受注:045-509-1970 |
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Synonyms | Storage (From the date of receipt) |
3 years -20°C powder | ||
化学式 | C19H16N4O3 |
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分子量 | 348.36 | CAS No. | 1628607-64-6 | |
Solubility (25°C)* | 体外 | DMSO | 70 mg/mL (200.94 mM) | |
Ethanol | 70 mg/mL (200.94 mM) | |||
Water | ˂1 mg/mL | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | INCB054329 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-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively. |
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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[1]. 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[2]. 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[3]. |
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[1]. In vivo, oral administration of INCB054329 inhibits tumor growth in several models of hematologic cancers[2]. |
細胞アッセイ | 細胞株 | Myeloma, AML, DLBCL cells |
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濃度 | -- | |
反応時間 | 72 h | |
実験の流れ | Cell viability assay |
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動物実験 | 動物モデル | KMS-12-BM tumors established in female Nu/Nu mice |
投薬量 | 3, 10, 30, or 100 mg/kg | |
投与方法 | oral |
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Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] | PubMed: 35758684 |
BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection [ Cell, 2021, S0092-8674(21)00354-8] | PubMed: 33811809 |
Bromodomain and Extraterminal Inhibition Blocks Inflammation-Induced Cardiac Dysfunction and SARS-CoV-2 Infection (Pre-Clinical) [ bioRxiv, 2021, 10.1101/2020.08.23.258574] | PubMed: N/A |
BRDT is a novel regulator of eIF4EBP1 in renal cell carcinoma [ Oncol Rep, 2020, 44(6):2475-2486] | PubMed: 33125143 |
Predicting response to BET inhibitors using computational modeling: A BEAT AML project study. [ Leuk Res, 2019, 77:42-50] | PubMed: 30642575 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。