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(S)-crizotinib (ent-crizotinib) 是一种选择性MTH1(mutT 同源物)抑制剂,IC50为 330 nM。它通过抑制 MTH1 破坏核苷酸库的稳态,诱导 DNA 单链断裂的增加,激活人结肠癌细胞的 DNA 修复,在动物模型中抑制肿瘤生长。
(S)-crizotinib (ent-crizotinib) 是一种选择性MTH1(mutT 同源物)抑制剂,IC50为 330 nM。它通过抑制 MTH1 破坏核苷酸库的稳态,诱导 DNA 单链断裂的增加,激活人结肠癌细胞的 DNA 修复,在动物模型中抑制肿瘤生长。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 218 | 现货 | |
2 mg | ¥ 297 | 现货 | |
5 mg | ¥ 496 | 现货 | |
10 mg | ¥ 745 | 现货 | |
25 mg | ¥ 1,230 | 现货 | |
50 mg | ¥ 1,820 | 现货 | |
100 mg | ¥ 2,880 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 546 | 现货 |
产品描述 | (S)-crizotinib (ent-crizotinib) (IC50 of 72 nM), an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib. |
靶点活性 | MTH1:72 nM |
体外活性 | 在SW480 结肠癌模型中,每天口服 50?mg/kg(S)-Crizotinib能够阻碍肿瘤的生长. |
体内活性 | (S)-crizotinib能够激活人结肠癌细胞中DNA修复机制,它抑制MTH1从而破坏核苷酸库的稳态,进一步诱导DNA单链断裂的增加。 |
激酶实验 | MTH1 catalytic assay: Half-maximal inhibitory concentrations (IC50) are determined using a luminescence-based assay with some minor modifications. Briefly, serial dilutions of compounds are dissolved in assay buffer (100?mM Tris-acetate pH?7.5, 40?mM NaCl and 10?mM Mg(OAc)2 containing 0.005% Tween-20 and 2?mM dithiothreitol (DTT). Upon addition of MTH1 recombinant protein (final concentration 2?nM), plates are incubated on a plate shaker for 15?min at room temperature. After addition of the substrate dGTP (final concentration 100?μM), 8-oxo-dGTP (final concentration 13.2?μM), or 2-OH-dATP (final concentration 8.3?μM) the generation of pyrophosphate (PPi) as a result of nucleotide triphosphate hydrolysis by MTH1 is monitored over a time course of 15?min using the PPi Light Inorganic Pyrophosphate Assay kit. IC50 values are determined by fitting a dose-response curve to the data points using nonlinear regression analysis using the GraphPad Prism software. |
细胞实验 | One day before treatment, cells are seeded per well in six-well plates and incubated for 24 h. The next day DMSO (equal to highest amount of compound dilution, maximum 0.2%) or compounds in increasing concentrations were added and cells incubated at 37 °C, 5% CO2, for 7-10 days. After washing with PBS, cells are fixed with ice-cold methanol, stained with crystal violet solution (0.5% in 25% methanol) and left to dry overnight. For quantification of results, ultraviolet absorbance of crystal violet is determined at 595 nm following solubilisation by 70% ethanol. Data are analysed using nonlinear regression analysis using the GraphPad Prism software. (Only for Reference) |
别名 | ent-crizotinib |
分子量 | 450.34 |
分子式 | C21H22Cl2FN5O |
CAS No. | 1374356-45-2 |
Smiles | C[C@H](Oc1cc(cnc1N)-c1cnn(c1)C1CCNCC1)c1c(Cl)ccc(F)c1Cl |
密度 | 1.47 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | 1eq. HCl: 9 mg/mL (20 mM)), Heating is recommended. DMSO: 22.5 mg/mL (50 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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