INCB-054329,INCB-54329 - Names and Identifiers
INCB-054329,INCB-54329 - Physico-chemical Properties
Molecular Formula | C19H16N4O3
|
Molar Mass | 348.36 |
Density | 1.46±0.1 g/cm3(Predicted) |
pKa | 12.48±0.40(Predicted) |
Storage Condition | 2-8℃ |
Use | INCB054329 is a potent BET inhibitor. |
In vitro study | INCB054329 at 3 μm had no significant inhibitory activity against the 16 non-BET bromine regions. The average GI50 for INCB054329 was 152 nM in 32 hematologic disease cancer cell lines containing cells isolated from acute myeloid leukemia, non-Hodgkin's lymphoma and multiple myeloma. In contrast, in T cells isolated from normal volunteers, stimulated with IL2 ex vivo, INCB054329 had a GI50 value of 2.435 μm. Its inhibitory effect on cell growth is related to the G1 phase arrest of cells. INCB054828 is also a selective inhibitor of FGFR1, 2, 3. In myeloma cell lines, treatment with INCB054329 inhibited expression by c-myc, inducing hexim1. In AML and lymphoma cell lines, INCB054329 induces apoptosis, with elevated expression of pro-apoptotic regulators. INCB054329 can reduce the expression of homologous recombination components, reduce cell growth, enhance PARPi and cisplatin-induced DNA damage and apoptosis. |
In vivo study | In mice, INCB054329 has high clearance and short half-life. INCB054329 was effective and well tolerated in the c-myc and mm1. s xenograft tumor models at exposure levels sufficient to effectively inhibit KMS-12-BM. In vivo, oral INCB054329 inhibits tumor growth in a variety of hematologic cancer models. |
INCB-054329,INCB-54329 - Introduction
INCB054329 is a chemical that is a molecularly targeted inhibitor. The following is a detailed description of the nature, use, preparation and safety information of INCB054329:
Nature:
INCB054329 is an organic compound with a chemical formula of C20H21N3O4S3 and a molecular weight of 475.59g/mol. It is a white solid and has a certain solubility.
Use:
INCB054329 is mainly used to treat certain types of cancer, especially malignant tumors of the blood system. It inhibits the activity of specific enzymes, blocking the growth and spread of cancer cells, thereby playing an anti-tumor effect.
Preparation Method:
INCB054329 is usually prepared by chemical synthesis. Specific preparation procedures may vary due to the commercial secrecy of a particular synthetic route. In general, the preparation route of the compound requires the use of organic synthesis technology and suitable raw materials, the reaction is carried out under specific reaction conditions, and the target compound is produced through a series of steps.
Safety Information:
Last Update:2024-04-10 22:29:15