| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
CUDC-101 is a novel, potent and multi-targeted histone deacetylase (HDAC) inhibitor with potential anticancer activity. Moreover, it has EGFR and HER2 inhibition at IC50 values of 2.4 nM, 15.7 nM, and 4.4 nM.
| Targets |
EGFR ( IC50 = 2.4 nM ); HER2 ( IC50 = 15.7 nM ); HDAC ( IC50 = 4.4 nM ); HDAC1 ( IC50 = 4.5 nM ); HDAC2 ( IC50 = 12.6 nM ); HDAC3 ( IC50 = 13.2 nM ); HDAC6 ( IC50 = 5.1 nM ); HDAC5 ( IC50 = 11.4 nM ); HDAC9 ( IC50 = 67.2 nM ); HDAC10 ( IC50 = 26.1 nM ); HDAC8 ( IC50 = 79.8 nM ); HDAC7 ( IC50 = 373 nM )
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Enzyme Assay |
The Biomol Color de Lys method is used to evaluate the actions of Class I and II HDACs. In a nutshell, HDACs are obtained from nuclear extracts from HeLa cells. HeLa cell nuclear extracts are treated with varying concentrations of CUDC-101 in the presence of an artificial colorimetric substrate. Enzyme activity is measured in the Wallac Victor II 1420 microplate reader at 405 nM after developer is added at the conclusion of the assay. HTScan EGF receptor and HER2 kinase assay kits are used to measure EGFR and HER2 kinase activity. In brief, 400 mM ATP is added to an incubation mixture containing different concentrations of CUDC-101 and synthetic biotinylated peptide substrate for the GST-EGFR fusion protein. Strapavidin-coated 96-well plates are used to capture phosphorylated substrate. Secondary antibodies labeled with antiphospho-tyrosine and europium measure the amount of phosphorylation. At the conclusion of the experiment, the enhancement solution is added, and the Wallac Victor II 1420 microplate reader is used to measure the enzyme activity at 615 nM.
|
|
| Cell Assay |
In 96-well flatbottomed plates, cancer cell lines are plated at 5000–10,000 cells per well at different CUDC–101 concentrations. For 72 hours, CUDC-101 is incubated with the cells in the presence of 0.5% fetal bovine serum. Using the Perkin-Elmer ATPlite kit, an adenosine triphosphate (ATP) content assay is used to evaluate growth inhibition. The Apo-ONE Homogeneous Assay Kit is used to measure the activities of Caspase-3 and -7 in order to routinely assess apoptosis.
|
|
| Animal Protocol |
|
|
| References |
| Molecular Formula |
C24H26N4O4
|
|
|---|---|---|
| Molecular Weight |
434.49
|
|
| Exact Mass |
434.2
|
|
| Elemental Analysis |
C, 66.34; H, 6.03; N, 12.89; O, 14.73
|
|
| CAS # |
1012054-59-9
|
|
| Related CAS # |
|
|
| Appearance |
Solid powder
|
|
| SMILES |
COC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCCCCCC(=O)NO
|
|
| InChi Key |
PLIVFNIUGLLCEK-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C24H26N4O4/c1-3-17-9-8-10-18(13-17)27-24-19-14-22(21(31-2)15-20(19)25-16-26-24)32-12-7-5-4-6-11-23(29)28-30/h1,8-10,13-16,30H,4-7,11-12H2,2H3,(H,28,29)(H,25,26,27)
|
|
| Chemical Name |
7-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide
|
|
| Synonyms |
CUDC-101; CUDC 101; CUDC101
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 15% Captisol: 30mg/mL Solubility in Formulation 5: 16.67 mg/mL (38.37 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01384799 | Completed | Drug: CUDC-101 Drug: Cisplatin |
Head and Neck Cancer | Curis, Inc. | November 2011 | Phase 1 |
| NCT01171924 | Completed | Drug: CUDC-101 | Head and Neck Cancer Liver Cancer |
Curis, Inc. | July 2010 | Phase 1 |
| NCT00728793 | Completed | Drug: CUDC-101 | Tumors | Curis, Inc. | August 2008 | Phase 1 |
| NCT01702285 | Terminated | Drug: CUDC-101 | Cancer | Curis, Inc. | September 2012 | Phase 1 |
 |
|---|
 |
 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA