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STM2457

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。

CAS号

2499663-01-1

分子式

C25H28N6O2

主要靶点

Apoptosis|Others

仅限科研使用

Cat No : CM08942

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Synonyms

验证数据展示

  • CAS No.: 2499663-01-1

    STM2457
    CAS#: 2499663-01-1

产品信息

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).

CAS号 2499663-01-1
分子式 C25H28N6O2
主要靶点 Apoptosis|Others
主要通路 凋亡|其他
分子量 444.53
纯度 99.06%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

体外活性

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].

溶解度

DMSO:100 mM,Sonification is recommended.

参考文献

1.Wesley Peter Blackaby, et al. Mettl3 inhibitory compounds. WO2020201773A1.
2.Eliza Yankova, et al. Small molecule inhibition of METTL3 as a strategy against myeloid leukaemia. Nature. 2021 Apr 26.

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