產(chǎn)品目錄

規(guī)格	5 mg 10 mg 25 mg 50 mg 100 mg
CAS	2067281-51-8
別名	N/A
化學(xué)名	N/A
分子式	C20H25F3N8O4
分子量	498.46
溶解度	N/A
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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