|(R)-3-甲基-4-(4-(1-甲基-1H-吡唑-5-基)-8-(1H-吡唑-3-基)-1,7-二氮杂萘-2-基)吗啉|CsnPharm

CAS No.: 1876467-74-1

Synonyms: BAY-1895344;free base

BAY-1895344 is a potent and selective ATR inhibitor with IC50 of 7 nM.

规格	价格	促销价格	库存	数量

400-920-2911

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生物活性

描述ATR (ataxia telangiectasia and Rad3-related) responds to a broad spectrum of DNA damage, including double-strand breaks (DSB) and lesions derived from interference with DNA replication as well as increased replication stress (e.g. in oncogene-driven tumor cells). Therefore, inhibition of ATR kinase activity could be the basis for a novel anti-cancer therapy in tumors with increased DNA damage, deficiency in DNA damage repair or replication stress. In vitro, BAY-1895344 was shown to be a very potent and highly selective ATR inhibitor (IC₅₀ = 7 nM), which potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC₅₀ = 78 nM). In cellular mechanistic assays, BAY 1895344 potently inhibited hydroxyurea-induced H2AX phosphorylation (IC₅₀ = 36 nM). Moreover, BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR (DNA damage response) deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models.
动物研究
剂量
Mice: 3 mg/kg - 50 mg/kg^[1] (p.o., BID)

给药途径
p.o.
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT03188965 Neoplasms Phase 1 Recruiting January 24, 2020 -
参考文献

动物研究
剂量	Mice: 3 mg/kg - 50 mg/kg^[1] (p.o., BID)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03188965	Neoplasms	Phase 1	Recruiting	January 24, 2020	-

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