≥43.2 mg/mL in DMSO; insoluble in H2O; ≥3.17 mg/mL in EtOH
form
solid
pka
5.38±0.70(Predicted)
color
White to off-white
Usage And Synthesis
Uses
TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells[1].
in vivo
TAI-1 (20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID) inhibits tumor growth in multiple cancer xenograft models[1].
Animal Model:
C.B-17 SCID mice (6-7 weeks, 21-24 g)[1].
Dosage:
20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID.
Administration:
QDx28 cycles.
Result:
Led to significant tumor growth retardation in Huh-7 and modest tumor inhibition was noted tor the Colo205 and MDA-MB-231 models.
Did not lead to any loss in body weight.
IC 50
NEK2
References
[1] Lynn Y L Huang, et al. Characterization of the Biological Activity of a Potent Small Molecule Hec1 Inhibitor TAI-1. J Exp Clin Cancer Res. 2014 Jan 9;33(1):6. DOI:10.1186/1756-9966-33-6
