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Gartisertib

CAS No. : 1613191-99-3

MCE 國際站：Gartisertib

產品活性：Gartisertib (VX-803) 是一種 ATP 競爭性的，具有口服活性的，選擇性的 ATR 抑制劑，K_i<150 pM。Gartisertib 抑制 ATR 驅動的磷酸化檢查點激酶-1 (Chk1) 磷酸化, IC₅₀值為 8 nM。具有抗腫瘤活性。

研究領域：Cell Cycle/DNA Damage  |  PI3K/Akt/mTOR

作用靶點：ATM/ATR

In Vivo: In monotherapy efficacy studies Gartisertib shows tumor stasis to regression in tumor models with alternative lengthening of telomeres (ALT). In combination with PARP inhibitors, tumor regression could be observed in triple-negative breast cancer xenograft models.

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