Powder: -20°C for 3 years | In solvent: -80°C for 1 year
OICR-9429 是一个新颖的相互作用的小分子Wdr5-MLL 拮抗剂,IC50是 5 uM,在体外抑制急性髓性白血病细胞。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 279 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 632 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,890 | 现货 | ||
50 mg | ¥ 3,280 | 现货 | ||
100 mg | ¥ 5,290 | 现货 | ||
500 mg | ¥ 10,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 779 | 现货 |
产品描述 | OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro. |
靶点活性 | WDR5:93 nM(Kd) |
体外活性 | OICR-9429 binds WDR5 with high affinity (Kd=93±28 nM) and competitively disrupts its interaction with a high-affinity Wdr5-interacting (WIN) peptide of MLL (Kdisp=64±4 nM)[1]. |
激酶实验 | AR binding affinity: AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1?nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100?μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100?μL of supernatant fraction in 200?μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4?°C. |
细胞实验 | 20,000 viable, actively proliferating primary human AML cells per well were seeded in 96-well plates in triplicates and treated with 0.05% DMSO or OICR-9429. Cell viability was measured using the Cell Titer-Glo luminescent cell viability assay on a VICTOR X4 luminometer after 72 h.(Only for Reference) |
别名 | OICR 9429 |
分子量 | 555.59 |
分子式 | C29H32F3N5O3 |
CAS No. | 1801787-56-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 38 mg/mL (68.39 mM)
Ethanol: 12 mg/mL(21.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.7999 mL | 8.9994 mL | 17.9989 mL | 44.9972 mL |
5 mM | 0.36 mL | 1.7999 mL | 3.5998 mL | 8.9994 mL | |
10 mM | 0.18 mL | 0.8999 mL | 1.7999 mL | 4.4997 mL | |
20 mM | 0.09 mL | 0.45 mL | 0.8999 mL | 2.2499 mL | |
DMSO | 50 mM | 0.036 mL | 0.18 mL | 0.36 mL | 0.8999 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。
OICR-9429 1801787-56-3 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Histone Methyltransferase JAK pancreatic MLL inhibit colon prostate cance OICR9429 bladder cancer (BCa) Inhibitor WD repeat domain 5 (WDR5) Apoptosis leukaemia H3K4 OICR 9429 inhibitor