D-64131 是一种具有口服活性的微管蛋白 (tubuli

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: 0.53 μM (tubulin polymerization)^[2]

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].

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].

251.28

Solid

C₁₆H₁₃NO₂

74588-78-6

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL (397.96 mM)

* "≥" means soluble, but saturation unknown.

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℃, 2 years; -20℃, 1 year。-80℃ 储存时，请在 2 年内使用， -20℃ 储存时，请在 1 年 内使用。

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。

• [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.  [Content Brief]

  [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.  [Content Brief]