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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Isotype
Human IgG2 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
[1]|
IL-12 |
In Vitro
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. Further protocols information, click here.
Parmacokinetics
| 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 |
In Vivo
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).
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Product Image
Anwendung
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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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- 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