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AZD-7762 hydrochloride

CAS No. : 1246094-78-9

MCE 站：AZD-7762 hydrochloride

产品活性：AZD-7762 hydrochloride 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 hydrochloride (AZD7762) is an equally potent inhibitor of Chk1 ａnd Chk2 in vitro. AZD-7762 hydrochloride 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 hydrochloride 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 hydrochloride is determined to be 3.6 nM. Kinetic characterization suggests that AZD-7762 hydrochloride binds in the ATP-binding site of Chk1 ａnd is thought to compete directly for ATP binding in a reversible manner. AZD-7762 hydrochloride 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 rat H460-DNp53 xenograft studies, AZD-7762 hydrochloride (10 mg/kg ａnd 20 mg/kg) potentiates the antitumor activity of NSC 613327 in a dose-dependent manner. That is, the inhibition rate (%T/C) decreases to 48% ａnd 32%, respectively, with increasing dose. In a mouse xenograft study in combination with CPT-11, treatment with AZD-7762 hydrochloride in combination with CPT-11 significantly increased CPT-11 activity with a significant increase in %T/C to -66% ａnd -67%, respectively. AZD7762 hydrochloride in combination with CX-5461 induces Tp53-null (Tp53^-/-) Eμ-Myc in vitro ａnd in vivo Lymphoma cell death.

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