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AZD8330

Catalog No. T6083 CAS 869357-68-6

Synonyms: ARRY-424704, ARRY-704

AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.

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

AZD8330, CAS 869357-68-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 67.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 173.00
25 mg	In stock	$ 313.00
50 mg	In stock	$ 471.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 98.72%

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Description	AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Targets&IC50	MEK1/2:7 nM
In vitro	AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 μM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines. [1]
In vivo	In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours. Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily. [1]
Kinase Assay	MEK1 enzymatic assays: NH2-terminal hexahistidine tagged, constitutively active MEK1 (S218D, S222D ΔR4F) is expressed in baculovirus-infected Hi5 insect cells and purified by immobilized metal affinity chromatography, ion exchange, and gel filtration. The activity of MEK1 is assessed by measuring the incorporation of [γ- 33P]phosphate from [γ-33P]ATP onto ERK2. The assay is carried out in a 96-well polypropylene plate with an incubation mixture (100 μL) composed of 25 mM HEPES (pH 7.4), 10 mM MgCl2, 5 mM β-glycerolphosphate, 100 μM sodium orthovanadate, 5 mM DTT, 5 nM MEK1, 1 μM ERK2, and 0 to 80 nM AZD8330 (final concentration of 1% DMSO). The reactions are initiated by the addition of 10 μM ATP (with 0.5 μC k[γ-33P]ATP/well) and incubated at room temperature for 45 min. An equal volume of 25% trichloracetic acid is added to stop the reaction and precipitate the proteins. Precipitated proteins are trapped onto glass fiber B filter plates, excess labeled ATP is washed off with 0.5% phosphoric acid, and radioactivity is counted in a liquid scintillation counter. ATP dependence is determined by varying the amount of ATP in the reaction mixture. The data are globally fitted.
Cell Research	Malme-3M melanoma cells are plated in 96-wells and treated with various concentrations of AZD8330 for 1 hour at 37 °C. The cells are fixed, permeabilized, and incubated with an anti-phospho-ERK antibody and an anti-ERK 1/2 antibody. Plates are washed and fluorescently-labeled secondary antibodies are added. Plates are analyzed on a LICOR fluorescence imager. The pERK signal is normalized to the total ERK signa (Only for Reference)

Synonyms	ARRY-424704, ARRY-704
Molecular Weight	461.23
Formula	C16H17FIN3O4
CAS No.	869357-68-6

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: 85 mg/mL (184.3 mM)

DMSO: 85 mg/mL (184.3 mM)

References and Literature

1. Wallace EM, et al. AACR Annual Meeting, 2009, Abst 3696. 2. Yeh TC, et al. Clin Cancer Res, 2007, 13(5), 1576-1583.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Reprogramming Compound Library Autophagy Compound Library MAPK Inhibitor Library

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Keywords

AZD8330 869357-68-6 MAPK MEK ERK ARRY 704 AZD 8330 ARRY-424704 ARRY-704 MAPKK Inhibitor Mitogen-activated protein kinase kinase ARRY 424704 inhibit MAP2K ARRY704 AZD-8330 ARRY424704 inhibitor

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