ML786 dihydrochloride
ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
For research use only. We do not sell to patients.
- CAS No.: 1237536-18-3
- Formula: C29H31Cl2F3N4O3
- Molecular Weight:611.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All VEGFR Isoforms
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Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
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| A-375 | IC50 |
56 nM
Compound: 6
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Inhibition of B-Raf V600E mutant in human A375 cell line assessed as inhibition of ERK phosphorylation for 3 hrs with compound by ELISA
Inhibition of B-Raf V600E mutant in human A375 cell line assessed as inhibition of ERK phosphorylation for 3 hrs with compound by ELISA
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[PMID: 26804230] |
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 AUC1-24h of 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude NCR (ν/ν) mice bearing A375 M xenografts[1]
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Dosage:75 mg/kg
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Administration:P.o. once daily for 21 days
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Result:Induced partial regressions of the tumor xenografts.
Showed no indication of toxicity or weight loss.
Chemical Information
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CAS No. 1237536-18-3
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Molecular Weight 611.48
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Formula C29H31Cl2F3N4O3
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SMILES
O=C(CC1)NC2=C1C(OC3=CC=C(CC[C@@H](NC(C4=CC(C(F)(F)F)=CC(C(C)(C)N)=C4)=O)C5)C5=C3)=CC=N2.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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