGFR激酶的效力要低得多。了解更多

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WZ8040

Catalog No. A10992
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EGFR 抑制剂

WZ8040是一种新型的EGFR抑制剂，可抑制含有EGFR-T790M的细胞系的生长并抑制EGFR磷酸化。了解更多

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CUDC-101

Catalog No. A10246
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HDAC 抑制剂

CUDC-101是一种抑制多种靶标的新型化合物，旨在抑制HDAC，EGFR和Her2。了解更多

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OSI-420

Catalog No. A10678
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EGFR 抑制剂

OSI-420 (Desmethyl Erlotinib,CP-473420)是一种口服活性EGFR酪氨酸激酶抑制剂，可通过抑制细胞间结构域来抑制受体酪氨酸激酶（TKs）。了解更多

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- Yuta Yamamoto, .et al. Quantitative determination of erlotinib in human serum using competitive enzyme-linked immunosorbent assay, J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Janet L. Martin, .et al. Inhibition of basal-like breast cancer growth by FTY720 in combination with epidermal growth factor receptor kinase blockade, Breast Cancer Res, 2017, 19: 90 PMID: 28778177
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AG-1478 (Tyrphostin AG-1478)

Catalog No. A11022
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EGFR 抑制剂

AG-1478 (Tyrphostin AG-1478)是EGFR激酶的抑制剂，IC50值为3 nM。了解更多

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- Khattab M, .et al. Conformational Plasticity in Tyrosine Kinase Inhibitor-Kinase Interactions Revealed with Fluorescence Spectroscopy and Theoretical Calculations, J Phys Chem B, 2018, May 3;122(17):4667-4679 PMID: 29629773
- Muhammad Khattab, .et al. A pH-induced conformational switch in a tyrosine kinase inhibitor identified by electronic spectroscopy and quantum chemical calculations, Sci Rep, 2017, 7: 16271 PMID: 29176733
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WZ4002

Catalog No. A10991
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EGFR 抑制剂

WZ4002是一种新型的，突变选择性EGFR抑制剂，作用于EGFR(L858R)/(T790M)，在BaF3细胞系中IC50为2 nM/8 nM；对ERBB2磷酸化(T798I)没有抑制作用。了解更多

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AZD8931 (Sapitinib)

Catalog No. A10116
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pan-EGFR/pan-erbB 抑制剂

AZD8931 (Sapitinib)是ErbB1，ErbB2和ErbB3受体信号传导的等效抑制剂。了解更多

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- Takeshi Ito, .et al. Mathematical analysis of gefitinib resistance of lung adenocarcinoma caused by MET amplification, Biochem Biophys Res Commun, 2019, in Press
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Pelitinib (EKB-569)

Catalog No. A10706
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EGFR 抑制剂

Pelitinib (EKB-569)是一种有效的,不可逆EGFR抑制剂,IC50为38.5 nM 了解更多

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- Shi P, .et al. The Third-Generation EGFR Inhibitor, Osimertinib, Promotes c-FLIP Degradation, Enhancing Apoptosis Including TRAIL-Induced Apoptosis in NSCLC Cells with Activating EGFR Mutations, Transl Oncol, 2019, Mar 8;12(5):705-713 PMID: 30856555
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Motesanib (AMG706)

Catalog No. A11496
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VEGFR 抑制剂

Motesanib(AMG706)是一种多激酶抑制剂，可选择性靶向VEGF受体，血小板衍生的生长因子受体（PDGFRs）和Kit受体，并带有IC50受体。值分别为2 nM（VEGFR1），3 nM（VEGFR2），6 nM（VEGFR3），84 nM（PDGFR）和8 nM（Kit）。了解更多

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- Angela Coxon,etc. Antitumor activity of motesanib alone and in combination with cisplatin or docetaxel in multiple human non–small-cell lung cancer xenograft models. Mol Cancer. 2012; 11: 70.
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E-7050 (Golvatinib)

Catalog No. A11396
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E-7050 (Golvatinib)是具有潜在抗肿瘤活性的c-Met(肝细胞生长因子受体)和VEGFR-2(血管内皮生长因子受体-2)酪氨酸激酶的口服生物可利用双重激酶抑制剂。了解更多

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LY 2874455

Catalog No. A11244
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FGFR/VEGFR2 抑制剂

LY2874455是一种新型有效的FGFR / VEGFR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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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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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

Product Citations (3)

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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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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

Product Citations (7)

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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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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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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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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

Product Citations (8)

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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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

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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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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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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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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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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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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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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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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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