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产品名称 | PD-1 ↓ ↑ | PD-1/PD-L1 ↓ ↑ | PD-1/PD-L1 interaction ↓ ↑ | PD-L1 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SR0987 | ✔ | 98% | |||||||||||||||||
Pembrolizumab | ✔ | 98% | |||||||||||||||||
Camrelizumab | ✔ | 5mg/mL | |||||||||||||||||
Spartalizumab | ✔ | 95% | |||||||||||||||||
BMS-1001 |
+
PD-1/PD-L1, EC50: 253 nM |
+
PD-1/PD-L1, EC50: 253 nM |
98% | ||||||||||||||||
INCB086550 |
++
PD-1/PD-L1, IC50: <10 nM |
++
PD-1/PD-L1, IC50: <10 nM |
98% | ||||||||||||||||
BMS-1 |
++
PD-1/PD-L1 interaction, IC50: 0.006 μM |
99%+ | |||||||||||||||||
BMS-202 |
+
PD-1/PD-L1 interaction, IC50: 0.018 μM |
99%+ | |||||||||||||||||
PD-1/PD-L1-IN 3 |
+++
PD-1/PD-L1 interaction, IC50: 5.6 nM |
98+% | |||||||||||||||||
Nivolumab |
+++
PD-1/PD-L1 interaction, IC50: 2.52 nM |
95% | |||||||||||||||||
BMS-1166 |
+++
PD-1/PD-L1 interaction, IC50: 1.4 nM |
99%+ | |||||||||||||||||
Durvalumab |
++++
PD-1/PD-L1 interaction, IC50: 0.1 nM |
95% | |||||||||||||||||
Evixapodlin |
++++
PD-1/PD-L1, IC50: 0.213 nM |
95% | |||||||||||||||||
CA-170 | ✔ | 97% (contains 2.7% ethanol) | |||||||||||||||||
Atezolizumab |
+++
hPD-L1, Kd: 0.4 nM |
98% | |||||||||||||||||
AUNP-12 | ✔ | 99% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | PD-1/PD-L1-IN-10 is an orally bioavailable inhibitor of PD-1/PD-L1 (IC50: 2.7 nM) with robust anticancer activity[1]. |
体内研究 | PD-1/PD-L1-IN-10 (5 mg/kg, administered via intragastric gavage) demonstrates potent anticancer efficacy in vivo in a mouse model with LLC-bearing allografts. It effectively inhibits tumor cell proliferation and induces apoptosis in LLC tumor tissues[1]. |
体外研究 | PD-1/PD-L1-IN-10 markedly enhances interferon-gamma secretion in a dose-dependent manner in vitro, even at the low concentration of 1 nM[1]. PD-1/PD-L1-IN-10 has no impact on the cell viability of LLC cells and lymph node T-cells[1]. PD-1/PD-L1-IN-10 (0-100 nM) enhances the stability of the PD-L1 protein in mouse Lewis lung carcinoma (LLC) cells. Specifically, PD-1/PD-L1-IN-10 maintains PD-L1 stability in a dose-dependent manner at 58 °C, indicating its potential to penetrate LLC cells and directly bind to the PD-L1 protein[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.72mL 0.34mL 0.17mL |
8.60mL 1.72mL 0.86mL |
17.19mL 3.44mL 1.72mL |
CAS号 | 2487550-41-2 |
分子式 | C33H31N3O7 |
分子量 | 581.615 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 105 mg/mL(180.53 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |