产品
编 号:F748622
分子式:C20H25F3N8O4
分子量:498.46
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10mM*1mL in DMSO
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5mg
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10mg
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生物活性:
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.

体内研究:
In rats, PF-06843195 can rapidly and quantitatively transform from PF-06862309.PF-06843195 exhibits oral bioavailability (rat 25 %) following oral administration (rat 10 mg/kg).PF-06843195 exhibits a moderate half-life (rat 3.6 h) due to high plasma clearance (30 mL/min/kg) combined with large volumes of distribution (3.0 L/kg) following intravenous administration (rat 2 mg/kg).Animal Model:Male Wistar Han Rats
Dosage:2 mg/kg (intravenous) and 10 mg/kg (oral gavage)(Pharmacokinetic Analysis)
Administration:Intravenous (IV) or oral gavage (PO)
Result:T1/2 of 3.6 h for rats.

体外研究:
PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively.PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells with IC50s of 7.8 nM and 8.7 nM, respectively.
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