ML786 dihydrochloride

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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。

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-Raf，wt B-Raf和C-Raf的IC₅₀值分别为2.1，4.2 和 2.5 nM。ML786 dihydrochloride 还抑制Abl-1，DDR2，EPHA2，KDR和RET(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 for^V600EΔB-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 AUC_1-24hof 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.