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Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Ki8751 suppressed the growth of the VEGF-stimulated human umbilical vein endothelial cell (HUVEC) and inhibits tumor growth in vivo. Ki8751 also inhibited the PDGFR family members such as PDGFRalpha and c-Kit at 67 nM and 40 nM, respectively. Ki8751 (10 nM) increases cellular senescence in metastatic colorectal cancer (CRC) cells MIP, RKO, SW620 and SW480. Ki8751 showed significant antitumor activity against five human tumor xenografts such as GL07 (glioma), St-4 (stomach carcinoma), LC6 (lung carcinoma), DLD-1 (colon carcinoma) and A375 (melanoma) in nude mice. Ki8751 also showed complete tumor growth inhibition with the LC-6 xenograft in nude rats following oral administration once a day for 14 days at 5 mg/kg without any body weight loss.
| Molecular Weight | 469.41 |
| Formula | C24H18F3N3O4 |
| CAS Number | 228559-41-9 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
|---|
| ABT-869
ABT-869 (Linifanib) is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of VEGFR and PDGFR. |
| Tivozanib (AV-951)
Tivozanib (AV-951) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively. |
| Axitinib
Axitinib (AG013736) inhibits multiple targets including VEGFR, PDGFR and cKit. |
| Regorafenib
Regorafenib (BAY 73-4506) is a novel oral multikinase inhibitor of c-KIT, VEGFR2, B-Raf with IC50s of 17, 40 and 69 nM respectively. |
| Nintedanib
Nintedanib (BIBF1120) is a novel, potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively. |
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