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GDC-0623

$150$980

Products Details

Product Description

– GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).

Web ID

– HY-15610

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C16H14FIN4O3

References

– [1]Takahashi RH, et al. Elucidating the Mechanisms of Formation for Two Unusual Cytochrome P450-Mediated Fused Ring Metabolites of GDC-0623, a MAPK/ERK Kinase Inhibitor. Drug Metab Dispos. 2015 Dec;43(12):1929-1933.|[2]Hatzivassiliou G, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 2013 Sep 12;501(7466):232-6.

CAS Number

– 1168091-68-6

Molecular Weight

– 456.21

Compound Purity

– 99.15

SMILES

– FC(C=C(I)C=C1)=C1NC2=C(C(NOCCO)=O)C=CC3=CN=CN23

Clinical Information

– Phase 1

Research Area

– Cancer

Solubility

– DMSO : 50 mg/mL (ultrasonic)

Target

– Apoptosis;MEK

Isoform

– MEK1

Pathway

– Apoptosis;MAPK/ERK Pathway

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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