NEO2734

Cas No.:	2081072-29-7
Chemical Name:	NEO2734
Synonyms:	NEO2734;NEO-2734;NEO 2734;EP-31670;EP 31670
SMILES:	O=C1C(C)=CC(C2=CC=C3N=C(C4CCOCC4)N(CCOC(F)(F)F)C3=C2)=CN1C
Formula:	C22H24F3N3O3
M.Wt:	435.44
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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[1]. NEO2734 is active in SPOP mutant and wild-type prostate cancer[2].
In Vivo:	NEO2734 (5, 8, 10 mg/kg, orally) inhibits growth and prolongs survival in pre-clinical xenograft models[1]. Animal Model: Mice (PER-403 and 14169 models)[1]. Dosage: 5, 8, 10 mg/kg Administration: Orally, once daily for 28 days. Result: Two of the three mice treated with NEO2734 were alive by day 100. Provided markedly improved survival compared with EP, i-BET-762, and even iBET-762+EP by day 100 following initiation of treatment.
In Vitro:	NEO2734 (1 μM) induces differentiation and G1-phase cell cycle arrest[1]. NEO2734 (1 μM) rapidly induces squamous differentiation in NMC cell lines, and expression of the terminal squamous differentiation marker, involucrin, or keratins[1]. NEO2734 is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo[2]. Western Blot Analysis[1] Cell Line: NUT carcinoma patient cell lines (TC-797 and PER-403). Concentration: 1 μM. Incubation Time: 6 h. Result: Results in greater loss of MYC protein.
References:	[1]. Chevaun D Morrison-Smit, et al. Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734. Mol Cancer Ther. 2020 Jul;19(7):1406-1414. [2]. Yuqian Yan, et al. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer. EMBO Mol Med. 2019 Nov 7;11(11):e10659.