NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains. NEO2734 is active in SPOP mutant and wild-type prostate cancer.

Product information

CAS Number: 2081072-29-7

Molecular Weight: 435.44

Formula: C22H24F3N3O3

Chemical Name: 1,3-dimethyl-5-[2-(oxan-4-yl)-1-[2-(trifluoromethoxy)ethyl]-1H-1,3-benzodiazol-6-yl]-1,2-dihydropyridin-2-one

Smiles: CN1C=C(C=C(C)C1=O)C1=CC=C2N=C(C3CCOCC3)N(CCOC(F)(F)F)C2=C1

InChiKey: KPWWFNXRLAAREN-UHFFFAOYSA-N

InChi: InChI=1S/C22H24F3N3O3/c1-14-11-17(13-27(2)21(14)29)16-3-4-18-19(12-16)28(7-10-31-22(23,24)25)20(26-18)15-5-8-30-9-6-15/h3-4,11-13,15H,5-10H2,1-2H3

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 100 mg/mL (229.65 mM; Need ultrasonic).

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: ≥12 months 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:

NEO2734 (1 μM) induces differentiation and G1-phase cell cycle arrest. NEO2734 (1 μM) rapidly induces squamous differentiation in NMC cell lines, and expression of the terminal squamous differentiation marker, involucrin, or keratins. NEO2734 is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo.

In Vivo:

NEO2734 (5, 8, 10 mg/kg, orally) inhibits growth and prolongs survival in pre-clinical xenograft models.

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