PF-06843195 |
| رقم الكتالوجGC62556 |
PF-06843195 هو مثبط PI3Kα انتقائي للغاية مع IC50 من 18 نانومتر في الخلايا الليفية Rat1إن Kis لـ PF-06843195 لـ PI3Kα و PI3Kδ في مقايسة كيناز البيوكيميائية أقل من 0.018 نانومتر و 0.28 نانومتر ، على التوالييتميز PF-06843195 بقمع كبير لمسار إشارات PI3K / mTOR وفعالية مقاومة دائمة للأورام
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Cas No.: 2067281-51-8
Sample solution is provided at 25 µL, 10mM.
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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[1].
PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively[1].PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells with IC50s of 7.8 nM and 8.7 nM, respectively[1].
In rats, PF-06843195 can rapidly and quantitatively transform from PF-06862309[1].PF-06843195 exhibits oral bioavailability (rat 25 %) following oral administration (rat 10 mg/kg)[1].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)[1].
[1]. Hengmiao Cheng, et al. Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195). J Med Chem. 2021 Jan 14;64(1):644-661.
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