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化学情報
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C19H18ClN5OS |
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| 分子量 | 399.90 | CAS No. | 1446144-04-2 | |
| Solubility (25°C)* | 体外 | DMSO | 79 mg/mL warmed with 50ºC water bath (197.54 mM) | |
| Ethanol | 46 mg/mL (115.02 mM) | |||
| Water | Insoluble | |||
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* <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. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4. |
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| in vitro | CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. [1] CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib. [2] |
| in vivo | BRD4 mediates CTD Ser2 phosphorylation in vivo. [1] In REC-1 tumor-bearing mice, the combination of lenalidomide with CPI203 (2.5 mg/kg i.p.) synergistically augments the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis. [2] |
プロトコル(参考用のみ)
| キナーゼアッセイ | BRD4 α-screen assay | |
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| The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. IC50 values are calculated using a 10-point serial dilution of BET inhibitor. | ||
| 細胞アッセイ | 細胞株 | 2 PBMC cultures from healthy donors and 9 MCL cell lines (Granta-519, JVM-2, UPN1, Z-138, JeKo-1, ZBR, JBR, Mino, REC-1 cells) |
| 濃度 | 10 μM | |
| 反応時間 | 72 hours | |
| 実験の流れ | MCL primary cells and cell lines are incubated as indicated with lenalidomide and/or CPI203. MTT is added for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Values are represented using untreated control cells. The GI50 is calculated as the concentration that produced 50 % growth inhibition. Combination indexes (CIs) are calculated by using the Calcusyn software version 2.0. The interaction between two drugs is considered synergistic when CI <1. |
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| 動物実験 | 動物モデル | REC-1 tumor-bearing mice |
| 投薬量 | 2.5 mg/kg twice daily | |
| 投与方法 | i.p | |
参考
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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| DELs enable the development of BRET probes for target engagement studies in cells [ Cell Chem Biol, 2023, 30(8):987-998.e24] | PubMed: 37490918 |
| Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] | PubMed: 35758684 |
| Targeting BET proteins BRD2 and BRD3 in combination with PI3K-AKT inhibition as a therapeutic strategy for ovarian clear cell carcinoma [ Mol Cancer Ther, 2021, molcanther.0809.2020] | PubMed: 33509905 |
| Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models [ Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0831] | PubMed: 34045230 |
| A new small-molecule compound, Q308, silences latent HIV-1 provirus by suppressing Tat- and FACT-mediated transcription [ Antimicrob Agents Chemother, 2021, AAC0047021] | PubMed: 34491808 |
| Genetically defined syngeneic mouse models of ovarian cancer as tools for the discovery of combination immunotherapy [ Cancer Discov, 2020, CD-20-0818] | PubMed: 33158843 |
| ARV-825-induced BRD4 protein degradation as a therapy for thyroid carcinoma. [ Aging (Albany NY), 2020, 12(5):4547-4557] | PubMed: 32163373 |
| Vitamin C supplementation expands the therapeutic window of BETi for triple negative breast cancer. [ EBioMedicine, 2019, 43:201-210] | PubMed: 30975544 |
| A novel bromodomain inhibitor, CPI-203, serves as an HIV-1 latency-reversing agent by activating positive transcription elongation factor b. [ Biochem Pharmacol, 2019, 164:237-251] | PubMed: 30991051 |
| Vitamin C Sensitizes Melanoma to BET Inhibitors. [ Cancer Res, 2018, 78(2):572-583] | PubMed: 29180474 |
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。