2. Immunology/Inflammation GPCR/G Protein
  3. PD-1/PD-L1 CXCR
  4. PD-1/PD-L1-IN-63

PD-1/PD-L1-IN-63 是一种具有口服活性的 PD-1/PD-L1 抑制剂，IC50 为 9.1 nM。PD-1/PD-L1-IN-63 可阻断 PD-1/PD-L1 相互作用，诱导癌细胞死亡并抑制肿瘤生长。PD-1/PD-L1-IN-63 可用于黑色素瘤的研究。

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PD-1/PD-L1-IN-63

PD-1/PD-L1-IN-63 Chemical Structure

CAS No. : 2691796-92-4

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PD-1/PD-L1-IN-63 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma[1].

体外研究
(In Vitro)

PD-1/PD-L1-IN-63 (compound P18) 可强效抑制 PD-1/PD-L1 蛋白相互作用，在 HTRF 结合实验中的 IC50 为 9.1 nM[1]。
PD-1/PD-L1-IN-63 可结合纯化的人源 PD-L1 (KD = 88.3 nM) 和鼠源 PD-L1 (KD = 174 nM) 蛋白[1]。
PD-1/PD-L1-IN-63 (0.05-5 μM) 可剂量依赖性结合纯化的人源 PD-L1 (KD = 202 nM) 和鼠源 PD-L1 (KD = 471 nM) 蛋白，该结果由 SPR 检测得出[1]。
PD-1/PD-L1-IN-63 (37-1000 nM; 48 h) 在 HepG2/hPD-L1 与 Jurkat/hPD-1 共培养细胞模型中以剂量依赖方式促进 HepG2 细胞死亡，在 1000 nM 浓度下可使 HepG2 细胞死亡率提升 58.2%[1]。
PD-1/PD-L1-IN-63 (48 h) 可在体外抑制 MCF-7、H1299、HeLa、HepG2 和 Jurkat 细胞的增殖，其 IC50 值范围为 2.3 μM 至 4.1 μM[1]。

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

PD-1/PD-L1-IN-63 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HepG2/hPD-L1, Jurkat/hPD-1
Concentration: 37, 111, 333, 1000 nM
Incubation Time: 48 h
Result: Promoted HepG2 cell death in a dose-dependent manner.
At 1000 nM, elevated the mortality rate of HepG2 cells by 58.2%, which was significantly higher than the positive control BMS-202.

Cell Viability Assay[1]

Cell Line: MCF-7, H1299, HeLa, HepG2, Jurkat
Concentration: /
Incubation Time: 48 h
Result: Had IC50 values of MCF-7 (3.2 μM), H1299 (3.7 μM), HeLa (4.1 μM), HepG2 (2.3 μM), Jurkat (2.8 μM).
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax CL Vz Cmax F
Rat[1] 1 mg/kg i.v. 718.8 ng·h/mL 831.7 ng·h/mL 11.6 h 19.9 h 18.1 h 0.083 h 1.3 L/h/kg 31 L/kg 257.2 ng/mL /
Rat[1] 10 mg/kg p.o. 771.2 ng·h/mL 961.3 ng·h/mL 17.2 h 29.7 h 20.9 h 6.3 h 10.8 L/h/kg 310.2 L/kg 52.7 ng/mL 12 %
体内研究
(In Vivo)

PD-1/PD-L1-IN-63 (50-100 mg/kg；灌胃；每日一次；连续 14 天) 在接种 B16-F10 黑色素瘤的人源化 PD-1 C57BL/6J 小鼠中展现出强效的剂量依赖性抗肿瘤活性[1]。
PD-1/PD-L1-IN-63 (P18) (50-100 mg/kg；灌胃；每日；14 天) 在健康 BALB/c 小鼠中以 50 或 100 mg/kg 的剂量每日灌胃给药 14 天时，不会引发心脏毒性或骨髓抑制[1]。

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

Animal Model: C57BL/6J-Pdcdem1(hPDCD1)/Smoc (n=5 per group)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: i.g.; daily; 14 days
Result: Reduced tumor weight by 69.7% and tumor volume by 89.6% at 50 mg/kg compared to vehicle control.
Reduced tumor weight by 78.1% and tumor volume by 94.1% at 100 mg/kg compared to vehicle control.
Did not cause significant changes in body weight, spleen weight, or thymus weight compared to vehicle control.
Significantly increased tumor mRNA expression of CXCR3, CXCL9, and CXCL10 in the 100 mg/kg group.
Significantly reduced PD-L1 mRNA expression in both treatment groups.
Significantly increased tumor-infiltrating CD3+CD4+ and CD3+CD8+ T cell percentages in a dose-dependent manner in tumor tissue (but not spleen).
Significantly reduced tumor PD-L1 protein expression in both treatment groups.
Showed no morphological aberrations in liver and kidney via H&E staining compared to vehicle control.
Showed no significant differences in serum liver and kidney function markers compared to vehicle control.
分子量

696.11

Formula

C37H41Cl3N4O3
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

PD-1/PD-L1-IN-63 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PD-1/PD-L1-IN-632691796-92-4PD-1/PD-L1CXCRPD-1/Programmed death-ligand 1CXC chemokine receptorsC-X-C motif chemokine receptorsH1299 cellscancer cell deathJurkat cellsPD-1/PD-L1 interactionimmune checkpoint humanized mouse modelsHeLa cellsHepG2 cellsMCF-7 cellstumor growthmelanomaInhibitorinhibitorinhibit

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