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BMS986260
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Catalog No. T8730Cas No. 2001559-19-7
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
BMS986260
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Purity: 97.67%
Catalog No. T8730Cas No. 2001559-19-7
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $80 | In Stock | In Stock | |
| 5 mg | $163 | In Stock | In Stock | |
| 10 mg | $243 | In Stock | In Stock | |
| 25 mg | $397 | In Stock | In Stock | |
| 50 mg | $598 | In Stock | In Stock | |
| 100 mg | $848 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $137 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:97.67%
Appearance:Solid
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM). |
| In vitro | BMS-986260 demonstrated functional activity in multiple TGFβ-dependent cellular assays, excellent kinome selectivity, favorable pharmacokinetic properties, and curative in vivo efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models. Since daily dosing of TGFβR1 inhibitors is known to cause class-based cardiovascular (CV) toxicities in preclinical species, a dosing holiday schedule in the anti-PD-1 combination efficacy studies was explored. An intermittent dosing regimen of 3 days on and 4 days off allowed mitigation of CV toxicities in one month dog and rat toxicology studies and also provided similar efficacy as once daily dosing. |
| Molecular Weight | 382.78 |
| Formula | C18H12ClFN6O |
| Cas No. | 2001559-19-7 |
| Smiles | C(CO)N1C(=C(N=C1)C2=CC(Cl)=C(F)C=C2)C3=NN4C(C=C3)=NC=C4C#N |
| Relative Density. | 1.52 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 25 mg/mL (65.31 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (5.22 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
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Calculator
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
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
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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