DF6002
DF6002 (BMS-986415) is a monovalent IL-12 immunoglobulin Fc fusion protein. DF6002 can promote sustained IFN-γ responses while reducing toxicity. DF6002 binds specifically to IL-12R on CD4+ T cells, CD8+ T cells, NK cells, and B cells. DF6002 can be used for the research of solid tumors .
For research use only. We do not sell to patients.
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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IL-2 |
DF6002 (200 nM) specifically binds to IL-12 receptor-expressing CD4+ T cells, CD8+ T cells, NK cells, and weakly to B cells in activated human PBMCs[1].
DF6002 (0.00596-6250 pM; 72 h) induces IFN-γ production in activated human PBMCs with an EC50 of 2.99 pM[1].
DF6002 (200 nM) specifically binds to IL-12 receptor-expressing CD4+ T cells, CD8+ T cells, NK cells, and weakly to B cells in activated cynomolgus monkey PBMCs[1].
DF6002 (0.00596-6250 pM; 72 h) induces IFN-γ production in activated cynomolgus monkey PBMCs with an EC50 of 6.91 pM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Cynomolgus Monkey[1] | 1 mg/kg | i.v. | 17.4-30.5 h |
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 µg/kg (IFNγ response); 19 µg/kg (tolerance, IFNγ response)
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Administration:i.v.; bolus on Days 1 and 8 (1 µg/kg); single dose (19 µg/kg)
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Result:Demonstrated in vivo half-life ranging from 17.4-30.5 h.
Induced peak IFNγ levels at 48 h post-dose (141-226 pg/mL) at 1 µg/kg.
Was well tolerated without cytokine release syndrome, fever, or adverse toxicity at 19 µg/kg.
Caused minor, dose-dependent minimal increases in aspartate aminotransferase and alanine aminotransferase activities in the liver.
Caused minor, dose-dependent mild decreases in white blood cells and altered cellularity in secondary lymphoid tissue.
| 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 version of IL-12-Fc
ELISA, FACS, Functional assay
Chemical Information
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SMILES
[DF6002]
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Synonyms
BMS-986415
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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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)