2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. PD-1/PD-L1-IN-NP19

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。

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

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

CAS No. : 2377916-66-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4640
In-stock
1 mg ￥1727
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5 mg ￥3800
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10 mg ￥6000
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Customer Review

PD-1/PD-L1-IN-NP19 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 10 μM
Compound: NP19
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 32667799]
B16-F10 IC50
> 10 μM
Compound: NP19
Cytotoxicity against mouse B16/F10 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against mouse B16/F10 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 32667799]
HEK293 IC50
> 1 μM
Compound: NP19
Inhibition of mouse biotin-labelled C-terminal Fc-fused/Avi-tagged PD1/Fc-fused PDL1 expressed in HEK293 cells protein-protein interaction measured after 2 hrs by ELISA
Inhibition of mouse biotin-labelled C-terminal Fc-fused/Avi-tagged PD1/Fc-fused PDL1 expressed in HEK293 cells protein-protein interaction measured after 2 hrs by ELISA
[PMID: 32667799]
HEK293 IC50
12.5 nM
Compound: NP19
Inhibition of human C-terminal Ig-Fc-tagged PD1 (Leu25 to Gln167 residues) expressed in HEK293 cells/human C-terminal epitope-His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction preincubated for 15 mins with PD
Inhibition of human C-terminal Ig-Fc-tagged PD1 (Leu25 to Gln167 residues) expressed in HEK293 cells/human C-terminal epitope-His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction preincubated for 15 mins with PD
[PMID: 32667799]
MCF7 IC50
> 10 μM
Compound: NP19
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 32667799]
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].

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

PD-1/PD-L1-IN-NP19 相关抗体:
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].

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[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
性状

固体

颜色

White to off-white

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
细胞实验： 

DMSO 中的溶解度 : 2 mg/mL (3.60 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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 --- --- ---
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.25%

COA (289 KB) HNMR (203 KB) LCMS (88 KB)

产品使用指南 (1538 KB)
参考文献

PD-1/PD-L1-IN-NP19 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8016 mL 9.0080 mL 18.0161 mL 45.0402 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD-1/PD-L1-IN-NP192377916-66-8PD-1/PD-L1PD-1/Programmed death-ligand 1interactionimmunemicroenvironmenttumorcancerInhibitorinhibitorinhibit

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