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INCB054329
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
INCB054329图片
CAS NO:1628607-64-6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
INCB054329是一种有效的BET抑制剂。
Cas No.1628607-64-6
Canonical SMILESO=C1NC2=C3N1[C@@H](C4=NC=CC=C4)COC3=C(C5=C(C)ON=C5C)C=C2
分子式C19H16N4O3
分子量348.36
溶解度DMSO : ≥ 100 mg/mL (287.06 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

INCB054329 is a potent BET inhibitor.

INCB054329 is a bromodomain and extra-terminal motif (BET) inhibitor[1]. INCB054329 inhibits binding of BRD2, BRD3 and BRD4 to an acetylated histone H4 peptide with low nanomolar potency. In myeloma cell lines, treatment with INCB054329 inhibits expression of c-MYC and induced HEXIM1. The majority of myeloma, AML, and lymphoma cell lines tested are growth inhibited by INCB054329 with potencies less than 200 nM. Selectivity is seen when compared with nontransformed cells as the potency for growth inhibition of IL-2 stimulated T-cells from normal donors is greater than 1300 nM. Cell cycle analysis reveals treatment-induced G1 arrest. Furthermore in both AML and lymphoma cell lines, INCB054329 induces apoptosis consistent with increased expression of pro-apoptotic regulators[2].

Oral administration of INCB054329 inhibits tumor growth in several models of hematologic cancers. In the MM1.S multiple myeloma xenograft model, inhibition of tumor growth is correlated with reduction of c-MYC levels. PK-PD analysis shows c-MYC suppression is associated with an IC50 value of less than 100 nM in vivo[2].

[1]. Pérez-Salvia M, et al. Bromodomain inhibitors and cancer therapy: From structures to applications. Epigenetics. 2017 May 4;12(5):323-339. [2]. Phillip CC Liu, et al. Abstract 3523: Discovery of a novel BET inhibitor INCB054329.