CUDC-101

目录号: HY-10223 纯度: 98.44%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

CUDC-101 是一种高效的 HDAC、EGFR 和 HER2 抑制剂，对应的 IC₅₀ 值分别为 4.4、2.4 和 15.7 nM。CUDC-101 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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CUDC-101 Chemical Structure

CAS No. : 1012054-59-9

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可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥770	In-stock
1 mg	￥318	In-stock
5 mg	￥700	In-stock
10 mg	￥890	In-stock
25 mg	￥1780	In-stock
50 mg	￥3200	In-stock
100 mg	￥5200	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 7 篇科研文献

•Patent. US20180263995A1.

: CUDC-101 purchased from MCE. Usage Cited in: Am J Cancer Res. 2018 Dec 1;8(12):2402-2418 [Abstract]; Western analysis of protein levels of p-p53, cl-caspase3 and the ratio of bax/bcl-2 in the treatment of Germ or/and CUDC.

: CUDC-101 purchased from MCE. Usage Cited in: Am J Cancer Res. 2018 Dec 1;8(12):2402-2418 [Abstract]; PANC-1 and MIA PaCa-2 cells are treated with CUDC-101 and/or gemcitabine for 48 h, and western blot analysis shows increased inhibition of the PI3K, p-Akt, p-S6, p-4EBP1 and p-Erk proteins.

CUDC-101 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 EGFR 亚型特异性产品:

查看所有亚型

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

查看 HDAC 亚型特异性产品:

查看所有亚型

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC₅₀s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

EGFR

2.4 nM (IC₅₀)

HER2

15.7 nM (IC₅₀)

HDAC

4.4 nM (IC₅₀)

HDAC1

4.5 nM (IC₅₀)

HDAC2

12.6 nM (IC₅₀)

HDAC3

9.1 nM (IC₅₀)

HDAC4

13.2 nM (IC₅₀)

HDAC6

5.1 nM (IC₅₀)

HDAC5

11.4 nM (IC₅₀)

HDAC9

67.2 nM (IC₅₀)

HDAC10

26.1 nM (IC₅₀)

HDAC8

79.8 nM (IC₅₀)

HDAC7

373 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	0.27 μM Compound: 8, CDUC-101	Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay	[PMID: 20143778]
CAPAN-1	IC₅₀	0.8 μM Compound: 8, CDUC-101	Antiproliferative activity against human Capan1 cells after hrs by ATP content assay Antiproliferative activity against human Capan1 cells after hrs by ATP content assay	[PMID: 20143778]
HCC827	IC₅₀	0.6 μM Compound: 8, CDUC-101	Antiproliferative activity against human HCC827 cells after hrs by ATP content assay Antiproliferative activity against human HCC827 cells after hrs by ATP content assay	[PMID: 20143778]
HeLa	IC₅₀	4.2 nM Compound: 7; CUDC-101	Inhibition of HDAC in human HeLa cell nuclear extract using COLOR DE LYS as substrate by fluorometric analysis Inhibition of HDAC in human HeLa cell nuclear extract using COLOR DE LYS as substrate by fluorometric analysis	[PMID: 27769671]
HeLa	IC₅₀	4.4 nM Compound: 7; CUDC-101	Inhibition of HDAC (unknown origin) in human HeLa cell nuclear extract using Color de Lys as substrate Inhibition of HDAC (unknown origin) in human HeLa cell nuclear extract using Color de Lys as substrate	[PMID: 30418766]
Hep 3B2	IC₅₀	0.23 μM Compound: 8, CDUC-101	Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay	[PMID: 20143778]
HepG2	IC₅₀	0.13 μM Compound: 8, CDUC-101	Antiproliferative activity against human HepG2 cells after hrs by ATP content assay Antiproliferative activity against human HepG2 cells after hrs by ATP content assay	[PMID: 20143778]
MCF7	IC₅₀	0.55 μM Compound: CUDC-101	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay	[PMID: 32320239]
MCF7	IC₅₀	0.55 μM Compound: 8, CDUC-101	Antiproliferative activity against human MCF7 cells after hrs by ATP content assay Antiproliferative activity against human MCF7 cells after hrs by ATP content assay	[PMID: 20143778]
MDA-MB-231	IC₅₀	0.1 μM Compound: 8, CDUC-101	Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay	[PMID: 20143778]
NCI-H358	IC₅₀	0.4 μM Compound: 8, CDUC-101	Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay	[PMID: 20143778]
NCI-H460	IC₅₀	0.7 μM Compound: 8, CDUC-101	Antiproliferative activity against human H460 cells after hrs by ATP content assay Antiproliferative activity against human H460 cells after hrs by ATP content assay	[PMID: 20143778]
SK-BR-3	IC₅₀	0.04 μM Compound: 8, CDUC-101	Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay	[PMID: 20143778]
SK-HEP1	IC₅₀	0.22 μM Compound: 8, CDUC-101	Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay	[PMID: 20143778]

