您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > Pan KRas-IN-1
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：
 
Pan KRas-IN-1
本产品不向个人销售，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。
Pan KRas-IN-1图片
CAS NO:2791263-84-6
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Pan KRas-IN-1 是一种泛KRas抑制剂，能够用于对KRas G12C抑制剂产生的癌症耐药性的研究。
生物活性

Pan KRas-IN-1 is a panKRasinhibitor, can be used for drug resistance incancerdeveloped with KRas G12C inhibitors[1].

IC50& Target

KRas G12D

9 nM (IC50)

KRas G12S

11 nM (IC50)

KRas G12C

6 nM (IC50)

KRas Q61H

12 mM (IC50)

KRas G12V

29 mM (IC50)

K-Ras WT

32 nM (IC50)

K-Ras G12R

681 nM (IC50)

K-Ras G13D

23 nM (IC50)

体外研究
(In Vitro)

Pan KRas-IN-1 (example 5) shows high binding capacity to KRas, with IC50s of<2 nm among different kras isform, including g12d, g12v, g12r, g12a, g12s, g13d, q61h, and wt[1].
Pan KRas-IN-1 inhibits the phosphorylation of ERK downstream of KRas in different cells; AsPC-1 (G12D, IC50=9 nM), A549 (G12S, IC50=11 nM), HCT116 (G13D, IC50=23 nM), NCI-H358 (G12C, IC50=6 nM), NCI-H460 (Q61H, IC50=12 nM), NCI-H727 (G12V, IC50=29 nM), MKN1 (WT, IC50=32 nM), PSN-1 (G12R, IC50=681 nM)[1].
Pan KRas-IN-1 (0-3000 nM; 5 d) exhibits anti-proliferative activity against mutation of reststance toAdagrasib(HY-130149, MRTX849) in mouse 3T3 fibroblasts, with IC50s of 32 nM (G12A), 28.1 nM (G12C), 20.25 nM (G12D), 1742 nM (G12R), 94 nM (G12V), 50 nM (G12W), 610 nM (G13D), 58 nM (Q61H)[1].

分子量

607.67

Formula

C33H36F3N5O3

CAS 号

2791263-84-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.