计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Oritinib (SH-1028), an irreversible third-generation EGFR TKI , overcomes T790M-mediated resistance in non-small cell lung cancer . Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR WT , EGFR L858R , EGFR L861Q , EGFR L858R/T790M , EGFR d746-750 and EGFR d746-750/T790M kinases, with IC 50 s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively
In Vitro
Oritinib (SH-1028) binds irreversibly to EGFR kinase by targeting cysteine-797 residue in the ATP binding site via covalent bond formation. Oritinib (0.001-10 μM) potently and selectively targets mutant EGFR cell lines in vitro. Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells at lower concentrations or even drug-free for at least 6 h. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: A431 (EGFR WT ), H3255 (EGFR L858R ), PC-9 (EGFR d746-750 ) and NCI-H1975 (EGFR L858R/T790M ) cells Concentration: 0.001, 0.01, 0.1, 1, and 10 μM Incubation Time: 72 hours Result: Selectively inhibited EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC 50 s of 3.93±1.12, 9.39±0.88 and 7.63±0.18 nmol/L, respectively, which were about 198-, 83- and 102-fold more sensitive than the inhibition of wild-type EGFR in A431 cells (IC 50 =778.89±134.74 nM).
In Vivo
Oral administration of Oritinib at a daily dose of 5 mg/kg significantly inhibits proliferation of tumor cells with EGFR sensitive mutation (exon 19 del) and resistant mutation (T790 M) for consecutive 14 days, with no TKI-induced weight loss in mouse xenograft models . Oritinib shows good bioavailability, and is distributed extensively from the plasma to the tissues . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 weeks old female mice bearing NCI-H1975 and A431 xenograft models Dosage: 2.5, 5, and 15 mg/kg Administration: Orally administrated once daily for consecutive 14 days Result: Led to a significant inhibition of tumor cell growth in both PC-9 (exon 19 del) and NCI-H1975 (L858R/T790M) xenograft models. Animal Model: NCI-H1975 tumor-bearing mice Dosage: 2.5, 5, and 15 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration for 1 day or 14 consecutive days. Result: The T max is 1.5-2 h, indicating rapidly distributed into tissues, including lung tumor tissues. The AUC 0–t values in plasma were 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively.
Form:Solid
IC50& Target:EGFR (WT) 18 nM (IC 50 ) EGFR L858R 0.7 nM (IC 50 ) EGFR L861Q 4 nM (IC 50 ) EGFR L858R/T790M 0.1 nM (IC 50 ) EGFR d746-750 1.4 nM (IC 50 ) EGFR d746-750/T790M 0.89 nM (IC 50 )
规格
别名
奥瑞替尼
规格或纯度
≥99%
英文名称
Oritinib
生化机理
奥利替尼（SH-1028）是一种不可逆的第三代表皮生长因子受体 TKI，可克服非小细胞肺癌中 T790M 介导的耐药性。奥利替尼（SH-1028）是一种具有突变选择性的表皮生长因子受体激酶活性抑制剂，可抑制表皮生长因子受体 WT、表皮生长因子受体 L858R、表皮生长因子受体 L861Q、表皮生长因子受体
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
539.67
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 125 mg/mL (231.62 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥99%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2035089-28-0，分子式为 C31H37N7O2，分子量为 539.67 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）