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CP-724714
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CP-724714图片
CAS NO:383432-38-0
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
CP724714
CP 724714
产品介绍
CP-724714 是一种高效、选择性口服活性的ErbB2 (HER2)酪氨酸激酶抑制剂,IC50为 10 nM。它能抑制完整细胞中 ErbB2 受体的自磷酸化,具有抗肿瘤活性。它对 EGFR 激酶有明显的选择性,IC50值为6400 nM。

产品描述

CP-724714 is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.

体外活性

CP-724714 is obvious selectively against EGFR (IC50: 6.4 μM). CP-724714 is >1,000-fold less potent for IGF-1R, IR, VGFR2, PDGFRβ, Src, ZAP-70, JNK-2/3, and CDK-2/5. CP-724714 markedly reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain (IC50: 32 nM). CP-724714 inhibits the proliferation of erbB2-amplified cells including BT-474 (IC50: 0.25 μM) and SKBR3 (IC50: 0.95 μM). CP-724714 (1 μM) induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells. CP-724714 inhibits TC transport in membrane vesicles expressing human bile salt export pump (IC50: 16 μM) and inhibits the major efflux transporter in bile canaliculi, MDR1 (IC50: 28 μM).

体内活性

CP-724714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft-bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without mortality or weight loss. In MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts, CP-724714 also has great antitumor activity. In BT-474 xenografts, CP-724714 (30/100 mg/kg) reduces the extracellular signal-regulated kinase and Akt phosphorylation.

Cas No.

383432-38-0

分子式

C27H27N5O3

分子量

469.545

别名

CP724714;CP 724714;CP-724714

储存和溶解度

DMSO:50 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years