AZD-3463
作者：齊岳
發(fā)布時(shí)間：2023-09-11
09:24:22
點(diǎn)擊數(shù)：
產(chǎn)品名稱：AZD-3463
產(chǎn)品描述：
| 產(chǎn)品描述 | AZD3463, an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency. |
| 靶點(diǎn)活性 | ALK:0.75 nM(Ki) |
| 體外活性 | 在體內(nèi),AZD-3463對(duì)突變型L1196M和野生型ALK的作用同等有效.在體內(nèi)作用于移植瘤時(shí),AZD-3463劑量依賴性抑制pALK,使體積停滯（H3122）或衰退（DEL,H2228）. |
| 體內(nèi)活性 | 在各種體外耐Crizotinib模型中,AZD3463對(duì)六分之五的細(xì)胞具有抗增殖的效力,4倍于親本H3122細(xì)胞。AZD3463對(duì)含ALK融合的細(xì)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。 |
| 激酶實(shí)驗(yàn) | 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. |
| 別名 | ALK/IGF1R inhibitor |
| 分子量 | 448.95 |
| 分子式 | C24H25ClN6O |
| CAS No. | 1356962-20-3 |
存儲(chǔ)
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 )
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