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Simlukafusp alfa
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:1776942-10-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
FAP-IL2v
产品介绍
Simlukafusp alfa (FAP-IL2v) 是一种免疫细胞因子,包括一种抗成纤维细胞活化蛋白 α (FAPα) 的抗体和一种只结合IL-2Rβγ的 IL-2 变体。Simlukafusp alfa 是一种人 IgG1 抗体。
生物活性

Simlukafusp alfa (FAP-IL2v) is an immunocytokine comprising an antibody against fibroblast activation protein α (FAPα) and anIL-2variant that only bindsIL-2Rβγ. Isotype: humanIgG1[1].

体外研究
(In Vitro)

Simlukafusp alfa (FAP-IL2v) 与 huIL-2Rβγ、cyIL-2Rβγ、muIL-2Rβγ、huFAP、cyFAP 和 muFAP的结合常数分别为43±9 pM、80±20 pM、660±80 pM、0.3 nM、0.23 nM 和 0.5 nM[1]
Simlukafusp alfa (0-100 nM; 5 days) 在体外激活 CD4+/CD8+ T 细胞和 NK 细胞,但不优先激活 Tregs[1]
Simlukafusp alfa (0-100 nM) 体外增强 Cetuximab (HY-P9905) 介导的抗体依赖细胞毒性 (ADCC) 和 Cibisatamab (HY-P99011) 介导的 T 细胞依赖细胞毒性 (TDCC)[1]

Cell Proliferation Assay[1]

Cell Line:NK cells, CD4+ and CD8+ T cells
Concentration:0-100 nM
Incubation Time:5 days
Result:Induced a dose-dependent proliferation of resting NK cells and resting and activated CD4+ and CD8+ T cells within peripheral blood mononuclear cells (PBMCs).
体内研究
(In Vivo)

Simlukafusp alfa (FAP-IL2v) (1 mg/kg; i.v.; weekly for 4 weeks) 在人类癌症小鼠模型中与治疗性抗体联合有效[1]

Animal Model:huCD16-transgenic SCID mice, lung orthotopic xenograft A549 model[1]
Dosage:1 mg/kg in combination with 25 mg/kg Cetuximab (HY-P9905) as single agents
Administration:IV, weekly starting at Day 14 for 4 weeks
Result:Achieved greater tumor control than either agent given as monotherapy. Reduced tumor volume and tumor growth.
Animal Model:CD-1 mice[1]
Dosage:1, 2 or 4 mg/kg
Administration:IV (Pharmacokinetic Analysis)
Result:Pharmacokinetic parameters after first dose of human FAP-IL2v (huFAP-IL2v) in CD-1 mice
CD-1 mice (n=10 per group) were given 1, 2, and 4 mg/kg huFAP-IL2v by IV administration once weekly. Multiple IV doses at 1 and 2 mg/kg were administered QW for up to a maximum of three doses, at which point toxicity was observed. Only a single dose was administered to the 4-mg/kg IV treatment group because of toxicity in these treatment groups. Blood was sampled at 0.5, 6, 24, 48, 72, and 168 h.
huFAP-IL2v dose (mg/kg)Cmax(μg/mL)AUC0-168h(μgoh/mL per mg/kg)CL (mL/d/kg)
119.055740.0
236.347946.8
478.754138.7

AUC0-168h, area under the concentration-time curve from 0 to 168 hours; Cmax, maximum serum concentration observed; CL, total clearance; FAP-IL2v, fibroblast activation protein-α -targeted interleukin 2 variant (IL2v) immunocytokine; hu, humanized; IV, intravenous.
CAS 号

1776942-10-9

储存方式

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