| Stereochemistry | ACHIRAL |
| Molecular Formula | C27H34F3N7O3 |
| Molecular Weight | 561.5992 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(NC2=NC=C3N(C)C(=O)C(F)(F)CN(C4CCCC4)C3=N2)C=C(F)C(=C1)C(=O)NC5CCN(C)CC5
InChI
InChIKey=GWRSATNRNFYMDI-UHFFFAOYSA-N
InChI=1S/C27H34F3N7O3/c1-35-10-8-16(9-11-35)32-24(38)18-12-22(40-3)20(13-19(18)28)33-26-31-14-21-23(34-26)37(17-6-4-5-7-17)15-27(29,30)25(39)36(21)2/h12-14,16-17H,4-11,15H2,1-3H3,(H,32,38)(H,31,33,34)
| Molecular Formula | C27H34F3N7O3 |
| Molecular Weight | 561.5992 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor(IC50=1.5 nM) that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1). In animal models, oral administration of TAK-960 increased pHH3 in a dose-dependent manner and significantly inhibited the growth of HT-29 colorectal cancer xenografts. Treatment with once daily TAK-960 exhibited significant efficacy against multiple tumor xenografts, including an adriamycin/paclitaxel-resistant xenograft model and a disseminated leukemia model. TAK-960 had been in phase I clinical trials by Takeda for the treatment of solid tumours. It had also been in preclinical trials for the treatment of acute myeloid leukaemia. However, these studies were discontinued.
Originator
Approval Year
PubMed
Sample Use Guides
Mice: Mice bearing established HT-29 colorectal tumors
were administered a single oral dose (5, 10, or 30 mg/kg,
Fig. 4A) of TAK-960.
Route of Administration:
Oral
