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%
| ALogP | 1.884 |
|---|---|
| hba_count | 5 |
| Recuento HBD | 1 |
| Enlace rotable | 2 |
| Isómeros SMILES | CC1=C(C(=NO1)C)C2=C3C4=C(C=C2)NC(=O)N4[C@H](CO3)C5=CC=CC=N5 |
|---|---|
| Peso molecular | 348.36 |
| Reaxy-Rn | 27453356 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27453356&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| DMSO (mg/ml) Solubilidad máxima | 70 |
|---|---|
| DMSO (mM) Solubilidad máxima | 200.941554713515 |
| Agua (mg/ml) Solubilidad máxima | ˂1 |
