WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407458
Description: EBE-A22 is a derivative of PD 153035. EBE-A22, has no effect on EGF-R TK but maintains a high cytotoxic profile. EBE-A22 binds to DNA and behave as typical intercalating agents. EBE-A22 unwinds supercoiled plasmid, stabilizes duplex DNA against heat denaturation, and produces negative CD and ELD signals, as expected for an intercalating agent. EBE-A22, but not PD153035, interacts preferentially with GC-rich sequences and discriminates against homooligomeric runs of A and T which are often cut more readily by the enzyme in the presence of the drug compared to the control.
MedKoo Cat#: 407458
Chemical Formula: C17H16BrN3O2
Exact Mass: 373.0426
Molecular Weight: 374.238
Elemental Analysis: C, 54.56; H, 4.31; Br, 21.35; N, 11.23; O, 8.55
Synonym: EBE-A22; EBE A22; EBEA22.
IUPAC/Chemical Name: N-(3-bromophenyl)-6,7-dimethoxy-N-methylquinazolin-4-amine
InChi Key: IPWGDOZPSOZFOD-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H16BrN3O2/c1-21(12-6-4-5-11(18)7-12)17-13-8-15(22-2)16(23-3)9-14(13)19-10-20-17/h4-10H,1-3H3
SMILES Code: CN(C1=CC=CC(Br)=C1)C2=C3C=C(OC)C(OC)=CC3=NC=N2
PD153035 exhibits a very high affinity and selectivity for the epidermal growth factor receptor tyrosine kinase (EGF-R TK) and shows a remarkable cytotoxicity against several types of tumor cell lines.
1: Goossens JF, Bouey-Bencteux E, Houssin R, Hénichart JP, Colson P, Houssier C,
Laine W, Baldeyrou B, Bailly C. DNA interaction of the tyrosine protein kinase
inhibitor PD153035 and its N-methyl analogue. Biochemistry. 2001 Apr
17;40(15):4663-71. PubMed PMID: 11294633.
2: Grunt TW, Tomek K, Wagner R, Puckmair K, Kainz B, Rünzler D, Gaiger A, Köhler
G, Zielinski CC. Upregulation of retinoic acid receptor-beta by the epidermal
growth factor-receptor inhibitor PD153035 is not mediated by blockade of ErbB
pathways. J Cell Physiol. 2007 Jun;211(3):803-15. PubMed PMID: 17286282.