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ML 786 dihydrochloride

Catalog No.GC15296

Raf kinase inhibitor

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ML 786 dihydrochloride Chemical Structure

Cas No.: 1237536-18-3

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10mg
$388.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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 [1].

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 [1].

Clinical trial: N/A

Reference:
[1] 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.

Chemical Properties

Cas No. 1237536-18-3 SDF
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/[C@]2([H])CCC3=CC=C(OC4=C5CCC(O)=NC5=NC=C4)C=C3C2)=C1)(N)C.Cl.Cl
Formula C29H29F3N4O3.2HCl M.Wt 611.48
Solubility <61.15mg/ml in DMSO; <61.15mg/ml in Water Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.6354 mL 8.1769 mL 16.3538 mL
5 mM 0.3271 mL 1.6354 mL 3.2708 mL
10 mM 0.1635 mL 0.8177 mL 1.6354 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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