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Cinrebafusp alfa  (Synonyms: PRS 343)

Cat. No.: HY-P99605 Purity: 98.53%
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Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research.

For research use only. We do not sell to patients.

CAS No. : 2218515-90-1

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Based on 1 publication(s) in Google Scholar

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Description

Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research[1][2].

Isotype

Human IgG4 kappa

Recommend Isotype Controls
Species

Fusion Protein

IC50 & Target[1]

4-1BB

5 nM (Kd)

HER2

0.3 nM (Kd)

In Vitro

Cinrebafusp alfa (PRS 343) binds HER2-expressing MCF-7 cells with an EC50 of 7.4 nmol/L and binds to CHO cells transfected with human 4-1BB with an EC50 of 6.2 nmol/L in a FACS assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cinrebafusp alfa (PRS 343; 0.2-10 mg/kg; IV; once weekly; for 20 day) leads to tumor growth inhibition and has a dose-dependent increase of tumor-infiltrating lymphocytes in a humanized mouse model engrafted with HER2-positive SK-OV-3 tumor cells[1].
Cinrebafusp alfa (10 mg/kg; IV; single dose) has the terminal elimination half-life of >14 days in male CD-1 mice. Cinrebafusp alfa (3 mg/kg; IV; single dose) has the terminal elimination half-life approximately 4 days in male cynomolgus monkeys[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SK-OV-3 ovarian cancer model in human PBMC-reconstituted NOG female mice, ages 5-7 weeks[1]
Dosage: 0.2, 1, 5, 10 mg/kg
Administration: IV; once weekly; for 20 day
Result: Displayed dose-dependent antitumor efficacy with doses ranging from 4 μg to 100 μg (approximately 0.2 mg/kg to 5 mg/kg), while the 200-μg dose (approximately 10 mg/kg) did not further enhance tumor regression.
Led to a significant increase in human CD45+ lymphocytes in tumor tissue.
Animal Model: Male CD-1 mice[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: IV; single dose
Result: Had the terminal elimination half-life of >14 days.
Clinical Trial
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Cinrebafusp alfa]

Shipping

Shipping with dry ice.

Storage

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

Format
  • Human IgG4 kappa
Biological Activity
  • Immobilized Cinrebafusp alfa can bind Human 4-1BB/CD137 Protein (ECD, His Tag). The EC50 for this effect is 1.33 ng/mL.
  • Immobilized Cinrebafusp alfa can bind Human Her2/ERBB2 Protein (ECD, His Tag). The EC50 for this effect is 1.66 ng/mL.
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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Cinrebafusp alfa
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HY-P99605
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