|1-(2-(5-((3-甲基氧杂环丁烷-3-基)甲氧基)-1H-苯并[d]咪唑-1-基)喹啉-8-基)哌啶-4-胺苯磺酸盐|CsnPharm

CAS No.: 670220-93-6

Synonyms: CP-868596;ARO 002;RO-002

Crenolanib is an orally bioavailable small molecule, targeting the platelet-derived growth factor receptor (PDGFR).

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400-920-2911

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描述Crenolanib (Crenolanib besylate) is a specific and potent inhibitor of class III receptor tyrosine kinases (RTK). The inhibitor-binding constant (Kd) of crenolanib for the wild-type receptors PDGFRA, PDGFRB, and FLT3 was 3.2, 2.1, and 0.74 nmol/L, respectively. The PDGFRA inhibitor crenolanib might be used to treat patients with imatinib-resistant, KIT-mutant GIST. Crenolanib was significantly more potent than imatinib in inhibiting the kinase activity of imatinib-resistant PDGFRA kinases (D842I, D842V, D842Y, DI842-843IM, and deletion I843). Crenolanib was 135-fold more potent than imatinib against D842V with an IC(50) of approximately 10 nmol/L. The IC50 for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1,000 versus 8 nmol/L for imatinib. Besides class III RTKs, crenolanib does not inhibit any other known tyrosine or serine/threonine kinases at clinically achievable concentrations. Crenolanib potently inhibits the kinase activity of the fusion oncogene with IC50 value of 21 nmol/L. In addition, crenolanib potently inhibits the proliferation of EOL-1 cells with a 50% growth inhibitory concentration of 0.2 pmol/L^[1]. Crenolanib potently inhibited the growth of both the imatinib-sensitive GIST-T1 and GIST882 cells (IC50≤8 nM) and the imatinib-resistant GIST-T1-5R cells (IC50=23±6 nM)^[2].
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