Description
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) . 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 . The effect of BIBU 1361 in the animal body has not been found.
Product information
CAS Number: 793726-84-8
Molecular Weight: 516.87
Formula: C22H29Cl3FN7
Chemical Name: N-(3-chloro-4-fluorophenyl)-6-{4-[(diethylamino)methyl]piperidin-1-yl}pyrimido[5,4-d][1,3]diazin-4-amine dihydrochloride
Smiles: Cl.Cl.CCN(CC1CCN(CC1)C1N=C2C(NC3C=C(Cl)C(F)=CC=3)=NC=NC2=CN=1)CC
InChiKey: ZNNWCQCQUKAMGL-UHFFFAOYSA-N
InChi: InChI=1S/C22H27ClFN7.2ClH/c1-3-30(4-2)13-15-7-9-31(10-8-15)22-25-12-19-20(29-22)21(27-14-26-19)28-16-5-6-18(24)17(23)11-16;;/h5-6,11-12,14-15H,3-4,7-10,13H2,1-2H3,(H,26,27,28);2*1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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