您好，欢迎来到半岛电竞官方网址 ！ [ 登录] [ 免费注册]
半岛电竞官方网址
发布求购
位置： 首页> 半岛bd体育手机客户端 库> Osimertinib dimesylate
立即咨询
咨询类型：
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
Osimertinib dimesylate
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Osimertinib dimesylate图片
CAS NO: 2070014-82-1
包装与价格：
包装 价格(元)
10 mM * 1 mL in Water 电议
5mg 电议
10mg 电议
50mg 电议
100mg 电议
200mg 电议
500mg 电议
1 g 电议
5 g 电议

半岛bd体育手机客户端 名称
奥希替尼二甲磺酸盐
AZD-9291 dimesylate
Mereletinib dimesylate
半岛bd体育手机客户端 介绍
Osimertinib dimesylate (AZD-9291 dimesylate) 是不可逆的突变体选择性 EGFR抑制剂；对EGFR L858R和EGFR L858R/T790M的 IC50值分别为12 和 1 nM。
生物活性

Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selectiveEGFRinhibitor withIC50s of 12 and 1 nM againstEGFRL858RandEGFRL858R/T790M, respectively.
IC50& Target[1]

EGFRL858R

12 nM (IC50)

EGFRL858R/T790M

1 nM (IC50)
体外研究
(In Vitro)

Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC50values ranging from 13 to 54 nM for Osimertinib (AZD-9291). Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50potency less than 15 nM[1].
体内研究
(In Vivo)

The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth[1]. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day[2].
Clinical Trial
分子量

691.82
性状

Solid
Formula

C30H41N7O8S2
CAS 号

2070014-82-1
中文名称

奥斯替尼二甲磺酸盐；奥希替尼二甲磺酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:

H2O : 100 mg/mL(144.55 mM;Need ultrasonic)

DMSO : 2.63 mg/mL(3.80 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 1.4455 mL 7.2273 mL 14.4546 mL
5 mM 0.2891 mL 1.4455 mL 2.8909 mL
10 mM 0.1445 mL 0.7227 mL 1.4455 mL
*

请根据半岛bd体育手机客户端 在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的半岛bd体育手机客户端 失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。
Baidu
map