S516

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S516  纯度: 98.03%

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。

S516

S516 Chemical Structure

CAS No. : 1016543-77-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3370 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
25 mg ￥9900 In-stock
50 mg ￥16500 In-stock
100 mg ￥25000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

S516 相关产品

•相关化合物库:

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  • Cell Cycle/DNA Damage Compound Library
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生物活性

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].

IC50 & Target

IC50: 4.29 μM (tubulin polymerization)[1]
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[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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%).

分子量

437.47

Formula

C21H19N5O4S
CAS 号

1016543-77-3
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL (28.57 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2859 mL 11.4294 mL 22.8587 mL
5 mM 0.4572 mL 2.2859 mL 4.5717 mL
10 mM 0.2286 mL 1.1429 mL 2.2859 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (2.86 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.86 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
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.

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