|5-(4-乙基亚苄基)-2-疏基-1,3-噻唑-4(5H)-酮|CsnPharm

CAS No.: 403811-55-2

5-(4-乙基苯亚甲基)绕丹宁 Catalog No. CSN12467

Synonyms: 10058-F4

10058-F4 is a cell-permeable thiazolidinone that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression and induces cell-cycle arrest and apoptosis.

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实验方案

技术信息

生物活性

描述C-Myc is helix–loop–helix–leucine zipper (HLH–ZIP) oncoprotein that is frequently deregulated in human cancers. 10058-F4 is an inhibitor of c-Myc through disruption of c-Myc-Max dimerization with Kd value of 5.3μM. Exposure to 10058-F4 at concentration ranging in 30-150μM for 24h showed dose-dependently antiproliferative effect on HL-60, U937 and NB4 cells, as well as time dependent antiproliferation at concentration of 100μM, which may due to the increased intrinsic apoptosis. Also the reduced c-Myc protein level and decreased binding of Myc/Max heterodimers to their DNA targets could be observed in HL-60 and U937 cells treated with 100 mM 10058-F4 for 24 hours, accompanied with induced cell-cycle arrest at G0/G1 phase through inhibition of specific binding of c-Myc to cyclin D2 promoter and p53-independent upregulation of p21 and p27 in HL-60 cells. Tumor growth inhibition could be observed up to 6 weeks in mice xenografted rat1a-c-Myc cells pretreated with 64μM for 3 days before inoculation. Significant decreased MYCN protein level could be observed in MNA NB cell lines treated with 75μM 10058-F4 for 48h. Inhibition of MYCN/Max interaction led to cell cycle arrest, apoptosis, and neuronal differentiation in MYCN-amplified neuroblastoma cells and to increased survival of MYCN transgenic mice, and resulted in lipid accumulation.
作用机制10058-F4 can inhibit the c-Myc-Max dimerization which is necessary for the DNA binding and target gene expression regulation^[3].

动物研究

剂量

Mice^[5] (i.v.): 20 mg/kg-30 mg/kg

给药途径

i.v.

动物药代数据

Animal	Mice^[5]
Dose	20 mg/kg
Administration	i.v.
K_cp	0.2459 ± 0.066 h_-1
K_pc	1.044 ± 0.157 h_-1
V_c	160.0 ± 17.54 ml/kg
CL_total	610.6 ± 39.89 ml/h/kg
T_1/2α	0.1672 ± 0.012 h
K_E	3.817 ± 0.229 h_-1
α	4.146 ± 0.292 h_-1
T_1/2β	0.7208 ± 0.096 h
β	0.9617 ± 0.123 h_-1

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0104 mL
- 20.0521 mL
- 40.1043 mL
- 5 mM
- 0.8021 mL
- 4.0104 mL
- 8.0209 mL
- 10 mM
- 0.4010 mL
- 2.0052 mL
- 4.0104 mL

技术信息

CAS号

403811-55-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H11NOS2

运输

蓝冰

分子量

249.35

别名

10058-F4

溶解度

DMSO	400.0 mg/mL (1604.2 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	2 mg/mL	clear
PO	0.5% CMC-Na	75 mg/mL	suspension

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5-(4-乙基苯亚甲基)绕丹宁 Catalog No. CSN12467

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