OTX015（MK-8628，Birabresib） - CAS:202590-98-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	OTX015（MK-8628，Birabresib）
英文名称:	OTX015（MK-8628，Birabresib）
别名:	6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
CAS No:	202590-98-5	分子式:	C₂₅H₂₂ClN₅O₂S	分子量:	491.99
CAS No:	202590-98-5
分子式:	C₂₅H₂₂ClN₅O₂S
分子量:	491.99

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O10010 OTX015（MK-8628，Birabresib） ≥98%（HPLC） (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(20mg/mL)

产品描述：

基本信息

产品编号：O10010
产品名称：OTX015（MK-8628，Birabresib）
CAS:	202590-98-5	储存条件	粉末	-20℃	四年

分子式：	C25H22ClN5O2S		溶于液体	-80℃	六个月
分子量：	491.99			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	98mg/mL (199.19mM)
		Ethanol	98mg/mL (199.19mM)
		Water	Insoluble
	体内（现配现用）	2% DMSO+30% PEG 300+5% Tween 80+ddH2O	5mg/mL
＜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	2.0326mL	10.1628mL	20.3256mL
5mM	0.4065mL	2.0326mL	4.0651mL
10mM	0.2033mL	1.0163mL	2.0326mL
50mM	0.0407mL	0.2033mL	0.4065mL

生物活性

产品描述	一种有效的BET bromodomain抑制剂，靶向BRD2/3/4，EC50范围为10nM到19nM。
靶点/IC50	BRDs (Cell-free assay)
靶点/IC50	10-19nM(EC50)
体外研究	Birabresib (OTX-015) (500nM) exposure induces a strong decrease of BRD2,BRD4 and c-MYC and increase of HEXIM1 proteins, while BRD3 expression is unchanged.c-MYC,BRD2,BRD3,BRD4 and HEXIM1 mRNA levels do correlate however with viability following exposure to Birabresib (OTX-015).Birabresib (OTX-015) (0.1,1,5μM) treatment induces HIV-1 fulllength transcripts and viral outgrowth in resting CD4+T cells from infected individuals receiving suppressive antiretroviral therapy (ART),while exerting minimal toxicity and effects on T cell activation.Birabresib-mediated activation of HIV-1 involves an increase in CDK9 occupancy and RNAP II C-terminal domain (CTD) phosphorylation.
体内研究	In MDA-MB-231 murine xenografts,tumor mass is significantly (p<0.05) reduced by Birabresib (OTX-015) (50mg/kg) with respect to vehicle-treated animals.Birabresib (OTX-015) in combination with 2mg/kg RAD001 shows more effective activity than Birabresib alone.

推荐实验方法(仅供参考)

激酶实验：

TR-FRET 试验

为了评估OTX015与BRD2，BRD3，以及BRD4的结合，BRD表达的CHO细胞裂解物(来自感染表达质粒的CHO细胞， Flag标记的BRD2，BRD3，或BRD4 或仅载体)，铕共轭的抗Flag抗体，XL-665共轭的链霉亲和素，和生物素化的OTX015在室温下培育0.2到2小时。荧光性通过TR-FRET使用EnVision 2103多标阅读器测量，结合的EC50使用5.02版PRISM通过非线性回归计算。

细胞实验:

For the MTT assay,cells are seeded in 24-well plates at 1×106 per well and treated with Birabresib (OTX-015) (0.01nM-10μM) for 72h.Cells are transferred to 96-well plates and incubated with 0.5mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) in the dark at 37℃for 4h.Cells are then lysed with 25% sodium dodecyl sulfate (SDS) lysis buffer and absorbance is read at 570nm using a Microplate Reader.Three independent experiments are run for each cell line and untreated cells are used as negative controls.

动物实验:

Mice are subcutaneously injected in the right flank with 10×106 MDA-MB-231 cells.When average tumor weight is appr 130mg,mice are randomized (nine animals/group) to one of the following experimental groups:vehicle (for Birabresib (OTX015),water,twice daily,oral;for RAD001 vehicle, 5% Tween-80/5% polyethylene glycol 400,thrice weekly,intraperitoneal);50mg/kg Birabresib (OTX-015),twice daily,oral;2mg/kg RAD001,thrice weekly,intraperitoneal;50mg/kg Birabresib (OTX015) +2mg/kg RAD001,according to the single agent dosing schedules.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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