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

Simlukafusp alfa  (Synonyms: FAP-IL2v)

Cat. No.: HY-P99902 Purity: 99.90%
COA

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.

For research use only. We do not sell to patients.

Simlukafusp alfa Chemical Structure

Simlukafusp alfa Chemical Structure

CAS No. : 1776942-10-9

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Description

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].

In Vitro

Simlukafusp alfa (FAP-IL2v) shows binding affinity constants of 43±9 pM, 80±20 pM, 660±80 pM, 0.3 nM, 0.23 nM and 0.5 nM with huIL-2Rβγ, cyIL-2Rβγ, muIL-2Rβγ, huFAP, cyFAP and muFAP, respectively[1].
Simlukafusp alfa (0-100 nM; 5 days) activates CD4+/CD8+ T cells and NK cells in vitro, but not preferentially Tregs[1].
Simlukafusp alfa (0-100 nM) enhances Cetuximab (HY-P9905)-mediated antibody-dependent cellular cytotoxicity (ADCC) and Cibisatamab (HY-P99011)-mediated T-cell-dependent cellular cytotoxicity (TDCC) in vitro[1].

MedChemExpress (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).
In Vivo

Simlukafusp alfa (FAP-IL2v) (1 mg/kg; i.v.; weekly for 4 weeks) is efficacious in combination with therapeutic antibodies in murine models of human cancer[1].

MedChemExpress (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 No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Simlukafusp alfa]

Shipping

Shipping with dry ice.

Storage

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

Purity & Documentation

Purity: 99.90%

References
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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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