BMS-1

製品コードS7911 バッチS791103

印刷

化学情報

 Chemical Structure Synonyms PD-1/PD-L1 inhibitor 1 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C29H33NO5

分子量 475.58 CAS No. 1675201-83-8
Solubility (25°C)* 体外 DMSO 95 mg/mL (199.75 mM)
Water 95 mg/mL (199.75 mM)
Ethanol 5 mg/mL (10.51 mM)
* <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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 BMS-1 is a small-molecule inhibitor of PD-1/PD-L1 interaction with IC50 of 6 nM.
in vitro

PD-1/PD-L1 inhibitor 1 causes half-reduced cell viability at lower concentrations in triple-negative breast cancer (TNBC), activates ERK in MDA-MB-231 and MCF7, significantly increases IL-8 expression in MDA-MB-231 and HCC1806 when administrated in combination with ERK1/2 inhibitor, also potently downregulates the IL-8 expression to its half amount in MDA-MB-231.[2]

in vivo

PD-1/PD-L1 inhibitor 1 combined with Jiedu Sangen Decoction (JSD) remarkably inhibits and reverses epithelial-mesenchymal transition (EMT) via PI3K/AKT signaling pathway.[3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MDA-MB-231 cells, HCC1937 cells, HCC1806 cells, MCF7 cells
濃度 --
反応時間 72 h
実験の流れ

Cell proliferation is determined by the MTS assay. A total of 1-2×103 cells are plated in 100 μl medium in each well of a 96-well plate. After 24 h, PD-1/PD-L1 inhibitor 1 and ERK1/2 inhibitor are diluted to the desired concentrations in test medium (DMEM containing 1% fetal bovine serum) and added as single or as combined treatment in triplicate for 72 h.

動物実験 動物モデル Male specific pathogen free BALB/c mice of hepatic metastatic colorectal cancer (CRC) model
投薬量 100 µg
投与方法 i.p.

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:

Development and In Vivo Evaluation of Small-Molecule Ligands for Positron Emission Tomography of Immune Checkpoint Modulation Targeting Programmed Cell Death 1 Ligand 1 [ J Med Chem, 2024, 67(5):4036-4062] PubMed: 38442487
Identification of CBPA as a New Inhibitor of PD-1/PD-L1 Interaction [ Int. J. Mol. Sci, 2023, 24(4)] PubMed: None
Identification of CBPA as a New Inhibitor of PD-1/PD-L1 Interaction [ Int J Mol Sci, 2023, 24(4)3971] PubMed: 36835382
Identification of CBPA as a New Inhibitor of PD-1/PD-L1 Interaction [ Int J Mol Sci, 2023, 24(4)3971] PubMed: 36835382
Hepatobiliary Tumor Organoids Reveal HLA Class I Neoantigen Landscape and Antitumoral Activity of Neoantigen Peptide Enhanced with Immune Checkpoint Inhibitors [ Adv Sci (Weinh), 2022, 9(22):e2105810] PubMed: 35665491
Alpha5 nicotinic acetylcholine receptor mediated immune escape of lung adenocarcinoma via STAT3/Jab1-PD-L1 signalling [ Cell Commun Signal, 2022, 20(1):121] PubMed: 35971127
Discovery of a new inhibitor targeting PD-L1 for cancer immunotherapy [ Neoplasia, 2021, 23(3):281-293] PubMed: 33529880
Inhibitors of PD-1/PD-L1 and ERK1/2 impede the proliferation of receptor positive and triple-negative breast cancer cell lines [ J Cancer Res Clin Oncol, 2021, 10.1007/s00432-021-03694-4] PubMed: 34185141
The Stone Guest: How Does pH Affect Binding Properties of PD-1/PD-L1 Inhibitors [ ChemMedChem, 2021, 16(3):568-577] PubMed: 33085193
Small-molecule PD-L1 inhibitor BMS1166 abrogates the function of PD-L1 by blocking its ER export [ Oncoimmunology, 2020, 9(1):1831153] PubMed: 33110706

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。