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STM2457

目录号 GC19771

A first-in-class, highly potent, selective and orally active METTL3 inhibitor

规格 价格 库存 购买数量
5mg
¥2,400.00
现货
10mg
¥3,840.00
现货
50mg
¥11,600.00
现货

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Sample solution is provided at 25 µL, 10mM.

文献引用

质量管理

Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

Inhibition of METTL3-METTL14

STM2457 inhibits METTL3-METTL14 activity with IC50 of 16.9 nM.

Cell experiment [1]:

Cell lines

human AML cells, mouse AML cells, MOLM-13

Preparation method

The solubility of this compound in DMSO is > 1 mM.

Reaction Conditions

3 days

Applications

STM2457 shows its anti-leukaemic activity by the pharmacological inhibition of METTL3 on SP1 and BRD4.

Animal experiment [1]:

Animal models

NSG mice (primary murine MLL-AF9/Flt3ITD/+)

Dosage form

50 mg/kg, intraperitoneal injection, STM2457 was dissolved in 20% (w/v) 2-hydroxyprolpy β-cyclodextrin vehicle.

Applications

STM2457 decrease total m6A levels on poly-A+-enriched RNA of METTL3, reduces human CD45+ cells in the bone marrow and spleen and impair engraftment and AML expansion in vivo at the dose of 50 mg/kg.

References:

[1]. Yankova, E., Blackaby, W., Albertella, M. et al. Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia. Nature 593, 597–601 (2021).

产品描述

STM2457, an inhibitor of METTL3-METTL14 catalytic activity with IC50 of 16.9 nM, can directly bind to the METTL3-METTL14 with a high affinity (Kd) of 1.4 nM. STM2457, also shows greater than 1,000-fold selectivity for METTL3 compared to other RNA, DNA and protein methyltransferases. [1]

STM2457 can inhibit the proliferation of human AML cells but not normal non-lekaemic haemopoietic cells. What’s more, STM2457 can reduce the clonogenic potential of primary mouse AML cells and inhibit METTL3 in MOLM-13 cells, which causes myeloid differentiation and cell cycle arrest. [1]

STM2457 can impair engraftment and AML expansion in vivo and significantly prolong the mouse lifespan. It also reduces human CD45+cells in the bone marrow and spleen. [1]

Reference:
[1] Yankova, E., Blackaby, W., Albertella, M. et al. Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia. Nature 593, 597–601 (2021).

Chemical Properties

Cas No. 2499663-01-1 SDF N/A
别名 N/A
化学名 N-((6-(((cyclohexylmethyl)amino)methyl)imidazo[1,2-a]pyridin-2-yl)methyl)-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxamide
Canonical SMILES O=C(C(N=C1N2C=CC=C1)=CC2=O)NCC3=CN4C=C(CNCC5CCCCC5)C=CC4=N3
分子式 C25H28N6O2 分子量 444.53
溶解度 DMSO : 270 mg/mL 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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