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• 產(chǎn)品描述： PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

• 靶點： CDK;cholecystokinin;GSK-3;cholecystokinin;GSK-3;CDK

• 體外研究：
  PHA-767491降低Chk1磷酸化并增加從裸鼠HCC異種移植物切片的腫瘤組織中的原位細(xì)胞凋亡

• 體內(nèi)研究：
  PHA-767491抑制兩種細(xì)胞系的增殖,在HCC1954細(xì)胞中的IC50為0.64 μM,在Colo-205細(xì)胞中的IC50為1.3 μM。PHA-767491（2 μM）在HCC1954細(xì)胞中24小時完全消除Mcm2磷酸化。PHA-767491與5-FU聯(lián)用對HCC細(xì)胞表現(xiàn)出更強(qiáng)的細(xì)胞毒性并誘導(dǎo)顯著的凋亡,表現(xiàn)為顯著增加的胱天蛋白酶3激活和聚（ADP-核糖）聚合酶片段化。 PHA-767491直接抵消5-FU誘導(dǎo)的Chk1的磷酸化并降低抗凋亡蛋白髓性白血病細(xì)胞1ine的表達(dá)。 PHA-767491（0-10 μM）以時間和劑量依賴方式降低成膠質(zhì)細(xì)胞瘤細(xì)胞活力,U87-MG和U251-MG細(xì)胞的IC50約為2.5 μM

• 細(xì)胞實驗： For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC50 values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 μL of this suspension is mixed with 30 μL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader.

• 參考文獻(xiàn)：
  1. Yecies D, et al. Acquired resistance to ABT-737 in lymphoma cells that up-regulate MCL-1 and BFL-1. Blood, 2010, 115(16), 3304-3313. 2. Natoni A, et al. Mechanisms of action of a dual Cdc7/Cdk9 kinase inhibitor against quiescent and proliferating CLL cells. Mol Cancer Ther, 2011, 10(9), 1624-1634. 3. Montagnoli A, et al. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol, 2008, 4(6), 357-365.

• 溶解性： soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	4.69 ml	23.448 ml	46.896 ml
  5 mM	0.938 ml	4.69 ml	9.379 ml
  10 mM	0.469 ml	2.345 ml	4.69 ml
  50 mM	0.094 ml	0.469 ml	0.938 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 *