D-64131

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

D-64131  纯度: 99.17%

D-64131 是一种具有口服活性的微管蛋白 (tubulin) 抑制剂,抑制微管蛋白聚合的 IC50 值为 0.53 μM。D-64131 具有抗丝分裂活性。D-64131 可用于癌症研究。

D-64131

D-64131 Chemical Structure

CAS No. : 74588-78-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥900 In-stock
10 mg ¥818 In-stock
50 mg ¥3500 In-stock
100 mg ¥5500 In-stock
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500 mg   询价  

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D-64131 相关产品

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生物活性

D-64131 is an orally active tubulin inhibitor, with an IC50 of 0.53 μM for tubulin polymerization. D-64131 has antimitotic activity. D-64131 can be used for cancer research[1][2].

IC50 & Target

IC50: 0.53 μM (tubulin polymerization)[2]

体外研究
(In Vitro)

D-64131 is antimitotic by binding to β-tubulin, thereby destabilizing microtubules and arresting mitotic cells in the M-phase[1].
D-64131 inhibits the proliferation of tumor cells from 12 of 14 different organs and tissues with mean IC50s of 62 nM[1].
D-64131 is cytotoxic toward MDR/MRP tumor cell lines[1].
D-64131 suppresses U373 proliferation and cell cycle with IC50s of 74 nM and 62.7nM, respectively[2].

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 Cycle Analysis[1]

Cell Line: HeLa/KB cervical carcinoma cells
Concentration: 1 nM-1 μM
Incubation Time: 48 hours
Result: Induced dose-dependently arrested in G2-M before induction of apoptotic cell death.

体内研究
(In Vivo)

D-64131 (200-400 mg/kg; p.o.; daily; days 1-5, 8-9, and 15-18) significantly inhibits tumor growth in the human amelanoic melanoma MEXF 989 tumor xenograft mice model[1].
D-64131 has oral bioavailability and is well tolerated at efficacious doses[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.

Animal Model: Outbred nude mice (6-8 weeks), human amelanoic melanoma MEXF 989 tumor xenograft model[1]
Dosage: 200 mg/kg, 400 mg/kg
Administration: Oral administration, daily, on days 1-5, 8-9, and 15-18 after xenograft
Result: Resulted in significant tumor growth inhibition during treatment.

分子量

251.28

Formula

C16H13NO2

CAS 号

74588-78-6

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 : ≥ 100 mg/mL (397.96 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9796 mL 19.8981 mL 39.7962 mL
5 mM 0.7959 mL 3.9796 mL 7.9592 mL
10 mM 0.3980 mL 1.9898 mL 3.9796 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: ≥ 2.5 mg/mL (9.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.95 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Thomas Beckers, et al. 2-Aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors. Cancer Research (2002), 62(11), 3113-3119.

    [2]. S Mahboobi, et al. Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents. J Med Chem. 2001 Dec 20;44(26):4535-53.

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