GDC-0623

Catalog No.S7553 Synonyms: G-868

GDC-0623 Chemical Structure

Molecular Weight(MW): 456.21

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

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Biological Activity

Description GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
Targets
MEK1 [1]
0.13 nM
In vitro

AMG 925 shows potent antiproliferation efficacy against U937, MOLM13 and Colo205 cells with IC50 of 52 nM, 19 nM and 55 nM, respectively, and induces cell apoptosis. AMG 925 also inhibits pSTAT5 in MOLM13 and pRb via FLT3 and CDK4 inhibition in Colo205 with IC50 of 0.005 and 0.023 μM, respectively. [1]

In vivo In NCR nude mice bearing MOLM13 tumors, AMG 925 (150 mg/kg, p.o.) inhibits STAT5 phosphorylation, and causes 100% tumor growth inhibition (TGI). [1] In mice bearing Colo205 xenografts, AMG 925 (50 mg/kg, p.o.) inhibits RB phosphorylation, and causes 97% tumor growth inhibition (TGI). [2]

Protocol

Kinase Assay:[1]
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Kinase Assays:

The inhibitory activity of FLT3 is determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) assay. An ULight-labeled synthetic peptide (ULight-JAK1, PerkinElmer, Waltham, MA) derived from human Janus kinase 1 (amino acids 1015–1027) is used as the phosphoacceptor substrate. The FLT3 assay is conducted in a 384-well white OptiPlate in a total volume of 20 μL. The reaction mixture contains 50 nM ULight-JAK1, 116 μM ATP (equal to Km), 0.5 nM FLT3, and serially diluted test compounds in a reaction buffer of 50 mM Hepes, pH 7.6, 1 mM EGTA, 10 mM MgCl2, 2 mM DTT, and 0.005% Tween 20. The reaction is allowed to proceed for 1 h at room temperature and stopped by adding 20 μL of 20 mM EDTA and 4 nM LANCE Eu-W1024 antiphospho-tyrosine antibody in LANCE detection buffer. The plates are incubated at room temperature for 2 h after addition of detection reagents and are then read on an Envision multimode reader. Fluorescence signals measured at 615 nm (8.5 nm bandwidth) and 665 nm (7.5 nm bandwidth) with a 60 μs delay after excitation at 320 nm (75 nm bandwidth). The signal ratio at 665/615 nm (APC/Eu) was used in all data analyses. For CDK4 and CDK6 kinase assays, Rb (amino acids 773–928), and histone H1 are used as substrate for CDK4/6 and CDK1/2, respectively. Assays are performed in 96-well filter plates with a final volume of 100 μL, containing 1 μg Rb, 25 ng CDK4/cyclin D1, 25 μM ATP, 1 μCi [r-33P]-ATP, and compound in kinase reaction buffer (20 mM Tris-HCl, pH 7.4, 10 mM magnesium chloride, 5 mM β-glycerophosphate, 1 mM dithiothreitol, and 0.1% bovine serum albumin). Plates with reaction mix are incubated at room temperature for 60 min, and reactions are terminated by addition of 200 μL of 20% trichloroacetic acid. Wells are washed with 200 μL of 10% trichloroacetic acid and left to dry at room temperature. The bottom of the plates is sealed with tape, and 100 μL of MicroScint-20 scintillation cocktail are added to each well. Plates are read on a TopCount to determine radioactive incorporation. IC50 values are calculated by nonlinear regression curve fitting using GraphPad Prism v5.01.
Cell Research:[1]
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  • Cell lines: MOLM13, U937, Colo205 cells
  • Concentrations: ~3 μM
  • Incubation Time: 72 hours
  • Method: Cell growth is measured by a DNA synthesis assay. Cells are seeded in a 96-well Cytostar T plate at a density of 5 × 103 cells/well in a total volume of 160 μL. The plates are incubated overnight to allow cells to attach. Test compounds are serially diluted into the plate (20 μL/well), and 20 μL/0.1 μCi of [14C]-thymidine are added to each well. Isotope incorporation is determined using a β plate counter after a further 72 h. IC50 values are determined by nonlinear regression curve fitting using GraphPad Prism v5.01.
    (Only for Reference)
Animal Research:[1] [2]
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  • Animal Models: NCR nude mice bearing MOLM13 tumors
  • Formulation: 2% hydroxypropyl methylcellulose/1% Tween 80
  • Dosages: 150 mg/kg
  • 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 individually and in order:
5% DMSO+45% PEG 300+ddH2O
20mg/mL

* 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
Formula

C16H14FIN4O3

CAS No. 1168091-68-6
Storage powder
Synonyms G-868

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01106599 Completed Solid Cancers Genentech, Inc. April 2010 Phase 1

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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MEK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID