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INCB054329

CAS No. : 1628607-64-6

MCE 站：INCB054329

产品活性：INCB054329 是一种有效的 BET 抑制剂。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: INCB054329 is a bromodomain ａnd extra-terminal motif (BET) inhibitor. 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.

In Vivo: 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.

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