Cat. No.: HY-10223

CUDC-101

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

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.

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Pureté: 99.05%
CAS No.: 1012054-59-9
Formule: C₂₄H₂₆N₄O₄
Masse moléculaire:434.49

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

CUDC-101 Chemical Structure

CAS No.: 1012054-59-9

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Antibody-Drug Conjugates

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (7)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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)

Voir tous les produits spécifiques à Isoform EGFR :

Voir tous les produits spécifiques à Isoform HDAC :

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]
HeLa	IC₅₀	4.4 nM Compound: 8, CDUC-101	Inhibition of HDAC in human HeLa cell nuclear extract Inhibition of HDAC in human HeLa cell nuclear extract	[PMID: 20143778]
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: 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]
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]
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]

In Vitro

CUDC-101 inhibits both class I and class II HDACs, but not class III, Sir-type HDACs. CUDC-101 displays broad antiproliferative activity in many human cancer cell types. CUDC-101 is a potent and selective HDAC, EGFR, and HER2 inhibitor with only weak inhibition of the following protein kinases (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), and Ret (3200 nM)^[1].
CUDC-101 (300 nM) inhibits both the full length AR (flAR) and the AR variant AR-V7^[2].
CUDC-101 is the most active agent in all three ATC cell lines screened for inhibitors of EGFR and HDACs, with half-maximal inhibitory concentration (IC₅₀) at 0.15 μM for 8505c, and 1.66 μM for both C-643 and SW-1736 cells. CUDC-101 inhibits cancer cell migration and modulates epithelial-mesenchymal transition marker expression in ATC cells. CUDC-101 also inhibits HDAC and MAPK pathway, induces p21, and decreases survivin and XIAP expression in ATC cells^[3].
CUDC-101 (1 μM) increases the acetylation of p53 and α-tubulin, nonhistone substrates of HDAC, in treated cancer cells. CUDC-101 modulates RTK activity and expression and exhibits immediate and stable inhibition of RTK and downstream Akt signaling^[4].

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

In Vivo

CUDC-101 (120 mg/kg, iv, daily) induces tumor regression in the Hep-G2 liver cancer model and is more efficacious than erlotinib at its maximum tolerated dose (MTD). In the erlotinib-resistant A549 NSCLC xenograft model, CUDC-101 (120 mg/kg) shows potent inhibition of tumor growth. In the erlotinib-sensitive H358 NSCLC models, CUDC-101 (15, 30, 60 mg/kg, i.v.) inhibits tumor growth in a dose-dependent manner. CUDC-101 (120 mg/kg) causes significant tumor regression in the lapatinib-resistant, HER2-negative, EGFR-overexpressing MDA-MB-468 breast cancer model and the EGFR-overexpressing CAL-27 head and neck squamous cell carcinoma (HNSCC) model. CUDC-101 (120 mg/kg) also inhibits tumor growth in the K-ras mutant HCT116 colorectal and EGFR/HER2 (neu)-expressing HPAC pancreatic cancer models^[1].
In an in vivo mouse model of metastatic ATC, CUDC-101 inhibits tumor growth and metastases, and significantly prolongs survival^[3].
CUDC-101 (120 mg/kg) is effective against a broad range of tumor types in xenograft models^[4].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1012054-59-9
Appearance Solid
Masse moléculaire 434.49
Formule C₂₄H₂₆N₄O₄
Color White to yellow
SMILES

C#CC1=CC=CC(NC2=NC=NC3=CC(OC)=C(C=C23)OCCCCCCC(NO)=O)=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (7)

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Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Elife

Cohesin mutations are synthetic lethal with stimulation of WNT signaling. [Abstract]

2020 Dec 7;9:e61405. PMID: 33284104
Cancers (Basel)

Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]

2022 Mar 19;14(6):1575. PMID: 35326726
Cancers

TGFα Promotes Chemoresistance of Malignant Pleural Mesothelioma. [Abstract]

2020 Jun 6;12(6):1484. PMID: 32517259
Am J Cancer Res

Antitumor activity of the novel HDAC inhibitor CUDC-101 combined with gemcitabine in pancreatic cancer. [Abstract]

2018 Dec 1;8(12):2402-2418 PMID: 30662800

CUDC-101 purchased from MedChemExpress. 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 MedChemExpress. 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.
Leuk Res

CUDC-101 enhances the chemosensitivity of gemcitabine-treated lymphoma cells. [Abstract]

2021 Jul:106:106575. PMID: 33878513
Patent

US20180263995A1.

Solvant et solubilité

In Vitro:

DMSO : 25 mg/mL (57.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 16.67 mg/mL (38.37 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

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.

MedChemExpress (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.

MedChemExpress (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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	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

Keywords

CUDC-101

7 Cited Publications

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CUDC-101

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

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Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) CUDC-101

Voir tous les produits spécifiques à Isoform EGFR

Voir tous les produits spécifiques à Isoform HDAC

Activité biologique

Chemical Information

Publications (7)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CUDC-101 Related Classifications

HY-10223 Related Classifications