GB1841
GB1841 is an orally active and selective galectin inhibitor with human galectin-1 Kd of 0.027 μM, human galectin-3 Kd of 0.14 μM, mouse galectin-1 Kd of 0.034 μM and mouse galectin-3 Kd of 1.170 μM. GB1841 can be used for the research of lung cancer.
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- CAS. Nr.: 2573135-33-6
- Formel: C18H16BrClN6O4S2
- Molecular Weight:559.84
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Galectin-1 0.027 μM (Kd) |
Galectin-3 0.14 μM (Kd) |
In Vitro
GB1841 potently binds human galectin-1 (Kd 0.027 μM), human galectin-3 (Kd 0.14 μM), and human galectin-4C (Kd 0.25 μM); it also [1].
GB1841 potently binds mouse galectin-1 (Kd 0.034 μM) and mouse galectin-3 (Kd 1.170 μM)[1].
GB1841 reduces A549 human lung adenocarcinoma cell viability by 62% at 90 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 17−19 g, syngeneic implantation of LL/2 lung cancer cells)[1]
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Dosage:30 mg/kg
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Administration:p.o.; b.i.d. for 3 days
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Result:Achieved free plasma Cmax levels of 1 μM.
Remained above the mouse galectin-1 Kd (0.034 μM) for over 24 h.
Did not reach levels above the mouse galectin-3 Kd (1.170 μM).
Demonstrated a >90-fold therapeutic window compared to cell toxicity levels (62% viability reduction at 90 μM in A549 cells).
Chemical Information
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CAS. Nr. 2573135-33-6
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Molecular Weight 559.84
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Formel C18H16BrClN6O4S2
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SMILES
O[C@@H]1[C@H](N2C=C(C3=NC(Cl)=CS3)N=N2)[C@@H](OC)[C@@H](SC4=C(C#N)N=CC(Br)=C4)O[C@@H]1CO
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)