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Danusertib

CAS No. : 827318-97-8

MCE 站：Danusertib

产品活性：Danusertib 是一种极光激酶 (aurora kinase) 抑制剂，能够抑制 Aurora A，Aurora B 和 Aurora C 的活性，IC₅₀ 值分别为 13，79 和 61 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy

作用靶点：Aurora Kinase  |  Autophagy

In Vitro: Danusertib (0.01 to 50 μM) significantly decreases viability of C13 and A2780cp cells. The IC₅₀s are 10.40 and 1.83 μM for C13 cells, and 19.89 and 3.88 μM for A2780cp cells after 24- and 48-h treatment. Danusertib induces cell cycle arrest in G2/M phase in C13 and A2780cp cells. Danusertib treatment results in a marked increase in the percentage of cells arrested in G2/M phase and an accumulation of polyploidy in C13 and A2780cp cells. Danusertib demotes the expression of CDK1/CDC2 and cyclin B1 but promotes the expression of p21 Waf1/Cip1, p27 Kip1, and p53. Danusertib induces autophagy in C13 and A2780cp cells with the involvement of PI3K/Akt/mTOR signaling pathway. PHA-739358 strongly inhibits proliferation of all leukemic cell lines tested, with IC₅₀ values ranging from 0.05 μM to 3.06 μM. PHA-739358 induces antiproliferative effects in BaF3-p210 cells, including IM-resistant M351T, E255K, and T315I mutants. PHA-739358 (5 μM) reduces phosphorylation of CrkL in BaF3-p210 wt cells and IM-resistant mutants. Danusertibsertib leads to cell-cycle arrest and completely inhibits cell proliferation of the GEP-NET cells in vitro.

In Vivo: PHA-739358 (15 mg/kg twice a day, i.p.) and IM are well tolerated, and significantly inhibit proliferation of K562 cells andvirtually suppressed tumor growth during the 10-day treatment period. In a subcutaneous murine xenograft model, danusertibsertib (2×15 mg/kg/d, i.p.) significantly reduces tumor growth in vivo compared with controls or mice treated with streptozotocine/5-fluorouracil.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Cytoskeleton Compound Library  |  Anti-Blood Cancer Compound Library  |  AT9283  |  KW-2449  |  PF-03814735  |  ZM-447439  |  SNS-314 mesylate  |  CCT 137690  |  SCH-1473759 hydrochloride  |  NU6140  |  Aurora kinase inhibitor-2  |  Tripolin A  |  Aurora B inhibitor 1  |  Aurora inhibitor 1

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