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Milciclib

CAS No. : 802539-81-7

MCE 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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Ro-3306  |  Seliciclib  |  Flavopiridol  |  NVP-2  |  SNS-032  |  AZD-5438  |  Kenpaullone  |  GSK 3 Inhibitor IX  |  AUZ 454  |  XL413 hydrochloride  |  CGP60474  |  Wogonin  |  CVT-313  |  NG 52  |  BMS-265246  |  (R)-CR8 trihydrochloride  |  R547  |  PHA-767491 hydrochloride  |  CDK12-IN-3  |  KH-CB19  |  CDK2-IN-4  |  Purvalanol A  |  Cucurbitacin E  |  THZ1-R  |  FMF-04-159-2  |  LY2857785  |  CP-10  |  ML167

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