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Raf inhibitor
Sorafenib Tosylate (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. , Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. , J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. , Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. , J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. , Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. , J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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VEGFR/PDGFR inhibitor
Linifanib (ABT-869) is a structurally novel, potent inhibitor of RTK, VEGF and PDGF with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGFR-β, KDR, and CSF-1R, respectively.
- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
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EGFR inhibitor
AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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VEGFR Inhibitor
Tivozanib (AV-951) is an oral VEGF receptor tyrosine kinase inhibitor that is designed to inhibit all three VEGF receptors.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 45954 PMID: 28383032
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 44075 PMID: 28287096
- Nicholas A. Manieri, .et al. , J Clin Invest, 2015, Sep 1; 125(9): 3606-3618 PMID: 26280574
- Usui T, .et al. , Acta Physiol (Oxf), 2014, 211, 385-394 PMID: 24612679
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VEGFR inhibitor
Axitinib is a small molecule tyrosine kinase inhibitor,which inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT (CD117).- Sophie J. Bakri, .et al. , PLoS One, 2024, 19(6): e0304782 PMID: 38833447
- Hongwan Ding, .et al. , Toxicol Appl Pharmacol, 2024, May:486:116950 PMID: 38701902
- Hongwan Ding, .et al. , Research Square, 2023, Dec 28
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Youcef M. Rustum, .et al. , Int J Mol Sci, 2018, Nov; 19(11): 3378 PMID: 30380599
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VEGFR inhibitor
BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR.- Yan Yang, .et al. , J Thorac Dis, 2024, Feb 29;16(2):1128-1140 PMID: 38505034
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Chun-Jung Chang, .et al. , Biochem Pharmacol, 2021, Jan;183:114356 PMID: 33285108
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c-Met inhibitor
BMS-794833 is a potent ATP competitive inhibitor to Met and VEGFR-2 with IC50 of 1.7 and 15 nmol. -
VEGFR inhibitor
Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling. -
VEGFR inhibitor
Cediranib (AZD2171) is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
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RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively. -
VEGFR inhibitor
Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.- Hasan U, .et al. , Research Square, 2023, 13 Apr
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. , Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. , Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. , Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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VEGFR-2 inhibitor
Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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VEGFR Inhibitor
E7080 is a multi-kinase inhibitor that inhibits both VEGFR2 and VEGFR3 kinases.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Mai Nakahara, .et al. , Biomed Rep, 2022, Aug 3;17(4):78 PMID: 36158319
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Keisuke Enomoto, .et al. , Cancers (Basel), 2021, Feb 18;13(4):862 PMID: 33670725
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Koide H, .et al. , Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Tomoko Ogawa-Morita, .et al. , Int J Anal Chem, 2017, 2017: 2341876 PMID: 28680445
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VEGFR-2 inhibitor
Ki8751 is a cell-permeable quinolyloxyphenyl-urea compound that acts as a Flk-1 (VEGFR-2)-selective inhibitior in both cell-based and cell-free assays.- Kohei Ashina, .et al. , Biochem Biophys Res Commun, 2015, Aug 21;464(2):590-5 PMID: 26163262
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c-Met inhibitor
MGCD265 is a multitargeted tyrosine kinase inhibitor that binds to and inhibits the phosphorylation of several RTKs, including the c-Met receptor (HGFR); the Tek/Tie-2 receptor; VEGFR types 1, 2, and 3; and MST1R. -
VEGFR inhibitor
Motesanib, also known as AMG-706, is an orally administered multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors, and Kit receptors. -
VEGFR/PDGFR/FGFR inhibitor
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Hideharu Yamada, .et al. , Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
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FGFR1/VEGFR2 Inhibitor
PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR.- Cheryl Q.E. Lee, .et al. , Stem Cell Reports, 2016, Feb 9; 6(2): 257-272 PMID: 26862703
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RAF/VEGFR Inhibitor
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. -
RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. -
RTK inhibitor
Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST).- Sophie J. Bakri, .et al. , PLoS One, 2024, 19(6): e0304782 PMID: 38833447
- Chern Ein Oon, .et al. , World J Gastrointest Oncol, 2023, May 15;15(5):810-827 PMID: 37275453
- Rachel K Toth, .et al. , Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. , Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
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VEGFR-2 Inhibitor
Taxifolin is found to bind at the ATP-binding site on VEGFR-2 kinase with large value of binding energy and act as type I competitive inhibitor.- Keji Yu, .et al. , Nat Commun, 2022, Jun 14;13(1):3425 PMID: 35701431
- Shinji Kondo, .et al. , Curr Issues Mol Biol, 2021, Sep 26;43(3):1293-1306 PMID: 34698101
- Shin-ichi Adachi, .et al. , Cytotechnology, 2017, Apr; 69(2): 329-336 PMID: 28101741
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VEGFR-2 inhibitor
Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. -
VEGFR inhibitor
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Shinya Kitamura, .et al. , Biochem Biophys Res Commun, 2020, Aug 13 PMID: 32800552
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Rintaro Sogawa, .et al. , JPA, 2018, in Press PMID: 30740257
- Park K, .et al. , Anat Sci Int, 2018, Jun;93(3):372-383 PMID: 29256114
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Park K, .et al. , Biomed Pharmacother, 2016, Mar;78:140-149 PMID: 26898435
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VEGFR inhibitor
Vatalanib (PTK787 or PTK/ZK) is a small molecule protein kinase inhibitor that inhibits angiogenesis that inhibits all known VEGF receptors, as well as platelet-derived growth factor receptor-beta and c-kit, but is most selective for VEGFR-2. CAS: 212141-51-0 (HCl) 212141-54-3 (Free base)- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
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VEGFR inhibitor
XL184 free base (Cabozantinib) is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Jhe-Cyuan Guo, .et al. , Journal of Clinical Oncology, 2024, May 29
- Feyza Oflaz, .et al. , Cumhuriyet Sci. J., 2023, 44(4): 650-655
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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c-MET inhibitor
Foretinib (GSK1363089), a multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces Anoikis, and impairs ovarian cancer metastasis.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Narges K Gortany, .et al. , Cancer Chemother Pharmacol, 2021, Mar 10 PMID: 33688998
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Hayato Ogura, .et al. , Sci Rep, 2017, 7: 5519 PMID: 28717217
- Fuse MJ, .et al. , Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
- Ryohei Katayama, .et al. , Clin Cancer Res, 2015, Jan 1; 21(1): 166-174 PMID: 25351743
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EGFR, HER2 and VEGFR inhibitor
XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4. -
VEGFR/EGFR Inhibitor
BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases. -
multiple receptor tyrosine kinases inhibitor
Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
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c-Met/VEGFR-2 inhibitor
E7050 (also known as golvatinib is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. -
VEGFR inhibitor
Apatinib (YN968D1) is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR) that inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue.- Wonjin Park, .et al. , Biomed Pharmacother, 2021, Feb;134:111110 PMID: 33338749
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 45954 PMID: 28383032
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RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.- Yunping Hu, .et al. , Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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M-CSFR, CSF1R inhibitor
Ki 20227 is an inhibitor of c-Fms tyrosine kinase (M-CSFR, CSF1R).- Wensheng Wang, .et al. , J Bone Miner Res, 2017, May; 32(5): 939-950 PMID: 28052488
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VEGFR Inhibitor
Motesanib (AMG706) is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors with IC?? values of 2 nM (VEGFR1), 3 nM (VEGFR2), 6 nM (VEGFR3), 84 nM (PDGFR), and 8 nM (Kit).- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
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VEGFR inhibitor
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.- Koide H, .et al. , Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. , Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. -
multi-targeted receptor tyrosine kinases inhibitor
SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT. -
VEGFR/FGFR/EGFR inhibitor?€?
SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively). -
c-Kit, PDGFR, VEGFR inhibitor
Toceranib is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.- Masaya Igase, .et al. , Can J Vet Res, 2016, Jan; 80(1): 21-31 PMID: 26733729
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VEGFR Antagonist
Buflomedil is a vasoactive agent used to treat peripheral vascular disease. -
VEGFR Inhibitor
ZM 323881 is a potent and selective inhibitor of the kinase activity of the human vascular endothelial growth factor receptor 2 (VEGFR2/KDR).