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GDC-0575

CAS No. : 1196541-47-5

MCE 国际站：GDC-0575

产品活性：GDC-0575 (ARRY-575, RG7741) 是高选择性，有口服活性的小分子 Chk1 抑制剂，其在异种移植模型中导致肿瘤缩小和生长延迟，IC₅₀ 值为1.2 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：Checkpoint Kinase (Chk)

In Vitro: GDC-0575 is significantly more potent in promoting DNA damage, replication stress and cell death than V158411, LY2603618, and MK-8776 in a panel of melanoma cell lines. GDC-0575 abrogates DNA damage-induced S and G2–M checkpoints, exacerbates DNA double-strand breaks and induces apoptosis in STS cells. GDC-0575 has a synergistic or additive effect together with gemcitabine. CHK1 inhibitor GDC-0575 in combination with AraC enhances the killing of primary acute myeloid leukemia cells ex vivo by inducing apoptosis.

In Vivo: GDC-0575 is active at 25 mg/kg as a single agent, but the efficacy is improved at the higher drug dose. GDC-0575 effectively blocks tumor growth in the D20 and C002 xenografts, and the effect is maintained for at least 10 days after the final dose is administered.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  Cancer Stem Cells Compound Library  |  Highly Selective Inhibitors Library  |  SB-218078  |  Chk2-IN-1  |  BML-277  |  Monalizumab  |  PV-1019  |  MU380  |  SCH900776  |  PD 407824  |  Prexasertib  |  CCT241533 dihydrochloride  |  GNE-900  |  GDC-0425  |  Chk1-IN-6  |  CHK1-IN-2  |  Zn-DPA-maytansinoid conjugate 1  |  CCT245737  |  CHK1-IN-3  |  SAR-020106  |  AZD-7762 hydrochloride  |  MRT00033659  |  CHIR-124  |  ANI-7  |  VER-00158411  |  CHK-IN-1  |  CHK1-IN-4  |  Chk1-IN-5

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