Target Validation Information
Target ID T14597
Target Name Receptor protein-tyrosine kinase erbB-2
Target Type
Successful
Drug Potency against Target Lapatinib Drug Info Ki = 9.2 nM [552263]
CI-1033 Drug Info IC50 = 19 nM [552773]
Pazopanib + Tyverb/Tykerb Drug Info pKi = 6.8 [552646]
HKI-272 Drug Info Ki = 59 nM [552437]
Lapatinib Drug Info Ki = 9.2 nM [552318]
CP-724714 Drug Info IC50 = 3.8 nM [552773]
BIBW 2992 Drug Info IC50 = 14 nM
TAK165 Drug Info Ki = 6 nM [552607]
Tyverb/Tykerb Drug Info Ki = 9.2 nM [552971]
(1-Benzyl-1H-indazol-5-yl)-quinazolin-4-yl-amine Drug Info IC50 = 10 nM [526072]
(1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine Drug Info IC50 = 90 nM [526072]
BMS-599626 Drug Info IC50 = 32 nM [552881]
AEE-788 Drug Info IC50 = 6 nM [552727]
Action against Disease Model Trastuzumab Overexpression of ErbB2 in breast cancer is associated with increased recurrence and worse prognosis. Acc uMulating evidences suggest that molecular targeted therapy is a promising anticancer strategy. In this study, we produced a novel anti-ErbB2 monoclonal antibody, 6G10, that recognized an epitope distinct from the trastuz uMab binding site. 6G10 induced aggregation of BT474 breast cancer cells and inhibited proliferation of various breast cancer cell lines including BT474. A growth inhibition assay showed that 6G10 had EC(50) values comparable to trastuz uMab, indicating that the drugs have a similar level of potency. Furthermore, intraperitoneal administration of 6G10 completely inhibited the growth of xenografted t uMors derived from BT474 and SK-BR-3 cells. These data suggested that 6G10 has great therapeutic potential and could be administered to patients alternatively, or synergistically, with trastuz uMab. [552934] Drug Info
References
Ref 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 552773A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358.
Ref 552646Selective agents for serotonin2C (5-HT2C) receptor. Curr Top Med Chem. 2006;6(18):1927-70.
Ref 552437Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004 Jun 1;64(11):3958-65.
Ref 552318The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94.
Ref 552934A novel mouse monoclonal antibody targeting ErbB2 suppresses breast cancer growth. Biochem Biophys Res Commun. 2009 Jul 3;384(3):329-33. doi: 10.1016/j.bbrc.2009.04.118. Epub 2009 May 4.
Ref 552773A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358.
Ref 552607Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int J Urol. 2006 May;13(5):587-92.
Ref 552971Small molecule inhibitors of PKCTheta as potential antiinflammatory therapeutics. Curr Top Med Chem. 2009;9(7):640-54.
Ref 526072Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5.Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Ref 526072Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5.Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Ref 552881Recent advances in the development of multi-kinase inhibitors. Mini Rev Med Chem. 2008 Nov;8(13):1312-27.
Ref 552727Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.

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