S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC 50 of 4.29 μM. S516 has marked antitumor activity In Vitro S516 has potent cytotoxicity with IC 50 s of 4.8 nM, 42.8 nM and 24.9 nM for HL-60, HCT116 and HCT15 cells, respectively. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell 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. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice bearing 3LL lung cancer Dosage: 5 mg/kg, 10 mg/kg Administration: Intraperitoneal injection Result: Had promising antitumor activity (inhibition ratio (IR)> 63%). Form:Solid IC50& Target:IC50: 4.29 μM (tubulin polymerization)
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S516
CAS number：1016543-77-3 molecular formula：C21H19N5O4S
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Specs
| Chinese alias | - | ||
| English alias | CS-0105868 | Methanone, [4-(2-amino-4-thiazolyl)-2-(1H-1,2,4-triazol-1-yl)phenyl](3,4,5-trimethoxyphenyl)- | HY-130233 | MS-27839 | SCHEMBL1044496 | S516 | S-516 | [4-(2-amino-1,3-thiazol-4-yl)-2-(1,2,4-triazol-1-yl)phenyl]-(3,4,5-trimethoxyphenyl)methano | ||
| CAS number | 1016543-77-3 | molecular formula | C21H19N5O4S |
| molecular weight | 437.47 g/mol | Exact mass | ≥98% |
| PSA | 143.000 Ų | logp | 3.300 |
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