Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD-5438 有效抑制 CDK1,CDK2,CDK9,IC50值分别为 16 nM, 6 nM, 20 nM,但它对 GSK3β,CDK5,CDK6 的抑制作用较弱。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 252 | 现货 | ||
5 mg | ¥ 568 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 3,490 | 现货 | ||
100 mg | ¥ 5,130 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 568 | 现货 |
产品描述 | AZD-5438 is an effective inhibitor of CDK, for CDK1(IC50=16 nM), CDK2(IC50=6 nM), CDK9(IC50=20 nM). |
靶点活性 | CDK1:16 nM, CDK9:20 nM, CDK2:6 nM |
体外活性 | 在SW620异种移植物模型中,AZD5438对于各种细胞周期蛋白(phH3,磷酸核仁素,PP1a等)有以剂量依赖的抑制作用.对于不同类型的癌症(乳腺癌,结肠癌,肺癌,前列腺癌和卵巢癌),AZD5438通过口服可以对肿瘤产生抑制作用. |
体内活性 | AZD5438会抑制p25-cdk5和糖原合成激酶3β的激酶活性,IC50分别为14 nM和17 nM。 在肿瘤细胞系中(肺,结肠直肠,乳腺,前列腺,和血液肿瘤),AZD5438(IC50=0.2 -1.7 μM)通过抑制cdk-依赖性底物的磷酸化作用诱导细胞周期阻滞,从而抑制细胞增殖。在细胞周期素依赖性激酶中,AZD5438对于其活性能够有效抑制,E-cdk2(IC50=6 nM),A-cdk2(IC50=45 nM),B1-cdk1(IC50=16 nM),D3-cdk6(IC50=21 nM),T-cdk9(IC50=20 nM)。 |
激酶实验 | Recombinant Kinase Assays [1]: The ability of AZD5438 to inhibit cdk activity is examined using a scintillation proximity assay with recombinant cdk-cyclin complexes of cyclin-Ecdk2, cdk2-cyclin A, cdk4-cyclin D, and recombinant retinoblastoma substrate (amino acids 792-928) or cdk1-cyclin B1 with a peptide substrate derived from the in vitro p34cdc2 phosphorylation site of histone H1 (biotin-X-Pro-Lys-Thr-Pro-Lys-Lys-Ala-Lys-Lys-Leu). The activity of AZD5438 against recombinant cdk5/p25 (at 2 μM ATP) is determined in a scintillation proximity assay-based assay using peptide substrate (AKKPKTPKKAKKLOH). Inhibition of glycogen synthase kinase 3β activity is determined with scintillation proximity assay based on the use of human purified glycogen synthase kinase 3βenzyme and eukaryotic initiation factor 2B substrate (at 1 μM ATP). AZD5438 is screened against active recombinant human cdk6-cyclin D3, cdk7-cyclin H/MAT1 (cdk activating kinase complex), and cdk9-cyclin T using the kinase selectivity screening service. |
细胞实验 | AZD5438 is tested against solid tumor cell lines. Briefly, cells are incubated for 48 hours with AZD5438 at a range of concentrations. At the end of incubation, the cells are pulsed with 5-bromo-2′-deoxyuridine (BrdUrd) and the amount of DNA synthesis is measured. The IC50 for inhibition of proliferation is specifically determined independently of cell death. Multiple myeloma cell lines are seeded into 96-well plates in RPMI 1640 supplemented with 10% FCS and glutamine and dosed with AZD5438 for 72 hours. Cell growth is measured using AlamarBlue and GI50 values are calculated with reference to pretreatment control values.(Only for Reference) |
别名 | AZD5438 |
分子量 | 371.46 |
分子式 | C18H21N5O2S |
CAS No. | 602306-29-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 63 mg/mL(169.6 mM)
DMSO: 74 mg/mL (199.21 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.6921 mL | 13.4604 mL | 26.9208 mL | 67.302 mL |
5 mM | 0.5384 mL | 2.6921 mL | 5.3842 mL | 13.4604 mL | |
10 mM | 0.2692 mL | 1.346 mL | 2.6921 mL | 6.7302 mL | |
20 mM | 0.1346 mL | 0.673 mL | 1.346 mL | 3.3651 mL | |
50 mM | 0.0538 mL | 0.2692 mL | 0.5384 mL | 1.346 mL | |
100 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.673 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。
AZD-5438 602306-29-6 Cell Cycle/Checkpoint CDK Cyclin dependent kinase AZD5438 inhibit AZD 5438 Inhibitor inhibitor