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| | CP-547632 (hydrochloride) Basic information |
| Product Name: | CP-547632 (hydrochloride) | | Synonyms: | CP-547632 hydrochloride >=98% (HPLC);CP-547632 HYDROCHLORIDE;CP-547632 hydrochloride (PAN-90806);CP 547632 hydrochloride,CP547632 hydrochloride | | CAS: | 252003-71-7 | | MF: | C20H25BrClF2N5O3S | | MW: | 568.86 | | EINECS: | | | Product Categories: | | | Mol File: | 252003-71-7.mol |  |
| | CP-547632 (hydrochloride) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 38.33 mg/mL (67.38 mM); Water: < 0.1 mg/mL (insoluble) | | form | Solid | | color | White to light yellow |
| | CP-547632 (hydrochloride) Usage And Synthesis |
| Biological Activity | CP-547632 hydrochloride is an orally active, ATP-competitive VEGFR-2 and FGF kinase inhibitor with IC50 of 11 nM and 9 nM, respectively. It is selective for VEGFR2 and bFGF over EGFR, PDGFRβ and related tyrosine kinases (TKs), and has an antitumor effects. | | in vitro | CP-547632 hydrochloride (1-1000 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC 50 value of 6 nM. Western Blot Analysis | Cell Line: | Serum-deprived cells | | Concentration: | 1, 4, 16, 63, 250, 1000 nM | | Incubation Time: | 1 hours | | Result: | Inhibited VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion. | | | in vivo | CP-547632 hydrochloride (po; 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.
CP-547632 hydrochloride (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours.
| Animal Model: | Mice bearing tumors (75-150 mm in size) | | Dosage: | 6.25, 12.5, 25, 50, 100 mg/kg | | Administration: | Po; daily; 10-24 days | | Result: | Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts. | | Animal Model: | < td class="col2"> H-ras tumor-bearing mice | Dosage: | 50 mg /kg | | Administration: | Oral | | Result: | A single oral dose of 50 mg/kg yielded plasma concentrations above 500 ng/ml for 12 hours. | | | target | | VEGFR-2 < span> 11 nM (IC 50 ) | FGFR 9 nM (IC 50 ) | |
| | CP-547632 (hydrochloride) Preparation Products And Raw materials |
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