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GDC-0623

Catalog No. T6843 CAS 1168091-68-6

Synonyms: G-868, GDC0623, RG 7421, MEK inhibitor 1

GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GDC-0623, CAS 1168091-68-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 67.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 337.00
50 mg	In stock	$ 472.00
100 mg	In stock	$ 677.00
1 mL * 10 mM (in DMSO)	In stock	$ 122.00

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Purity: 98.95%

Purity: 98.27%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
Targets&IC50	MEK1:0.13 nM(ki)
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]
Kinase Assay	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	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)

Synonyms	G-868, GDC0623, RG 7421, MEK inhibitor 1
Molecular Weight	456.21
Formula	C16H14FIN4O3
CAS No.	1168091-68-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 5 mg/mL(11 mM)

DMSO: 91 mg/mL(198.82 mM), Heating is recommended.

References and Literature

1. Hatzivassiliou G, et al. Nature. 2013, 501(7466), 232-236. 2. Zaanan A, et al. J Biol Chem. 2015. doi/10.1074/jbc.M115.657833.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Obesity Compound Library Clinical Compound Library NO PAINS Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GDC-0623 1168091-68-6 Apoptosis MAPK MEK G-868 G 868 Mitogen-activated protein kinase kinase GDC 0623 GDC0623 inhibit Inhibitor MAP2K MAPKK MEK inhibitor1 G868 RG 7421 MEK inhibitor-1 RG-7421 RG7421 MEK inhibitor 1 inhibitor

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