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Binimetinib, also known as MEK162, ARRY-162 or ARRY-438162, is a selective and oral MKE inhibitor. Binimetinib is used to treat various cancers as an anti-cancer small molecule and is a central kinase in the tumor-promoting MAPK pathway. Combined with encorafenib, Binimetinib was approved by FDA in 2018 to treat unresectable or metastatic BRAF V600E or V600K mutation-positive melanoma.
CAS No. |
606143-89-9 |
Purity |
99.55% |
Target |
MEK, Autophagy |
IC50 |
12 nM |
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In Vitro |
Combing PIK3 inhibition with Binimetinib or BI-D1870 can fully reverse the resistance of RSK-expressing cells. In all HRAS mutant cell lines, the basal ERK phosphorylation is blocked by Binimetinib. By combining RAD001 with AZD6244 or MEK162, a stronger blocking effect on cell growth in HRAS mutant cells is also produced, stronger than in a signle use. Binimetinib displays greater synergism with RAD001 than AZD6244. |
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In Vivo |
In both animal models, Binimetinib descreases disease severity in a treatment in a dose-related manner. In the CIA model, at 1 and 3 mg/kg, ankle diameter incraeses are inhibited by 27% and 50% by Binimetinib and Ibuprofen makes 46% inhibition in the same model. In combination with lbuprofen the outcome is 74% and 72% inhibiton with the same doeses. At 1 and 3 mg/kg, Binimetinib shows significant lesions(inflammation, cartilage damage, pannus formation and bone resorption) inhibition of 32% and 60%, in the microscopic examination of the ankle joints. However, in another treatment using lbuprofen alone only leads to 17% inhibiton. At 1 and 3 mg/kg, Binimetinib shows significant lesions(inflammation, cartilage damage, pannus formation and bone resorption) inhibition of 32% and 60%, in the microscopic examination of the ankle joints. However, in another treatment using lbuprofen alone only leads to 17% inhibiton. When combined Binimetinib with ibuprofen at the same doses, 54% and 77% inhibition of joint destruction are achieved. Combining Binimetinib with BEZ23 significantly reduces growth of tumbor (P=0.01) with a reduction of phospho-ERK and phospho-S6 staining. |
Formula |
C₁₇H₁₅BrF₂N₄O₃ |
SMILES |
BrC1=CC=C(C(F)=C1)NC2=C(C3=C(C=C2C(NOCCO)=O)N(C=N3)C)F |
M. Weight |
441.2 |
Storage |
Powder -20°C 3 years |
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Solvent & Solubility |
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Documentation |
Contact us for relevant PDF documents. |
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http://www.medchemhub.com/
