For research use only. Not for therapeutic Use.
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity[1].
(1E)-CFI-400437 (25 mg/kg; intraperitoneal injection; daily for 21 days) dihydrochloride shows effective in a mouse xenograft model of tumor growth[1].
The plasma levels of (1E)-CFI-400437 (50 mg/kg; IP; mice) dihydrochloride shows a Cmax of 92 ng/mL and AUC of 190 ng•h/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i.e., unbound compound in plasma is 1%[1].
| Catalog Number | I045405 |
| CAS Number | 1247000-76-5 |
| 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 |
| Molecular Formula | C29H30Cl2N6O2 |
| Purity | ≥95% |
| 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 |
| 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. |
