| Description |
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].
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| Related Catalog |
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| Target |
IC50: 4.29 μM (tubulin polymerization)[1]
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| In Vitro |
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 Concentration: 30 nM Incubation Time: 16 hours Result: Caused significant arrest of cells at the G2/M phase, resulting in apoptosis with concomitant loss of G0/G1 phase.
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| In Vivo |
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] Dosage: 5 mg/kg, 10 mg/kg Administration: Intraperitoneal injection Result: Had promising antitumor activity (inhibition ratio (IR)> 63%).
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| References |
[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.
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