Garadacimab
Based on 2 publication(s) in Google Scholar
Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research.
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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。
- 純度: ≥99.0%
- CAS 番号: 2162134-62-3
- 分子量:146.5 kDa
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 Garadacimab
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生物活性
Human IgG4 lambda
Human
F12/Factor XII
Garadacimab (CSL312) displays high affinity to activated βFXIIa with a KD of 140 pM and shows potency in an activated partial thromboplastin time (aPTT) assay with human plasma. Garadacimab shows high selectivity over a panel of relevant human serine proteases (FVIIa, FIXa, FXa, FXIa, kallikrein, tissue plasminogen activator, activated protein C, and urokinase plasminogen activator)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Garadacimab has an inhibitory effect on FXII-mediated kallikrein activity. Furthermore, Garadacimab causes a clear dose-dependent prolongation of activated partial thromboplastin time (aPTT) with no associated effect on the prothrombin time[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG4 lambda
ELISA, FACS, Functional assay
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Immobilized Factor FXIIa, Human can bind Garadacimab. The EC50 for this effect is 12.81 ng/mL.
化学情報
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CAS 番号 2162134-62-3
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性状 Liquid
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分子量 146.5 kDa
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Color Colorless to light yellow
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SMILES
[Garadacimab]
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別名
CSL312
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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.
Publications (2)
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Journal Impact Factor
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Most Recent
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Drug Resist Updat
Targeted dual degradation of HER2 and EGFR obliterates oncogenic signaling, overcomes therapy resistance, and inhibits metastatic lesions in HER2-positive breast cancer models. [Abstract]2024 May:74:101078. PMID: 38503142 -
Sci Rep
A degrader of HER2 and EGFR abolishes p95HER2 and shows robust antitumor efficacy in HER2-positive breast cancer. [Abstract]2026 Apr 20;16(1):12890. PMID: 42009845
純度とドキュメンテーション
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データシート (260 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
[1]. Dipti Pawaskar, et al. Pharmacokinetic/pharmacodynamic modeling for dose selection for the first-in-human trial of the activated Factor XII inhibitor garadacimab (CSL312). Clin Transl Sci. 2022 Mar;15(3):709-720. [Content Brief]
[2]. Helen Cao, et al. Antibody-mediated inhibition of FXIIa blocks downstream bradykinin generation. J Allergy Clin Immunol. 2018 Oct;142(4):1355-1358. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)