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Osimertinib

Osimertinib

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产品编号 T2490   CAS 1421373-65-0
别名: AZD-9291, Mereletinib, 奥希替尼

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。

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Osimertinib Chemical Structure
Osimertinib, CAS 1421373-65-0
规格 价格/CNY 货期 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 * 10 mM (in DMSO) ¥ 535 现货
其他形式的 Osimertinib:
618惊喜特惠 4重福利大放送
药物设计专题培训
产品目录号及名称: Osimertinib (T2490)
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纯度: 100%
纯度: 100%
纯度: 99.83%
纯度: 99.54%
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生物活性
化学信息
存储 & 溶解度
参考文献
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 AZD-9291, Mereletinib, 奥希替尼
化合物与蛋白结合的复合物

T2490_1

Crystal Structure of EGFR(L858R/T790M/C797S) in complex with Osimertinib

分子量 499.61
分子式 C28H33N7O2
CAS No. 1421373-65-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 22 mg/mL(44 mM)

DMSO: 55 mg/mL (110.09 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.0016 mL 10.0078 mL 20.0156 mL 50.039 mL
5 mM 0.4003 mL 2.0016 mL 4.0031 mL 10.0078 mL
10 mM 0.2002 mL 1.0008 mL 2.0016 mL 5.0039 mL
20 mM 0.1001 mL 0.5004 mL 1.0008 mL 2.502 mL
DMSO 50 mM 0.04 mL 0.2002 mL 0.4003 mL 1.0008 mL
100 mM 0.02 mL 0.1001 mL 0.2002 mL 0.5004 mL

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TargetMol Library Books参考文献

1. Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750. 2. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. 3. Wang N, et al. Osimertinib (AZD9291) increases radio‑sensitivity in EGFR T790M non‑small cell lung cancer. Oncol Rep. 2019 Jan;41(1):77-86. 4. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. 5. Nanjo S, et al. High efficacy of third generation EGFR inhibitor AZD9291 in a leptomeningeal carcinomatosis model with EGFR-mutant lung cancer cells. Oncotarget. 2016 Jan 26;7(4):3847-56.

TargetMol Library Books文献引用

1. Liu Y, Lai M, Li S, et al. LS‐106, a novel EGFR inhibitor targeting C797S, exhibits anti‐tumor activities both in vitro and in vivo. Cancer Science. 2021 2. Lv S, Pan Q, Lu W, et al.Tenovin 3 induces apoptosis and ferroptosis in EGFR 19del non small cell lung cancer cells.Scientific Reports.2024, 14(1): 7654. 3. Yu J, Zhang L, Peng J, et al. Dictamnine, a novel c-Met inhibitor, suppresses the proliferation of lung cancer cells by downregulating the PI3K/AKT/mTOR and MAPK signaling pathways. Biochemical pharmacology. 2022, 195: 114864. 4. Shang J, Ning S, Chen Y, et al. MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer. Acta Pharmacologica Sinica. 2021, 42(1): 120-131 5. Jin Y, Zhang Y, Huang A, et al.Overexpression of SERPINA3 suppresses tumor progression by modulating SPOP/NF‑κB in lung cancer.International Journal of Oncology.2023, 63(2): 1-16. 6. Liang J, Bi G, Sui Q, et al.Transcription factor ZNF263 enhances EGFR-targeted therapeutic response and reduces residual disease in lung adenocarcinoma.Cell Reports.2024, 43(2). 7. Tan J, Zhu L, Shi J, et al.Evaluation of drug resistance for EGFR-TKIs in Lung Cancer via Multicellular lung-on-a-chip.European Journal of Pharmaceutical Sciences.2024: 106805. 8. Zhang Y, Chen Y, Wang B, et al.A novel selenium nanocomposite modified by AANL inhibits tumor growth by upregulating CLK2 in lung cancer.Bioorganic Chemistry.2024: 107459. 9. Wei X, Zhang G, Liu Q, et al.Almonertinib and alflutinib show novel inhibition on rare EGFR S768I mutant cells.Clinical and Translational Oncology.2024: 1-16.
20(S)-Ginsenoside Rg3 Nuvenzepine Labuxtinib PROTAC EGFR degrader 8 Poziotinib hydrochloride ALK/EGFR-IN-1 EGFR/ErbB-2 inhibitor-1 Avitinib maleate

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抗癌活性化合物库 抗癌临床化合物库 抗癌药物库 药物功能重定位化合物库 膜蛋白靶向化合物库 EMA 上市药物库 激酶抑制剂库 高选择性抑制剂库 抗癌上市药物库

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Keywords

Osimertinib 1421373-65-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR AZD-9291 AZD 9291 Inhibitor Ba/F3 cells H1975 PC-9 tumor xenograft model ErbB-1 AZD9291 HER1 inhibit cancer Mereletinib 奥希替尼 Epidermal growth factor receptor inhibitor

 

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