PD-1/PD-L1-IN-NP19

CAS: 2377916-66-8 货号: P656651 分子式: C33H31ClN2O4 分子量: 555.06 PubChem CID: 154573771
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
P656651-1ml
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¥4,640.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC 50 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

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. PD-1/PD-L1-IN-NP19 exhibits much lower activity for inhibiting mouse PD-1/PD-L1 interaction with an IC 50 in the micromolar range (>1µM), as compared to the inhibition of human PD1/PD-L1 interaction (IC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . 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 . MCE 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.

IC50& Target:IC50: 12.5 nM (human PD-1/PD-L1)

规格

规格或纯度
10mM in DMSO
英文名称
PD-1/PD-L1-IN-NP19
生化机理
PD-1/PD-L1-IN-NP19是一种PD-1/PD-L1抑制剂,与人类PD-1/PD-L1相互作用的IC50为12.5 nM。PD-1/PD-L1-IN-NP19可激活肿瘤的免疫微环境,这可能是其发挥抗肿瘤作用的原因之一。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=C(C=CC=C1C2=CC=CC=C2)COC3=C(C=C(C(=C3)OCC4=CC(=CC=C4)C#N)CNC(C)(C)C(=O)O)Cl
PubChem CID
分子量
555.06

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常见问题

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请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
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本产品采用干冰配冷袋冷冻运输。收货后请立即拆包,并按上述储存条件保存;处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少?
本产品的 CAS 号为 2377916-66-8,分子式为 C33H31ClN2O4,分子量为 555.06 g/mol。
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