Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pimasertib (AS703026) 是一种高效选择性和ATP 非竞争性的MEK1/2抑制剂,可用于癌症研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 415 | 现货 | ||
10 mg | ¥ 541 | 现货 | ||
50 mg | ¥ 1,497 | 现货 | ||
100 mg | ¥ 2,376 | 现货 | ||
200 mg | ¥ 2,995 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 456 | 现货 |
产品描述 | Pimasertib (AS703026) is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. |
靶点活性 | MEK1/2 (MM cell line):5 nM-2 μM |
体外活性 | 10 mg/kg AS703026抑制人类K-Ras突变 (D-MUT) 的结肠直肠移植瘤生长,且明显降低p-ERK水平.15和30 mg/kg AS703026明显抑制人类浆细胞H929 mM移植瘤生长,这可能与下调的pERK1/2,诱导的PARP切割和微血管减少相关. |
体内活性 | AS703026(10 μM)能有效抑制携带K-Ras突变等位基因(D-MUT)的人DLD-1结直肠癌细胞中的ERK途径,增殖和转化。AS703026抑制人类多发性骨髓瘤细胞(包括U266和INA-6细胞)生长和存活,IC50分别为5和11 nM。AS703026的这种抑制作用由G0-G1细胞周期停滞介导,并伴随MAF致癌基因表达减少。在存在或不存在骨髓基质细胞(BMSC)的情况下,AS703026通过半胱天冬酶-3和PARP在MM细胞中裂解进一步诱导细胞凋亡。 AS703026可有效治疗由K-Ras突变引起的结直肠癌。 |
激酶实验 | The Aurora kinase activity is measured with 10 μM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif. |
细胞实验 | Method: Measuring incorporation of 14C-labelled thymidine into newly synthesized DNA within the cells to determine the ability of JNJ-7706621 to inhibit the proliferation of cell growth. Cells are trypsinized and counted and 3-8 ×103 cells are added to each well of a 96-well CytoStar tissue culture treated scintillating microplate in 100 μL complete medium in a volume. Cells are incubated for 24 hours at 37 °C in an atmosphere containing 5% CO2. Next, 1 μL JNJ-7706621 is added to the wells of the plate. Cells are incubated for another 24 hours. Methyl 14C-thymidine 56 mCi/mmol is diluted in complete medium and 0.2 μCi/well is added to each well of the CytoStar plate in a volume of 20 μL. The plate is incubated for 24 hours at 37 °C in JNJ-7706621 with 14C-thymidine. The contents of the plate are discarded and the plate is washed twice with 200 μL PBS. 200 μL of PBS is added to each well. The top of the plate is sealed with a transparent plate sealer and a white plate backing sealer is applied to the bottom of the plate. The degree of methyl 14C-thymidine incorporation is quantified on a Packard Top Count. |
别名 | AS703026, MSC1936369B, N-[(2S)-2,3-二羟基丙基]-3-[(2-氟-4-碘苯基)氨基]-4-吡啶甲酰胺, SAR 245509 |
分子量 | 431.2 |
分子式 | C15H15FIN3O3 |
CAS No. | 1236699-92-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 80 mg/mL (185.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3191 mL | 11.5955 mL | 23.1911 mL | 57.9777 mL |
5 mM | 0.4638 mL | 2.3191 mL | 4.6382 mL | 11.5955 mL | |
10 mM | 0.2319 mL | 1.1596 mL | 2.3191 mL | 5.7978 mL | |
20 mM | 0.116 mL | 0.5798 mL | 1.1596 mL | 2.8989 mL | |
50 mM | 0.0464 mL | 0.2319 mL | 0.4638 mL | 1.1596 mL | |
100 mM | 0.0232 mL | 0.116 mL | 0.2319 mL | 0.5798 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。
Pimasertib 1236699-92-5 MAPK MEK AS703026 MAPKK MSC1936369B Inhibitor SAR245509 inhibit N-[(2S)-2,3-二羟基丙基]-3-[(2-氟-4-碘苯基)氨基]-4-吡啶甲酰胺 MAP2K Mitogen-activated protein kinase kinase SAR 245509 AS-703026 AS 703026 SAR-245509 inhibitor