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CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 28 € | In Stock | |
2 mg | 40 € | In Stock | |
5 mg | 64 € | In Stock | |
10 mg | 93 € | In Stock | |
25 mg | 170 € | In Stock | |
50 mg | 242 € | In Stock | |
1 mL x 10 mM (in DMSO) | 76 € | In Stock |
Description | CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity. |
Targets&IC50 | VEGFR2:11 nM, FGFR:9 nM |
In vitro | CP-547632 (1-1000 nM ; 1 h) suppresses VEGF-induced VEGFR-2 phosphorylation in a concentration-dependent manner (IC50: 6 nM). [1] |
In vivo | CP-547632 (oral ; 50 mg/kg) yieldes plasma concentrations above 500 ng/ml for 12 hours. CP-547632 (p.o. ; 6.25-100 mg/kg/day ; for 10-24 days) causes a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts.[1] |
Molecular Weight | 532.4 |
Formula | C20H24BrF2N5O3S |
Cas No. | 252003-65-9 |
Smiles | NC(=O)c1c(NC(=O)NCCCCN2CCCC2)snc1OCc1c(F)cc(Br)cc1F |
Relative Density. | 1.532 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90.0 mg/mL (169.0 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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