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.
For research use only. We do not sell to patients.
- Purity: 95.90%
- CAS No.: 1776942-10-9
- Molecular Weight:159.66 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Human IgG1 kappa
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).
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG1 kappa
ELISA, FACS, Functional assay
Chemical Information
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CAS No. 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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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (262 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Simlukafusp alfa Related Classifications
HY-P99902 Related Classifications
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