產(chǎn)品目錄

規(guī)格	5mg 25mg 500mg 1g
CAS	1627494-13-6
別名	N/A
化學(xué)名	(R)-8-(1-((3,5-difluorophenyl)amino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide
分子式	C24H25F2N3O4
分子量	457.47
溶解度	≥ 45.7mg/mL in DMSO with ultrasonic
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：

Description:

IC50: 0.003 μM for PI3Kβ and 0.017 μM for PI3Kδ

The PI3K-Akt signaling pathway plays a critical role in cell growth, proliferation, motility, and survival. In human cancer, this pathway is activated by several mechanisms, including somatic mutations, deletions, and amplifications. Class I PI3Ks are further divided into class IA enzymes (PI3Kα, PI3Kβ, and PI3Kδ) and class IB enzymes (PI3Kγ). AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ.

In vitro: AZD8186 gave potent inhibition of p-Akt in cells sensitive to PI3Kβ inhibition and in cells sensitive to PI3Kδ inhibition but not to cells sensitive to PI3Kα inhibition. The overall kinase selectivity of AZD8186 was evaluated in several panels of recombinant protein and lipid kinase assays. 13 did not show significant activity against a panel of 59 protein kinases tested at 1 μM [1].

In vivo: The antitumor activity of AZD8186 was evaluated in the PTEN deficient PC3 prostate tumor xenograft model in nude mice, either at 100 mg/kg b.i.d. without ABT coadministration, or at 60, 30, and 10 mg/mg b.i.d. with ABT coadministration. Higher inhibition was seen in the 60 and 30 mg/kg groups with ABT coadministration than in the 100 mg/kg group without ABT coadministration [1].

Clinical trial: AZD8186 was selected as a clinical candidate for treatment of PTENdeficient cancers and has recently entered phase I clinical trials [2].

特別提醒：

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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