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CUDC-101

Cat. No. M1693
CUDC-101 Structure
Synonym:

Curis

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 70 In stock
50mg USD 270 In stock
200mg USD 720 In stock
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Quality Control
Biological Activity

CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 synergistically blocked key regulators of EGFR/HER2 signaling pathways, also attenuating multiple compensatory pathways, such as AKT, HER3, and MET, which enable cancer cells to escape the effects of conventional EGFR/HER2 inhibitors.

Customer Product Validations & Biological Datas
Source Oncotarget (2015). Figure 5. CUDC-101
Method Apoptosis arrays
Cell Lines ATC cells
Concentrations 1.1 μM
Incubation Time 24 h
Results Treatment with CUDC-101 also significantly reduced the expression of survivin and XIAP, known inhibitors of caspases
Protocol
Cell Experiment
Cell lines A431, H292 and BT474 cells
Preparation method Cell growth, viability, and apoptosis assay Cancer cell lines were obtained from the American Type Culture Collection and were maintained according to the supplier's instructions. Cancer cell lines were plated at 5,000 to 10,000 cells per well in 96-well flat-bottomed plates with varying concentrations of compounds. The cells were incubated with compounds for 72 hours in the presence of 0.5% of fetal bovine serum. Growth inhibition was assessed by an ATP content assay using the Perkin-Elmer ATPlite kit. Apoptosis was routinely assessed by measuring the activities of caspase-3 and caspase-7 using the Promega Apo-ONE Homogeneous Assay kit.
Concentrations 0, 0.1, 1, or 10 µM
Incubation time 72h
Animal Experiment
Animal models HepG2 hepatoma cells xenograft models nude mice
Formulation 30% Captisol solution
Dosages 120 mg/kg daily
Administration i.v./i.p
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 434.49
Formula C24H26N4O4
CAS Number 1012054-59-9
Purity 98.92%
Solubility DMSO
Storage at -20°C
References

CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity.
Lai et al. Cancer Res. 2010 May 1;70(9):3647-56. PMID: 20388807.

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.
Cai et al. J Med Chem. 2010 Mar 11;53(5):2000-9. PMID: 20143778.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CUDC-101, Curis supplier, HDAC, inhibitors

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