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PF-06843195
🥰Excellent
Catalog No. T36308Cas No. 2067281-51-8
Alias PF06843195
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.
PF-06843195
🥰Excellent
Purity: 98.01%
Catalog No. T36308Alias PF06843195Cas No. 2067281-51-8
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 | Availability | Quantity |
|---|---|---|---|
| 2 mg | $239 | In Stock |
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Purity:98.01%
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Product Introduction
Bioactivity
Chemical Properties
| 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:0.28 nM (Ki), PI3Kδ:160 nM (IC50, in Rat1 fibroblasts), 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] |
| Alias | 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 & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50.00 mg/mL (100.31 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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