Tasisulam(Synonyms: LY 573636)

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Tasisulam (Synonyms: LY 573636) 纯度: 99.13%

Tasisulam 是一种小分子抗肿瘤药物,通过内在途径诱导细胞凋亡,导致细胞色素 c 释放和 caspase 依赖性细胞死亡。Tasisulam 可以抑制有丝分裂进程并诱导血管正常化。

Tasisulam(Synonyms: LY 573636)

Tasisulam Chemical Structure

CAS No. : 519055-62-0

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25 mg ¥1500 In-stock
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Tasisulam 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library

生物活性

Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization[1].

体外研究
(In Vitro)

Tasisulam (200 nM-200 μM; 48 hours) induces an antiproliferative response across a wide range of tumor histologies with EC50s of 10 μM and 25 μM for Calu-6 and A-375 cell lines, respectively[1].
Tasisulam (25, 50 μM; 72 hours) induces a concentration-dependent increase in 4N DNA and G2-M accumulation[1].
Tasisulam (200 nM-200 μM; 48 hours) induces apoptosis in a broad range of in vitro cancer cell models[1].
Tasisulam also blocks VEGF, epidermal growth factor, and fibroblast growth factor-induced endothelial cell cord formation[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Calu-6 non-small cell lung carcinoma and A-375 melanoma models
Concentration: 200 nM-200 μM
Incubation Time: 48 hours
Result: Induced an antiproliferative response across a wide range of tumor histologies with EC50s are 10 μM and 25 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: Calu-6 and A-375 cell lines
Concentration: 25, 50 μM
Incubation Time: 72 hours
Result: Induced a concentration-dependent increase in 4N DNA and G2-M accumulation.

Apoptosis Analysis[1]

Cell Line: Calu-6 non-small cell lung carcinoma and A-375 melanoma models
Concentration: 200 nM-200 μM
Incubation Time: 48 hours
Result: Induced apoptosis in a broad range of in vitro cancer cell models.

Clinical Trial

分子量

415.11

Formula

C11H6BrCl2NO3S2

CAS 号

519055-62-0

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 : 250 mg/mL (602.25 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4090 mL 12.0450 mL 24.0900 mL
5 mM 0.4818 mL 2.4090 mL 4.8180 mL
10 mM 0.2409 mL 1.2045 mL 2.4090 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: ≥ 2.08 mg/mL (5.01 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.01 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.01 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.01 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Meier T, et al. Tasisulam sodium, an antitumor agent that inhibits mitotic progression and induces vascular normalization. Mol Cancer Ther. 2011 Nov;10(11):2168-78.

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