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BMS-202

BMS-202

产品编号 T3146   CAS 1675203-84-5
别名: PD1-PDL1 inhibitor 2, PD-1/PD-L1 inhibitor 2

BMS-202 (PD1-PDL1 inhibitor 2) 是一种非肽类 PD-1/PD-L 复合物抑制剂,其 IC50为 18 nM,KD 为 8 μM。它与 PD-L1 直接结合并阻断人类 PD-1/PD-L 的相互作用,具有抗肿瘤活性。

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BMS-202 Chemical Structure
BMS-202, CAS 1675203-84-5
规格 价格/CNY 货期 数量
1 mg ¥ 311 现货
5 mg ¥ 925 现货
10 mg ¥ 1,432 现货
25 mg ¥ 2,953 现货
50 mg ¥ 3,490 现货
100 mg ¥ 4,990 现货
1 mL * 10 mM (in DMSO) ¥ 976 现货
其他形式的 BMS-202:
产品目录号及名称: BMS-202 (T3146)
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选择批次  
纯度: 99.09%
纯度: 98.54%
纯度: 98.24%
纯度: 97.92%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.
靶点活性 PD-1/PD-L1 interaction:0.018 μM
体外活性 BMS-202 inhibits PD-1/PD-Ll interaction, and may augment therapeutic immune response to a number of histologically distinct tumors. Blockade of the PD-1/PD-Ll ligation using antibodies to PD-Ll has been shown to restore and augment T cell activation in many systems[1].
激酶实验 All binding studies are performed in an HTRF assay buffer consisting of dPBS supplemented with 0.1% (with v) bovine serum albumin and 0.05% (v/v) Tween-20. For the PD-l-Ig/PD-Ll-His binding assay, inhibitors are pre-incubated with PD-Ll-His (10 nM final) for 15 m in 4 μL of assay buffer, followed by addition of PD-l-Ig (20 nM final) in 1 μL of assay buffer and further incubation for 15 m. PD-L1 from either human, cyno, or mouse are used. HTRF detection is achieved using europium crypate-labeled anti- Ig (1 nM final) and allophycocyanin (APC) labeled anti-His (20 nM final). Antibodies are diluted in HTRF detection buffer and 5 μL is dispensed on top of binding reaction. The reaction mixture is allowed to equilibrate for 30 minutes and signal (665 nm/620 nm ratio) is obtained using an En Vision fluorometer. Additional binding assays are established between PD-1-Ig/PD-L2-His (20, 5 nM, respectively), CD80-His/PD-Ll-Ig (100, 10 nM, respectively) and CD80-His/CTLA4-Ig (10, 5 nM, respectively).
别名 PD1-PDL1 inhibitor 2, PD-1/PD-L1 inhibitor 2
分子量 419.52
分子式 C25H29N3O3
CAS No. 1675203-84-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 76 mg/mL(181.2 mM)

Ethanol: 83 mg/mL (197.85 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.3837 mL 11.9184 mL 23.8368 mL 59.5919 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 mL 11.9184 mL
10 mM 0.2384 mL 1.1918 mL 2.3837 mL 5.9592 mL
20 mM 0.1192 mL 0.5959 mL 1.1918 mL 2.9796 mL
50 mM 0.0477 mL 0.2384 mL 0.4767 mL 1.1918 mL
100 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5959 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Louis S. Chupak, et al. Compounds useful as immunomodulators. WO 2015034820 A1 2. Yang X, Cheng B, Xiao Y, et al. Discovery of Novel CA-4 Analogs as Dual Inhibitors of Tubulin Polymerization and PD-1/PD-L1 Interaction for Cancer Treatment[J]. European Journal of Medicinal Chemistry. 2020: 113058.

文献引用

1. Dai W, Wu J, Peng X, et al. CDK12 orchestrates super‐enhancer‐associated CCDC137 transcription to direct hepatic metastasis in colorectal cancer. Clinical and Translational Medicine. 2022, 12(10): e1087. 2. Yang X, Cheng B, Xiao Y, et al. Discovery of Novel CA-4 Analogs as Dual Inhibitors of Tubulin Polymerization and PD-1/PD-L1 Interaction for Cancer Treatment. European Journal of Medicinal Chemistry. 2021 Mar 5;213:113058. doi: 10.1016 3. Zhang H, Zhou S, Plewka J, et al.Design, Synthesis, and Antitumor Activity Evaluation of 2-Arylmethoxy-4-(2, 2′-dihalogen-substituted biphenyl-3-ylmethoxy) Benzylamine Derivatives as Potent PD-1/PD-L1 Inhibitors.Journal of Medicinal Chemistry.2023 4. Zhang H, Zhou S J, Shen C F, et al.PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway.Journal of Enzyme Inhibition and Medicinal Chemistry.2023, 38(1): 2230388.
Oncrasin-1 CDK8-IN-13 CCT128930 hydrochloride Azoramide Isosilybin A Chelidonine Aurintricarboxylic acid Devimistat

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 经典已知活性库 细胞周期化合物库 抗乳腺癌化合物库 PPI抑制剂库 抗癌化合物库 表型筛选靶点鉴定库 血脑屏障通透化合物库 细胞凋亡化合物库 肿瘤免疫治疗小分子化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BMS-202 1675203-84-5 Apoptosis Cell Cycle/Checkpoint Immunology/Inflammation PD-1/PD-L1 BMS202 antitumor PD1-PDL1 inhibitor 2 PD-1/PD-L1 inhibitor 2 dimeric anti-proliferation BMS 202 nonpeptidic immune-response Thermal stabilization Inhibitor inhibit hydrophobic inhibitor

 

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