1. Immunology/Inflammation
  2. Interleukin Related
  3. Simlukafusp alfa

Simlukafusp alfa  (Synonyms: FAP-IL2v)

目录号: HY-P99902 纯度: 99.90%
COA

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-2RβγIL-2 变体。Simlukafusp alfa 是一种人 IgG1 抗体。

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Simlukafusp alfa Chemical Structure

Simlukafusp alfa Chemical Structure

CAS No. : 1776942-10-9

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1 mg ¥17000
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Simlukafusp alfa (FAP-IL2v) is an immunocytokine comprising an antibody against fibroblast activation protein α (FAPα) and an IL-2 variant that only binds IL-2Rβγ. Isotype: human IgG1[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]

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

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处理性抗体联合有效[1]

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

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 (μg•h/mL per mg/kg) CL (mL/d/kg)
1 19.0 557 40.0
2 36.3 479 46.8
4 78.7 541 38.7

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.
Clinical Trial
CAS 号
性状

液体

颜色

Colorless to light yellow

运输条件

Shipping with dry ice.

储存方式

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

纯度 & 产品资料

纯度: 99.90%

参考文献

Simlukafusp alfa 相关分类

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  • 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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