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AZD6244

Cat. No. M1661
AZD6244 Structure
Synonym:

Selumetinib, ARRY-142886

Size Price Availability Quantity
100mg USD 95 In stock
500mg USD 250 In stock
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Quality Control
Biological Activity

AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. AZD6244 has potential to inhibit proliferation and induce apoptosis and differentiation, but the response varies between different xenografts.

Protocol
Cell Experiment
Cell lines HT-29, Malme-3M, MIAPaCa-2, SK-MEL-2, SK-MEL-28, BxPC3, BT-474, Zr-75-1, Malme-3
Preparation method Cellular viability assays Cells plated in 96-well plates were incubated with multiple concentrations of compound for 3 days. The number of viable cells was determined using the CellTiter 96 Aqueous Nonradioactive Cell Proliferation Assay (Promega, Madison, WI).
Concentrations 0-50µM
Incubation time 3 days
Animal Experiment
Animal models HT-29 and BxPC3 xenograft
Formulation 10% ethanol/10% cremophor EL/80% D5W
Dosages 10, 25, 50, or 100 mg/kg BID
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 457.68
Formula C17H15BrClFN4O3
CAS Number 606143-52-6
Purity 99.17%
Solubility DMSO
Storage at -20°C
References

Combination of the ERK inhibitor AZD6244 and low-dose sorafenib in a xenograft model of human renal cell carcinoma.
Yuen et al. Int J Oncol. 2012 Aug;41(2):712-20. PMID: 22641227.

Activity of the MEK inhibitor selumetinib (AZD6244; ARRY-142886) in nasopharyngeal cancer cell lines.
Ma BB et al. Invest New Drugs. 2012 May 8. PMID: 22565394.

Selumetinib (AZD6244; ARRY-142886) in the treatment of metastatic melanoma.
Patel et al. Expert Opin Investig Drugs. 2012 Apr;21(4):531-9. PMID: 22394161.

The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models.
Holt et al. Br J Cancer. 2012 Feb 28;106(5):858-66. PMID: 22343622.

MEK1/2 inhibitor selumetinib (AZD6244) inhibits growth of ovarian clear cell carcinoma in a PEA-15-dependent manner in a mouse xenograft model.
Bartholomeusz et al. Mol Cancer Ther. 2012 Feb;11(2):360-9. PMID: 22144664.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD6244, Selumetinib, ARRY-142886 supplier, MEK, inhibitors

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