恩扎妥林 - CAS:170364-57-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	恩扎妥林促销
英文名称:	Enzastaurin
别名:	3-(1-甲基-1H-吲哚-3-基)-4-(1-(1-(2-吡啶甲基)-4-哌啶基)-1H-吲哚-3-基)-1H-吡咯-2,5-二酮 LY317615 DB102 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione
CAS No:	170364-57-5	分子式:	C₃₂H₂₉N₅O₂	分子量:	515.6
CAS No:	170364-57-5
分子式:	C₃₂H₂₉N₅O₂
分子量:	515.6
MDL:	MFCD11040980

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E10032 恩扎妥林 ≥98% (HPLC) (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(10mg/mL 加热)。

产品描述：

基本信息

产品编号：E10032
产品名称：Enzastaurin
CAS:	170364-57-5	储存条件	粉末	-20℃	四年

分子式：	C32H29N5O2		溶于液体	-80℃	六个月
分子量：	515.60			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	30mg/mL (58.18mM)
		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	1.9395mL	9.6973mL	19.3945mL
5mM	0.3879mL	1.9395mL	3.8789mL
10mM	0.1939mL	0.9697mL	1.9395mL
50mM	0.0388mL	0.1939mL	0.3879mL

生物活性

产品描述	一种有效的PKCβ抑制剂,IC50:6nM,对其选择性是对 PKCα、PKCγ和 PKCε的 6-20 倍。
靶点/IC50	PKCβ (Cell-free assay)	PKCα (Cell-free assay)	PKCγ (Cell-free assay)	PKCε (Cell-free assay)
靶点/IC50	6nM	39nM	83nM	110nM
体外研究	Enzastaurin (LY317615) application results in a marked dose-dependent inhibition of growth in all MM cell lines investigated,including MM.1S,MM.1R,RPMI 8226 (RPMI),RPMI-Dox40 (Dox40),NCI-H929,KMS-11,OPM-2,and U266,with IC50 from 0.6-1.6μM.Enzastaurin direct impacts human tumor cells,inducing apoptosis and suppressing proliferation in cultured tumor cells.Enzastaurin also suppresses the phosphorylation of GSK3βser9,ribosomal protein S6S240/244,and AKTThr308 while having no direct effect on VEGFR phosphorylation.Enzastaurin increases apoptosis in malignant lymphocytes of CTCL.When combined with GSK3 inhibitors,enzastaurin demonstrates an enhancement of cytotoxicity levels.Treatment with a combination of enzastaurin and the GSK3 inhibitor AR-A014418 leads to increased levels of β-catenin total protein and β-catenin-mediated transcription.Blocking of β-cateninmediated transcription or small hairpin RNA (shRNA) knockdown of β-catenin induces the same cytotoxic effects as that of enzastaurin plus AR-A014418.Additionally,treatment with enzastaurin and AR-A014418 decreases the mRNA levels and surface expression of CD44.
体内研究	Treatment of xenografts with Enzastaurin and radiation produces greater reductions in density of microvessels than either treatment alone.The decrease in microvessel density corresponds to delayed tumor growth.

推荐实验方法(仅供参考)

激酶实验：

激酶实验

使用滤板法测定髓鞘碱性蛋白基底33P的渗透率，而测定用Enzastaurin阻断PKCβII, PKCα, PKCε,或PKCγ的活性。在96孔板上加100μl反应物进行反应，反应物包括90mM HEPES (pH 为7.5),0.001% Triton X-100,4% DMSO,5mM MgCl2,100μM CaCl2,0.1mg/ml磷脂酰丝氨酸,5μg/ml 二乙酰甘油,30μM ATP,0.005μCi/μl 33ATP,0.25mg/ml髓鞘碱性蛋白,enzastaurin的连续稀释物 (浓度为1-2,000nM),及重组人类PKCβII,PKCα,PKCε,或 PKCγ酶(分别为390,169,719,或128pM)。加入酶反应开始，在室温下温育60分钟，加入10% H3PO4结束反应，转移到多屏阴离子磷酸纤维素96孔滤板上，温育30到90分钟，过滤，在真空歧管用4体积的0.5% H3PO4冲洗。加入闪烁混合物，板在Microbeta闪烁计数器上读数。

细胞实验:

Induction of apoptosis by enzastaurin is measured by nucleosomal fragmentation and terminal deoxynucleotidyl transferase-mediated nick-end labeling (TUNEL) and staining in HCT116 and U87MG cell lines.Briefly,5×103 cells are plated per well in 96-well plates (1% FBS-supplemented media conditions),incubated with or without Enzastaurin for 48 to 72 hours.The absorbance values are normalized to those from control-treated cells to derive a nucleosomal enrichment factor at all concentrations as per the manufacturer's protocol.The concentrations studied ranges from 0.1 to 10μM.In situ TUNEL staining is assayed with the In situ Cell Death Detection.Cells (7.5×104) are plated per well in 6-well plates and incubated 72 hours in 1% FBS-supplemented media Enzastaurin.