MEK162 (ARRY-162, ARRY-438162)

Description

Biological Activity

Protocol(Only for Reference)

Clinical Trial Information( data from http://clinicaltrials.gov)

Chemical Information

Animal Study: ^[4]

References

Name: MEK162 (ARRY-162, ARRY-438162)
Brand: Selleckchem
SKU: S7007

貨號 Cat. No.: S7007
規格 Size: 10mgã€50mg
品牌 Brand: Selleckchem

MEK162 (ARRY-162, ARRY-438162)

Catalog No.S7007

ARRY-438162 is a potent inhibitor of MEK1/2 with IC50 of 12 nM.

Size

Price

Stock

Quantity

10mg	USD 122	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 466	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Animal Models	immunodeficient mice injected with MCF7-RSK4 cells.
Dosages	6 mg/kg
Administration	oral
Solubility	1% CMC/0.5% Tween-80, 30 mg/mL

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT00959127	Completed	Advanced Solid Tumors\|Advanced or Metastatic Biliary Cancer\|Metastatic Colorectal Cancer	Array BioPharma	2009-08	Phase 1
NCT01859026	Not yet recruiting	Lung Cancer\|Non-Small Cell Lung Cancer	H. Lee Moffitt Cancer Center and Research Institute\|Novartis	2013-10	Phase 1

Description

ARRY-438162 is a potent inhibitor of MEK1/2 with IC50 of 12 nM.

In vitro

ARRY-438162 (625 nM) inhibits in vitro osteoclast differentiation with IC50 of 39 nM. ARRY-438162 (10 μM) inhibits in vitro osteoclast resorption with IC50 of 625 nM. ARRY-438162 (2 μM) weakly affects osteoblast differentiation. ^[2] ARRY-438162 is a recently disclosed potent and selective ATP non-competitive MEK1/2 inhibitor, inhibits pERK in cells with an IC50 of11 nM. ^[3] MEK162 (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells. ^[4]

ARRY-438162 (10 mg/kg, po, bid) reduces disease severity in a dose-related manner in rat collagen-induced arthritis (CIA) and rat adjuvant-induced arthritis (AIA) models. ARRY-438162 (po, bid) inhibits increases in ankle diameter by 27% and 50% at 1 mg/kg and 3 mg/kg in the rat collagen-induced arthritis (CIA) model, while ibuprofen has 46% inhibition. ARRY-438162 (10 mg/kg, po, bid) significantly inhibits lesions (inflammation, cartilage damage, pannus formation and bone resorption) by 32% and 60% at 1 mg/kg and 3 mg/kg in the rat collagen-induced arthritis (CIA) model. ARRY-438162 inhibits AIA ankle diameter 11% and 34% at 3 mg/kg and 10 mg/kg in rat adjuvant-induced arthritis (AIA) models. ^[1] ARRY-438162 demonstrates dose-related inhibition of ankle swelling in rat adjuvant-induced arthritis (AIA) models, significant at 10 mg/kg and 30 mg/kg when compared to vehicle control. ARRY-438162 demonstrates dose-related inhibition of serum IL-6 concentration in rat adjuvant-induced arthritis (AIA) models, with complete inhibition at 10 mg/kg when compared to vehicle control. ARRY-438162 (30 mg/kg) demonstrates dose-related inhibition of relative spleen weights in rat adjuvant-induced arthritis (AIA) models. ARRY-438162 (30 mg/kg) significantly inhibits bone resorption and inflammation with delayed dosing when compared to vehicle in rat adjuvant-induced arthritis (AIA) models. ^[2]MEK162 (6 mg/kg, BID) combined with BEZ235 results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells. ^[4]

Download MEK162 (ARRY-162, ARRY-438162) SDF

Molecular Weight (MW)	441.23
Formula	C₁₇H₁₅BrF₂N₄O₃
CAS No.	606143-89-9

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	88 mg/mL (199 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	1% CMC/0.5% Tween-80,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * 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.