(1E)-CFI-400437 dihydrochloride

• CAT Number: I045405
• CAS Number: 1247000-76-5
• Molecular Formula: C29H30Cl2N6O2
• Molecular Weight: 565.49
• Purity: ≥95%
• Synonyms: 5-methoxy-3-[(E)-[3-[(E)-2-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]ethenyl]indazol-6-ylidene]methyl]-1H-indol-2-ol;dihydrochloride
• InChI: InChI=1S/C29H28N6O2.2ClH/c1-34-11-13-35(14-12-34)28-10-5-19(18-30-28)4-8-26-22-7-3-20(16-27(22)33-32-26)15-24-23-17-21(37-2)6-9-25(23)31-29(24)36;;/h3-10,15-18,31,36H,11-14H2,1-2H3;2*1H/b8-4+,20-15+
• InChIKey: NYCYUHRNBLSJAP-LIZIWEMKSA-N
• SMILES: CN1CCN(CC1)C2=NC=C(C=C2)C=CC3=C4C=CC(=CC5=C(NC6=C5C=C(C=C6)OC)O)C=C4N=N3.Cl.Cl

(1E)-CFI-400437 dihydrochloride (Cat No.: I045405) is a potent and selective Mps1/TTK kinase inhibitor, developed to target mitotic checkpoint dysregulation in cancer cells. By inhibiting TTK, it disrupts spindle assembly checkpoint function, leading to mitotic catastrophe and apoptosis in rapidly dividing tumor cells. This compound has shown promising activity in triple-negative breast cancer and other solid tumors with chromosomal instability. It is widely used in preclinical oncology research to study cell cycle regulation and develop targeted therapies for aggressive cancers.

Reference

[1]. Laufer R, et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013;56(15):6069-6087.
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