1. MAPK/ERK Pathway
    Protein Tyrosine Kinase/RTK
  2. Raf
    Bcr-Abl
    Discoidin Domain Receptor
    VEGFR
    RET
    Ephrin Receptor
  3. ML786 dihydrochloride

ML786 dihydrochloride 

Cat. No.: HY-14979A
Handling Instructions

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.

ML786 dihydrochloride Chemical Structure

ML786 dihydrochloride Chemical Structure

CAS No. : 1237536-18-3

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Description

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[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)

In Vitro

ML786 (3 h) inhibits the kinase phosphorylation of extracellular signal-regulated kinase (ERK) (pERK) in A375 cells, with an IC50 of 60 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 AUC1-24h 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

611.48

Formula

C₂₉H₃₁Cl₂F₃N₄O₃

CAS No.

1237536-18-3

SMILES

O=C(CC1)NC2=C1C(OC3=CC=C(CC[[email protected]@H](NC(C4=CC(C(F)(F)F)=CC(C(C)(C)N)=C4)=O)C5)C5=C3)=CC=N2.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ML786ML 786ML-786RafBcr-AblDiscoidin Domain ReceptorVEGFRRETEphrin ReceptorRaf kinasesVascular endothelial growth factor receptorB-RafC-RafAbl-1DDR2EPHA2KDRcancerInhibitorinhibitorinhibit

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ML786 dihydrochloride
Cat. No.:
HY-14979A
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