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.
Kinase Assay
Cell Assay
Animal Administration
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.
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