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Chemical Structure : Bezuclastinib
Catalog No.: PC-73407Not For Human Use, Lab Use Only.
Bezuclastinib (CGT9486, PLX9486) is a potent, selective tyrosine kinase inhibitor (TKI) targeting mutated KIT and demonstrating potent activity in vitro against primary exon 9 and 11 mutations, as well as secondary exon 17 and 18 mutations.
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Bezuclastinib (CGT9486, PLX9486) is a potent, selective tyrosine kinase inhibitor (TKI) targeting mutated KIT and demonstrating potent activity in vitro against primary exon 9 and 11 mutations, as well as secondary exon 17 and 18 mutations.
Bezuclastinib (CGT9486, PLX9486) is a potent inhibitor of growth and KIT phosphorylation in the imatinib-sensitive and imatinib-resistant BaF3 cell lines, with growth IC50=61 nM for KIT-WT and more potently against BaF3 KIT p.D816V (IC50=6.6 nM) and BaF3 KIT p.V560G/D816V (IC50=7.1 nM).
Bezuclastinib (CGT9486, PLX9486) demonstrated signifcant tumor regression and strong inhibition of MAPK activation in imatinib-resistant GIST patient-derived xenograft (PDX) models.
| M.Wt | 331.379 | |
| Formula | C19H17N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Gebreyohannes YK, et al. Clin Exp Med. 2019 May;19(2):201-210.
2. Wagner AJ, et al. JAMA Oncol. 2021 Sep 1;7(9):1343-1350.
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