252003-71-7
252003-71-7 structure
- Name: CP-547632 hydrochloride
- Chemical Name: CP-547632 hydrochloride
- CAS Number: 252003-71-7
- Molecular Formula: C20H25BrClF2N5O3S
- Molecular Weight: 568.86
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK FGFR
- Create Date: 2019-10-08 16:34:52
- Modify Date: 2024-01-09 19:21:04
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CP-547632 hydrochloride is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is an ATP-competitive kinase inhibitor and it is selective relative to epidermal growth factor receptor, platelet-derived growth factor β, and other related TKs. CP-547632 hydrochloride has antitumor efficacy[1].
| Name | CP-547632 hydrochloride |
|---|
| Description | CP-547632 hydrochloride is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is an ATP-competitive kinase inhibitor and it is selective relative to epidermal growth factor receptor, platelet-derived growth factor β, and other related TKs. CP-547632 hydrochloride has antitumor efficacy[1]. |
|---|---|
| Related Catalog | |
| Target |
VEGFR-2:11 nM (IC50) FGFR:9 nM (IC50) |
| In Vitro | CP-547632 hydrochloride (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC50 value of 6 nM[1]. Western Blot Analysis[1] 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 (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]. CP-547632 hydrochloride (oral; 50 mg/kg) of a single oral dose of 50 mg/kg yieldes plasma concentrations above 500 ng/ml for 12 hours[1]. Animal Model: Mice bearing tumors (75-150 mm in size)[1] Dosage: 6.25, 12.5, 25, 50, 100 mg/kg Administration: P.o.; daily; 10-24 days Result: Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts. Animal Model: H-ras tumor-bearing mice[1] 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. |
| References |
| Molecular Formula | C20H25BrClF2N5O3S |
|---|---|
| Molecular Weight | 568.86 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |