PF-06843195 (C007B-386658)

PF-06843195 is a highly selective PI3Kα inhibitor with an IC 50 of 18 nM in Rat1 fibroblasts. The K i s 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 efficacyIn VitroPF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC 50 s of 62 nM and 32 nM, respectively. PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells with IC 50 s of 7.8 nM and 8.7 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoIn 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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: T 1/2 of 3.6 h for rats.Form:SolidIC50& Target:PI3Kα 18 nM (IC 50 , in Rat1 fibroblasts) PI3Kβ 360 nM (IC 50 , in Rat1 fibroblasts) PI3Kδ 160 nM (IC 50 , in Rat1 fibroblasts) PI3Kα 0.018 nM (Ki) PI3Kδ 0.28 nM (Ki).

Specifications and Purity: ≥99%

Molecular Formula: C20H25F3N8O4

Molecular Weight: 498.46

PubChem CID: 124193915

Isomeric SMILES: C1CN(C[C@@]1(CO)NC2=NC(=NC(=C2F)C3=CN=C(N=C3)N)N4CCOCC4)C(=O)OCC(F)F