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Products are for research use only. Not for human use. We do not sell to patients.

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Selumetinib

HY-50706

(AZD6244; Array142886; ARRY-142886; AZD-6244)

Selumetinib

Selumetinib Chemical Structure

Selumetinib (AZD6244; ARRY-142886) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc.

Price and Availability of Selumetinib

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Size Price Stock Quantity
10 mM * 1 mL $66 In-stock
50 mg $60 In-stock
100 mg $80 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL €65 In-stock
50 mg €59 In-stock
100 mg €78 In-stock
200 mg Get quote
500 mg Get quote

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Selumetinib Data Sheet

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    Purity: 99.46%

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    DataSheet

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Related Compound Libraries

Inhibitor Kit

Biological Activity of Selumetinib

Selumetinib (AZD6244; ARRY-142886) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc.
IC50 value: 14 nM [1]
Target: MEK1
in vitro: ZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. AZD6244 also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase. AZD6244 has little effects on the p38, c-Jun-NH2-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways [1]. AZD6244 is sensitive to Raf mutations in breast cancer cell lines and Ras mutations in NSCLC cell lines [2].
in vivo: AZD6244 significantly inhibits phosphorylation of ERK1/2 in 2-1318, 5-1318, 26-1004 and 4-1318 xenografts and induces apoptosis in primary 2-1318 cells by activating the caspase pathway [1]. AZD6244 could inhibit the tumor growth in HT-29 xenograft, which is a colorectal tumor model carrying a B-Raf mutation, at a dose of 100 mg/kg and the tumor growth inhibition of AZD6244 is better than it of Gemcitabine [3].

Chemical Information

M.Wt 457.68 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C17H15BrClFN4O3
CAS No 606143-52-6
Solvent & Solubility

DMSO ≥90mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.1849 mL 10.9247 mL 21.8493 mL
5 mM 0.4370 mL 2.1849 mL 4.3699 mL
10 mM 0.2185 mL 1.0925 mL 2.1849 mL

Clinical Information of Selumetinib

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Selumetinib AstraZeneca plc Metastatic non small cell lung cancer 31-DEC-12 31-JUL-14 Phase 2 06-NOV-13
AstraZeneca plc Metastatic non small cell lung cancer 31-OCT-13 31-MAR-17 Phase 3 06-NOV-13
AstraZeneca plc Thyroid tumor 31-AUG-13 31-OCT-17 Phase 2 15-NOV-13
National Cancer Institute Metastatic pancreas cancer 31-AUG-12 Phase 2 17-JUL-13
National Cancer Institute Gallbladder tumor 31-JAN-13 31-MAY-13 Phase 2 11-OCT-13
National Cancer Institute Biliary cancer 31-JAN-13 31-MAY-13 Phase 2 11-OCT-13

References on Selumetinib

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