2805804-54-8

Name	CP-547632 TFA
CAS	2805804-54-8
Molecular Formula	C20H24BrF2N5O3S.C2HF3O2
Molecular Weight	646.43
MOL File	2805804-54-8.mol

Synonyms

CP-547632 TFA

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Chemical Properties

form	Solid
color	Off-white to light yellow

Hazard Information

Uses

CP-547632 TFA 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 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy[1].

in vivo

CP-547632 TFA (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 TFA (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours^[1].

Animal Model:	Athymic female mice (CD-1 nu/nu) bearing tumors (75-150 mm in size)^[1]
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:	Female athymic mice bearing H-Ras tumor^[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.

IC 50

VEGFR2: 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

Supplier

Shanghai YuanYe Biotechnology Co., Ltd.

Telephone 13636370518

Websitehttps://www.shyuanye.com

Beijing Jin Ming Biotechnology Co., Ltd.

Telephone010-60605840 15801484223;

Websitehttp://www.jm-bio.com/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Lucheng (Shenzhen) Technology Co., Ltd.

Telephone13128698830

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList879695/0_EN.htm

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