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Cinrebafusp alfa (PRS 343) is an anticalin-based bispecific drug with high affinity for both CD137/HER2, displaying dissociation constants (Kd) of 0.3 nM to recombinant human HER2 and 5 nM to human monomeric CD137 (4-1BB). It promotes T-cell costimulation via tumor-localized, HER2-mediated 4-1BB clustering and activation, thereby enhancing T-cell receptor-driven responses and facilitating tumor cell eradication. This compound shows promising potential in research concerning HER2-positive solid tumors [1] [2].
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Description | Cinrebafusp alfa (PRS 343) is an anticalin-based bispecific drug with high affinity for both CD137/HER2, displaying dissociation constants (Kd) of 0.3 nM to recombinant human HER2 and 5 nM to human monomeric CD137 (4-1BB). It promotes T-cell costimulation via tumor-localized, HER2-mediated 4-1BB clustering and activation, thereby enhancing T-cell receptor-driven responses and facilitating tumor cell eradication. This compound shows promising potential in research concerning HER2-positive solid tumors [1] [2]. |
Targets&IC50 | HER2:0.3 nM (Kd), 4-1BB:5 nM (Kd) |
In vitro | Cinrebafusp alfa (PRS 343) binds to HER2-expressing MCF-7 cells and CHO cells transfected with human 4-1BB, exhibiting EC50 values of 7.4 nmol/L and 6.2 nmol/L, respectively, as determined by FACS analysis [1]. |
In vivo | Cinrebafusp alfa (PRS 343; 0.2-10 mg/kg; 静脉给药; 每周一次; 持续20天) demonstrated tumor growth inhibition and dose-dependent increases in tumor-infiltrating lymphocytes in a humanized mouse model bearing HER2-positive SK-OV-3 tumor cells [1]. In male CD-1 mice, Cinrebafusp alfa (10 mg/kg; 静脉给药; 单剂量) exhibited a terminal elimination half-life of >14 days. Furthermore, a single intravenous dose of Cinrebafusp alfa (3 mg/kg) in male cynomolgus monkeys resulted in an approximate terminal elimination half-life of 4 days [1]. |
Synonyms | PRS 343 |
Molecular Weight | N/A |
CAS No. | 2218515-90-1 |
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Cinrebafusp alfa 2218515-90-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR PRS 343 inhibitor inhibit