AZD-3463
作者：齐岳
发布时间：2023-09-11
09:24:22
点击数：
产品名称：AZD-3463
产品描述：
| 产品描述 | AZD3463, an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency. |
| 靶点活性 | ALK:0.75 nM(Ki) |
| 体外活性 | 在体内,AZD-3463对突变型L1196M和野生型ALK的作用同等有效.在体内作用于移植瘤时,AZD-3463剂量依赖性抑制pALK,使肿瘤体积停滞（H3122）或衰退（DEL,H2228）. |
| 体内活性 | 在各种体外耐Crizotinib模型中,AZD3463对六分之五的细胞具有抗增殖的效力,4倍于亲本H3122细胞。AZD3463对含ALK融合的肿瘤细胞系均有效果,包括DEL(ALCL NPM-ALK),H2228(NSCLC EML4-ALK)和H3122(NSCLC EML4-ALK),抑制ALK并降低其自身磷酸化。 |
| 激酶实验 | HDAC enzymatic assays: Tubastatin A is dissolved and diluted in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine) to 6-fold of the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with Tubastatin A for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated. |
| 别名 | ALK/IGF1R inhibitor |
| 分子量 | 448.95 |
| 分子式 | C24H25ClN6O |
| CAS No. | 1356962-20-3 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
DMSO: 23 mg/mL (51.2 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
