CAS NO: | 793726-84-8 |
包装 | 价格(元) |
1mg | 电议 |
10mg | 电议 |
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 SMILES | ClC1=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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: |