TC-Mps1-12

• CAT Number: I011016
• CAS Number: 1206170-62-8
• Molecular Formula: C17H20N6O
• Molecular Weight: 324.38
• Purity: ≥95%
• Synonyms: 4-[[4-amino-6-(tert-butylamino)-5-cyanopyridin-2-yl]amino]benzamide
• InChI: InChI=1S/C17H20N6O/c1-17(2,3)23-16-12(9-18)13(19)8-14(22-16)21-11-6-4-10(5-7-11)15(20)24/h4-8H,1-3H3,(H2,20,24)(H4,19,21,22,23)
• InChIKey: XDEFNAWAKYQBQY-UHFFFAOYSA-N
• SMILES: CC(C)(C)NC1=C(C(=CC(=N1)NC2=CC=C(C=C2)C(=O)N)N)C#N

TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM[1].
TC-Mps1-12 inhibits the growth of pMps1 cell lines with IC50 values of 131 nM in autophosphorylation assay[1].
TC-Mps1-12 (72 hours) inhibits the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM[1].
TC-Mps1-12 (25-100 mg/kg; p.o.; daily; for 19 days) inhibits the growth of A549 cells in a dose-dependent manner in vivo. At a dose of 100 mg/kg, TC-Mps1-12 exhibits 47% tumor growth inhibition without body weight loss[1].
TC-Mps1-12 shows good PK properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL at an oral dose of 25 mg/kg[1].

Reference

[1]. Kusakabe K, et al. Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation. ACS Med Chem Lett. 2012 Jun 6;3(7):560-4.
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