CUDC-101

SKU: orb1304532

Description

CUDC-101 is a multi-targeted small molecule inhibitor with potent activity against HDAC, EGFR, and HER2, exhibiting IC50 values of 4.4 nM, 2.4 nM, and 15.7 nM, respectively. It has been investigated in preclinical cancer research for its potential to overcome resistance and has shown efficacy in both cellular and animal models of various solid tumors.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Molecular Biology, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1012054-59-9
MW	434.49
Purity	99.17%
Formula	C₂₄H₂₆N₄O₄
SMILES	N(C=1C2=C(C=C(OC)C(OCCCCCCC(NO)=O)=C2)N=CN1)C3=CC(C#C)=CC=C3
Target	HDAC,EGFR,HER
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.3 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:0.35 mg/mL (0.81 mM)

Bioactivity

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Target IC50	HDAC:4.4 nM\|HDAC5:11.4 nM\|HDAC9:67.2 nM\|HDAC2:12.6 nM\|HDAC7:373 nM\|HDAC1:4.5 nM\|HDAC4:13.2 nM\|HER2:15.7 nM\|EGFR:2.4 nM\|HDAC8:79.8 nM\|HDAC6:5.1 nM\|HDAC3:9.1 nM\|HDAC10:26.1 nM Read more...
In Vivo	CUDC-101 exhibits broad-spectrum antiproliferative activity in numerous human cancer cell lines with an IC50 range of 0.04 μM to 0.80 μM. It demonstrates higher potency compared to erlotinib, lapatinib, and combinations of these with either vorinostat or combinations of erlotinib or lapatinib. Notably, CUDC-101 can inhibit the proliferation of cancer cell lines resistant to lapatinib and erlotinib. This compound increases the acetylation of histones H3 and H4 and non-histone substrates like p53 and α-tubulin in a dose-dependent manner across various cancer cell lines. Additionally, CUDC-101 suppresses the expression of HER3, the amplification of Met, and the reactivation of AKT in tumor cells. Read more...
In Vitro	CUDC-101 exhibits a dose-dependent inhibition of growth in erlotinib-sensitive H358 NSCLC xenografts and effectively suppresses tumor growth in erlotinib-resistant A549 NSCLC xenograft models. Additionally, CUDC-101 significantly promotes tumor regression in lapatinib-resistant, HER2-negative, EGFR-overexpressing MDA-MB-468 breast cancer models, and EGFR-overexpressing CAL-27 head and neck squamous cell carcinoma (HNSCC) models. Administration of CUDC-101 at a daily dose of 120 mg/kg in the Hep-G2 liver tumor model induces tumor deterioration more effectively than the maximum tolerated dose of erlotinib (25 mg/kg/day) and an equimolar dose of vorinostat (72 mg/kg/day). Read more...
Cell Research	Cancer cell lines are plated at 5000 to 10000 cells per well in 96-well flatbottomed plates with varying concentrations of CUDC-101. The cells are incubated with CUDC-101 for 72 hours 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. Apoptosis is routinely assessed by measuring the activities of Caspase-3 and -7 using Apo-ONE Homogeneous Assay Kit.(Only for Reference) Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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CUDC 101, CUDC101, CUDC-101, HDAC1, HDAC3, HDAC2, HDAC4, HDAC10, HDAC8, HDAC5, HDAC, HDAC7, HDAC9, HDAC6, HER2, HER1, Histone deacetylases, Epidermal growth factor receptor, ErbB-1, EGFR, Inhibitor, inhibit

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Compound Identifiers

PubChem CID

24756910 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	1012054-59-9
MW:	434.4876
Formula:	C₂₄H₂₆N₄O₄

CUDC-101

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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