1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Acetyltransferase
  3. NEO2734

NEO2734 (Synonyms: EP31670)

目录号: HY-136938 纯度: 99.66%
产品使用指南

NEO2734 (EP31670) 是具有口服活性的 p300/CBPBET bromodomain 的选择性抑制剂,其IC50 值均 <30 nM。 NEO2734 在 SPOP 突变型和野生型前列腺癌模型中均有活性。

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NEO2734 Chemical Structure

NEO2734 Chemical Structure

CAS No. : 2081072-29-7

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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 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.
Molecular Weight

435.44

Formula

C₂₂H₂₄F₃N₃O₃

CAS No.

2081072-29-7

SMILES

O=C1C(C)=CC(C2=CC=C3N=C(C4CCOCC4)N(CCOC(F)(F)F)C3=C2)=CN1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

NEO2734EP31670NEO 2734NEO-2734EP 31670EP-31670Epigenetic Reader DomainHistone AcetyltransferaseHATsHATMYCp300CBPTC-797PER-403SPOPInhibitorinhibitorinhibit

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NEO2734
目录号:
HY-136938
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