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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-ATM/ATR-M4344
M4344

Chemical Structure : M4344

CAS No.: 1613191-99-3

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M4344 (VX-803, Gartisertib, VX803, M 4344)

货号: PC-72163Not For Human Use, Lab Use Only.

M4344 (VX-803, Gartisertib) is a highly potent, selective ATR inhibitor with Ki<0.15 nM.

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5 mg ￥1880 In stock
10 mg ￥2980 In stock
25 mg ￥4780 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

M4344 (VX-803, Gartisertib) is a highly potent, selective ATR inhibitor with Ki<0.15 nM.
M4344 (VX-803, Gartisertib) showed minimal inhibitory activity against unrelated kinases, with >100-fold selectivity for ATR over 308/312 kinases tested.
M4344 suppressed cancer cell proliferation at lower concentrations, similarly to BAY1895344 and was more potent than berzosertib (VX-970, M6620), ceralasertib, and VE-821.
M4344 (25 nM) strongly suppressed cell viability of prostate DU145 cancer cells in combination of CPT at nanomolar concentrations, M4344 (10 nM) blocked CPT-induced activation of CHK1, a main downstream effector of ATR.
M4344 kills cancer cells under replication stress (RepStress) and with NE genomic signatures by replication-mediated DNA damage.
M4344 synergizes with clinical TOP1 inhibitor (Exatecan), as well as a broad range of widely used clinical agents including etoposide, gemcitabine, cisplatin, and talazoparib.
M4344 is active in patient-derived tumor organoids and xenograft models.

物理化学性质&存储条件

分子量 541.564
分子式 C25H29F2N9O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (5.4 mg/mL)
Chemical Name/SMILES

2-amino-6-fluoro-N-(5-fluoro-4-(4-(4-(oxetan-3-yl)piperazine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

参考文献

1. Ukhyun Jo, et al. Mol Cancer Ther. 2021 Aug;20(8):1431-1441.

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