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CH5132799 (also known as PA-799) is a novel class I PI3K inhibitor, exhibiting potent inhibition of PI3Kα with an IC(50) of 0.014 μM. This compound demonstrates significant antiproliferative effects on human tumor cell lines with an activated PI3K pathway. Administrable orally, CH5132799 shows notable antitumor activity in human cancer xenograft mouse models where the PI3K pathway is activated. It specifically inhibits class I PI3K and PI3Kα mutants, as confirmed by in vitro kinase assays. Tumors harboring the PIK3CA mutation are highly sensitive to CH5132799 in vitro and are significantly regressed in in vivo mouse xenograft models.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | CH5132799 (also known as PA-799) is a novel class I PI3K inhibitor, exhibiting potent inhibition of PI3Kα with an IC(50) of 0.014 μM. This compound demonstrates significant antiproliferative effects on human tumor cell lines with an activated PI3K pathway. Administrable orally, CH5132799 shows notable antitumor activity in human cancer xenograft mouse models where the PI3K pathway is activated. It specifically inhibits class I PI3K and PI3Kα mutants, as confirmed by in vitro kinase assays. Tumors harboring the PIK3CA mutation are highly sensitive to CH5132799 in vitro and are significantly regressed in in vivo mouse xenograft models. |
| Synonyms | PA-799 mesylate, IZORLISIB MESYLATE, IZORLISIB MESILATE, CH5132799 Mesylate, CH-5132799 Mesilate, CH 5132799 Mesylate PA 799 mesylate |
| Molecular Weight | 473.53 |
| Formula | C16H23N7O6S2 |
| Cas No. | 2242053-82-1 |
| Smiles | O=S(=O)(O)C.O=S(=O)(N1C2=NC(=NC(C3=CN=C(N=C3)N)=C2CC1)N4CCOCC4)C |
| 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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