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Osimertinib (AZD-9291) 是一种 EGFR 三代抑制剂,抑制二代 EGFR 抑制剂产生的 T790M 耐药突变,具有不可逆性和口服活性。Osimertinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。
Osimertinib (AZD-9291) 是一种 EGFR 三代抑制剂,抑制二代 EGFR 抑制剂产生的 T790M 耐药突变,具有不可逆性和口服活性。Osimertinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 198 | 现货 | |
2 mg | ¥ 283 | 现货 | |
5 mg | ¥ 473 | 现货 | |
10 mg | ¥ 653 | 现货 | |
25 mg | ¥ 987 | 现货 | |
50 mg | ¥ 1,230 | 现货 | |
100 mg | ¥ 1,660 | 现货 | |
200 mg | ¥ 2,570 | 现货 | |
500 mg | ¥ 4,730 | 现货 | |
1 g | ¥ 6,490 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 535 | 现货 |
产品描述 | Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer. |
靶点活性 | EGFR (WT):493.8 nM, EGFR (L858R/T790M):11.44 nM, EGFR (exon 19 deletion):12.92 nM |
体外活性 | 方法:人非小细胞肺癌细胞 PC-9 (exon 19del)、H3255 (L858R)、PC-9ER (exon 19del+T790M) 和 H1975 (L858R+T790M) 用 Osimertinib (0.0001-10 µmol/L) 处理 72 h,使用 MTS 方法检测细胞生长抑制情况。 结果:Osimertinib 剂量依赖诱导 PC-9、H3255、PC-9ER 和 H1975 细胞生长,IC50 分别为 41、26、41 和 31 nM。[1] 方法:EGFR 突变的人非小细胞肺癌细胞 PC-9、H1975、H1650 和 H3255 用 Osimertinib (0.1-1000 nM) 处理 6 h,使用 Western Blot 方法检测靶点蛋白表达水平。 结果:Osimertinib 抑制 EGFR 突变肿瘤细胞的 pEGFR(Y1068)、pERK(P-p44/42)、pAKT(S473)。[2] 方法:人非小细胞肺癌细胞 NCI-H1975 用 Osimertinib (10-100 nM) 处理 24 h,然后用 2-20 Gy 的剂量照射,使用 Flow Cytometry 方法分析细胞周期情况。 结果:联合治疗组 G2/M 和 S 期细胞比例呈剂量依赖性降低。Osimertinib 减少照射后 G2/M 期细胞周期停滞。[3] |
体内活性 | 方法:为检测体内抗肿瘤活性,将 Osimertinib (5-10 mg/kg) 口服给药给携带人肺癌肿瘤 H1975、PC9 和 A431 的 SCID 小鼠,每天一次,持续七天。 结果:Osimertinib 治疗显著抑制 H1975、PC9 和 A431 肿瘤的生长,表明在体内具有抗肿瘤活性。[4] 方法:为检测体内抗肿瘤活性,将 Osimertinib (6 mg/kg) 口服给药给用 PC-9/ffluc 细胞构建软脑膜癌病 (LMC) 模型的 SHO-SCID 小鼠,每天一次,持续五十天。 结果:Osimertinib 治疗明显延缓了 LMC 的发展。第三代 EGFR-TKI Osimertinib 可能是由 EGFR 突变型肿瘤引起的第一代或第二代 EGFR-TKI 耐药性 LMC 的有效治疗方法。[5] |
激酶实验 | ACY-1215 is dissolved and subsequently 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 the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 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[1]. |
细胞实验 | AZD-9291 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM Gefitinib, 1.5 μM Afatinib, 1.5 μM WZ4002 or 160 nM AZD-9291 are achieved[1]. |
别名 | 奥希替尼, Mereletinib, AZD-9291 |
分子量 | 499.61 |
分子式 | C28H33N7O2 |
CAS No. | 1421373-65-0 |
Smiles | CN1C=C(C=2C1=CC=CC2)C3=NC(NC4=C(OC)C=C(N(CCN(C)C)C)C(NC(C=C)=O)=C4)=NC=C3 |
密度 | 1.19 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 | Ethanol: 22 mg/mL (44 mM) DMSO: 55 mg/mL (110.09 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 9.2 mg/mL (18.41 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||||||||||||
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