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BIBU 1361 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIBU 1361 dihydrochloride图片
CAS NO:793726-84-8
包装与价格:
包装价格(元)
1mg电议
10mg电议

产品介绍
Cas No.793726-84-8
别名N-(3-氯-4-氟苯基)-6-[4-[(二乙基氨基)甲基]-1-哌啶基]嘧啶并[5,4-D]嘧啶-4-胺
化学名N-(3-chloro-4-fluorophenyl)-6-(4-((diethylamino)methyl)piperidin-1-yl)pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride
Canonical SMILESClC1=CC(NC2=NC=NC3=CN=C(N=C32)N4CCC(CN(CC)CC)CC4)=CC=C1F.Cl.Cl
分子式C22H27ClFN7.2HCl
分子量516.87
溶解度<51.69mg/ml in Water;<12.92mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BIBU 1361 dihydrochloride is a selective inhibitor of epidermal growth factor receptor (EGFR) kinase with an IC50 value of 0.038 ± 0.007 μM [1, 2].

The EGFR signaling pathway is associated with multiple intracellular signaling events that promote proliferation and survival. It plays a key role in the progression of glioblastoma multiforme (GBM) [2].

In glioma cells, EGFR signaling can induce the phosphorylation of Akt, Erk1/2 and STAT3. BIBU 1361 decreased levels of EGFR and subsequently decreased levels of p-EGFR. This effect was accompanied by the decrease in pAkt and the downstream target p-mTOR. P-S6 kinase and p-P70S6 kinase are two key targets of p-mTOR. Both of them are associated with cell proliferation. In glioma cells treated with BIBU 1361, P-S6 kinase and p-P70S6 kinase were also downregulated. E2F1 is a G1/S regulator. E2F1 is known to be interacted with by EGFR. The inhibition of Akt/mTOR signaling can affect cell cycle progression. In glioma cells, BIBU 1361 inhibited the expression of Akt/mTOR and decreased EGFR. In glioma cells, BIBU 1361 decreased the expression of cyclin E and E2F1, increased the level of p21, and increased cell number at the S and G2/M phase of the cell cycle [2].

The effect of BIBU 1361 in the animal body has not been found.

References:
[1].  Antczak C, Mahida JP, Bhinder B, et al. A High-Content Biosensor-Based Screen Identifies Cell-Permeable Activators and Inhibitors of EGFR Function Implications in Drug Discovery. Journal of biomolecular screening, 2012, 17(7): 885-899.
[2].  Ghildiyal R, Dixit D, Sen E. EGFR inhibitor BIBU induces apoptosis and defective autophagy in glioma cells. Molecular carcinogenesis, 2013, 52(12): 970-982.