SAR444200
SAR444200 is a nanobody targeting GPC3 (glypican-3) and TCRαβ (T-cell receptor αβ). The KD of SAR444200 for human GPC3 is 0.023 nM, and its KD for human TCRαβ is 5.2 nM. SAR444200 mediates T cell-dependent cytotoxicity, and exhibits high selectivity and killing activity against GPC3-positive tumor cells. SAR444200 binds to GPC3 in a dual-epitope manner, and binds to TCRαβ via its N-terminal nanobody, forming an artificial immunological synapse between T cells and tumor cells. SAR444200 can be used in studies of GPC3+ solid tumors, including liver cancer, lung squamous cell carcinoma and melanoma.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
Human
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IL-6 |
IL-2 |
SAR444200 binds to human and cynomolgus monkey TCRαβ with single-digit nanomolar affinity, human and cynomolgus monkey GPC3 with sub-nanomolar affinity, and human and cynomolgus monkey albumin with single-digit nanomolar affinity, with lower affinity to mouse orthologues and no cross-reactivity to mouse TCR[1].
SAR444200 (24 h) binds to membrane-bound human GPC3 with sub-nanomolar affinity and membrane-bound cynomolgus monkey GPC3 with low sub-nanomolar affinity[1].
SAR444200 (60 h) potently induces T-cell-dependent cellular cytotoxicity of GPC3+ human HepG2, NCI-H661, and HuH-7 cells with sub-nanomolar EC50 values, shows cross-reactive cytotoxicity against cynomolgus monkey GPC3-expressing HEK293 cells, and exhibits no activity against GPC3-low NCI-H23 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOG (NOD.Cg-PrkdcscidIL2tm1Sug/Jital) (10-week-old female, humanized with HepG2 cells and human T cells)[1]
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Dosage:2.0 mg/kg; 0.7 mg/kg; 0.2 mg/kg
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Administration:i.v.; every third day; 5 doses
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Result:SAR444200 showed significant antitumor activity with 100% tumor inhibition at day 33, and induced 1 complete regression and 5 partial regressions at 2.0 mg/kg.
SAR444200 showed significant antitumor activity with 100% tumor inhibition at day 33, and induced 1 complete regression and 3 partial regressions at 0.7 mg/kg.
SAR444200 showed non‑significant antitumor activity with 29% tumor inhibition at day 33 at 0.2 mg/kg.
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Animal Model:NOG (NOD.Cg-PrkdcscidIL2tm1Sug/Jital) (10-week-old female, humanized with HuH-7 cells and human T cells)[1]
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Dosage:2.0 mg/kg; 0.7 mg/kg; 0.2 mg/kg
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Administration:i.v.; every third day; 5 doses
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Result:SAR444200 achieved significant antitumor activity with 100% tumor inhibition at day 35 and induced 3 complete regressions and 1 partial regression at 0.7 mg/kg.
SAR444200 displayed significant antitumor activity with 67% tumor inhibition at day 35 and induced 1 complete regression and 3 partial regressions at 2.0 mg/kg.
SAR444200 showed non-significant antitumor activity with 54% tumor inhibition at day 35 at 0.2 mg/kg.
TCRαβ & GPC3
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
化学情報
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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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)