Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CP-466722 是一种有效且可逆的 ATM 抑制剂,IC50值为 4.1 μM。它不会抑制细胞中的 ATR 和 PI3K 或 PIKK 家族成员。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 282 | 现货 | ||
2 mg | ¥ 395 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 1,160 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,160 | 现货 | ||
100 mg | ¥ 4,660 | 现货 | ||
500 mg | ¥ 9,950 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 792 | 现货 |
产品描述 | CP-466722, an effective and reversible ATM inhibitor, does not inhibit ATR and PI3K or PIKK family members in cells. |
靶点活性 | ATM:410 nM |
体外活性 | CP-466722 is used as a potential inhibitor to inhibits the activity of ATM kinase, which phosphorylates GST-p53(1–101) substrate. CP-466722 also exhibits the decreasing activities against abl and src kinases. In MCF-7 human breast cancer cells and primary and immortalized diploid human fibroblasts, CP-466722 suppress ATM-dependent p53 induction. In HeLa cells, CP-466722(6 μM), leads to the inhibition in ATM-dependent phosphorylation by reversibly inhibiting ionizing radiation (IR)-induced ATM kinase activity. |
激酶实验 | In vitro kinase assays [1] : To screen for small molecule inhibitors of ATM kinase activity, an in vitro kinase assay is adapted, and an ELISA assay develops which measured the phosphorylation status of the ATM downstream target p53. Recombinant GST-p53(1-101) and full-length Flag-tagged ATM & ATR are purified for use in the ELISA and in vitro kinase assays. Briefly, Nunc 96 well Maxisorp plates are coated overnight (4 °C) with 2μg of purified, recombinant GST-p53(1-101) in PBS. All subsequent incubations are performed at room temperature. The plates are washed (0.05%v/v-Tween/PBS) before addition of purified recombinant full-length ATM kinase (30 ng–60 ng) in a final volume of 80μL of reaction buffer (20 mM HEPES, 50 mM NaCl, 10 mM MgCl2, 10 mM MnCl2, 1 mM DTT and 1 μM ATP) in the presence or absence of CP-466722. CP-466722 (10 μM) is added to plates in duplicate and the kinase assay is incubated (90 minutes). Plates are washed (0.05%v/v-Tween/PBS), blocked (1hour, 1%w/v-BSA/PBS) and rinsed before anti-Phospho(Ser15)-p53 antibody (1:1000/PBS) is added to the plates and incubated (1hour). To reduce non-specific binding plates are washed (0.05%v/v-Tween/PBS) prior to incubation (1hour) with HRP-conjugated goat anti-rabbit IgG secondary antibody (1:5000/PBS). Secondary antibody that is linked to the phosphorylated GST-p53(1–101) protein is detected with TMB substrate reagent. Plates are developed (15 minutes–30 minutes) and the reaction is stopped (1 M H2SO4 final concentration) before absorbance is determined (λ450 nM). CP-466722 that inhibits ATM kinase activity in ELISA assays, are characterized with respect to inhibition of ATM/ATR kinases using in vitro kinase assays. Western blotting using the anti-Phospho(Ser15)-p53 antibody is used as a readout of ATM/ATR inhibition. Extended analysis of CP466722 (10 μM) against a commercially available panel of kinases is performed by Upstate. |
细胞实验 | HeLa or A-T (GM02052 expressing hTERT) cells are plated in triplicate and incubated for 24 hours. Cells are pre-treated: DMSO, CP466722 or KU55933 prior to IR (0-10 gy). Cells are incubated for 4 hours following IR before media is removed, cells washed (PBS), trypsined, counted and re-plated (2000 cells/plate, 10 cm plates) in the absence of drug and incubated for 10 days. Prior to colony counting, cells are washed (PBS), stained (PBS, 0.0037%v/v-formaldehyde, 0.1%w/v-crystal violet), rinsed (dWater) and dried. Defined populations (>50 cells) are counted as one surviving colony, data are calculated as percentage surviving colonies relative to control plates +/− SE. (Only for Reference) |
别名 | CP 466722, CP466722 |
分子量 | 349.35 |
分子式 | C17H15N7O2 |
CAS No. | 1080622-86-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7 mg/mL (20.04 mM), Need warming
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8625 mL | 14.3123 mL | 28.6246 mL | 71.5615 mL |
5 mM | 0.5725 mL | 2.8625 mL | 5.7249 mL | 14.3123 mL | |
10 mM | 0.2862 mL | 1.4312 mL | 2.8625 mL | 7.1561 mL | |
20 mM | 0.1431 mL | 0.7156 mL | 1.4312 mL | 3.5781 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。
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