您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > ML786 dihydrochloride
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:
 
ML786 dihydrochloride
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。
ML786 dihydrochloride图片
CAS NO:1237536-18-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
ML786 dihydrochloride 是一种有效和具有口服活性的Raf抑制剂,对V600EΔB-Rafwt B-RafC-RafIC50值分别为2.1,4.2 和 2.5 nM。ML786 dihydrochloride 还抑制Abl-1DDR2EPHA2KDRRET(IC50=<0.5, 7.0, 11, 6.2, 0.8 nM)。ML786 dihydrochloride 可用于癌症研究。
生物活性

ML786 dihydrochloride is a potent and orally bioavailableRafinhibitor, withIC50s of 2.1, 4.2, and 2.5 nM forV600EΔB-Raf,wt B-Raf, andC-Raf, respectively. ML786 dihydrochloride also inhibitsAbl-1,DDR2,EPHA2,KDR, andRET(IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers[1].

IC50& Target[1]

RAF

2.1 nM (IC50)

Abl1

<0.5 nM (IC50)

DDR2

7.0 nM (IC50)

KDR

6.2 nM (IC50)

EPHA2

11 nM (IC50)

RET

0.8 nM (IC50)

体外研究
(In Vitro)

ML786 (3 h) inhibits the kinase phosphorylation of extracellular signal-regulated kinase (ERK) (pERK) in A375 cells, with an IC50of 60 nM[1].

体内研究
(In Vivo)

ML786 (75 mg/kg; p.o. once daily for 21 d) inhibits the subcutaneous A375 M xenografts in immunocompromised mice[1].
ML786 (75 mg/kg; a single p.o.) strongly inhibits the Raf pathway in mice[1].
ML786 (10 mg/kg; p.o.) exhibits oral bioavailability of 85% and AUC1-24hof 35.9 μM·h in rats[1].
ML786 (1 mg/kg; i.v.) exhibits plasma clearance of 0.44 L/h/kg and Vss of 3.93 L/kg in rats[1].

Animal Model:Nude NCR (ν/ν) mice bearing A375 M xenografts[1]
Dosage:75 mg/kg
Administration:P.o. once daily for 21 days
Result:Induced partial regressions of the tumor xenografts.
Showed no indication of toxicity or weight loss.
分子量

611.48

Formula

C29H31Cl2F3N4O3

CAS 号

1237536-18-3

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.