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STM2457 Sale

(Synonyms: N-[[6-[[(环己基甲基)氨基]甲基]咪唑并[1,2-A]吡啶-2-基]甲基]-4-氧代-4H-吡啶并[1,2-A]嘧啶-2-甲酰胺) 目录号 : GC19771

An inhibitor of the METTL3/14 complex

STM2457 Chemical Structure

Cas No.:2499663-01-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,602.00
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1mg
¥693.00
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5mg
¥1,456.00
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10mg
¥2,464.00
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25mg
¥4,122.00
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50mg
¥5,880.00
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Sample solution is provided at 25 µL, 10mM.

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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]

STM2457是METTL3-METTL14催化活性的抑制剂,其IC50为16.9nM,可以以1.4nM的高亲和力(Kd)直接结合METTL3-METTL14。STM2457与其他RNA、DNA和蛋白质甲基转移酶相比,对METTL3也显示出大于1000倍的选择性。[1]

STM2457可以抑制人AML细胞的增殖,但不能抑制正常非白血病造血细胞的增殖。此外,STM2457可以降低原代小鼠AML细胞的克隆潜能,并抑制MOLM-13细胞中的METTL3,从而导致骨髓分化和细胞周期停滞。[1]

STM2457可在体内损害植入和AML扩增,并显著延长小鼠寿命。它还减少了骨髓和脾脏中的人类CD45+细胞。[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
别名 N-[[6-[[(环己基甲基)氨基]甲基]咪唑并[1,2-A]吡啶-2-基]甲基]-4-氧代-4H-吡啶并[1,2-A]嘧啶-2-甲酰胺
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
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1 mg 5 mg 10 mg
1 mM 2.2496 mL 11.2478 mL 22.4957 mL
5 mM 0.4499 mL 2.2496 mL 4.4991 mL
10 mM 0.225 mL 1.1248 mL 2.2496 mL
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