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PF-06843195 is a potent and selective PI3Kα inhibitor that binds to the active site of PI3Kα and prevents it from catalyzing the conversion of PIP2 to PIP3, thereby inhibiting the activation of AKT, with anti-tumor activity in vitro and in vivo.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $99 | - | In Stock |
| Description | PF-06843195 is a potent and selective PI3Kα inhibitor that binds to the active site of PI3Kα and prevents it from catalyzing the conversion of PIP2 to PIP3, thereby inhibiting the activation of AKT, with anti-tumor activity in vitro and in vivo. |
| Targets&IC50 | PI3Kδ:160 nM (IC50, in Rat1 fibroblasts), PI3Kδ:0.28 nM (Ki), PI3Kα:0.018 nM (Ki) |
| In vitro | PF-06843195 is able to inhibit the proliferation of T47D and MCF7 cells with IC50 values of 32 nM and 62 nM, respectively. [1] |
| In vivo | Methods: PF-06843195 (10 mg/kg, oral) and (2 mg/kg, intravenous) were used to treat rats and study its pharmacokinetics. Results: It showed excellent bioavailability (25%) after oral administration and high plasma clearance (30 mL/min/kg) and large distribution volume (3.0 L/kg) after intravenous injection. [1] |
| Synonyms | PF06843195 |
| Molecular Weight | 498.46 |
| Formula | C20H25F3N8O4 |
| Cas No. | 2067281-51-8 |
| Smiles | N([C@]1(CO)CN(C(OCC(F)F)=O)CC1)C=2C(F)=C(N=C(N2)N3CCOCC3)C=4C=NC(N)=NC4 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (100.31 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.01 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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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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