Tubulin inhibitor 11

目录号: HY-152156 纯度: 99.92%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Tubulin inhibitor 11 是一种有效的具有口服活性的微管蛋白 (tubulin) 抑制剂。Tubulin inhibitor 11 靶向微管蛋白上的秋水仙碱结合位点，抑制微管蛋白聚合，促进有丝分裂阻断和细胞凋亡 (apoptosis)。

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Tubulin inhibitor 11 Chemical Structure

CAS No. : 2366260-33-3

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Free Sample (0.1 - 0.2 mg)		Apply now
10 mM * 1 mL in DMSO	￥1341	In-stock
1 mg	￥645	In-stock
5 mg	￥1488	In-stock
10 mg	￥2475	In-stock
25 mg	￥4213	In-stock
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生物活性
纯度 & 产品资料
参考文献

生物活性

Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.025 μM Compound: 48	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
A549	IC₅₀	0.03 μM Compound: 48	Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
B16-F10	IC₅₀	0.002 μM Compound: 48	Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
BGC-823	IC₅₀	0.021 μM Compound: 48	Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
DU-145	IC₅₀	0.004 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 96 hrs by real-time cell analysis Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 96 hrs by real-time cell analysis	[PMID: 36511661]
DU-145	IC₅₀	0.008 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
DU-145	IC₅₀	0.009 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by real-time cell analysis Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by real-time cell analysis	[PMID: 36511661]
DU-145	IC₅₀	0.01 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 24 hrs by real-time cell analysis Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 24 hrs by real-time cell analysis	[PMID: 36511661]
DU-145	IC₅₀	0.01 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by real-time cell analysis Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by real-time cell analysis	[PMID: 36511661]
HCT-116	IC₅₀	0.004 μM Compound: 48	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
HCT-8	IC₅₀	0.022 μM Compound: 48	Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
HepG2	IC₅₀	0.003 μM Compound: 48	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
HGC-27	IC₅₀	0.006 μM Compound: 48	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
HUVEC	IC₅₀	0.032 μM Compound: 48	Anti-angiogenesis activity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Anti-angiogenesis activity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
MCF7	IC₅₀	0.006 μM Compound: 48	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
MCF7R	IC₅₀	0.014 μM Compound: 48	Antiproliferative activity against paclitaxel-resistant human MCF7R cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against paclitaxel-resistant human MCF7R cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
MDA-MB-231	IC₅₀	0.009 μM Compound: 48	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
NCI-H1299	IC₅₀	0.004 μM Compound: 48	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
NCI-H1437	IC₅₀	0.002 μM Compound: 48	Antiproliferative activity against human NCI-H1437 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1437 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
NCI-H460	IC₅₀	0.077 μM Compound: 48	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
SW1990	IC₅₀	0.015 μM Compound: 48	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
Vero	IC₅₀	0.04 μM Compound: 48	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs	[PMID: 36511661]

体外研究
(In Vitro)

Tubulin inhibitor 11 (Compound 48; 0.03-0.1 μM; 12 hours) causes cell cycle arrest at G2/M phase. Tubulin inhibitor 11 reduces cdc2 phosphorylation and increases cyclin B1 and phosphorylation of histone H3 at Ser10 in cells^[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM; 48 hours) causes cancer cell apoptosis^[1].
Tubulin inhibitor 11 (Compound 48) demonstrates favorable antiproliferative activities in DU145 cells with an IC₅₀ of 8 nM^[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM) significantly reduces the expression levels of acetyl-α-tubulin and α-tubulin in a dose-dependent manner^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	DU145 cells
Concentration:	0.01 μM, 0.03 μM, and 0.1 μM
Incubation Time:	12 hours
Result:	Caused cell cycle arrest at G2/M phase.

Apoptosis Analysis^[1]

Cell Line:	DU145 cells
Concentration:	0.03 μM, 0.1 μM, and 0.3 μM
Incubation Time:	48 hours
Result:	Induced cancer cell apoptosis.

Western Blot Analysis^[1]

Cell Line:	DU145 cells
Concentration:	0.01 μM, 0.03 μM, and 0.1 μM
Incubation Time:	12 hours
Result:	Reduced cdc2 phosphorylation and increased cyclin B1 and phosphorylation of histone H3 at Ser10 in cells.

体内研究
(In Vivo)

Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies^[1].

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

Animal Model:	Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells^[1]
Dosage:	5 mg/kg, 10 mg/kg
Administration:	p.o; once daily
Result:	Effectively suppressed tumor growth.

分子量

409.50

Formula

C₂₂H₂₃N₃O₃S

CAS 号

2366260-33-3

性状

固体

颜色

Off-white to pink

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

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (244.20 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4420 mL	12.2100 mL	24.4200 mL
5 mM	0.4884 mL	2.4420 mL	4.8840 mL
10 mM	0.2442 mL	1.2210 mL	2.4420 mL

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.11 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.11 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.11 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.92%

选择批次：

Data Sheet (621 KB) SDS (251 KB)

COA (261 KB) HNMR (274 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Songwen Lin, et al. Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. J Med Chem. 2022 Dec 22;65(24):16372-16391. [Content Brief]

Tubulin inhibitor 11 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4420 mL	12.2100 mL	24.4200 mL	61.0501 mL
	5 mM	0.4884 mL	2.4420 mL	4.8840 mL	12.2100 mL
	10 mM	0.2442 mL	1.2210 mL	2.4420 mL	6.1050 mL
	15 mM	0.1628 mL	0.8140 mL	1.6280 mL	4.0700 mL
	20 mM	0.1221 mL	0.6105 mL	1.2210 mL	3.0525 mL
	25 mM	0.0977 mL	0.4884 mL	0.9768 mL	2.4420 mL
	30 mM	0.0814 mL	0.4070 mL	0.8140 mL	2.0350 mL
	40 mM	0.0611 mL	0.3053 mL	0.6105 mL	1.5263 mL
	50 mM	0.0488 mL	0.2442 mL	0.4884 mL	1.2210 mL
	60 mM	0.0407 mL	0.2035 mL	0.4070 mL	1.0175 mL
	80 mM	0.0305 mL	0.1526 mL	0.3053 mL	0.7631 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6105 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tubulin inhibitor 112366260-33-3Tubulin inhibitor11Tubulin inhibitor-11Microtubule/TubulinApoptosisorally activetubulin inhibitortubulin polymerizationcycle arrestcdc2Inhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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上海工商

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Tubulin inhibitor 11

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