1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. PD-L1-IN-5

PD-L1-IN-5 (X22) 是一个口服活性的PD-L1抑制剂,IC50 值为 785.6 nM。PD-L1-IN-5 具有体内抗肿瘤活性。

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PD-L1-IN-5 Chemical Structure

PD-L1-IN-5 Chemical Structure

CAS No. : 2597056-85-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PD-L1-IN-5 (X22) is an orally active PD-L1 inhibitor, with the IC50 value of 785.6 nM. PD-L1-IN-5 has anti-tumor activity in vivo[1].

体外研究
(In Vitro)

PD-L1-IN-5 (X22) (0-150 μM, 12 h) 在体外对 MC38 和 CT26 细胞没有明显的细胞毒作用[1]

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

体内研究
(In Vivo)

PD-L1-IN-5 (X22) (5 or 25 mg/kg , 每天口服持续20天) 通过上调肿瘤浸润和 CD8+ T 细胞的部分毒性,在 MC38 和 CT26 结肠癌的小鼠模型中表现出明显的抗肿瘤效果,但在免疫缺陷裸鼠同基因 CT26 结直肠癌模型中表现出较低的抗肿瘤作用,表明其抗肿瘤机制依赖于免疫系统[1]

SD 大鼠和 C57blo/6小鼠中的药代动力学分析[1]

Animal model Route Dose (mg/kg) t1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) CL (mL/h/kg) F (%)
SD rat p.o. 45 4.3 4.00 49.8 405.6 / 3.4
C57blo/6 mice p.o. 10 1.6 0.7 255.7 315.6 / 11.5

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

Animal Model: MC38 and CT26 tumor mouse model, Balb/c mice (female, 8 week old)[1]
Dosage: 0-50 mg/kg/day for 20 days
Administration: p.o.
Result: Inhibited colon tumor growth in mice with tumor growth inhibition rates (TGI) of 49.5% and 73.6% at doses of 5 mg/kg and 25 mg/kg, respectively.
分子量

763.25

Formula

C40H44ClFN4O8

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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-L1-IN-5
目录号:
HY-162357
需求量: