2. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK
  3. Raf Bcr-Abl Discoidin Domain Receptor VEGFR RET Ephrin Receptor
  4. 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.

ML786 dihydrochloride Chemical Structure

ML786 dihydrochloride Chemical Structure

CAS No. : 1237536-18-3

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Other Forms of ML786 dihydrochloride:

ML786 dihydrochloride Related Antibodies

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  • Biological Activity

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  • References

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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)

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
56 nM
Compound: 6
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
[PMID: 26804230]
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].

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

ML786 dihydrochloride Related Antibodies
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].

MedChemExpress (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.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ML786 dihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ML7861237536-18-3ML 786ML-786RafBcr-AblDiscoidin Domain ReceptorVEGFRRETEphrin ReceptorRaf kinasesVascular endothelial growth factor receptorB-RafC-RafAbl-1DDR2EPHA2KDRcancerInhibitorinhibitorinhibit

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