| Chemical Properties | Back Directory | [Boiling point ]
598.0±50.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
4.83±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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.
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| [IC 50]
CBP/p300 | [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. DOI:10.1158/1535-7163.MCT-20-0087
[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. DOI:10.15252/emmm.201910659 |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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