|5-(3-(三氟甲基)亚苄基)噻唑烷-2,4-二酮|CsnPharm

CAS No.: 438190-29-5

5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione Catalog No. CSN15804

Synonyms: TCS PIM-1 4a;(Z)-TCS-PIM-1-4a

SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.

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技术信息

生物活性

描述Pim (provirus integration site for Moloney murine leukemia virus) family proteins are highly conserved serine/threonine kinases implicated in transcription, translation, cell cycle, survival, and drug resistance through the numerous targets. SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM (measured by kinase activity assay), as well as shows modest potency to Pim-2. As BAD is a novel substrate of Pim-1, SMI-4a < 5 μM caused dose-dependent reduction of p-BAD in prostate and hematopoietic cells tested. Treatment with 5 μM SMI-4a for 72 h showed various degree of growth inhibition (10-40%) of PC3, DU145, LNCaP, U937, K562 and MV4;11 cells cultured in media containing 10% FBS. Because SMI-4a showed to be serum-bound, it was found that DU145 cells became considerably more sensitive under serum-free conditions. For many substrates of Pim-1 play a role in cell cycle progression, as prediction, treatment with 5 μM SMI-4a for 72 h caused a significant G1 cell cycle arrest of DU145 cells growing in 2% serum and MV4;11 cells plated in 10% serum, as well as a considerable amount of apoptosis (sub-G1 29.2%) of 22Rv1 cells cultured under serum starvation condition. The translocation of p27^Kip1 to the nucleus and reduced Cdk2 activity (shown by decreased p-H1) can also observed in K562 cells cultured in RPMI containing 10% FCS after treatment with SMI-4a. SMI-4a can synergize with rapamycin to cause significant growth inhibition, as well as decreased phosphorylation level of 4E-BP1 of MV4;11 and FDCP1 (IL-3 dependent) cells^[1]. Combination treatment of ABT-737 (50 mg/kg; i.p., QD) and SMI-4a (60 mg/kg, oral gavage, BID) for 16 days significantly reduce the tumor growth of LNCaP xenograft model^[2].
作用机制SMI-4a can compete with respect to ATP, suggesting that it may bind within the ATP-binding pocket of the kinase.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
DLD-1 cell	-	Function assay	96 h	Inhibition of growth of DLD-1 cell line after 96 hours of exposure time with the compound dissolved in DMSO, IC50=17.8 μM	15993594
HCT116 cell	-	Function assay	72 h	Inhibition of growth of HCT116 cell line after 72 hours of exposure time with the compound dissolved in DMSO, IC50=48.8 μM	15993594
HEK293T cells	0.5 μM	Function assay	1 h	Inhibition of human recombinant Flag-Pim1 autophosphorylation expressed in HEK293T cells labeled with [32PO4] at 0.5 uM after 1hr by Western blotting	19072652

动物研究

剂量

Mice: 60 mg/kg^[4] (p.o.), 5 mg/kg - 40 mg/kg^[5], 15 mg/kg^[6] (intratumorally)

给药途径

p.o., intratumorally

动物药代数据

Animal	Mice^[4]
Dose	60 mg/kg
Administration	p.o.
C_max	200 μM
T_1/2	6 h
T_max	1 h

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
- 3.6599 mL
- 18.2996 mL
- 36.5992 mL
- 5 mM
- 0.7320 mL
- 3.6599 mL
- 7.3198 mL
- 10 mM
- 0.3660 mL
- 1.8300 mL
- 3.6599 mL

技术信息

CAS号

438190-29-5

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

C11H6F3NO2S

运输

蓝冰

分子量

273.23

别名

TCS PIM-1 4a;(Z)-TCS-PIM-1-4a

溶解度

DMSO	500.0 mg/mL (1830.0 mM)
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	5 mg/mL	clear
PO	0.5% CMC-Na	43 mg/mL	suspension

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5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione Catalog No. CSN15804

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