Vistusertib
作者：齊岳
發(fā)布時間：2023-09-11
09:27:48
點擊數(shù)：
產(chǎn)品名稱：Vistusertib
產(chǎn)品描述：
| 產(chǎn)品描述 | AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. |
| 靶點活性 | P-Akt (S473):80 nM, mTOR:2.8 nM, pS6 (S235/236):200 nM |
| 體外活性 | 在人類ER+乳腺*移植模型中,AZD2014通過調(diào)控mTORC1和mTORC2底物,抑制生長. |
| 體內(nèi)活性 | 在乳腺*細胞系（抗激素療法的ER+細胞系）中,AZD2014抑制細胞生長,促使細胞凋亡。AZD2014能夠抑制mTORC2的生物標記pAKTSer473和 pNDRG1Thr346。 |
| 激酶實驗 | Recombinant truncated FLAG-tagged mTOR expressed in HEK 293 cells is used in biochemical assays, together with a biotinylated p70S6K peptide substrate. Streptavidin donor and protein A acceptor beads are used to assemble the capture complex for generation of the assay signal. The activity of the lipid kinases, PI3K alpha, beta, delta, and gamma are measured using recombinant proteins and the lipid PIP2 as substrate. Assays for ATM and DNA-PK activity are performed. The mTOR cellular activity is measured in MDAMB468 cells, using an Acumen laser scanning cytometer to analyze the levels of phosphorylation of S6 (Ser235/236) and AKT (Ser473)[1]. |
| 細胞實驗 | AZD2014 is prepared in DMSO (10 mM) and stored under nitrogen, and then diluted with appropriate media before use[1]. Cells are plated in 96-well plates for the indicated time. For CellTiterGlo assays: CellTiterGlo is mixed with the cells. Cells are normalized to day 0 control and net growth is determined using the following formula: ((x?y)/(z?y))=net growth, where x=reading of treated sample at end of study, y=average reading on day 0, and z=reading of DMSO-treated sample at end of study. The concentration of DMSO does not exceed 0.03% for any experiment. For MTS assays: adherent cell lines are grown in 96-well plates. MTS reagent is added on day 0 and on day 3 post-AZD2014 addition. Suspension lines are assayed using the Alamar Blue reagent, 72 hours after AZD2014 addition[1]. |
| 別名 | AZD2014 |
| 分子量 | 462.54 |
| 分子式 | C25H30N6O3 |
| CAS No. | 1009298-59-2 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 36 mg/mL (77.8 mM)
H2O: <1 mg/mL
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業(yè)務范圍包括化學試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學品、中間體和化工材料等領(lǐng)域。
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