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Milciclib

CAS No. : 802539-81-7

MCE 国际站：Milciclib

产品活性：Milciclib (PHA-848125) 是一种有效的、ATP 竞争性的 CDK 和 Tropomyosin receptor kinase (TRK) 双重抑制剂，对 cyclin A/CDK2，cyclin H/CDK7，cyclin D1/CDK4，cyclin E/CDK2，cyclin B/CDK1 和 TRKA 的 IC₅₀ 值分别为 45，150，160，363，398 和 53 nM。

研究领域：Cell Cycle/DNA Damage  |  Autophagy

作用靶点：CDK  |  Autophagy

In Vitro: Milciclib (PHA-848125; 0.156 or 0.625 μM) up-regulates the expression of PDCD4, DDIT4, SESN2/sestrin 2 and DEPDC6/DEPTOR in GL-Mel cells. Milciclib (PHA-848125) potently inhibits the kinase activity of CDK2/cyclin A complex and of TRKA in a biochemical assay, with IC₅₀s of 45 and 53 nM, respectively. Milciclib induces a clear accumulation of cells in G1 phase. Milciclib strongly inhibits NGF-induced phosphorylation of TRKA in a dose-dependent manner.

In Vivo: Milciclib (PHA-848125; 5, 10, and 15 mg/kg, p.o.) inhibits the growth of tumor in 7,12-dimethylbenz(a) anthracene (DMBA)-induced rat mammary carcinoma model. Milciclib has significant antitumor activity in various human xenografts and carcinogen-induced tumors as well as in disseminated primary leukemia models, with plasma concentrations in rodents in the same range as those found active in inhibiting cancer cell proliferation. Milciclib (PHA-848125; 40 mg/kg) induces a significant tumor growth inhibition in K-Ras^G12DLA2 mice, and this is accompanied by a reduction in the cell membrane turnover.

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