Simlukafusp alfa
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 95.90%
- CAS. Nr.: 1776942-10-9
- Molecular Weight:159.66 kDa
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Speicherung:Shipping with dry ice
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Isotype
Human IgG1 kappa
Recommend Isotype Controls
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.
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Cell Line:NK cells, CD4+ and CD8+ T cells
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Concentration:0-100 nM
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Incubation Time:5 days
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:huCD16-transgenic SCID mice, lung orthotopic xenograft A549 model[1]
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Dosage:1 mg/kg in combination with 25 mg/kg Cetuximab (HY-P9905) as single agents
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Administration:IV, weekly starting at Day 14 for 4 weeks
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Result:Achieved greater tumor control than either agent given as monotherapy. Reduced tumor volume and tumor growth.
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Animal Model:CD-1 mice[1]
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Dosage:1, 2 or 4 mg/kg
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Administration:IV (Pharmacokinetic Analysis)
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG1 kappa
Anwendung
ELISA, FACS, Functional assay
Chemical Information
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CAS. Nr. 1776942-10-9
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Appearance Liquid
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Molecular Weight 159.66 kDa
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Color Colorless to light yellow
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SMILES
[Simlukafusp alfa]
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Synonyms
FAP-IL2v; RO6874281; RG7461
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Versand
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Data Sheet (262 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Inhibitory Antibodies User Guide (603 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)