CUDC-101，HDAC/EGFR/HER2 Inhibitor

CUDC-101 is a multi-targeted, small-molecule inhibitor of histone deacetylase (HDAC), epidermal growth factor receptor tyrosine kinase (EGFR/ErbB1), and human epidermal growth factor receptor 2 tyrosine kinase (HER2/neu or ErbB2) with potential antineoplastic activity. HDAC/EGFR/HER2 inhibitor CUDC-101 inhibits the activity of these three enzymes but the exact mechanism of action is presently unknown. This agent may help overcome resistance to inhibition of EGFR and Her2 through a simultaneous, synergistic inhibition of EGFR, Her2, and HDAC.

Product information

CAS Number: 1012054-59-9

Molecular Weight: 434.49

Formula: C24H26N4O4

Chemical Name: 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide

Smiles: COC1=CC2=NC=NC(NC3=CC=CC(=C3)C#C)=C2C=C1OCCCCCCC(=O)NO

InChiKey: PLIVFNIUGLLCEK-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

CUDC-101 was used at 1 µM final concentration in vitro and in cellular assays.

In Vivo:

CUDC-101 was IP or IV dosed to mice at 120 mg/kg once per day in the xenograft tumor model of Hep-G2, H358, A549, MDA-MB468, HCT116, CAL-27, HepG2, or HPAC.

References:

1. Cai X, 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. (2010) J Med Chem. 53(5):2000-9.
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. (2010) Cancer Res. 70(9):3647-56.

Products are for research use only. Not for human use.