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Products are for research use only. Not for human use. We do not sell to patients.
(AZD6244; Array142886; ARRY-142886; AZD-6244)
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.
IC50 value: 14 nM 
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 . AZD6244 is sensitive to Raf mutations in breast cancer cell lines and Ras mutations in NSCLC cell lines .
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 . 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 .
|M.Wt||457.68||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: 34 mg/mL
|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|
|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|
. Huynh H, et al, Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol Cancer Therapy, 2007, 6 (1), 138-146
. Garon EB, et al. Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines. Mol Cancer Thera, 2010, 9 (7), 1985-1994.
AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 (mu)M in MM cell lines.
AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM.
BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.
GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, (addition)ATP); 6-fold weaker potency against HCT116 (KRAS(G13D), EC50=42 nM) versus A375 (BRAF(V600E), EC50=7 nM).
MEK inhibitor is a potent MEK inhibitor, antitumor agent.
MEK162(ARRY-438162; ARRY-162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM.
OTS964 is a potent TOPK inhibitor with an IC50 value of 28 nM.
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