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MRX-2843
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。
MRX-2843图片
CAS NO:1429882-07-4
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

产品名称
UNC2371
产品介绍
MRX-2843 是ATP 竞争性的、具有口服活性的MERTK和FLT3酪氨酸激酶抑制剂 (TKI),它们的IC50分别为 1.3 nM 和 0.64 nM。

产品描述

MRX-2843 is a potent and orally active inhibitor of MERTK and FLT3(IC50s of 1.3 nM and 0.64 nM, respectively).

体外活性

MRX-2843, a type 1 small-molecule tyrosine kinase inhibitor that abrogates activation of both MERTK and FLT3 and their downstream effectors.?MRX-2843 treatment induces apoptosis and inhibits colony formation in AML cell lines and primary patient samples expressing MERTK and/or FLT3-ITD, with a wide therapeutic window compared with that of normal human cord blood cells[1].

体内活性

In murine orthotopic xenograft models, once-daily oral therapy prolonged survival 2- to 3-fold over that of vehicle-treated controls.?Additionally, MRX-2843 retained activity against quizartinib-resistant FLT3-ITD-mutant proteins with clinically relevant alterations at the D835 or F691 loci and prolonged survival in xenograft models of quizartinib-resistant AML.?Together, these observations validate MRX-2843 as a translational agent and support its clinical development for the treatment of AML[1].

Cas No.

1429882-07-4

分子式

C29H40N6O

分子量

488.67

别名

UNC2371

储存和溶解度

DMSO:26.25mg/ml (53.72 Mm),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years