PD-1/PD-L1-IN-NP19|cas:2377916-66-8|西域试剂

PD-1/PD-L1-IN-NP19,98.05%

产品编号：Bellancom-131347| CAS NO：2377916-66-8| 分子式：C₃₃H₃₁ClN₂O₄| 分子量：555.06

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货号	价格	库存与货期
Bellancom-131347	￥3800.00	杭州北京（现货）
Bellancom-131347	￥6000.00	杭州北京（现货）
Bellancom-131347	￥11500.00	杭州北京（现货）
Bellancom-131347	￥18000.00	杭州北京（现货）
Bellancom-131347	￥28500.00	杭州北京（现货）

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PD-1/PD-L1-IN-NP19

产品介绍

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。

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.

体外研究

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.
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).
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.
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.
PD-1/PD-L1-IN-NP19 (1 mg/kg; i.v.) shows the half time (t_1/2=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.
PD-1/PD-L1-IN-NP19 (10 mg/kg; p.o.) shows the oral absorption (T_max=0.6±0.2 h), long half-life (t_1/2=10.9±7.7 h) and oral bioavailability (F=5%) in rats.

西域 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
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
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.: t_1/2=1.5 h; C_max=1751 μg/L; CL=0.9 L/h/kg. P.o.: t_1/2=10.9 h; C_max=69.5 μg/L; CL=23.1 L/h/kg.

体内研究

西域 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
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
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.: t_1/2=1.5 h; C_max=1751 μg/L; CL=0.9 L/h/kg. P.o.: t_1/2=10.9 h; C_max=69.5 μg/L; CL=23.1 L/h/kg.

性状

Solid

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式