PD-1/PD-L1-IN-10

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PD-1/PD-L1-IN-10  纯度: 99.29%

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。

PD-1/PD-L1-IN-10

PD-1/PD-L1-IN-10 Chemical Structure

CAS No. : 2487550-41-2

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PD-1/PD-L1-IN-10 相关产品

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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[1].

IC50 & Target

IC50: 2.7 nM (PD-1/PD-L1)[1].
体外研究
(In Vitro)

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[1].
PD-1/PD-L1-IN-10 (compound B2) does not affect cell viability of LLC cells and lymph node T-cells[1].
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[1].

上海金畔生物科技有限公司 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-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.[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: LLC tumor-bearing mice[1].
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.

分子量

581.62

Formula

C33H31N3O7
CAS 号

2487550-41-2
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
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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Yiqiang OuYang, et al. Design, Synthesis, and Evaluation of o-(Biphenyl-3-ylmethoxy)nitrophenyl Derivatives as PD-1/PD-L1 Inhibitors with Potent Anticancer Efficacy In Vivo. J Med Chem. 2021 May 26.

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