ML 786 dihydrochloride
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf, respectively
ML 786 is a potent Raf kinase inhibitor.
As one component of MAPK signal transduction pathway, the Raf isoform B-Raf has a high rate of activating mutation in melanoma (50-70%) and other cancers including papillary thyroid, ovarian, and colorectal. Inhibition of mutant B-Raf signaling, via either direct inhibition of the enzyme or inhibition of MEK, which is the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth.
In vitro: ML 786 and its analog had been found to inhibit a significant number of kinases and were inhibitors of wild-type B-Raf and C-Raf. Although ML 786 and its analog displayed significant receptor tyrosine kinase activity, it was likely that such additional activity would not significantly contribute to pERK inhibition in melanoma tumors with constituitively activated B-Raf .
In vivo: ML 786 and its analog were found to have activity in vivo, as demonstrated by the fact that both compounds strongly inhibited the in vivo Raf pathway following a 75 or 100 mg/kg oral dose .
Clinical trial: N/A
 Gould AE,Adams R,Adhikari S. Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. J Med Chem.2011 Mar 24;54(6):1836-46.
|Physical Appearance||White solid|
|Storage||Store at -20°C|
|Solubility||<61.15mg/ml in DMSO; <61.15mg/ml in H2O|
|Chemical Name||(R,Z)-3-(2-aminopropan-2-yl)-N-(7-((7-hydroxy-5,6-dihydro-1,8-naphthyridin-4-yl)oxy)-1,2,3,4-tetrahydronaphthalen-2-yl)-5-(trifluoromethyl)benzimidic acid dihydrochloride|
|Canonical SMILES||CC(C1=CC(C(F)(F)F)=CC(/C(O)=N/[[email protected]]2([H])CCC3=CC=C(OC4=C5CCC(O)=NC5=NC=C4)C=C3C2)=C1)(N)C.Cl.Cl|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|