STM2457 是一种具有口服活性的METTL3选择性抑制剂，可研究急性白血病。

STM2457 is a first-in-class, highly potent, selective and orally active inhibitor of METTL3 . It can be used for the research of acute myeloid leukaemia (AML).

STM2457 (Compound 72) inhibits MOLM13 cells proliferation with an IC50?of 8.699 μM[1]. STM2457, a highly potent and selective first-in-class catalytic inhibitor of METTL3, and a crystal structure of STM2457 in complex with METTL3-METTL14. Treatment of tumours with STM2457 leads to reduced AML growth and an increase in differentiation and apoptosis. These cellular effects are accompanied by selective reduction of m6A levels on known leukaemogenic mRNAs and a decrease in their expression consistent with a translational defect. We demonstrate that pharmacological inhibition of METTL3 in vivo leads to impaired engraftment and prolonged survival in various mouse models of AML, specifically targeting key stem cell subpopulations of AML[2].

2499663-01-1

C25H28N6O2

444.539

DMSO:125 mg/mL (281.20 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years