NSC781406 - CAS:1676893-24-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	NSC781406 一键复制产品信息
英文名称:	NSC781406
别名:	NSC781406 2,4-Difluoro-N-[2-methoxy-5-[4-[3-(4-methylsulfonylpiperazin-1-yl)prop-1-ynyl]quinolin-6-yl]pyridin-3-yl]benzenesulfonamide
CAS No:	1676893-24-5	分子式:	C₂₉H₂₇F₂N₅O₅S₂	分子量:	627.68
CAS No:	1676893-24-5
分子式:	C₂₉H₂₇F₂N₅O₅S₂
分子量:	627.68

点击下载产品说明书(PDF)

N11404 NSC781406 ≥98% (普西唐-psaitong)

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包装规格：

1mg 5mg 10mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO(150mg/mL超声）

产品描述：

基本信息

产品编号：	N11404
产品名称：	NSC781406
CAS:	1676893-24-5	储存条件	粉末	-20℃	四年

分子式：	C29H27F2N5O5S2		溶于液体	-80℃	6个月
分子量：	627.68			-20℃	1个月
化学名：	2,4-Difluoro-N-[2-methoxy-5-[4-[3-(4-methylsulfonylpiperazin-1-yl)prop-1-ynyl]quinolin-6-yl]pyridin-3-yl]benzenesulfonamide
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
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	1.5932mL	7.9658mL	15.9317mL
5mM	0.3186mL	1.5932mL	3.1863mL
10mM	0.1593mL	0.7966mL	1.5932mL

生物活性

产品描述	一种高效的PI3K和mTOR抑制剂，对PI3Kα的IC50值为2nM。
靶点	PI3K;mTOR
体外研究	NSC781406 demonstrates potent PI3K inhibition (PI3KαIC50=2.0nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20nM).NSC781406 displays reasonable liver microsome stability.NSC781406 demonstrates cytotoxic activities against leukemia,non-small cell,lung cancer,colon cancer,central nervous system cancer,melanoma,ovarian cancer,renal cancer,prostate cancer,and breast cancer.It is potent against 60 cancer cell lines with a mean GI50 value of 65nM,and with a GI50 value less than 10nM against four cancer cell lines.
体内研究	In the xenograft models, treatment with 30mg/kg of NSC781406 results in statistically significant antitumor activity,with a mean reduction in relative tumor volume ratio of 52%.Sorafenib displays an inhibition ratio of 44% at 50mg/kg.NSC781406 is well tolerated at 30mg/kg,with no observed mortality or significant reduction of body weight.

推荐实验方法(仅供参考)

激酶实验：

IC50 values for inhibition of the PI3K is measured.PI-103 is used as the reference compound.The compounds (NSC781406) are tested in duplicate for 10 concentrations,100nM or 500nM as the top concentration.All reagents are diluted in kinase buffer.Three-fold,ten-point serial compound (NSC781406) dilutions are performed in kinase buffer.

细胞实验:

Cytotoxic effects are tested in the human lung adenocarcinoma cells A549,human colon cancer cells HCT-116,human breast cancer cells MDA-MB-231 and human hepatocellular carcinoma cells BEL-7404.These four tumor cells are diluted to a density of 40,000–50,000 cells/mL in logarithmic phase.After the cells are treated with compounds (NSC781406) for 72h,MTT solution (5mg/mL,20μL) is added another 4h at 37℃.IC50 values are determined by a nonlinear regression analysis.

动物实验:
Mice:NSC781406 is orally administered once a day 30mg/kg for 14 consecutive days or with sorafenib at 50mg/kg.The relative tumor volume to vehicle-treated control mice is monitored.