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

NEO2734  (Synonyms: EP31670)

Cat. No.: HY-136938 Purity: 99.79%
COA Handling Instructions

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. NEO2734 is active in SPOP mutant and wild-type prostate cancer.

For research use only. We do not sell to patients.

NEO2734 Chemical Structure

NEO2734 Chemical Structure

CAS No. : 2081072-29-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 385 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

435.44

Appearance

Solid

Formula

C22H24F3N3O3
CAS No.
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
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (229.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2965 mL 11.4826 mL 22.9653 mL
5 mM 0.4593 mL 2.2965 mL 4.5931 mL
10 mM 0.2297 mL 1.1483 mL 2.2965 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.79%

COA (250 KB) HNMR (284 KB) LCMS (101 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

NEO27342081072-29-7EP31670NEO 2734NEO-2734EP 31670EP-31670Epigenetic Reader DomainHistone AcetyltransferaseHATsHATMYCp300CBPTC-797PER-403SPOPInhibitorinhibitorinhibit

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