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CP-609754
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-609754图片
CAS NO:1190094-64-4
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
CP-609754 是高效的、可逆的法尼基转移酶抑制剂,对重组人 H-Ras 和重组 K-Ras法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。

产品描述

CP-609754 shows selective inhibition of farnesyltransferase.

体外活性

CP-609754 inhibits farnesylation (IC50 = 1.72 ng/mL) of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines. CP-609754 selectively inhibits farnesylation of both H- and K-Ras proteins in 3T3 transfectants. CP-609754 is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI. CP-609754 interacts with the farnesyltransferase-farnesyl PPI complex and competes for the binding of the Ras protein[1].

体内活性

CP-609754 has in vivo antitumor activity against 3T3 H-ras (61L) tumors. With twice daily oral dosing of CP-609754, tumor regression is achieved with a dose of 100 mg/kg; the ED50 for tumor growth inhibition is 28 mg/kg. With continuous i.p. infusion of CP-609754, tumor growth is inhibited by >50%, and tumor farnesyltransferase activity inhibited by >30% in mice in which the plasma concentration of CP-609754 is maintained above 118 ng/mL[1].

Cas No.

1190094-64-4

分子式

C29H22ClN3O2

分子量

479.96

储存和溶解度

DMSO:100 mg/mL (208.35 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years