PD-1/PD-L1-IN-10|cas:2487550-41-2|西域试剂

PD-1/PD-L1-IN-10,99.29%

产品编号：Bellancom-132202| CAS NO：2487550-41-2| 分子式：C₃₃H₃₁N₃O₇| 分子量：581.62

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货号	价格	库存与货期
Bellancom-132202	￥1300.00	杭州北京（现货）
Bellancom-132202	￥2100.00	杭州北京（现货）
Bellancom-132202	￥7200.00	杭州北京（现货）
Bellancom-132202	￥11500.00	杭州北京（现货）

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PD-1/PD-L1-IN-10

产品介绍

PD-1/PD-L1-IN-10 (compound B2) 是具有口服活性的 PD-1/PD-L1 抑制剂 (IC₅₀ of 2.7 nM)，具有抗肿瘤活性。

生物活性

PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC₅₀ of 2.7 nM) with potent anticancer efficacy.

体外研究

PD-1/PD-L1-IN-10 (compound B2) significantly promotes interferongamma secretion in a dose-dependent manner in vitro even at the low concentration of 1 nM.
PD-1/PD-L1-IN-10 (compound B2) does not affect cell viability of LLC cells and lymph node T-cells.
PD-1/PD-L1-IN-10 (compound B2, 0-100 nM) stabilizes the PD-L1 protein in mouse Lewis lung carcinoma (LLC) cells. In particular, PD-1/PD-L1-IN-10 (compound B2) maintains the PD-L1 stability in a dose-dependent manner at 58 °C. Suggesting that PD-1/PD-L1-IN-10 (compound B2) could enter LLC cells and then directly binds to the PD-L1 protein.

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-10 (compound B2, 5 mg/kg, intragastric gavage) exhibits potent in vivo anticancer efficacy in an LLC-bearing allograft mouse model. PD-1/PD-L1-IN-10 (compound B2) effectively blocks tumor cell proliferation and induces apoptosis in LLC tumor tissues..

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

Animal Model:	LLC tumor-bearing mice.
Dosage:	2, 5 mg/kg.
Administration:	i.g., qd., for 21 days
Result:	Significantly suppressed the growth of the tumor in a dose-dependent manner compared with the vehicle group.

体内研究

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

Animal Model:	LLC tumor-bearing mice.
Dosage:	2, 5 mg/kg.
Administration:	i.g., qd., for 21 days
Result:	Significantly suppressed the growth of the tumor in a dose-dependent manner compared with the vehicle group.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (171.93 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7193 mL	8.5967 mL	17.1934 mL
5 mM	0.3439 mL	1.7193 mL	3.4387 mL
10 mM	0.1719 mL	0.8597 mL	1.7193 mL

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明