体外研究
(In Vitro)

CUDC-101 抑制 I 类和 II 类 HDAC，但不抑制 III 类 Sir 型 HDAC。 CUDC-101 在许多人类癌细胞类型中显示出广泛的抗增殖活性。 CUDC-101 是一种有效的选择性 HDAC、EGFR 和 HER2 抑制剂，仅对以下蛋白激酶有微弱抑制 (IC₅₀)：KDR (VEGFR2) (849 nM)、Src (11000 nM) 、Lyn (840 nM)、Lck (5910 nM)、Abl-1 (2890 nM)、FGFR-2 (3430 nM)、Flt-3 (1500 nM) 和 Ret (3200 nM)^{[1]< /sup>。
CUDC-101 (300 nM) 抑制全长 AR (flAR) 和 AR 变体 AR-V7[2]}。
CUDC-101 是筛选 EGFR 和 HDAC 抑制剂的所有三种 ATC 细胞系中最活跃的药物，8505c 的半数最大抑制浓度 (IC₅₀) 为 0.15 μM，两种药物的半数抑制浓度 (IC₅₀) 均为 1.66 μM C-643 和 SW-1736 细胞。 CUDC-101 抑制癌细胞迁移并调节 ATC 细胞中上皮间质转化标志物的表达。 CUDC-101 还可抑制 HDAC 和 MAPK 通路，诱导 p21，并降低 ATC 细胞中 survivin 和 XIAP 的表达^[3]。
CUDC-101 (1 μM) 增加经治疗的癌细胞中 p53 和 α-微管蛋白（HDAC 的非组蛋白底物）的乙酰化。 CUDC-101 调节 RTK 活性和表达，并对 RTK 和下游 Akt 信号传导具有立即且稳定的抑制作用^[4]。

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

体内研究
(In Vivo)

CUDC-101（120 mg/kg，静脉注射，每日）可在 Hep-G2 肝癌模型中诱导肿瘤消退，并且在最大耐受剂量 (MTD) 下比厄洛替尼更有效。在厄洛替尼耐药的 A549 NSCLC 异种移植模型中，CUDC-101 (120 mg/kg) 显示出对肿瘤生长的有效抑制作用。在厄洛替尼敏感的 H358 NSCLC 模型中，CUDC-101（15、30、60 mg/kg，静脉注射）以剂量依赖性方式抑制肿瘤生长。 CUDC-101 (120 mg/kg) 在拉帕替尼耐药、HER2 阴性、EGFR 过表达 MDA-MB-468 乳腺癌模型和 EGFR 过表达 CAL-27 头颈鳞状细胞癌 (HNSCC) 中引起显着的肿瘤消退。）模型。 CUDC-101 (120 mg/kg) 还可抑制 K-ras 突变型 HCT116 结直肠癌和表达 EGFR/HER2 (neu) 的 HPAC 胰腺癌模型中的肿瘤生长^[1]。
在转移性 ATC 小鼠体内模型中，CUDC-101 抑制肿瘤生长和转移，并显着延长生存期^[3]。
CUDC-101 (120 mg/kg) 可有效对抗异种移植模型中的多种肿瘤类型^[4]。

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

Clinical Trial

分子量

434.49

Formula

C₂₄H₂₆N₄O₄

CAS 号

1012054-59-9

性状

固体

颜色

White to yellow

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	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (57.54 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	2.3015 mL	11.5077 mL	23.0155 mL
5 mM	0.4603 mL	2.3015 mL	4.6031 mL
10 mM	0.2302 mL	1.1508 mL	2.3015 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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: ≥ 2.08 mg/mL (4.79 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.79 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.79 mM); 澄清溶液

此方案可获得 ≥ 2.08 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： 50% PEG300 50% Saline
Solubility: 16.67 mg/mL (38.37 mM); 悬浊液; 超声助溶

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: 98.84%

选择批次：

Data Sheet (662 KB) SDS (393 KB)

COA (189 KB) HNMR (183 KB) LCMS (451 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Xiong Cai et al Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer J. Med. Chem., 2010, 53 (5), pp 2000–2009 [Content Brief]

