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。

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

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].

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].

1429882-07-4

C29H40N6O

488.67

UNC2371

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