BIBU 1361 dihydrochloride

EGFR inhibitor

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库存: 现货

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1mg

￥1937.00

1550.00

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10mg

￥4137.00

3310.00

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货号: ajci5872
CAS: 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
分子式: C22H27ClFN7.2HCl
分子量: 516.87
纯度: >98%
溶解度: <51.69mg/ml in Water; <12.92mg/ml in DMSO
储存: Store at -20°C
库存: 现货

Background

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.

参考文献:
[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.