PD-1/PD-L1-IN-NP19

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PD-1/PD-L1-IN-NP19  纯度: 98.05%

PD-1/PD-L1-IN-NP19 是 PD-1/PD-L1 的抑制剂，抑制人类 PD-1/PD-L1 相互作用的 IC50 值为 12.5 nM。PD-1/PD-L1-IN-NP19 可以激活肿瘤的免疫微环境，这可能有助于其抗肿瘤作用。

PD-1/PD-L1-IN-NP19

PD-1/PD-L1-IN-NP19 Chemical Structure

CAS No. : 2377916-66-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4640 In-stock
5 mg ￥3800 In-stock
10 mg ￥6000 In-stock
25 mg ￥11500 In-stock
50 mg ￥18000 In-stock
100 mg ￥28500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PD-1/PD-L1-IN-NP19 相关产品

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生物活性

PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects[1].

IC50 & Target

IC50: 12.5 nM (human PD-1/PD-L1)[1]
体外研究
(In Vitro)

PD-1/PD-L1-IN-NP19 (compound NP19) (0.37-10 μM; 72 h) significantly elevates the production of IFN-γ in a dose dependent manner from T cells co-cultured with tumor cells[1].
PD-1/PD-L1-IN-NP19 exhibits much lower activity for inhibiting mouse PD-1/PD-L1 interaction with an IC50 in the micromolar range (>1µM), as compared to the inhibition of human PD1/PD-L1 interaction (IC50=12.5 nM)[1].
PD-1/PD-L1-IN-NP19 (10 µM; 48 h) displays no apparent cytotoxic effects on A549, MCF-7, and B16-F10 cells at a concentration of 10 µM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PD-1/PD-L1-IN-NP19 (compound NP19) (25-100 mg/kg; intragastric gavage once daily for 15 d) inhibits the growth of melanoma tumors dramatically in mice[1].
PD-1/PD-L1-IN-NP19 (25 mg/kg; i.p. daily for 14 d) demonstrates significant antitumor efficacy with a tumor growth inhibition (TGI) of 76.5% and is well tolerated in an H22 hepatoma mouse model[1].
PD-1/PD-L1-IN-NP19 (1 mg/kg; i.v.) shows the half time (t1/2=1.5±0.5 h), clearance rate (CL=0.9±0.2 L/h/kg) and apparent distribution volume (Vss=2.1±0.5 L/kg) in rats[1].
PD-1/PD-L1-IN-NP19 (10 mg/kg; p.o.) shows the oral absorption (Tmax=0.6±0.2 h), long half-life (t1/2=10.9±7.7 h) and oral bioavailability (F=5%) in rats[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (6-8 weeks) with B16-F10 melanoma tumors[1]
Dosage: 25, 50, 100 mg/kg
Administration: Intragastric gavage once daily for 15 days
Result: Inhibited the growth of melanoma tumors up to 51.1, 75 and 80.9% at dose of 25, 50, 100 mg/kg, respectively.
Exhibited normal physical activity and increased body weights slightly.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: 1 mg/kg for i.v. and 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: I.v. and p.o.
Result: I.v.: t1/2=1.5 h; Cmax=1751 μg/L; CL=0.9 L/h/kg.
P.o.: t1/2=10.9 h; Cmax=69.5 μg/L; CL=23.1 L/h/kg.

分子量

555.06

Formula

C33H31ClN2O4
CAS 号

2377916-66-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 2 mg/mL (3.60 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8016 mL 9.0080 mL 18.0161 mL
5 mM — — —
10 mM — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Cheng B, et, al. Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction As Potential Anticancer Agents. J Med Chem. 2020 Jul 15.

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