ATR inhibitor 2

VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk

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5mg

￥3775.00

3020.00

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10mg

￥6300.00

5040.00

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50mg

￥17812.00

14250.00

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100mg

￥26712.00

21370.00

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货号: ajcx17024
CAS: 1613191-99-3
别名: 2-氨基-6-氟-N-(5-氟-4-(4-(4-(噁丁环烷-3-基)哌嗪-1-羰基)哌啶-1-基)吡啶-3-基)吡唑并[1,5-A]嘧啶-3-甲酰胺,VX-803; M4344; ATR inhibitor 2
分子式: C25H29F2N9O3
分子量: 541.55
纯度: >98%
溶解度: DMSO: 25 mg/mL (46.16 mM)
储存: Store at -20°C
库存: 现货

Background

M4344 is determined to be an adenosine triphosphate (ATP)-competitive, highly potent, and tight-binding inhibitor of ATR with a Ki of < 150 pM. Minimal inhibitory activity is observed against a large panel of unrelated protein kinases, with 308 of 312 kinases tested having a measured Ki corresponding to more than 100-fold selectivity. M4344 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with an IC50 of 8 nM. Profiling on a selected set of cancer cell lines shows synergy with several types of DNA damaging chemotherapeutics as well as PARP1/2 and CHK1 inhibitors.[1]

In monotherapy efficacy studies M4344 shows tumor stasis to regression in tumor models with alternative lengthening of telomeres (ALT). In combination with PARP inhibitors, tumor regression can be observed in triple-negative breast cancer xenograft models.[1]

[1] Frank T. Zenke, et al. AACR; Cancer Res 2019;79(13 Suppl):Abstract nr 369.