Free shipping on all orders over $ 500

GDC-0623

Cat. No. M14169
GDC-0623 Structure
Synonym:

RG 7421; MEK inhibitor 1

Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 250  USD250 In stock
50mg USD 650  USD650 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

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).

Product Citations
Chemical Information
Molecular Weight 456.21
CAS Number 1168091-68-6
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] C Ethan Byrne, et al. Lignin-graft-PLGA drug-delivery system improves efficacy of MEK1/2 inhibitors in triple-negative breast cancer cell line

[2] Thomas A Baillie, et al. Biotransformation and bioactivation reactions - 2015 literature highlights

[3] Ryan H Takahashi, et al. Elucidating the Mechanisms of Formation for Two Unusual Cytochrome P450-Mediated Fused Ring Metabolites of GDC-0623, a MAPK/ERK Kinase Inhibitor

[4] Aziz Zaanan, et al. The Mutant KRAS Gene Up-regulates BCL-XL Protein via STAT3 to Confer Apoptosis Resistance That Is Reversed by BIM Protein Induction and BCL-XL Antagonism

[5] Georgia Hatzivassiliou, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

Related MEK Products
Glycinexylidide

Glycinexylidide (GX) is the active metabolite of Lidocaine.

Xantocillin

Xantocillin (Xanthocillin X) is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.

MEK-IN-6 hydrate

MEK-IN-6 hydrate is a MEK inhibitor.

MS934

MS934 is a novel improved VHL-recruiting MEK 1/2 degrader.

Nedometinib

Nedometinib is a tyrosine kinase inhibitor targeting to MEK1.

  Catalog
Abmole Inhibitor Catalog




Keywords: GDC-0623, RG 7421; MEK inhibitor 1 supplier, MEK, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.