S516

目录号: PL07183 纯度: ≥98%
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。
CAS No. :1016543-77-3
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中文名称
S516
英文名称
S516
英文别名
S516;(4-(2-aminothiazol-4-yl)-2-(1h-1,2,4-triazol-1-yl)phenyl)(3,4,5-trimethoxyphenyl)methanone;[4-(2-Amino-1,3-thiazol-4-yl)-2-(1,2,4-triazol-1-yl)phenyl]-(3,4,5-trimethoxyphenyl)methanone
Cas No.
1016543-77-3
分子式
C21H19N5O4S
分子量
437.47
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
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。
产品详情
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。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
IC50: 4.29 μM (tubulin polymerization)
体外研究(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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Cycle Analysis
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (28.57 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[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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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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