奥希替尼甲磺酸盐|T3634|TargetMol

Osimertinib mesylate
1421373-66-1

￥155 1mg 起订

￥358 5mg 起订

￥500 10mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 奥希替尼甲磺酸盐

英文名称：: Osimertinib mesylate

CAS号：: 1421373-66-1

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.53%

产品类别：: 抑制剂

货号：: T3634

Product Introduction

Bioactivity

名称	Osimertinib mesylate
描述	Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
细胞实验	PC-9 cells were seeded into T75 flasks (5 × 10^5 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media was replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes were 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 were continued until a final concentration of 1.5μM gefitinib, 1.5μM afatinib, 1.5μM WZ4002 or 160nM AZD9291 were achieved [1].
激酶实验	Kinase assays were performed as per the EMD Millipore profiling service protocol using peptide or protein substrates in a filter-binding radioactive ATP transferase assay for protein [1].
动物实验	The generation of EGFRL858R and EGFRL858R+T790M mice (male and female) was previously described Doxycycline was administered by feeding mice (aprox 3 week old) with doxycycline-impregnated food pellets (625 ppm) and treated for about 3 months during which time tumors developed. Afatinib and AZD9291 were suspended in 1% Polysorbate 80 and administered via oral gavage once daily at the doses of 7.5 mg/kg and 5 mg/kg, respectively. Mice were imaged weekly at the Vanderbilt University Institute of Imaging Science. For immunoblot analysis, mice were treated for eight hours with drug as described before dissection and flash freezing of the lungs. Lungs were pulverized in liquid nitrogen before lysis as described above [1].
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 mesylate (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 mesylate (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 mesylate (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 mesylate (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 mesylate (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]
存储条件	store at low temperature,store under nitrogen \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 5.96 mg/mL (10 mM), Sonication is recommended. H2O : 33 mg/mL (55 mM), Sonication is recommended.
关键字	EGFR \| Osimertinib \| Osimertinib Mesylate \| PC-9 \| tumor xenograft model \| Osimertinib mesylate \| inhibit \| AZD9291 \| AZD-9291 \| cancer \| Inhibitor \| Epidermal growth factor receptor \| Mereletinib \| HER1 \| H1975 \| AZD 9291 \| Mereletinib Mesylate \| ErbB-1 \| AZD-9291 Mesylate \| Ba/F3 cells \| AZD9291 Mesylate \| AZD 9291 Mesylate
相关产品	Lapatinib \| Neratinib \| Chalcone \| Gefitinib \| Erlotinib \| Osimertinib \| Erlotinib hydrochloride \| Afatinib Dimaleate \| Lidocaine Hydrochloride hydrate \| Genistein
相关库	抑制剂库 \| 抗癌活性化合物库 \| 激酶抑制剂库 \| EMA 上市药物库 \| 高选择性抑制剂库 \| 膜蛋白靶向化合物库 \| 药物功能重定位化合物库 \| FDA 上市激酶抑制剂库 \| 酪氨酸激酶分子库 \| 抗癌药物库

奥希替尼甲磺酸盐|||甲磺酸奥希替尼|||Mereletinib mesylate|||AZD-9291 mesylate|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
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经营模式	贸易,试剂,定制,服务
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