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Umbralisib Tosylate (TGR-1202) is a potent, selectively dual inhibitor targeting PI3Kδ and casein kinase-1-ε (CK1ε), demonstrating oral activity. With EC50 values of 22.2 nM and 6.0 μM for PI3Kδ and CK1ε respectively, it shows unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). This compound is utilized in the research of hematological malignancies.

| 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 | Umbralisib Tosylate (TGR-1202) is a potent, selectively dual inhibitor targeting PI3Kδ and casein kinase-1-ε (CK1ε), demonstrating oral activity. With EC50 values of 22.2 nM and 6.0 μM for PI3Kδ and CK1ε respectively, it shows unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). This compound is utilized in the research of hematological malignancies. |
| Targets&IC50 | PI3Kγ:1400 nM (Kd), PI3Kα:>10000 nM (Kd), PI3Kβ:>10000 nM (Kd), PI3Kδ:6.2 nM (Kd) |
| Synonyms | TGR-1202 tosylate ; RP5264 tosylate, TGR-1202 tosylate, RP5264 tosylate |
| Molecular Weight | 743.75 |
| Formula | C38H32F3N5O6S |
| Cas No. | 1532533-72-4 |
| Smiles | S(=O)(=O)(O)C1=CC=C(C)C=C1.NC1=C2C(=NN([C@@H](C)C3=C(C(=O)C=4C(O3)=CC=C(F)C4)C5=CC(F)=CC=C5)C2=NC=N1)C6=CC(F)=C(OC(C)C)C=C6 |
| 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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