Fidasimtamab
Based on 1 Customer Validation
Fidasimtamab (IBI315) is a bispecific antibody targeting human epidermal growth factor receptor 2 (Her2) and programmed death protein 1 (PD-1), with a Ka of 3.55e-10 M for human Her2 and a Ka of 1.17e-9 M for human PD-1. Fidasimtamab cross-links Her2-positive tumor cells with PD-1-positive T cells to form immune synapses, blocks PD-1-ligand interactions, preserves antibody-dependent cellular cytotoxicity, induces gasdermin B (GSDMB)-mediated pyroptosis, and activates T cells. Fidasimtamab is applicable to relevant research on Her2-positive gastric cancer.
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- 純度 : ≥95.0%
- CAS 番号: 2377419-89-9
- 分子量:144.62 kDa
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保管条件:Shipping with dry ice
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
Isotype
Human IgG1 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
ERBB2 & PDCD1
体外実験
Fidasimtamab binds to purified human PD-1 and Her2 proteins with high affinity, with KD values of 1.17 × 10-9 M and 3.55 × 10-10 M, respectively[1].
Fidasimtamab (600 nM; 30 min at 4 °C) induces a 24.10% association rate between N87 gastric cancer cells and activated human T cells[1].
Fidasimtamab (serial dilutions; 3 d) dose-dependently activates human CD4+ T cells in an MLR assay, inducing secretion of IFNγ and IL-2 with potency comparable to the parental anti-PD-1 antibody[1].
Fidasimtamab (600 nM; 24 h) significantly enhances T cell-mediated cytotoxicity against N87 and SNU-216 Her2-positive gastric cancer cells, as measured by increased LDH release[1].
Fidasimtamab (600 nM; 6 h) induces pyroptosis in N87 and SNU-216 Her2-positive gastric cancer cells in the presence of activated T cells, and increases IL-18 secretion by 24 h, via cleavage of GSDMB to its active N-terminal fragment[1].
Fidasimtamab (serial dilutions; 4 h at 37 °C) exhibits potent ADCC activity against N87 Her2-positive gastric cancer cells when incubated with human NK cells[1].
Fidasimtamab (600 nM; 24 h) induces a 2-3 fold increase in cell death in PDXO-1 Her2-positive gastric cancer organoids in the presence of T cells, and promotes association between T cells and organoids[1].
Conditioned media from Her2-positive gastric cancer cell-T cell cocultures treated with Fidasimtamab (600 nM; 24 h) activates human CD8+ T cells, increasing CD25 expression and enhancing IFNγ secretion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:N87 (Her2-positive gastric cancer) cells, SNU-216 (Her2-positive gastric cancer) cells, activated human T cells
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Concentration:600 nM
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Incubation Time:24 h
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Result:Significantly increased LDH release from N87 and SNU-216 cells compared to control groups, indicating enhanced T cell-mediated tumor cell killing.
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Cell Line:N87 (Her2-positive gastric cancer) cells, human NK cells
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Concentration:Serial dilutions
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Incubation Time:4 h at 37 °C
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Result:Demonstrated potent ADCC activity against N87 cells, with stronger tumor-killing activity than its parental trastuzumab.
体内実験
Fidasimtamab (IBI315/BH2950) (5 mg/kg; i.p.; every 3 days; 2 weeks) achieves a 77% tumor volume reduction in human PBMC-reconstituted NOG mice bearing PDX-1 Her2-positive gastric cancer, with enhanced intratumoral T cell infiltration, activation, and proliferation[1].
Fidasimtamab (IBI315/BH2950) (5 mg/kg; i.p.; every 3 days; 2 weeks) loses its significant tumor inhibitory activity in human PBMC-reconstituted NOG mice bearing GSDMB-knockdown N87 Her2-positive gastric cancer, confirming dependency on GSDMB-mediated pyroptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOG (NOD/ShiLtj-scid IL2rg
) (female, 4 weeks old, subcutaneously implanted with N87 human Her2-positive gastric cancer cells, reconstituted with human PBMCs)[1] -
Dosage:5 mg/kg
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Administration:i.p.; every 3 days; 2 weeks
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Result:Achieved a tumor volume of 54.1 mm3 (day 31), corresponding to a 116.8% tumor inhibition rate relative to control.
Induced the highest infiltration of CD3+, CD8+, and CD4+ lymphocytes in N87 tumors compared to control, parental antibodies, and parental antibody combination groups.
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Animal Model:NOG (NOD/ShiLtj-scid IL2rg
) (female, 4 weeks old, subcutaneously implanted with PDX-1 human Her2-positive gastric cancer tissue, reconstituted with human PBMCs)[1] -
Dosage:5 mg/kg
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Administration:i.p.; every 3 days; 2 weeks
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Result:Achieved a tumor volume of 182.2 mm3 (day 39), corresponding to a 77% reduction relative to control.
Induced the highest infiltration of CD3+, CD8+, and CD4+ lymphocytes in PDX-1 tumors compared to control, parental antibodies, and parental antibody combination groups.
Increased the proportion of granzyme A-positive CD8+ T cells in PDX-1 tumors relative to control.
Boosted the frequency of Ki67+ proliferating CD8+ and CD4+ T cells, CD107a+ activated CD8+ and CD4+ T cells, CD25+ activated CD8+ and CD4+ T cells, and Tbet+IFNγ+ CD3+ T cells in PDX-1 tumors relative to control.
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Animal Model:NOG (NOD/ShiLtj-scid IL2rg
) (female, 4 weeks old, subcutaneously implanted with GSDMB-knockdown N87 human Her2-positive gastric cancer cells, reconstituted with human PBMCs)[1] -
Dosage:5 mg/kg
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Administration:i.p.; every 3 days; 2 weeks
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Result:Showed almost completely blocked tumor inhibitory effect in GSDMB-knockdown N87 tumors, with no significant reduction in tumor volume relative to control.
Reduced infiltration of CD3+ and CD8+ T cells in GSDMB-knockdown N87 tumors compared to its effect in wild-type N87 tumors.
遺伝子ID
アクセッション番号
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG1 kappa
アプリケーション
ELISA, FACS, Functional assay
化学情報
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CAS 番号 2377419-89-9
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性状 Liquid
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分子量 144.62 kDa
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Color Colorless to light yellow
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SMILES
[Fidasimtamab]
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別名
IBI315; BH2950
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輸送条件
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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データシート (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Keywords
- Fidasimtamab
- 2377419-89-9
- IBI315
- BH2950
- IBI 315
- IBI-315
- BH2950
- BH 2950
- BH-2950
- EGFR
- PD-1/PD-L1
- Her2-positive tumor cells
- programmed cell death protein 1
- interferon-gamma
- pyroptosis
- gasdermin B
- Her2-positive breast cancer cells
- PD-1-positive T cells
- human epidermal growth factor receptor 2
- NOG mice
- Her2-positive gastric cancer cells
- Inhibitor
- inhibitor
- inhibit