生物试剂
>
生化试剂
>
信号通路
> Birabresib
加入收藏 取消收藏

Birabresib  99.2973%(HPLC)

促销价¥{{model.attbuying.price}}

市场价¥0.00

累计销量0 累计评价0 人评论

别称 {{model.alias}}
中文名称 {{model.name}}
英文名称 {{model.enname}}
品牌 {{model.brand}}
CAS {{model.cas}}
分子式
分子量 {{model.molecularweight}}
MDL {{model.mdl}}
货号 {{model.procode}}
数量

+ -

件 库存{{model.attbuying.number}}件
立即购买 加入购物车 下载说明书

看了又看
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) 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℃

猜你喜欢