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 Chemical Structure

CAS No. : 74588-78-6

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D-64131 相关产品


  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
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  • Orally Active Compound Library
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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]

(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.

(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.








Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
In Vitro: 

DMSO : ≥ 100 mg/mL (397.96 mM)

* “≥” means soluble, but saturation unknown.

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


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

  • 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。
  • [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.