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AZD-7762

CAS No. : 860352-01-8

MCE 国际站：AZD-7762

产品活性：AZD-7762 是一种有效的ATP竞争性的细胞周期检测点激酶 (checkpoint kinase，Chk) 抑制剂，抑制Chk1的 IC₅₀ 为 5 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：Checkpoint Kinase (Chk)

In Vitro: AZD-7762 (AZD7762) is an equally potent inhibitor of Chk1 and Chk2 in vitro. AZD-7762 potently inhibits Chk1 and Chk2, abrogates DNA damage-induced S and G₂ checkpoints, enhances the efficacy of NSC 613327 and SKF 104864A, and modulates downstream checkpoint pathway proteins. AZD-7762 potently inhibits Chk1 phosphorylation of a cdc25C peptide with an IC₅₀ of 5 nM as measured by a scintillation proximity assay. The K_i for AZD-7762 is determined to be 3.6 nM. Kinetic characterization suggests that AZD-7762 binds in the ATP-binding site of Chk1 and is thought to compete directly for ATP binding in a reversible manner. AZD-7762 is shown to abrogate the G₂ arrest induced by Camptothecin with an average EC₅₀ of 10 nM (n=12) and maximal abrogation in the range of 100 nM.

In Vivo: In the rat H460-DNp53 xenograft study, AZD-7762 (AZD7762) potentiates the antitumor activity of NSC 613327 in a dose-dependent manner by a decrease in %T/C with increasing dose (48% and 32%, 10 and 20 mg/kg AZD-7762, respectively). In the mouse xenograft study in combination with CPT-11, SW620 established tumors are treated with vehicle, CPT-11 alone, AZD-7762 alone, or AZD-7762 in combination with CPT-11. AZD-7762 dosed alone shows insignificant antitumor activity, whereas CPT-11 alone displays striking and significant activity (%T/C with increasing dose is 9 and 1, respectively ). In combination with AZD-7762, %T/C increases significantly to -66% and -67%, respectively. AZD7762 combination with CX-5461 induces cancer cell death of Tp53-null (Tp53^-/-) Eμ-Myc lymphoma cells in vitro and in vivo.

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  |  Anti-Blood Cancer Compound Library  |  Cancer Stem Cells Compound Library  |  Heterocyclic Compound Library  |  SB-218078  |  Chk2-IN-1  |  BML-277  |  Monalizumab  |  PV-1019  |  MU380  |  SCH900776  |  PD 407824  |  Prexasertib  |  GDC-0575  |  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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