S516 (Compound 22) 是 CKD-516 的活性代谢产物，是一种有效的微管蛋白聚合抑制剂，其 IC50 值为 4.29 μM。S516 具有显著的抗肿瘤活性。
货号:ajcx15674
CAS:1016543-77-3
分子式:C21H19N5O4S
分子量：437.47
溶解度:DMSO: 12.5 mg/mL (28.57 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity[1].

S516 has potent cytotoxicity with IC50s of 4.8 nM, 42.8 nM and 24.9 nM for HL-60, HCT116 and HCT15 cells, respectively[1].S516 (Compound 22; 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[1]. Cell Cycle Analysis[1] Cell Line: HL60 cells

S516 (Compound 22; 5-10 mg/kg; intraperitoneal injection; mice) treatment has promising antitumor activity (inhibition ratio (IR)>63%) in human LX-1 lung cancer and CX-1 colon cancer mouse xenografts[1]. Animal Model: Mice bearing 3LL lung cancer[1]

[1]. Lee J, et al. Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors. J Med Chem. 2010 Sep 9;53(17):6337-54.