| Identification | Back Directory | [Name]
CP-547632 (hydrochloride) | [CAS]
252003-71-7 | [Synonyms]
CP-547632 HYDROCHLORIDE
CP-547632 hydrochloride >=98% (HPLC) | [Molecular Formula]
C20H25BrClF2N5O3S | [MDL Number]
MFCD20268381 | [MOL File]
252003-71-7.mol | [Molecular Weight]
568.86 |
| Chemical Properties | Back Directory | [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 | [InChIKey]
NNPJZJJMQDXYGN-UHFFFAOYSA-N | [SMILES]
NC(C1=C(NC(NCCCCN2CCCC2)=O)SN=C1OCC3=C(F)C=C(Br)C=C3F)=O.[H]Cl |
| Hazard Information | Back Directory | [Uses]
CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy[1]. | [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 ) | | [IC 50]
VEGFR-2: 11 nM (IC50); FGFR: 9 nM (IC50) | [References]
[1] Beebe JS, et al. Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res. 2003 Nov 1;63(21):7301-9. PMID:14612527 |
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| Company Name: |
TOSUN PHARM
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| Tel: |
61855200 13326451905 |
| Website: |
www.toref.cn/ |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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