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Elimusertib (BAY-1895344) hydrochloride

Names

[ CAS No. ]:
1876467-74-1

[ Name ]:
Elimusertib (BAY-1895344) hydrochloride

[Synonym ]:
MFCD31561442

Biological Activity

[Description]:

BAY-1895344 is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> ATM/ATR
Signaling Pathways >> PI3K/Akt/mTOR >> ATM/ATR

[Target]

ATR:7 nM (IC50)


[In Vitro]

BAY-1895344 potently inhibits the proliferation of a broad spectrum of human tumor cell lines with a median IC50 of 78 nM[1]. BAY-1895344 potently suppresses hydroxyurea-induced H2AX phosphorylation (IC50, 36 nM)[1].

[In Vivo]

BAY-1895344 shows potent anti-tumor efficacy in monotherapy in a variety of xenograft models of ovarian and colorectal cancer, and causes complete tumor remission in mantle cell lymphoma models[2].

[References]

[1]. Ulrich T. Luecking, et al. Abstract 983: Identification of potent, highly selective and orally available ATR inhibitor BAY 1895344 with favorable PK properties and promising efficacy in monotherapy and combination in preclinical tumor models. Cancer Research. July 2017 Volume 77, Issue 13 Supplement.

[2]. Antje Margret Wengner, et al. Abstract 836: ATR inhibitor BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride in preclinical tumor models. Cancer Research. July 2017 Volume 77, Issue 13 Supplement

Chemical & Physical Properties

[ Molecular Formula ]:
C20H22ClN7O

[ Molecular Weight ]:
411.89

[ Storage condition ]:
-20℃

Safety Information

[ Hazard Codes ]:
N

Related Compounds