2081072-29-7
2081072-29-7 structure
- Name: NEO2734
- Chemical Name: NEO2734
- CAS Number: 2081072-29-7
- Molecular Formula: C22H24F3N3O3
- Molecular Weight: 435.44
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2020-10-27 15:42:46
- Modify Date: 2024-01-17 12:05:20
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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].
| Name | NEO2734 |
|---|
| 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]. |
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| Related Catalog | |
| 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. |
| 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. |
| References |
| Molecular Formula | C22H24F3N3O3 |
|---|---|
| Molecular Weight | 435.44 |
| Storage condition | -20°C |