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TGFβRI-IN-2 is a selective, potent and orally active inhibitor of (Activin-Like Kinase 5) ALK 5(pIC50 and pEC50 values of 7.6 and 6.63, respectively).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $1,980 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,500 | 6-8 weeks | 6-8 weeks |
| Description | TGFβRI-IN-2 is a selective, potent and orally active inhibitor of (Activin-Like Kinase 5) ALK 5(pIC50 and pEC50 values of 7.6 and 6.63, respectively). |
| Targets&IC50 | ALK5: |
| In vitro | Umbralisib R-enantiomer exhibits IC50 with respect to the δ type PI3-kinase that is at least 20-fold lower than the inhibitor's IC50 with respect to the rest of the other PI3K isoforms (i.e., a, β, and γ). |
| In vivo | TGFβRI-IN-2 oral administation with 50, 150 and 500 mg/kg and 5 days induces cardiovascular toxicity characterized by valvular interstitial cell proliferation, neutrophil presence, hemorrhage and fibrin deposition in the heart valves. |
| Synonyms | TGFβRI-IN-2 |
| Molecular Weight | 411.82 |
| Formula | C20H15ClFN5O2 |
| Cas No. | 1976038-41-1 |
| Smiles | O=C1N(C=2C(N1CC(N)=O)=CN=CC2)C=3C=C(N=CC3C)C4=C(F)C=CC(Cl)=C4 |
| Relative Density. | 1.450 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. |
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.
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.
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