10058-F4

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Chemical Structure| 403811-55-2 同义名 : -
CAS号 : 403811-55-2
货号 : A2666914
分子式 : C12H11NOS2
纯度 : 99%+
分子量 : 249.35
MDL号 : MFCD04969046
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(160.42 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 10058-F4 inhibits the growth of leukemic cells and the dimerization of Myc and Max. It induces cell-cycle arrest and apoptosis of AML cells, primarily arresting them at the G0/G1 phase. Moreover, 10058-F4 downregulates c-Myc expression and upregulates CDK inhibitors, such as p21 and p27. Additionally, it induces apoptosis through the activation of the mitochondrial pathway, characterized by the downregulation of Bcl-2, upregulation of Bax, release of cytoplasmic cytochrome C, and cleavage of caspase 3, 7, and 9. Furthermore, 10058-F4 promotes myeloid differentiation, possibly via the activation of multiple transcription factors. Similarly, 10058-F4-induced apoptosis and differentiation are also evident in primary AML cells [1]. 10058-F4 reduces c-Myc protein levels and inhibits proliferation of HepG2 cells, likely by upregulating the cyclin-dependent kinase (cdk) inhibitor, p21WAF1, and decreasing intracellular levels of alpha-fetoprotein (AFP). Treatment with 10058-F4 also suppresses human telomerase reverse transcriptase (hTERT) at the transcriptional level. Moreover, besides inhibiting the proliferation of HepG2 cells, 10058-F4 enhances sensitivity to conventional chemotherapeutic agents, including doxorubicin, 5-fluorouracil (5-FU), and cisplatin [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.01mL

0.80mL

0.40mL

20.05mL

4.01mL

2.01mL

40.10mL

8.02mL

4.01mL
参考文献

[1]Huang MJ, et al. A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia. Exp Hematol. 2006 Nov;34(11):1480-9.

[2]Lin CP, et al. Small-molecule c-Myc inhibitor, 10058-F4, inhibits proliferation, downregulates human telomerase reverse transcriptase and enhances chemosensitivity in human hepatocellular carcinoma cells. Anticancer Drugs. 2007 Feb;18(2):161-70.

[3]Guo J, et al. Efficacy, pharmacokinetics, tisssue distribution, and metabolism of the Myc-Max disruptor, 10058-F4 [Z,E]-5-[4-ethylbenzylidine]-2-thioxothiazolidin-4-one, in mice. Cancer Chemother Pharmacol. 2009 Mar;63(4):615-25