Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ceralasertib (AZD6738) 是一种具有口服活性的选择性 ATR 激酶抑制剂,IC50 为 1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 469 | 现货 | ||
2 mg | ¥ 671 | 现货 | ||
5 mg | ¥ 970 | 现货 | ||
10 mg | ¥ 1,516 | 现货 | ||
25 mg | ¥ 2,823 | 现货 | ||
50 mg | ¥ 3,980 | 现货 | ||
100 mg | ¥ 5,680 | 现货 | ||
500 mg | ¥ 11,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 915 | 现货 |
产品描述 | Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. |
靶点活性 | ATR:1 nM |
体外活性 | In four Kras mutant cell lines: H23, H460, A549, and H358,AZD6738 inhibits ATR kinase activity and impairs cell viability. AZD6738 strongly synergizes with cisplatin in an ATM-deficient NSCLC cell line in vitro[1]. In p53 or ATM defective cells, AZD6738 treatment resulted in replication fork stalls and accumulation of unrepaired DNA damage, as evidenced by γH2AX and 53BP1 foci formation, which was carried through into mitosis, resulting in cell death by mitotic catastrophe[2]. |
体内活性 | The combination of 50 mg/kg AZD6738 and cisplatin resulted in a 75.5% mean tumor growth inhibition (TGI) of H460 xenografts at day 14 (P ≤ 0.0001 compared to vehicle). Growth of tumors treated with the combination was also significantly different from that of tumors treated with cisplatin or AZD6738 alone [1]. In LoVo derived mouse xenograft, a combination of AZD6738 (50?mg/kg)?+?IR (2?Gy) can be adjusted to avoid toxicity while still maintaining efficacy[3]. |
激酶实验 | General procedure for the EC50 test: DDR1 is induced by 2 Gg/ml doxycycline for 48 hrs prior to DDR1 activation by rat tail collagen I. The DDR1 over-expressed U2OS is pre-treated by media containing each concentration of the compound for 1 hr and treated by changing the media to the EC50 test media containing 10 Gg/ml collagen and each concentration of the compound for 2 hrs. Each cells is washed with cold PBS three times and lysed with the lysis buffer (50 mMTris, pH 7.5, 1% Triton X-100, 0.1% SDS, 150 mM NaCl, 5 mM EDTA, 100 mMNaF, 2 mM Na3VO4, 1 mM PMSF, 10 Gg/ml aprotinin, and 10 Gg/ml leupeptin). The activation of DDR1 is quantified by density using program ImageJ to determine EC50 following Western blot using anti-activated human DDR1b (Y513). |
细胞实验 | Cells are treated in white walled, clear bottom 96-well plates with the indicated doses of AZD6738, cisplatin, gemcitabine, or combination for 48 h. ATP levels are assessed as surrogate measure of viability was assessed using the CellTiter-Glo Luminescent Cell Viability Assay and Safire 2 plate reader. Raw data are corrected for background luminescence prior to further analysis. For AZD6738 treatment, log dose response curves are generated in GraphPad Prism 6 by nonlinear regression (log(inhibitor) vs. response with variable slope) of log-transformed (x = log(x)) data normalized to the mean of untreated controls. GI values, defined as the dose X at which Y = 50%, were extrapolated from dose response curves. |
别名 | AZD6738 |
分子量 | 412.51 |
分子式 | C20H24N6O2S |
CAS No. | 1352226-88-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 39 mg/mL (94.5 mM)
5% DMSO+95% Saline: 3.8 mg/mL (9.21 mM, suspension)
DMSO: 55 mg/mL (133.33 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / 5% DMSO+95% Saline / DMSO | 1 mM | 2.4242 mL | 12.1209 mL | 24.2418 mL | 60.6046 mL |
5 mM | 0.4848 mL | 2.4242 mL | 4.8484 mL | 12.1209 mL | |
Ethanol / DMSO | 10 mM | 0.2424 mL | 1.2121 mL | 2.4242 mL | 6.0605 mL |
20 mM | 0.1212 mL | 0.606 mL | 1.2121 mL | 3.0302 mL | |
50 mM | 0.0485 mL | 0.2424 mL | 0.4848 mL | 1.2121 mL | |
DMSO | 100 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.606 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。
Ceralasertib 1352226-88-0 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR inhibit Ataxia telangiectasia mutated ATM and RAD3 related Inhibitor AZD 6738 AZD-6738 AZD6738 inhibitor