1. Immunology/Inflammation
  2. Transmembrane Glycoprotein Interleukin Related
  3. 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.

KHK2840

KHK2840 Chemical Structure

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Description

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[1].

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.

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 (0.038-1.2 mg/kg; i.v.; single dose) exhibits dose-dependent CD40 agonistic activity and antitumor efficacy in female hCD40 BAC transgenic mice with colon cancer, melanoma, or pancreatic ductal adenocarcinoma models[1].
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.

Animal Model: hCD40 BAC transgenic mice with colon cancer, melanoma, or pancreatic ductal adenocarcinoma models (female, C57Bl/6J background)[1]
Dosage: 0.038, 0.075, 0.15, 0.3, 0.6, 1.2 mg/kg
Administration: I.v.; single dose
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

958  [NCBI]

Accession
Application

ELISA, FACS, Functional assay

Conjugated

Unconjugated

Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.

Formulation

Please refer to the lot-specific COA for specific buffer information.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
KHK2840
Cat. No.:
HY-P991918
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