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CAS No.: 1675203-84-5

BMS-202 Catalog No. CSN17334

Synonyms: PD-1/PD-L1 Inhibitor 2;Programmed Cell Death 1/Programmed Cell Death-Ligand 1 Inhibitor 2;PD1-PDL1 Inhibitor 2

PD1-PDL1 inhibitor 2 is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction with IC50 of 18 nM.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PD-1/PD-L1

IC50:18nM
描述Activation of PD-1/PD-L1 signaling can induce T-cell hybridoma apoptosis, as well as negatively regulate antigen-specific T-cell-mediated immunologic responses. Also, PD-1/PD-L1 signaling blockade is an effective cancer immunotherapy. PD-1/PD-L1 inhibitor 2 (also called BMS202) is a small-molecule PD-1/PD-L1 interaction inhibitor with IC50 value of 18nM. Blockade of the PD-1 /PD-L1 ligation can enhance the immune response and improve T cell activity in chronic infection systems, as well as enhance the responses to therapeutic vaccination. Within concentrations ranging in 0.01-10μΜ, PD1-PDL1 Inhibitor 2 could improve the immune response to a tumor antigen, a viral antigen, a bacterial antigen or any pathogen in a subject by provoking and amplifying autoimmune responses. Incubation with PD1-PDL1 Inhibitor 2 could stabilize PD-L1 thermally and induce unfolding of PD-L1, while PD-L2 was characterized by a comparable melting temperature. In a crystal structure of PD1-PDL1 Inhibitor 2/PD-L1 complex, PD1-PDL1 Inhibitor 2 binds at a hydrophobic cavity forming upon PD-L1 dimerization. PD1-PDL1 Inhibitor 2 dissociated PD-1/PD-L1 interaction at stoichiometric concentration, consistent with the estimated KD of the PD-1/PD-L1 complex of 8μM, which is specific for PD-L1.
动物研究
动物给药方法
i.p.
剂量
Mice: 20 mg/kg ^[1] (i.p.)
临床研究

动物研究
动物给药方法	i.p.
剂量	Mice: 20 mg/kg ^[1] (i.p.)

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03469713	Renal Cancer Metastatic	Phase 2	Recruiting	July 14, 2020	Italy ... more >> Struttura Complessa di OncologiaIRCCS- Istituto in Tecnologie Avanzate e Modelli Assistenziali in Oncologia Arcispedale Santa Maria Nuova Recruiting Reggio Emilia, Italy, 42123 Contact: Roberta gnoni, biologist +390522295181 gnoni.roberta@ausl.re.it Sub-Investigator: Carmine Pinto, MD Collapse <<

参考文献

[1] Ashizawa T, Iizuka A, Tanaka E, Kondou R, Miyata H, Maeda C, Sugino T, Yamaguchi K, Ando T, Ishikawa Y, Ito M, Akiyama Y. Antitumor activity of the PD-1/PD-L1 binding inhibitor BMS-202 in the humanized MHC-double knockout NOG mouse. Biomed Res. 2019;40(6):243-250. doi: 10.2220/biomedres.40.243. PMID: 31839668.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3837 mL
- 11.9185 mL
- 23.8370 mL
- 5 mM
- 0.4767 mL
- 2.3837 mL
- 4.7674 mL
- 10 mM
- 0.2384 mL
- 1.1918 mL
- 2.3837 mL

技术信息

CAS号

1675203-84-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H29N3O3

运输

蓝冰

分子量

419.52

别名

PD-1/PD-L1 Inhibitor 2;Programmed Cell Death 1/Programmed Cell Death-Ligand 1 Inhibitor 2;PD1-PDL1 Inhibitor 2

溶解度

DMSO	83.0 mg/mL (197.8 mM)
Water	Insoluble
Ethanol	83.0 mg/mL (197.8 mM)

动物实验配方

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