NEO2734( EP31670 )

Catalog No. M22391 CAS No. 2081072-29-7

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

Get Quotation Bulk Inquiry Add to Cart

Product Name

NEO2734
Note

Research use only, not for human use.
Brief Description

NEO2734 is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).
Description

NEO2734 is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).NEO2734, a novel dual inhibitor of BET and CBP/p300, is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo.
In Vitro

Western Blot Analysis 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

Animal Model:Mice (PER-403 and 14169 models).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.
Synonyms

EP31670
Pathway

Chromatin/Epigenetic
Target

Epigenetic Reader Domain
Recptor

p300/CBP|BET bromodomain
Research Area

——
Indication

——

1. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer.

Calculator

molnova catalog