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Cat. No. M1661
AZD6244 Structure

Selumetinib, ARRY-142886

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL USD 54  USD60 In stock
25mg USD 31.5  USD35 In stock
50mg USD 54  USD60 In stock
100mg USD 81  USD90 In stock
200mg USD 117  USD130 In stock
500mg USD 216  USD240 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.

Product Citations
Customer Product Validations & Biological Datas
Source Apoptosis (2018). Figure 6. AZD6244 (Abmole Bioscience. USA)
Method Western Blot
Cell Lines HT29 and SW480 cells
Concentrations 32 μmol/l
Incubation Time 24 h
Results Resembling the WB results from the BZA treatment, the inhibitors AG490, NVP-BEZ23 and AZD6244 imitated BZA function, down-regulating the pivotal protein of the JAK/STAT3, PI3K/AKT/mTOR and Ras/Raf/MEK/ERK signal pathways
Source Apoptosis (2018). Figure 5. AZD6244 (Abmole Bioscience. USA)
Method cell apoptosis assay
Cell Lines HT29 and SW480 cells
Concentrations 32 μmol/l
Incubation Time 24 h
Results In addition, using the respective AG490 (50 μmol/l), NVP-BEZ235 (96 nmol/l) and AZD6244 (32 μmol/l) inhibitors for 24 h to mimic the BZA effect in colon cancer cells, we observed that the Bad/Bcl-2 ratio was significantly up-regulated and that Ki-67 mRNA expression was substantially down-regulated in this treatment group compared with the control group
Source Cell Biol Int (2014). Figure 5. AZD6244
Method Western blots
Cell Lines Raji and MOLT-4 cells
Concentrations 10 μM
Incubation Time 48 h
Results Consistent with role in the growth inhibition, silencing of Bim decreases the AZD6244-induced apoptosis (Figure 5D) and abrogates AZD6244 induced G1 arrest (Figure 5E).
Source Cell Biol Int (2014). Figure 1. AZD6244
Method apoptosis assay
Cell Lines Raji and MOLT4 cells
Concentrations 10 μM
Incubation Time 48 h
Results AZD6244 significantly blocked ERK phosphorylation in Raji and MOLT4 cells (Figure 1A). AZD6244 significantly inhibited proliferation of both Raji and MOLT4 in a dose-dependent manner (n¼3, P<0.01; Figure 1B).
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 457.68
Formula C17H15BrClFN4O3
CAS Number 606143-52-6
Purity 100.0%
Solubility DMSO 30 mg/mL
Storage at -20°C

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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Abmole Inhibitor Catalog 2017

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

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