耗材描述
Cudarolimab
产品活性:Cudarolimab (IBI101) 是一种完全人抗 OX40 (CD134,一种由激活的免疫细胞表达的共刺激分子) 抗体。Cudarolimab 抑制 OX40 与其配体 OX40L 的结合。Cudarolimab 具有抗肿瘤活性,可用于癌症相关研究。
产品来源: https://www.medchemexpress.cn/cudarolimab.html
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Orexin Receptor (OX Receptor)
In Vitro: Cudarolimab (0.01, 1, 100 or 10000 nM) binds to OX40 and partially blocks the binding of OX40 to its ligand OX40L in CHO-S cells overexpressing human OX40 (CHO-S-hOX40). Cudarolimab activates OX40 dependent NF-κB reporters with an EC50 value of 4.432 nM in Jurkat-OX40 reporter cells co-cultured with Raji cells.
Cudarolimab (0.01, 0.1, 1, 10, 100 or 1000 nM) binds to activated human CD4+ T cells and activated cynomolgus monkey CD4+ T cells in a dose dependent manner.
Cudarolimab (0.4, 4.0 and 40.4 nM) increases IL-2 secretion with dose dependent manner in human CD4+ T cells.
In Vivo: Cudarolimab (10 mg/kg; i.p.; single dose on days 3, 7, 11, 14 and 15) significantly reduces tumor volume in humanized NOG mice bearing LoVo tumors.
Cudarolimab (0.1, 1 and 10 mg/kg; i.p.; single dose on days 6, 9, 12 and 16) significantly reduces tumor volume, increases IFN-γ+ and IFN-α+ expression in CD8+ T cells in tumor and spleen of human OX40 knock-in mice bearing MC38 tumors.
Cudarolimab (10 mg/kg; i.p.; single dose on days 10 and 14) significantly reduces the expression of CD3+CD8+, CD3+CD4+, CD4+CD25highFoxP3+ in the tumor and spleen of human OX40 knock-in mice bearing MC38 tumors.
Pharmacokinetic (PK) parameters of Cudarolimab in cynomolgus macaques
Dose (mg/kg)
Cmax (µg/mL )
Tmax (h)
AUC0-∞ (h•µg/mL )
T1/2 (h)
Cl (mL/h/kg)
MRTlast (h)
0.1
3.07±0.40
0.08±0.00
347.98±99.30
162.98±103.01
0.31±0.08
186.34±110.68
0.5
9.78±3.27
0.40±0.78
1429.19±607.21
129.47±114.44
0.40±0.14
136.03±108.05
2.5
63.10±15.29
0.08±0.00
10304.06±3403.59
190.89±92.94
0.27±0.09
212.29±114.61
12.5
296.57±58.05
0.40±0.78
33511.65±14982.36
120.30±153.26
0.44±0.20
114.93±87.66
相关产品:Orexin A (human, rat, mouse) (TFA) | Danavorexton | Almorexant | SB-334867 free base | YNT-185 dihydrochloride | Seltorexant | EMPA | JNJ-10397049 | Orexin 2 Receptor Agonist | SB-674042 | Filorexant | Orexin B, human TFA | SB-649868 | MK-1064 | OXA(17-33) | TCS 1102 | TCS-OX2-29 | ACT-462206 | GSK1059865 | Revdofilimab | Firazorexton | Orexin B, rat, mouse | RTIOXA-43 | SB-408124 | Vornorexant
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