For research use only.

Catalog No.S7553 Synonyms: G-868

7 publications

GDC-0623 Chemical Structure

CAS No. 1168091-68-6

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

Selleck's GDC-0623 has been cited by 7 publications

1 Customer Review

  • Three types of selective inhibitors of MAPK signaling produce expected differential kinase inhibition and activation responses in HCT116 colorectal cancer cells. HCT116 cells were treated with 250nM of GDC-0973, GDC-0623, SCH772984 or DMSO for 1, 4, or 24 hours. In the washout samples, cells were drug treated for 24 hours, then changed into fresh media and harvested after 0.5 or 2 hours. Lysates were used for western blots of total and phosphorylated MEK, ERK and RSK; blotting for COX IV was used as the loading control.

    Mol Cell Proteomics, 2017, 16(2):265-277. GDC-0623 purchased from Selleck.

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Biological Activity

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

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]


Kinase Assay:[1]
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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.
Animal Research:[1]
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  • Animal Models: Mice bearing MiaPaCa-2, A375 and HCT116 xenografts
  • Dosages: 40 mg/kg daily
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL warmed (199.46 mM)
Ethanol 5 mg/mL warmed (10.95 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 456.21


CAS No. 1168091-68-6
Storage powder
in solvent
Synonyms G-868
Smiles C1=CC(=C(C=C1I)F)NC2=C(C=CC3=CN=CN32)C(=O)NOCCO

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01106599 Completed Drug: GDC-0623 Solid Cancers Genentech Inc. April 2010 Phase 1

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MEK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID