首页工具

购物车

Osimertinib mesylate

产品编号 T3634 CAS 1421373-66-1

别名: 甲磺酸奥希替尼, Mereletinib mesylate, 奥希替尼甲磺酸盐, AZD-9291 mesylate

Osimertinib mesylate (Mereletinib mesylate) 是一种不可逆的突变选择性 EGFR 抑制剂，对EGFRL858R 和EGFRL858R/T790M 的IC50值分别为 12 和 1 nM。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Osimertinib mesylate, CAS 1421373-66-1

规格	价格/CNY	货期
1 mg	￥ 155	现货
5 mg	￥ 358	现货
10 mg	￥ 500	现货
25 mg	￥ 893	现货
50 mg	￥ 1,160	现货
100 mg	￥ 1,580	现货
200 mg	￥ 2,320	现货
500 mg	￥ 4,000	现货
1 g	￥ 5,680	现货
1 mL * 10 mM (in DMSO)	￥ 543	现货

大包装超大折扣，点击咨询

其他形式的 Osimertinib mesylate:

Osimertinib
现货
Osimertinib dimesylate
询价

选择批次

纯度: 100%

纯度: 99.53%

纯度: 99.46%

纯度: 99.38%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Osimertinib mesylate (Mereletinib mesylate) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)).
靶点活性	EGFR (L858R):12 nM (cell free), EGFR (L858R/T790M):1 nM (cell free)
体外活性	In EGFR recombinant enzyme assays, osimertinib (AZD9291) showed an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. The drug exhibited nearly 200 times greater potency against L858R/T790M than wild-type EGFR. AZD9291 showed similar potency to early generation TKIs in inhibiting EGFR phosphorylation in EGFR cells harboring sensitizing EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC50 values ranging from 13 to 54 nM for AZD9291. AZD9291 also potently inhibited phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50 potency less than 15 nM [1]. In the presence of osimertinib, the intracellular accumulations of DOX and Rho 123 significantly increased in KBv200 and S1-MI-80 cells while not in the sensitive KB and S1 cells. Osimertinib increased the intracellular accumulation of Hoechst 33342 in resistant H460/MX20 and HEK293/ABCG2 cells rather than in sensitive H460 and HEK293/Vector cells. Furthermore, the increased effect produced by osimertinib at 0.2 μmol/L or 0.4 μmol/L was comparable with that of FTC at 2.5 μmol/L or VRP at 10 μmol/L [2].
体内活性	Once daily dosing of AZD9291 induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models, with tumor shrinkage observed at doses as low as 2.5mg/kg/day in both models after 14 days. Similar tumor shrinkage was seen after administration of 5 mg/kg/day AZD9291 in H3255 (L858R) and PC-9VanR (ex19 del/ T790M) xenografts after 14 days [1]. The combination of osimertinib and paclitaxel produced a greater inhibitory effect on xenograft growth compared with animals treated with only saline, paclitaxel, or osimertinib, and the inhibition rate was 52.7% [2]. AZD9291 demonstrated improved rat PK, reduced hERG affinity, and improved IGF1R margins. AZD9291 also offered an additional degree of broader chemical and profile diversity. Upon dosing AZD9291 in our three efficacy models, comparable efficacy was observed at relatively low doses (10 mg/kg/day). Excellent efficacy was also observed when 8 was dosed at 5 mg/kg/day [3].
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].
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].
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].

别名	甲磺酸奥希替尼, Mereletinib mesylate, 奥希替尼甲磺酸盐, AZD-9291 mesylate
分子量	595.71
分子式	C29H37N7O5S
CAS No.	1421373-66-1

存储

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

溶解度

DMSO: 5.96 mg/mL (10 mM), Sonification is recommended

H2O: 33 mg/mL (55 mM), Sonification is recommended

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O	1 mM	1.6787 mL	8.3933 mL	16.7867 mL	41.9667 mL
	5 mM	0.3357 mL	1.6787 mL	3.3573 mL	8.3933 mL
	10 mM	0.1679 mL	0.8393 mL	1.6787 mL	4.1967 mL
H2O	20 mM	0.0839 mL	0.4197 mL	0.8393 mL	2.0983 mL
H2O	50 mM	0.0336 mL	0.1679 mL	0.3357 mL	0.8393 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. 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. 2. Chen Z, et al. Osimertinib (AZD9291) Enhanced the Efficacy of Chemotherapeutic Agents in ABCB1- and ABCG2-Overexpressing Cells In Vitro, In Vivo, and Ex Vivo. Mol Cancer Ther. 2016 Aug;15(8):1845-58. 3. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistancemutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.

文献引用

1. Liu N N, Zhou J, Jiang T, et al. A dual action small molecule enhances azoles and overcomes resistance through co-targeting Pdr5 and Vma1: Osimertinib targets Pdr5 and Vma1. Translational Research. 2022

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Osimertinib mesylate 1421373-66-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Osimertinib Osimertinib Mesylate PC-9 tumor xenograft model 甲磺酸奥希替尼 inhibit AZD9291 AZD-9291 cancer Mereletinib mesylate Inhibitor Epidermal growth factor receptor 奥希替尼甲磺酸盐 Mereletinib HER1 H1975 AZD 9291 Mereletinib Mesylate ErbB-1 AZD-9291 Mesylate Ba/F3 cells AZD9291 Mesylate AZD-9291 mesylate AZD 9291 Mesylate inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

沪公网安备 31010602006700号

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼

Osimertinib mesylate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords