MAPK-IN-2 

MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR^WT IC₅₀=281 nM, c-MET IC₅₀=205 nM, B-RAF^WT IC₅₀=112 nM, and CDK4/6 IC₅₀=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR^T790M IC₅₀=69 nM and B-RAF^V600E IC₅₀=83 nM)^[1].

IC50: 281 nM (EGFR^WT), 69 nM (EGFR^T790M), 205 nM (c-MET), 112 nM (B-RAF^WT), 83 nM (B-RAF^V600E), 95 nM (CDK4), 184 nM (CDK6)^[1]

380.23

C₂₀H₁₁Cl₂N₃O

Solid

Light yellow to orange

O=C1C(C#N)=C(C2=CC=C(Cl)C=C2Cl)C=C(C3=CNC4=C3C=CC=C4)N1

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Saleh MM, et al. The mystery of titan hunter: Rationalized striking of the MAPK pathway via Newly synthesized 6-Indolylpyridone-3-Carbonitrile derivatives. Eur J Med Chem. 2023 Nov 5;259:115675.  [Content Brief]