Amtabafusp alfa
Amtabafusp alfa (GS-8588) is an envelope-targeting bispecific T-cell engager for HIV treatment. Amtabafusp alfa redirects effector T cells by binding to CD3 via a humanized anti-CD3 Fab domain and to HIV envelope proteins via an engineered CD4 domain 1 variant. Amtabafusp alfa exhibits potent, broad-spectrum activity against a variety of HIV isolates and specifically kills HIV-infected cells. Amtabafusp alfa can be used for research on HIV infection.
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- Purity: 99%
- CAS No.: 2839531-84-7
- 분자량:109.429 kDa
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
Fusion-half-IGG1-lambda2/CD4-h-CH2-CH3
Human
CD3 & gp120/Glycoprotein 120
Amtabafusp alfa (dilution series) binds to HIV-infected CEM cells, with EC50 values ranging from 6 to 67 nM against 24 subtype B isolates[1].
Amtabafusp alfa (dilution series) binds to CD4 and CD8 T cells of healthy cynomolgus monkeys and rhesus monkeys with similar potency, with geometric mean EC50 values of 9.9 nM and 12.0 nM, respectively[1].
Amtabafusp alfa (dilution series) potently kills HIV-infected resting primary CD4 T cells (with a median EC50 of 0.1 μg/mL for 29 out of 32 isolates) and kills the remaining 3 isolates in activated PBMC-based and CEM-based assays[1].
Amtabafusp alfa (dilution series) shows no detectable binding or cytotoxic effect on MHCII-expressing B cells, but mediates the killing of HIV-infected CD4 cells in the same experiment[1].
Amtabafusp alfa (10-8-104 μg/mL) induces low-level CD69 upregulation and cytokine production in peripheral blood mononuclear cells (PBMCs) derived from people with HIV (PWH) during both ART-suppressed viral suppression phase and viremic phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkeys[1]
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Dosage:1 mg/kg (single dose); 10 mg/kg (single dose); 10 mg/kg/week (repeat-dose); 30 mg/kg/week (repeat-dose); 100 mg/kg/week (repeat-dose)
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Administration:i.v. (single dose); i.v. (30-minute infusion, weekly for 5 doses on days 1, 8, 15, 22, 29)
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Result:Exhibited a biphasic serum pharmacokinetic profile with a clearance of 14.4 mL/day/kg and a half-life of 5.8 days following a single 1 mg/kg i.v. dose.
Detected antidrug antibodies in 2 of 3 monkeys at ≥24 days with minimal impact on pharmacokinetics following a single 1 mg/kg i.v. dose.
Had a lymph node to serum exposure ratio of ~25% (AUC0-ᵢ-based ratio of 24.4%) following a single 10 mg/kg i.v. dose.
Was well tolerated at doses up to 100 mg/kg/week in a 5-week repeat-dose study, with no mortality, adverse clinical signs, or pathological findings.
Showed dose-proportional serum pharmacokinetics in a 5-week repeat-dose study.
Demonstrated estimated safety margins relative to the projected minimally efficacious dose of >100-fold in a 5-week repeat-dose study.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Fusion-half-IGG1-lambda2/CD4-h-CH2-CH3
ELISA, FACS, Functional assay
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Loaded GS-8588 on ACH2 biosensor, can bind HY-P76390 envelope glycoprotein gp120 Protein, HIV-1 (AAC31819, HEK293, His) with an affinity constant of 5.260E-09 M as determined in BLI assay.
Chemical Information
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CAS No. 2839531-84-7
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Appearance Liquid
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분자량 109.429 kDa
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Color Colorless to light yellow
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SMILES
[GS-8588]
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Synonyms
GS-8588
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선적
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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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)
Amtabafusp alfa Related Classifications
HY-P991479 Related Classifications
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