1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. PD-1/PD-L1-IN-9 hydrochloride

PD-1/PD-L1-IN-9 hydrochloride 

目录号: HY-132192A 纯度: 99.26%
COA 产品使用指南

PD-1/PD-L1-IN-9 盐酸盐是一种有效和具有口服活性的 PD-1/PD-L1 相互作用抑制剂,IC50 值为 3.8 nM。PD-1/PD-L1-IN-9 盐酸盐可以增强免疫细胞对肿瘤细胞的杀伤活性。PD-1/PD-L1-IN-9 盐酸盐在 CT26 小鼠模型中表现出显着的体内抗肿瘤活性。

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PD-1/PD-L1-IN-9 hydrochloride Chemical Structure

PD-1/PD-L1-IN-9 hydrochloride Chemical Structure

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5 mg ¥2800
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10 mg ¥4200
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25 mg ¥6700
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50 mg ¥9100
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Customer Review

Other Forms of PD-1/PD-L1-IN-9 hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model[1].

体外研究
(In Vitro)

PD-1/PD-L1-IN-9 盐酸盐(compound 24) (46.9-1500 nM; 预处理 2 h) 剂量依赖性地激活外周血单核细胞 (PBMCs) 对 MDB-MB 231 细胞的抗肿瘤免疫,EC50 约为 100 nM[1]

MCE 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-9 盐酸盐 (化合物24) (40-80 mg/kg; 口服; 每天一次,持续 2 周) 以剂量依赖的方式抑制肿瘤生长,并且不会导致小鼠体重减轻或死亡[1]
PD-1/PD-L1-IN-9 盐酸盐 (3 mg/kg; 静脉注射; 单次剂量) 在大鼠中的半衰期 T1/2=4.2 h、血浆清除率 Cl=11.5 L/h/kg,Cmax=1233 ng/mL[1]
PD-1/PD-L1-IN-9 盐酸盐 (25 mg/kg; 口服; 单次剂量) 在大鼠中表现出中等的口服生物利用度 (F= 22%)、半衰期 (t1/2=6.4 h),和 Cmax (=192 ng/mL)[1]

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

Animal Model: Male BALB/c mice (5-6 weeks) were inoculated CT26 cells[1]
Dosage: 40 mg/kg, 80 mg/kg
Administration: Oral gavage; once daily, for 2 weeks
Result: Significantly decreased the final tumor weight, with TGI values of 60 and 67% at the dose of 40 and 80 mg/kg, respectively.
Animal Model: Pharmacokinetic analysis in sprague-Dawley (SD) rats[1]
Dosage: 3 mg/kg and 25 mg/kg
Administration: Intravenous injection or oral gavage; single dose
Result:
Route Dose (mg/kg) AUC(0-t) (ng·h/mL) Cmax (ng/mL) t1/2 (h) Tmax Cl (L·h/kg) Vz (L/kg) F (%)
i.v. 3 430.5 1233 4.2 0.03 11.5 78.6 /
p.o. 25 787.4 192 6.4 0.69 28.8 249.3 22
分子量

384.90

Formula

C22H25ClN2O2

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (324.76 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 2.5981 mL 12.9904 mL 25.9808 mL
5 mM 0.5196 mL 2.5981 mL 5.1962 mL
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 (sealed storage, away from moisture)。-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

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
参考文献

PD-1/PD-L1-IN-9 hydrochloride 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 (sealed storage, away from moisture)。-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 2.5981 mL 12.9904 mL 25.9808 mL 64.9519 mL
5 mM 0.5196 mL 2.5981 mL 5.1962 mL 12.9904 mL
10 mM 0.2598 mL 1.2990 mL 2.5981 mL 6.4952 mL
15 mM 0.1732 mL 0.8660 mL 1.7321 mL 4.3301 mL
20 mM 0.1299 mL 0.6495 mL 1.2990 mL 3.2476 mL
25 mM 0.1039 mL 0.5196 mL 1.0392 mL 2.5981 mL
30 mM 0.0866 mL 0.4330 mL 0.8660 mL 2.1651 mL
40 mM 0.0650 mL 0.3248 mL 0.6495 mL 1.6238 mL
50 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2990 mL
60 mM 0.0433 mL 0.2165 mL 0.4330 mL 1.0825 mL
80 mM 0.0325 mL 0.1624 mL 0.3248 mL 0.8119 mL
100 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6495 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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产品名称:
PD-1/PD-L1-IN-9 hydrochloride
目录号:
HY-132192A
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