MEK Inhibitor Binimetinib

CAS No.

606143-89-9

Purity

99.55%

Target

MEK, Autophagy

IC50

12 nM

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.
* Above data is for reference only. Accuracy is not confirmed.

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.
* Above data is for reference only. Accuracy is not confirmed.

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
4°C 2 years
In solvent  -80°C 6 months
-20°C 1 month

Solvent & Solubility

Documentation

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