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10058-F4

CAS No. : 403811-55-2

MCE 站：10058-F4

产品活性：10058-F4是 c-Myc 抑制剂，其阻止c-Myc-Max二聚化和c-Myc靶基因表达的反式激活。

研究领域：Apoptosis  |  Autophagy

作用靶点：c-Myc  |  Autophagy

In Vitro: 10058-F4 inhibits growth of leukemic cells ａnd dimerization of Myc ａnd Max. 10058-F4 induces cell-cycle arrest ａnd apoptosis of AML cells. 10058-F4 arrests AML cells at G0/G1 phase, downregulates c-Myc expression ａnd upregulated CDK inhibitors, p21 ａnd p27. Meanwhile, 10058-F4 induces apoptosis through activation of mitochondrial pathway shown by downregulation of Bcl-2, upregulation of Bax, release of cytoplasmic cytochrome C, ａnd cleavage of caspase 3, 7, ａnd 9. Furthermore, 10058-F4 also induces myeloid differentiation, possibly through activation of multiple transcription factors. Similarly, 10058-F4-induced apoptosis ａnd differentiation could also be observed in primary AML cells. 10058-F4 decreases c-Myc protein levels, inhibites proliferation of HepG2 cells likely through upregulation of cyclin-dependent kinase (cdk) inhibitor, p21WAF1 ａnd lowers intracellular levels of [alpha]-fetoprotein (AFP). Treatment with 10058-F4 also downregulates human telomerase reverse transcriptase (hTERT) at the transcriptional level. In addition to inhibiting the proliferation of HepG2 cells, 10058-F4 enhances sensitivity to conventional chemotherapeutic agents, doxorubicin, 5-fluorouracil (5-FU) ａnd cisplatin.

In Vivo: Peak plasma 10058-F4 concentrations of approximately 300 μM are seen at 5 min ａnd declined to below the detection limit at 360 min following a single iv dose. Plasma concentration versus time data are best approximated by a two-compartment, open, linear model. The highest tissue concentrations of 10058-F4 are found in fat, lung, liver, ａnd kidney. Peak tumor concentrations of 10058-F4 are at least tenfold lower than peak plasma concentrations. Eight metabolites of 10058-F4 are identified in plasma, liver, ａnd kidney. The terminal half-life of 10058-F4 is approximately 1 h, ａnd the volume of distribution is > 200 mL/kg. No significant inhibition of tumor growth is seen after i.v. treatment of mice with either 20 or 30 mg/kg 10058-F4.

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