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• 產(chǎn)品描述： GDC-0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC-0084 specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and survival in susceptible tumor cell populations

• 靶點： mTOR;PI3K;PI3K;mTOR

• 體外研究：
  GDC-0084對小鼠腦中的PI3K信號通路有明顯抑制效果,可抑制高達(dá)90%的pAkt信號.在U87和GS2原位移植瘤模型中,GDC-0084對腫瘤生長分別具有70%和40%的抑制作用.GDC-0084的療效正處于臨床患者檢測評估階段,暴露的耐受劑量與小鼠模型中的有效劑量一致

• 體內(nèi)研究：
  在人微粒體及干細(xì)胞培養(yǎng)中,GDC-0084顯示出良好的代謝穩(wěn)定性,能抑制正常腦組織中PI3K通路的關(guān)鍵信號pAKT。GDC-0084抑制多種神經(jīng)膠質(zhì)瘤細(xì)胞的增殖（IC50：0.3-1.1 μM）。GDC-0084與血漿蛋白結(jié)合率較低,在CD-1小鼠血漿中游離分?jǐn)?shù)為29.5±2.7%（n=3,5 μM）,而在CD-1小鼠中與腦組織結(jié)合率較高,游離分?jǐn)?shù)只有6.7±1%(n=3)

• 細(xì)胞實驗： For transport studies, cells are seeded on 24-well Millicell plates 4 days prior to use(polyethylene terephtalate membrane, 1 μm pore size) at a seeding density of 1.3×105 cells/ml). GDC-0084 is tested at 5 μM in the apical-tobasolateral (A-B) and basolateral-to-apical (B-A) directions. The compound is dissolved in transport buffer consisting of Hanks' balanced salt solution with 10 mM HEPES. Lucifer Yellow is used as the paracellular and monolayer integrity marker. GDC-0084 concentrations in the donor and receiving compartments are determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. The apparent permeability (Papp), in the apical to A-B and B-A directions, is calculated after 2-hour incubation.(Only for Reference)

• 參考文獻(xiàn)：
  1: Salphati L, Alicke B, Heffron TP, Shahidi-Latham S, Nishimura M, Cao T, Carano RA, Cheong J, Greve J, Koeppen H, Lau S, Lee LB, Nannini-Pepe M, Pang J, Plise EG, Quiason C, Rangell L, Zhang X, Gould SE, Phillips HS, Olivero AG. Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma. Drug Metab Dispos. 2016 Dec;44(12):1881-1889. Epub 2016 Sep 16. PubMed PMID: 27638506.
  
  2: Heffron TP, Ndubaku CO, Salphati L, Alicke B, Cheong J, Drobnick J, Edgar K, Gould SE, Lee LB, Lesnick JD, Lewis C, Nonomiya J, Pang J, Plise EG, Sideris S, Wallin J, Wang L, Zhang X, Olivero AG. Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. ACS Med Chem Lett. 2016 Feb 16;7(4):351-6. doi: 10.1021/acsmedchemlett.6b00005. eCollection 2016 Apr 14. PubMed PMID: 27096040; PubMed Central PMCID: PMC4834666.

• 溶解性： soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.615 ml	13.075 ml	26.149 ml
  5 mM	0.523 ml	2.615 ml	5.23 ml
  10 mM	0.261 ml	1.307 ml	2.615 ml
  50 mM	0.052 ml	0.261 ml	0.523 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *