crenolanib
An orally bioavailable benzimidazole targeting the platelet-derived growth factor receptor (PDGFR) subtypes alpha and beta and FMS-related tyrosine kinase 3 (Flt3), with potential antineoplastic activity. Upon oral administration, crenolanib binds to and inhibits both wild-type and mutated forms of PDGFR and Flt3, which may result in the inhibition of PDGFR- and Flt3-related signal transduction pathways. This results in inhibition of tumor angiogenesis and tumor cell proliferation in PDGFR and/or Flt3 overexpressing tumor cells. PDGFR and Flt3, class III receptor tyrosine kinases, are upregulated or mutated in many tumor cell types.
| Synonym: | PDGFR inhibitor CP-868596 |
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| Code name: | CP-868,596 CP-868596 |
| Chemical structure: | [1-[2-[5-(3-methyloxetan-3-ylmethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-yl]amine 4-piperidinamine, 1-[2-[5-[(3-methyl-3-oxetanyl)methoxy]-1Hbenzimidazol-1-yl]-8-quinolinyl]- |