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SB-505124 hydrochloride

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Catalog No. T21637Cas No. 356559-13-2
Alias SB505124 hydrochloride, SB 505124 hydrochloride

SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer.

SB-505124 hydrochloride

SB-505124 hydrochloride

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Purity: 98.71%
Catalog No. T21637Alias SB505124 hydrochloride, SB 505124 hydrochlorideCas No. 356559-13-2
SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$35In StockIn Stock
5 mg$73In StockIn Stock
10 mg$105In StockIn Stock
25 mg$196In StockIn Stock
50 mg$328In StockIn Stock
100 mg$489-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.71%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer.
In vitro
METHODS: Rabbit subconjunctival fibroblasts were incubated with 10 μM SB-505124 or 0.04% MMC and then incubated with or without TGF-β2 (2 ng/ml) in 12-well plates for 48 h. The effects of ALK-5 inhibitor SB-505124 on TGF-β2-induced downstream effects were analyzed by Western blotting.
RESULTS: The levels of pSmad2, CTGF, and α-SMA in rabbit subconjunctival fibroblasts treated with SB-505124 were decreased in a concentration-dependent manner. [3]
In vivo
SB-505124 (5 mg/kg; i.p.) alone does not elicit any response in C57Bl6 mice bearing A549 xenografts. However, when combined with a single dose of Carboplatin (60 mg/kg), SB-505124 induces sustained therapeutic effects in five subjects, eliminating the need for ongoing maintenance therapy. This synergy presents a potent treatment strategy without continuous intervention in the specified animal model, highlighting its potential efficacy.
SynonymsSB505124 hydrochloride, SB 505124 hydrochloride
Chemical Properties
Molecular Weight371.86
FormulaC20H22ClN3O2
Cas No.356559-13-2
SmilesCl.N=1C(=CC=CC1C)C=2N=C(NC2C=3C=CC=4OCOC4C3)C(C)(C)C
Relative Density.no data available
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Methanol: 120 mg/mL (322.7 mM), Sonication is recommended.
DMSO: 40 mg/mL (107.57 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.38 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO/Methanol
1mg5mg10mg50mg
1 mM2.6892 mL13.4459 mL26.8918 mL134.4592 mL
5 mM0.5378 mL2.6892 mL5.3784 mL26.8918 mL
10 mM0.2689 mL1.3446 mL2.6892 mL13.4459 mL
20 mM0.1345 mL0.6723 mL1.3446 mL6.7230 mL
50 mM0.0538 mL0.2689 mL0.5378 mL2.6892 mL
100 mM0.0269 mL0.1345 mL0.2689 mL1.3446 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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