store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Oprozomib (PR-047) 是一种可口服的选择性肽环氧酮类蛋白酶体抑制剂,诱导多发性骨髓瘤细胞凋亡。它对蛋白酶体 (β5) 和免疫蛋白酶体 (LMP7) 的 IC50分别为 36 和 82 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 813 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 2,980 | 现货 | ||
100 mg | ¥ 4,390 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 949 | 现货 |
产品描述 | Oprozomib (PR-047) (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity. |
靶点活性 | 20S proteasome β5:36 nM, 20S proteasome LMP7:82 nM |
体外活性 | 在多种人类肿瘤移植瘤和小鼠同系模型中,Oprozomib能够抑制>80%蛋白酶,诱导抗肿瘤反应.Oprozomib经过重复口服后,在动物的大多数组织具有良好的安全性与耐受性. |
体内活性 | Oprozomib具有抗MM活性,可以抑制MM细胞的迁移和血管生成。Oprozomib也能抑制caspase-8,caspase-9,caspase-3和PARP的激活。 |
激酶实验 | ELISA-based active site binding assay: Samples (lysed cells or tissue homogenates) are treated for 1 h at room temperature with the biotinylated active site probe PR-584 (5-15 μM). Samples are denatured by addition of SDS (0.9% final) and heating to 100 °C for 5 min. The denatured samples are transferred to a 96-well or 384-well filter plat, mixed with streptavidin-sepharose beads (2.5-5 μL packed beads/well), and incubated for 1 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer (PBS, 1% bovine serum albumin, 0.1% Tween-20) by vacuum filtration. The beads are incubated overnight at 4 °C on a plate shaker with the following antibodies recognizing the six catalytic subunits diluted into ELISA buffer: β5, β1, and β2 diluted 1:3000, LMP7 and LMP2 diluted 1:5000, and MECL-1 diluted 1:1000. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and incubated with HRP-conjugated secondary antibody diluted 1:5000 in ELISA buffer and incubated 2 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and developed for chemiluminsecence signal using the supersignal ELISA pico substrate following the manufacturer's instructions. Luminescence is measured on a plate reader and converted to ng of proteasome or μg/ml of lysate by comparison with 20S proteasome or untreated cell lysate standard curves. For proteasome inhibitor studies, active site probe binding values are expressed as the percent of binding relative to DMSO treated cells. |
细胞实验 | MTT assay(Only for Reference) |
别名 | PR-047, 奥泼佐米, ONX 0912 |
分子量 | 532.61 |
分子式 | C25H32N4O7S |
CAS No. | 935888-69-0 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (174.6 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8775 mL | 9.3877 mL | 18.7755 mL | 46.9387 mL |
5 mM | 0.3755 mL | 1.8775 mL | 3.7551 mL | 9.3877 mL | |
10 mM | 0.1878 mL | 0.9388 mL | 1.8775 mL | 4.6939 mL | |
20 mM | 0.0939 mL | 0.4694 mL | 0.9388 mL | 2.3469 mL | |
50 mM | 0.0376 mL | 0.1878 mL | 0.3755 mL | 0.9388 mL | |
100 mM | 0.0188 mL | 0.0939 mL | 0.1878 mL | 0.4694 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。
Oprozomib 935888-69-0 Autophagy Proteases/Proteasome Ubiquitination Proteasome apoptosis inhibit bioavailable immunoproteasome LMP7 PR-047 PR047 PR 047 orally ONX0912 ONX-0912 Inhibitor epoxyketone 奥泼佐米 ONX 0912 inhibitor