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 No.: 2573135-33-6
- Formule: C18H16BrClN6O4S2
- Masse moléculaire:559.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Galectin-1 0.027 μM (Kd) |
Galectin-3 0.14 μM (Kd) |
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.
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 No. 2573135-33-6
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Masse moléculaire 559.84
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)