SMI-16a - CAS:587852-28-6 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	SMI-16a
英文名称:	SMI-16a
别名:	PIM1/2 Kinase Inhibitor VI
CAS No:	587852-28-6	分子式:	C₁₃H₁₃NO₃S	分子量:	263.31
CAS No:	587852-28-6
分子式:	C₁₃H₁₃NO₃S
分子量:	263.31

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S10045 SMI-16a ≥98% (psaitong)

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包装规格：

1mg 5mg 25mg in glass bottle

溶解性：

溶于DMSO(≥150mg/ml)

产品描述：

基本信息

产品编号：	S10045
产品名称：	SMI-16a
CAS:	587852-28-6	储存条件	粉末	-20℃	四年

分子式：	C13H13NO3S		溶于液体	-80℃	6个月
分子量：	263.31			-20℃	1个月
化学名：	(5E)-5-[(4-PROPOXYPHENYL)METHYLIDENE]-1,3-THIAZOLIDINE-2,4-DIONE
Solubility (25°C)：
体外:	DMSO	53mg/mL (201.28mM)
	Ethanol	3mg/mL (11.39mM)
	Water	Insoluble
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	3.7978mL	18.9890mL	37.9780mL
5mM	0.7596mL	3.7978mL	7.5956mL
10mM	0.3798mL	1.8989mL	3.7978mL
50mM	0.0760mL	0.3798mL	0.7596mL

生物活性

产品描述	一种选择性的Pim激酶抑制剂。
靶点	Pim2	Pim1
	20nM	150nM
体外研究	SMI-16a has excellent potency for inhibition of both Pim-1 and Pim-2.Treatment with Pim-2 short-interference RNA as well as the Pim inhibitor SMI-16a successfully restores osteoblastogenesis suppressed by all the above inhibitory factors and MM cells.The SMI-16a treatment potentiates BMP-2-mediated anabolic signaling while suppressing TGF-β signaling.
体内研究	Mice tolerate intraperitoneal dose of SMI-16a is 50mg/kg daily for 5 days,while 100mg/kg is overtly toxic.Treatment of the animals with SMI-16a for 5 days per week reduces the growth of tumors by approximately 50% and does not cause a loss of body weight.Subchronic dosing with SMI-16a does not affect the levels of red,white blood cells,including lymphocytes,monocytes,and granulocytes,indicating that the compound does not have myelosuppressive effects.SMI-16a does not have toxicity toward the liver as the albumin,alkaline phosphatase,and alanine aminotransferase levels are unchanged.SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models.

推荐实验方法(仅供参考)

激酶实验：

Recombinant human Pim-1 (Upstate) is incubated with S6 kinase/Rsk-2 peptide 2 (KKRNRTLTK) as the substrate in the presence 100µM of compounds from the screening library,1µM ATP and 10mM MgCl2 for 1h.The Kinase-Glo luciferase kit is used to measure residual ATP levels after the kinase reaction.

细胞实验:

Human prostate cancer PC3 cells are seeded in 96-well tissue culture dishes at approximately 10% confluency and allowed to attach and recover for 24h.Varying concentrations of the test compounds (SMI-16a) are then added to each well,and the plates are incubated for an additional 48h.The number of surviving cells is determined by the MTS assay.The percentage of cells killed is calculated as the percentage decrease in MTS metabolism compared with control cultures.

动物实验:
Mice:Female Balb/C mice are injected subcutaneously with JC cells suspended in PBS.After palpable tumor growth,animals are treated five days per week by intraperitoneal injection of vehicle alone or 50mg/kg of SMI-16a.Whole body weights and tumor volume measurements are performed three times per week.