D-64131|cas:74588-78-6|西域试剂

D-64131,98.98%

产品编号：Bellancom-15482| CAS NO：74588-78-6| 分子式：C₁₆H₁₃NO₂| 分子量：251.28

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货号	价格	库存与货期
Bellancom-15482	￥818.00	杭州北京（现货）
Bellancom-15482	￥3500.00	杭州北京（现货）
Bellancom-15482	￥5500.00	杭州北京（现货）

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D-64131

产品介绍

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。

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.

体外研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

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.
D-64131 has oral bioavailability and is well tolerated at efficacious doses.

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

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