BI-2493

BI-2493 is an inhibitor of mutant K-Ras. It selectively decreases the proliferation of Ba/F3 cells expressing K-Ras containing a glycine-to-cysteine substitution at position 12 (K-RasG12C), K-RasG12D, or K-RasG12V (EC50s = 118, 52, and 81 nM, respectively) over Ba/F3 cells expressing H-Ras or N-Ras (EC50s = 2,359 and 1,576 nM, respectively). BI-2493 (30 mg/kg twice per day) reduces tumor volume in SW480 colon adenocarcinoma and NCI H358 non-small cell lung cancer (NSCLC) mouse xenograft models. Formal Name: (4'S)-2'-amino-5,6,6',7'-tetrahydro-3-[2-[(2S)-2-methyl-1-piperazinyl]-4-pyrimidinyl]-spiro[1,2-benzisoxazole-7(4H),4'(5'H)-benzo[b]thiophene]-3'-carbonitrile. CAS Number: 2937344-16-4. Molecular Formula: C24H27N7OS. Formula Weight: 461.6. Purity: >98%. Formulation (Request formulation change): A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml DMSO: Slightly soluble: 0.1-1 mg/ml. SMILES: N#CC1=C(N)SC2=C1[C@]3(CCC2)C4=C(CCC3)C(C5=NC(N6[C@H](CNCC6)C)=NC=C5)=NO4. InChi Code: InChI=1S/C24H27N7OS/c1-14-13-27-10-11-31(14)23-28-9-6-17(29-23)20-15-4-2-7-24(21(15)32-30-20)8-3-5-18-19(24)16(12-25)22(26)33-18/h6,9,14,27H,2-5,7-8,10-11,13,26H2,1H3/t14-,24-/m0/s1. InChi Key: PVOYBVVIBNPTPJ-BSEYFRJRSA-N. Storage: -20°C. Stability: > 4 years.