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Zilurgisertib fumarate
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Catalog No. T84860Cas No. 2173390-30-0
Alias INCB-000928 fumarate, ,NBU-928 fumarate
Zilurgisertib fumarate (INB-000928 fumarate) is a potent and selective inhibitor of Activin Receptor-Like Kinase 2 (ALK2/ACVR1). It significantly inhibits ALK2 kinase activity (IC50 = 15 nM) and downregulates BMP-6-induced SMAD1/5 phosphorylation (IC50 = 63 nM). By blocking ALK2-mediated signaling, Zilurgisertib suppresses the production of hepcidin in hepatocytes (IC50 = 20 nM), thereby modulating iron metabolism. In preclinical studies, Zilurgisertib demonstrates the potential to improve anemia in cancer-induced models by effectively increasing hemoglobin levels.
Zilurgisertib fumarate
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Purity: 99.96%
Catalog No. T84860Alias INCB-000928 fumarate, ,NBU-928 fumarateCas No. 2173390-30-0
Zilurgisertib fumarate (INB-000928 fumarate) is a potent and selective inhibitor of Activin Receptor-Like Kinase 2 (ALK2/ACVR1). It significantly inhibits ALK2 kinase activity (IC50 = 15 nM) and downregulates BMP-6-induced SMAD1/5 phosphorylation (IC50 = 63 nM). By blocking ALK2-mediated signaling, Zilurgisertib suppresses the production of hepcidin in hepatocytes (IC50 = 20 nM), thereby modulating iron metabolism. In preclinical studies, Zilurgisertib demonstrates the potential to improve anemia in cancer-induced models by effectively increasing hemoglobin levels.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $189 | - | In Stock | |
| 5 mg | $472 | - | In Stock | |
| 10 mg | $783 | - | In Stock | |
| 25 mg | $1,390 | - | In Stock | |
| 50 mg | $1,880 | - | In Stock | |
| 100 mg | $2,570 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
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Purity:99.96%
Appearance:Solid
Color:Yellow
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Product Introduction
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Chemical Properties
Storage & Solubility Information
| Description | Zilurgisertib fumarate (INB-000928 fumarate) is a potent and selective inhibitor of Activin Receptor-Like Kinase 2 (ALK2/ACVR1). It significantly inhibits ALK2 kinase activity (IC50 = 15 nM) and downregulates BMP-6-induced SMAD1/5 phosphorylation (IC50 = 63 nM). By blocking ALK2-mediated signaling, Zilurgisertib suppresses the production of hepcidin in hepatocytes (IC50 = 20 nM), thereby modulating iron metabolism. In preclinical studies, Zilurgisertib demonstrates the potential to improve anemia in cancer-induced models by effectively increasing hemoglobin levels. |
| Targets&IC50 | ALK2:15 nM, Smad1/5:63 nM, Hepcidin production:20 nM |
| In vitro | Zilurgisertib fumarate inhibits ALK2 kinase activity (IC50 = 15 nM) and suppresses BMP-6-induced SMAD1/5 phosphorylation (IC50 = 63 nM). In Huh-7 cells, it potently reduces BMP-6-stimulated hepcidin production with an IC50 of 20 nM [2]. |
| In vivo | Systemic administration of Zilurgisertib fumarate improves anemia in mouse models of cancer-induced anemia. It effectively increases hemoglobin (Hb) levels and red blood cell (RBC) counts, demonstrating its potential to restore iron homeostasis in chronic disease environments [2]. |
| Synonyms | INCB-000928 fumarate, ,NBU-928 fumarate |
| Molecular Weight | 502.66 (free base) |
| Formula | C30H38N4O3.xC4H4O4 |
| Cas No. | 2173390-30-0 |
| Smiles | C(=C/C(O)=O)\C(O)=O.C(NC12CCC(O)(CC1)CC2)(=O)C3=CC(C4=CC=C([C@]56[C@](C5)(CN(C6)C7CCOCC7)[H])C=C4)=CN=C3N |
| Relative Density. | no data available |
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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