[2]. Lai CJ, et al. CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity.Cancer Res. 2010 May 1;70(9):3647-56. Epub 2010 Apr 13. [Content Brief]

[3]. Sun H, et al. CUDC-101, a Novel Inhibitor of Full-Length Androgen Receptor (flAR) and Androgen Receptor Variant 7 (AR-V7) Activity: Mechanism of Action and In Vivo Efficacy. Horm Cancer. 2016 Jun;7(3):196-210. [Content Brief]

[4]. Zhang L, et al. Dual inhibition of HDAC and EGFR signaling with CUDC-101 induces potent suppression of tumor growth and metastasis in anaplastic thyroid cancer. Oncotarget. 2015 Apr 20;6(11):9073-85. [Content Brief]

Kinase Assay ^[1]	The activities of Class I and II HDACs are assessed using the Biomol Color de Lys system. Briefly, HeLa cell nuclear extracts are used as a source of HDACs. Different concentrations of drugs are added to HeLa cell nuclear extracts in the presence of a colorimetric artificial substrate. Developer is added at the end of the assay and enzyme activity is measured in the Wallac Victor II 1420 microplate reader at 405 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cancer cell lines are plated at 5000 to 10 000 cells per well in 96-well flat-bottomed plates with varying concentrations of compounds. The cells are incubated with compounds for 72 h in the presence of 0.5% of fetal bovine serum. Growth inhibition is assessed by an adenosine triphosphate (ATP) content assay using the Perkin-Elmer ATPlite kit. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Four- to six-week-old female athymic mice (nude nu/nu CD-1) are inoculated subcutaneously into the right hind flank region with 1 to 5×10⁶ cells in a medium suspension of 100−200 μL. For orthotopic implantation of breast cancer cells, a cell suspension in 100 μL of medium is injected directly into the mammary fat pads through a 27G needle. Different doses of CUDC-101, standard anticancer agents and vehicle are administered orally, intraperitoneally, or via tail vein injection as indicated. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Xiong Cai et al Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer J. Med. Chem., 2010, 53 (5), pp 2000–2009 [Content Brief] [2]. Lai CJ, et al. CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity.Cancer Res. 2010 May 1;70(9):3647-56. Epub 2010 Apr 13. [Content Brief] [3]. Sun H, et al. CUDC-101, a Novel Inhibitor of Full-Length Androgen Receptor (flAR) and Androgen Receptor Variant 7 (AR-V7) Activity: Mechanism of Action and In Vivo Efficacy. Horm Cancer. 2016 Jun;7(3):196-210. [Content Brief] [4]. Zhang L, et al. Dual inhibition of HDAC and EGFR signaling with CUDC-101 induces potent suppression of tumor growth and metastasis in anaplastic thyroid cancer. Oncotarget. 2015 Apr 20;6(11):9073-85. [Content Brief]

CUDC-101 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	2.3015 mL	11.5077 mL	23.0155 mL	57.5387 mL
	5 mM	0.4603 mL	2.3015 mL	4.6031 mL	11.5077 mL
	10 mM	0.2302 mL	1.1508 mL	2.3015 mL	5.7539 mL
	15 mM	0.1534 mL	0.7672 mL	1.5344 mL	3.8359 mL
	20 mM	0.1151 mL	0.5754 mL	1.1508 mL	2.8769 mL
	25 mM	0.0921 mL	0.4603 mL	0.9206 mL	2.3015 mL
	30 mM	0.0767 mL	0.3836 mL	0.7672 mL	1.9180 mL
	40 mM	0.0575 mL	0.2877 mL	0.5754 mL	1.4385 mL
	50 mM	0.0460 mL	0.2302 mL	0.4603 mL	1.1508 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:

CUDC-1011012054-59-9CUDC101CUDC 101EGFRHDACEpidermal growth factor receptorErbB-1HER1Histone deacetylasesInhibitorinhibitorinhibit

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CUDC-101

Customer Review

MCE 顾客使用本产品发表的 7 篇科研文献

CUDC-101 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 EGFR 亚型特异性产品:

查看 HDAC 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

CUDC-101 相关分类

完整储备液配制表

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CUDC-101

Customer Review

CUDC-101 相关抗体

MCE 顾客使用本产品发表的 7 篇科研文献

CUDC-101 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 EGFR 亚型特异性产品:

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生物活性

实验参考方法

纯度 & 产品资料

参考文献

CUDC-101 相关抗体:

摩尔计算器

稀释计算器

CUDC-101 相关分类

完整储备液配制表

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