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

PD-1/PD-L1-IN-NP19 是 PD-1/PD-L1 的抑制劑,抑制人類 PD-1/PD-L1 相互作用的 IC50 值為 12.5 nM。PD-1/PD-L1-IN-NP19 可以激活腫瘤的免疫微環(huán)境,這可能有助于其抗腫瘤作用。

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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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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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]

細胞效力
(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]
體外研究
(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.

體內(nèi)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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 2 mg/mL (3.60 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.8016 mL 9.0080 mL 18.0161 mL
5 mM --- --- ---
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.25%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱:
PD-1/PD-L1-IN-NP19
目錄號:
HY-131347
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