Mps1-IN-3

Mps1-IN-3 is an inhibitor of monopolar spindle 1 (Mps1, IC50 = 50 nM). It inhibits the proliferation of U251 glioblastoma cells (IC50 = ~5 µM). Mps1-IN-3 (2 µM) prevents checkpoint-mediated mitotic arrest induced by nocodazole (Cay-13857) in U2OS osteosarcoma cells and, when used at a concentration of 5 µM in combination with the antimitotic agents vincristine (Cay-11764) or paclitaxel (Cay-10461), induces nuclear aberrancies and chromosome missegregation defects in U251-FM-H2B-GFP cells, which express firefly luciferase, mCherry, and a histone H2B-GFP fusion reporter. It sensitizes U251-FM cells to vincristine and increases survival in an orthotopic mouse model of glioblastoma when administered at a dose of 2 mg/kg.Formal Name: 1-[3-methoxy-4-[[6-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-9H-purin-2-yl]amino]phenyl]-4-piperidinol. CAS Number: 1609584-72-6. Synonyms: Monopolar Spindle1-IN-3, Monopolar Spindle 1 Inhibitor 3, Mps1 Inhibitor 3. Molecular Formula: C26H31N7O4S. Formula Weight: 537.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly Soluble: 0.1-1 mg/ml. SMILES: CC(S(C1=C(C=CC=C1)NC2=NC(NC(C(OC)=C3)=CC=C3N4CCC(CC4)O)=NC5=C2NC=N5)(=O)=O)C. InChi Code: InChI=1S/C26H31N7O4S/c1-16(2)38(35,36)22-7-5-4-6-20(22)29-25-23-24(28-15-27-23)31-26(32-25)30-19-9-8-17(14-21(19)37-3)33-12-10-18(34)11-13-33/h4-9,14-16,18,34H,10-13H2,1-3H3,(H3,27,28,29,30,31,32). InChi Key: OFRMASLPWOMYHN-UHFFFAOYSA-N.