中文名：INCB054329
英文名：INCB054329
英文別名：INCB-054329, INCB-54329;Imidazo[1,?5,?4-?de]?[1,?4]?benzoxazin-?2(1H)?-?one, 7-?(3,?5-?dimethyl-?4-?isoxazolyl)?-?4,?5-?dihydro-?4-?(2-?pyridinyl)?-?, (4S)?-
純度：10mM in DMSO
貨號(hào)：I408086
包裝：1ml
Cas號(hào)：1628607-64-6
存儲(chǔ)溫度：-80℃儲(chǔ)存
產(chǎn)品介紹：
Information
INCB054329 INCB054329 (INCB-054329, INCB-54329) is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-B
In?vitro
INCB054329 shows no significant inhibitory activity against 16 non-BET bromodomains at 3 μM. In a panel of 32 hematologic cancer cell lines derived from acute myeloid leukemia, non-Hodgkin lymphoma, and multiple myeloma, the median 50% growth inhibition (GI50) value of INCB054329 is 152 nM (range, 26-5000 nM). In contrast to tumor cell lines, the GI50 value against T cells isolated from non-diseased donors stimulated ex vivo with IL-2 is 2.435 μM. Growth inhibition correlates with a concentration-dependent accumulation of cells in the G1 phase of the cell cycle. INCB054828 is also a selective kinase inhibitor of the FGFR 1, 2, and 3. In myeloma cell lines, treatment with INCB054329 inhibits expression of c-MYC and induced HEXIM1. In both AML and lymphoma cell lines, INCB054329 induces apoptosis consistent with increased expression of pro-apoptotic regulators. INCB054329 reduces expression of Homologous recombination (HR) components and co-operatively reduces cell growth and increases DNA damage and apoptosis induced by PARPi and cisplatin.
In?vivo
INCB054329 exhibits high clearance in mice resulting in a short half-life. At exposures that effectively suppressed c-MYC, INCB054329 is found to be efficacious and well tolerated in both the KMS-12-BM and MM1.S xenograft models. In vivo, oral administration of INCB054329 inhibits tumor growth in several models of hematologic cancers.
Cell?Data
cell?lines：
Concentrations：--
Incubation?Time：72 h
Powder?Purity:≥98%
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關(guān)鍵字： INCB-054329, INCB-54329;Imidazo[1,?5,?4-?de]?[1,?4]?benzoxazin-?2(1H)?-?one, 7-?(3,?5-?dimethyl-?4-?isoxazolyl)?-?4,?5-?dihydro-?4-?(2-?pyridinyl)?-?, (4S)?-
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