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RMC-4550
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。
RMC-4550图片
CAS NO:2172651-73-7
包装与价格:
包装价格(元)
2 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
RMC-4550 是选择性的蛋白酪氨酸磷酸酶 2 的变构抑制剂,其IC50=0.583 nM。

产品描述

RMC-4550 is an effective and allosteric inhibitor of SHP2 (IC50: 0.583 nM).

体外活性

RMC-4550 stabilizes the auto-inhibited conformation of wild-type SHP2 enzyme, with a mode of inhibition similar to SHP099. RMC-4550 inhibits the activity of full-length wild-type SHP2 enzyme activated by a di-phosphotyrosine peptide but lacks activity against the free catalytic domain of SHP2 [1].

体内活性

RMC-4550 has moderate to high bioavailability and has a half-life amenable for once daily oral administration. In the EGFR-driven KYSE-520 human esophageal cancer xenograft model, RMC-4550 has a dose dependent efficacy consistent with target modulation, assessed by phospho-ERK inhibition in tumors. RMC-4550 is well tolerated at doses that achieved maximal and sustained efficacy in this model[2].

Cas No.

2172651-73-7

分子式

C21H26Cl2N4O2

分子量

437.36

储存和溶解度

DMSO:260 mg/mL (571.61 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years