Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Birabresib (MK-8628) 是一种 BRD2/3/4抑制剂,IC50值为 92 到 112 nM 之间,具有潜在的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 282 | 现货 | ||
2 mg | ¥ 398 | 现货 | ||
5 mg | ¥ 822 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,160 | 现货 | ||
50 mg | ¥ 3,390 | 现货 | ||
100 mg | ¥ 4,990 | 现货 | ||
200 mg | ¥ 6,960 | 现货 | ||
500 mg | ¥ 10,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 888 | 现货 |
产品描述 | Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity. |
靶点活性 | BRDs:10-19 nM(EC50) |
体外活性 | OTX015 inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50 ranging from 92 to 112 nM, and inhibits the growth of a variety of human cancer cell lines with GI50 ranging from 60 to 200 nM. [1] OTX015 results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. [2] |
体内活性 | OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg bid, respectively. [1] |
激酶实验 | TR-FRET Assay <a href="#s_ref" class="sref">[1]: To assess binding of OTX015 to BRD2, BRD3, and BRD4, BRD-expressing CHO cell lysate (from CHO cells transfected with expression plasmids for Flag-tagged BRD2, BRD3, or BRD4 or vector alone), europium-conjugated anti-Flag antibody, XL-665-conjugated streptavidin, and biotinylated OTX015 are incubated at room temperature for 0.2 to 2 h. Fluorescence is measured by TR-FRET using an EnVision 2103 Multilabel Reader and EC50 for binding is calculated by nonlinear regression using PRISM version 5.02. |
细胞实验 | Effects of OTX015 on cancer cell proliferation are evaluated by incubating human tumor cells for 72 h with increasing concentrations of OTX015 and assessing proliferation using a tetrazolium salt (WST-8)-based colorimetric assay.(Only for Reference) |
别名 | OTX-015, OTX015 (MK 8628/Birabresib), MK-8628 |
分子量 | 491.99 |
分子式 | C25H22ClN5O2S |
CAS No. | 202590-98-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 9.8 mg/mL (20 mM)
DMSO: 49.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.0326 mL | 10.1628 mL | 20.3256 mL | 50.814 mL |
5 mM | 0.4065 mL | 2.0326 mL | 4.0651 mL | 10.1628 mL | |
10 mM | 0.2033 mL | 1.0163 mL | 2.0326 mL | 5.0814 mL | |
20 mM | 0.1016 mL | 0.5081 mL | 1.0163 mL | 2.5407 mL | |
DMSO | 50 mM | 0.0407 mL | 0.2033 mL | 0.4065 mL | 1.0163 mL |
100 mM | 0.0203 mL | 0.1016 mL | 0.2033 mL | 0.5081 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Birabresib 202590-98-5 Chromatin/Epigenetic Epigenetic Reader Domain OTX 015 Inhibitor OTX-015 OTX015 MK8628 MK 8628 MK 8628/Birabresib OTX015 (MK 8628/Birabresib) inhibit MK-8628 inhibitor