STM2457
作者：齊岳
發(fā)布時(shí)間：2023-09-06
08:59:46
點(diǎn)擊數(shù)：
產(chǎn)品名稱：STM2457
產(chǎn)品描述：
| 產(chǎn)品描述 | 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). |
| 體外活性 | 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]. |
| 化合物與蛋白結(jié)合的復(fù)合物 |
METTL3-METTL14 heterodimer bound to the SAM competitive small molecule inhibitor STM2457 |
| 分子量 | 444.53 |
| 分子式 | C25H28N6O2 |
| CAS No. | 2499663-01-1 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 100 mM,Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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