Masitinib-resistant KIT mutants

Stable Identifier
Homo sapiens
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Mastinib is a class II tyrosine kinase inhibitor that targets mutant and wild-type FGFR3, PDGFR and c-KIT (Dubreuil, 2009). Masitinib, like imatinib, is effective in inhibiting the activity of juxtamembrane mutant forms of KIT, but is ineffective against many of the mutations in the activation loop and ATP-binding cleft of the receptor (Dubreuil, 2009; Serrano et al, 2019; reviewed in Demetri, 2011).

Literature References
PubMed ID Title Journal Year
19789626 Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT

Gros, L, Hajem, B, Hermine, O, Humbert, M, Lermet, A, Letard, S, Leventhal, PS, Mansfield, CD, Arock, M, Voisset, E, Sippl, W, Auclair, C, Moussy, A, Borge, L, Castéran, N, Ciufolini, M, Dubreuil, P

PLoS One 2009
21419931 Differential properties of current tyrosine kinase inhibitors in gastrointestinal stromal tumors

Demetri, GD

Semin. Oncol. 2011
30792533 Complementary activity of tyrosine kinase inhibitors against secondary kit mutations in imatinib-resistant gastrointestinal stromal tumours

Heinrich, MC, Ketzer, J, Bauer, S, Zhu, M, Presnell, A, Raut, CP, George, S, Mannan, AM, Serrano, C, Yu, C, Sicinska, E, Tao, DL, Rubin, BP, Fletcher, JA, Mariño-Enríquez, A, Demetri, GD, Eilers, G, Czaplinski, JT, McKinley, A

Br. J. Cancer 2019
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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