Pelitinib - CAS:257933-82-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Pelitinib
英文名称:	Pelitinib
别名:	培利替尼 EKB 569;(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
CAS No:	257933-82-7	分子式:	C₂₄H₂₃ClFN₅O₂	分子量:	467.92
CAS No:	257933-82-7
分子式:	C₂₄H₂₃ClFN₅O₂
分子量:	467.92

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P10102 Pelitinib ≥98%（HPLC） (psaitong)

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外观与性状：

白色至类白色固体

包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(5mg/mL 加热）

产品描述：

基本信息

产品编号：P10102
产品名称：Pelitinib
CAS:	257933-82-7	储存条件	粉末	-20℃	四年

分子式：	C24H23ClFN5O2		溶于液体	-80℃	六个月
分子量	467.92			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	13mg/mL (27.78mM)
		Ethanol	Insoluble
		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	2.1371mL	10.6856mL	21.3712mL
5mM	0.4274mL	2.1371mL	4.2742mL
10mM	0.2137mL	1.0686mL	2.1371mL

生物活性

产品描述	一种EGFR(表皮生长因子受体)抑制剂，IC50:38.5nM。
靶点/IC₅₀	EGFR 38.5nM (IC50)
体外研究	Pelitini has much greater inhibitory activity against the EGFR kinase than against Src, MEK/ERK, Cdk4, c-Met, Raf and ErbB2,for example, the IC50 for EGFR is 32-fold lower than the IC50 for the closely related ErbB2. Pelitinib results in a dramatic reduction in EGFR phosphorylation but no change in the total amount of EGFR protein. It requires at least 10-fold more drug to equivalently inhibit ErbB2 phosphorylation in similar assays, and EKB-569 does not block phosphorylation of another receptor tyrosine kinase (c-Met) assessed in the same manner[1]. EKB-569 is a potent inhibitor of proliferation in NHEK, A431,and MDA-468 cells (IC50=61, 125, and 260nM, respectively) but not MCF-7 cells (IC50=3600nM). EKB-569 is also a potent inhibitor of EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells (IC50=20-80nM).
体内研究	A single oral dose of 10mg/kg EKB-569 inhibits EGFR phosphorylation in A431 xenografts within 60minutes. Twenty-four hours later, EGFR activity is still inhibited by over 50% by this single oral dose. The half-life of EKB-569 in mouse plasma is about 2hours.

推荐实验方法(仅供参考)

细胞实验:

For experiments using cells in culture, A431 cells or 3T3/c-erbB-2 cells over-expressing c-erbB2 are are treated with various concentrations of EKB-569 for 2.75 h before co-incubation with 100ng/mL EGF (A431 cells) or no growth factor (3T3/c-erbB2 cells) for 0.25h. Cells are ished twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer for 20min on ice, before immunoprecipitation and SDS–PAGE-immunoblotting.

动物实验:
Mice: For in vivo experiments, athymic nu/nu female mice are implanted subcutaneously with 5×106 A431 tumor cells. When tumors reach a mass of 200-300mg, animals are treated with a single dose of 10mg/kg EKB-569 in pH 2.0 water per gavage.Tumors from control and drug-treated animals are excised and minced into 1-mm pieces for anlysis.