S516 is an active CKD-516 metabolite and is a potent inhibitor of tubulin polymerization(IC50 of 4.29 μM), has marked antitumor activity.

S516 has potent cytotoxicity(HL-60, HCT116 and HCT15 cells with IC50s of 4.8 nM, 42.8 nM and 24.9 nM, respectively). S516 (30 nM; 16 hours; HL60 cells) treatmemt causes significant arrest of cells at the G2/M phase, resulting in apoptosis with concomitant loss of G0/G1 phase.

In human LX-1 lung cancer and CX-1 colon cancer mouse xenografts,S516 (5-10 mg/kg; intraperitoneal injection; mice) treatment has promising antitumor activity (inhibition ratio (IR)>63%) .

1016543-77-3

C21H19N5O4S

437.47

DMSO:12.5 mg/mL (28.57 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years