PAN-90806

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PAN-90806 (CP-547632, CP547632) 是一种高效、ATP 竞争性、口服活性的 VEGFR-2 抑制剂，可阻断 VEGFR-2 激酶自身磷酸化 (IC50=11 nM) 和 VEGF 诱导的 VEGFR-2 磷酸化 (IC50=5)纳米）。

PAN-90806 (CP-547632, CP547632) is a highly potent, ATP-competitive, orally active VEGFR-2 inhibitor that blocks VEGFR-2 kinase autophosphorylation (IC50=11 nM) and VEGF-induced VEGFR-2 phosphorylation (IC50=5 nM); is approximately equipotent (<10-fold) against VEGFR-2, bFGF receptor and EGFR/Tie-2 chimera, 250-1000-fold selectivity over PDGFRβ, EGFR and InsR; inhibits tumor-associated VEGFR-2 phosphorylation with decreased microvascular density and significant tumor growth inhibition in a number of tumor models.

CP-547632 (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC50 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.

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. CP-547632 (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours. Animal Model:Athymic female mice (CD-1 nu/nu) 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:Female athymic mice bearing H-Ras tumor 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.

CP-547632 | CP547632

Angiogenesis

VEGFR

VEGFR

Other Indications

Other Disease

252003-65-9

532.4

C20H24BrF2N5O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (187.83 mM)

O=C(C1=C(NC(NCCCCN2CCCC2)=O)SN=C1OCC3=C(F)C=C(Br)C=C3F)N

3-((4-bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years