PD168393

• CAT Number: I002483
• CAS Number: 194423-15-9
• Molecular Formula: C17H13BrN4O
• Molecular Weight: 369.2
• Purity: ≥95%
• Target: EGFR
• Solubility: DMSO: ≥ 30 mg/mL
• Storage: 3 years -20C powder
• InChI: InChI=1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22)
• InChIKey: HTUBKQUPEREOGA-UHFFFAOYSA-N
• SMILES: BrC1=CC(NC2=NC=NC3=C2C=C(NC(C=C)=O)C=C3)=CC=C1

PD168393 is an potent, cell-permeable, irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773, inactive against insulin, PDGFR, FGFR and PKC.target: EGFRIC 50: 0.7 nM [1](1) PD 168393 inhibite EGFr autophosphorylation in A431 human epidermoid carcinoma cells with >9-fold greater potency than PD 174265.[1](2) PD 168393 decrease the production of TNF-α and phosphrylation of ERK1/2 and p38 induced by LPS in cardiomyocytes.[2](3) PD168393 completely inhibits AKT and ERK phosphorylation at concentrations as low as 0.03 umol/L.[3](4) PD168393 could induce apoptosis and inhibit cell growth in ErbB2 positive lung and breast cancer cell lines.[3](5) PD168393 disrupted MEK1/p44/42 ERK signaling in HaCaT cells as determined by inhibition of phospho-p44/42 ERK. [4]

Reference

1:Effects of ROCK inhibitor Y27632 and EGFR inhibitor PD168393 on human neural precursors co-cultured with rat auditory brainstem explant. Novozhilova E, Englund-Johansson U, Kale A, Jiao Y, Olivius P.Neuroscience. 2015 Feb 26;287:43-54. doi: 10.1016/j.neuroscience.2014.12.009. Epub 2014 Dec 13. PMID: 25514049 2:The pan erbB inhibitor PD168393 enhances lysosomal dysfunction-induced apoptotic death in malignant peripheral nerve sheath tumor cells. Kohli L, Kaza N, Lavalley NJ, Turner KL, Byer S, Carroll SL, Roth KA.Neuro Oncol. 2012 Mar;14(3):266-77. doi: 10.1093/neuonc/nor226. Epub 2012 Jan 18. PMID: 22259051 Free PMC Article3:A liquid chromatography mass spectrometry assay for determination of PD168393, a specific and irreversible inhibitor of erbB membrane tyrosine kinases, in rat serum. Prasain JK, Arabshahi A, Moore R, Barnes S, Carroll SL.J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Dec 15;876(2):219-24. doi: 10.1016/j.jchromb.2008.10.046. Epub 2008 Nov 6. PMID: 19010087 Free PMC Article4:Epidermal growth factor receptor inhibitor (PD168393) potentiates cytotoxic effects of paclitaxel against androgen-independent prostate cancer cells. Pu YS, Hsieh MW, Wang CW, Liu GY, Huang CY, Lin CC, Guan JY, Lin SR, Hour TC.Biochem Pharmacol. 2006 Mar 14;71(6):751-60. Epub 2006 Jan 18. PMID: 16413505