KHK2840
KHK2840 is a potent CD40 agonist with a Kd value of 0.485 nM for hCD40. KHK2840 delivers agonistic signals in tumor-bearing hCD40 transgenic mice and human peripheral blood B cells. KHK2840 upregulates CD80, CD86, CD95 and IL-12p70 expression. KHK2840 enhances antitumor efficacy of anti-PD-1 antibody and Paclitaxel (HY-B0015). KHK2840 can be used for the research of cancer, such as colon cancer and melanoma.
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.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Human IgG2 kappa
Human
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IL-12 |
KHK2840 (0.0625-1.00 μg/mL) binds specifically to human and cynomolgus monkey CD40 proteins (Kd = 0.485 nM for human; 1.46 nM for cynomolgus monkey) and does not bind to rat or mouse CD40 proteins[1].
KHK2840 (2 days) activates human monocyte-derived dendritic cells to upregulate CD80, CD86, and IL-12p70 (EC50 = 0.188 μg/mL for CD80, 0.072 μg/mL for CD86, 0.436 μg/mL for IL-12p70)[1].
KHK2840 (0.01-10 μg/mL; 0.5-48 h) increases CD86 and CD95 expression in a concentration- and time-dependent manner[1].
KHK2840 (overnight) induces CD69, CD86, and CD95 expression in human peripheral blood B cells (EC50 = 0.018 μg/mL for CD69, 0.015 μg/mL for CD86, 0.016 μg/mL for CD95)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Vss |
|---|---|---|---|---|
| Cynomolgus Monkey[1] | 0.1 mg/kg | i.v. | 2.13 (Male) μg/mL | 68.8 (Male) mL/kg |
| Cynomolgus Monkey[1] | 0.3 mg/kg | i.v. | 6.64 (Male) μg/mL | 60.9 (Male) mL/kg |
| Cynomolgus Monkey[1] | 1 mg/kg | i.v. | 25.6 (Male) μg/mL | 45.3 (Male) mL/kg |
| Cynomolgus Monkey[1] | 3 mg/kg | i.v. | 73.1 (Male) μg/mL | 40.8 (Male) mL/kg |
KHK2840 (0.1-3 mg/kg; i.v.; once every 2 weeks; 3 doses) induces dose-dependent CD40 agonistic signaling in male and female (with a NOAEL of 0.3 mg/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:hCD40 BAC transgenic mice with colon cancer, melanoma, or pancreatic ductal adenocarcinoma models (female, C57Bl/6J background)[1]
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Dosage:0.038, 0.075, 0.15, 0.3, 0.6, 1.2 mg/kg
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Administration:I.v.; single dose
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Result:Significantly suppressed MC-38 tumor growth (P=0.0128) with 1.2 mg/kg monotherapy.
Achieved significant tumor growth suppression.
Induced tumor remission in 8/10 mice in pancreatic cancer model when combined with anti-PD-1.
Observed dose-dependent increases in CD80-, CD86-, CD95- positive B cells and cytokines (IL-12p70, IFN-γ, IL-6, IL-10, TNF-α, IL-1β, CXCL1) in peripheral blood.
Increased cell type scores of Th1 cells (lymph nodes), DCs (tumors/lymph nodes), and CD8 T cells (tumors).
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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Synonyms
IgG2-AAS
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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)
KHK2840 Related Classifications
Cat. No.: HY-P991918
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- KHK2840
- IgG2-AAS
- KHK 2840
- KHK-2840
- Transmembrane Glycoprotein
- Interleukin Related
- cynomolgus monkeys
- pancreatic ductal adenocarcinoma
- hCD40 transgenic mice
- cytotoxic T lymphocytes
- human CD40
- cynomolgus monkey CD40
- colon cancer
- melanoma
- antiprogrammed cell death 1 antibody
- human peripheral blood B cells
- Inhibitor
- inhibitor
- inhibit