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Art. -Nr.: HY-14979

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ML786

ML786 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 also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC₅₀=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1237586-97-8
Formel: C₂₉H₂₉F₃N₄O₃
Molecular Weight:538.56

Speicherung:

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

Data Sheet (268 KB)

ML786 Chemical Structure

CAS. Nr.: 1237586-97-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Raf Isoform-spezifische Produkte anzeigen :

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen :

DDR1
DDR2

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle Ephrin Receptor Isoform-spezifische Produkte anzeigen :

EphB
EphA

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	60 nM Compound: 27, ML786	Inhibition of raf kinase in human A375 cells assessed as decrease in MEK-mediated ERK phosphorylation after 3 hrs using 3,3',5,5'-tetramethylbenzidine liquid substrate system Inhibition of raf kinase in human A375 cells assessed as decrease in MEK-mediated ERK phosphorylation after 3 hrs using 3,3',5,5'-tetramethylbenzidine liquid substrate system	[PMID: 21341678]

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.

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 AUC_1-24h 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.

Chemical Information

CAS. Nr. 1237586-97-8
Molecular Weight 538.56
Formel C₂₉H₂₉F₃N₄O₃
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Gould AE, et, al. Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. J Med Chem. 2011 Mar 24;54(6):1836-46. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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ML786

Alle Raf Isoform-spezifische Produkte anzeigen

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle Ephrin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

ML786 Related Classifications

HY-14979 Related Classifications