Home MAPK MEK inhibitor GDC-0623 For research use only.

GDC-0623

Synonyms: G-868

GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

GDC-0623 Chemical Structure

GDC-0623 Chemical Structure

CAS No. 1168091-68-6

Purity & Quality Control

GDC-0623 Related Products

Signaling Pathway

MEK Signaling Pathways

MEK Signaling Pathway

Biological Activity

Description GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
Targets
MEK1 [1]
0.13 nM
In vitro
In vitro In a panel of mutant cancer cell lines, GDC-0623 inhibits cellular proliferation with EC50 of 4 nM, 53 nM, 11 nM, 18 nM and 94 nM for A375 (BRAFV600E), HCT116 (KRASG13D), COLO 205 (V600E), HT-29 (V600E), and HCT116 (G13D) cells, respectively. [1] In isogenic KRAS HCT116 and mutant KRAS SW620 colon cells, GDC-0623 upregulates BIM via its loss of phosphorylation at Ser69. GDC-0623 plus ABT-263 induces a synergistic cell apoptosis. [2]
Kinase Assay In vitro Kinase assays
0.14 μM of purified inactive recombinant MEK-1 (Upstate) protein is preincubated with inhibitors in 15 μL of kinase buffer including (20 mM MOPS pH7.2, 25 mM beta glycerol phosphate, 5 mM EGTA, 1 mM sodium orthovanadate, 1 mM DTT, 100 μM ATP, 15 mM MgCl2). After incubating 10 minutes at 30°C, 1 ng of BRAF, CRAF or BRAF V600E combined with 0.5 μg of inactive recombinant ERK2 is added to the reaction in total volume of 20 μL. After incubating 30 minutes at 30°C the reaction is stopped by adding Laemmle sample buffer. Enzyme activity is measured by determining level of phosphor-MEK by SDS-PAGE. Immunoreactive proteins are visualized with SuperSignal West Pico Chemiluminescent Substrate.
In Vivo
In vivo In vivo, GDC-0623 (40 mg/kg, p.o.) causes potent tumor growth inhibition (TGI) in mouse MiaPaCa-2 (120%), A375 (102%) and HCT116 (115%) xenografts. [1]
Animal Research Animal Models Mice bearing MiaPaCa-2, A375 and HCT116 xenografts
Dosages 40 mg/kg daily
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01106599 Completed
Solid Cancers
Genentech Inc.
 April 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 456.21 Formula

C16H14FIN4O3
CAS No. 1168091-68-6 SDF Download GDC-0623 SDF
Smiles C1=CC(=C(C=C1I)F)NC2=C(C=CC3=CN=CN32)C(=O)NOCCO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (199.46 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : ˂1 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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