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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 |
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| Conbercept
Conbercept (KH902) is a monoclonal antibody targeting VEGFRA fused to the IGHG1 Fc fragment. Conbercept is produced by the fusion of the second C-LIKE of FLT1 and the third and fourth C-LIKE of KDR with IGHG1 Fc. |
| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
| VEGFR-IN-1
VEGFR-IN-1 is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively. |
| (Z)-Orantinib
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. |
| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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