Crenolanib
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IUPAC name
1-(2-{5-[(3-Methyloxetan-3-yl)methoxy]-1H-benzimidazol-1-yl}quinolin-8-yl)piperidin-4-amine
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| Other names
CP-868,596; ARO 002
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3D model (Jmol)
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| Properties | |
| C26H29N5O2 | |
| Molar mass | 443.55 g·mol−1 |
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Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Crenolanib besylate (CP-868,596-26; 4-piperidinamine, 1-[2-[5-[(3-Methyl-3-oxetanyl) methoxy]-1H-benzimidazol-1-yl]- 8-quinolinyl]-, monobenzenesulfonate) is an investigational inhibitor being developed by AROG Pharmaceuticals, LLC. The compound is currently being evaluated for safety and efficacy in clinical trials for various types of cancer, including acute myeloid leukemia (AML),gastrointestinal stromal tumor (GIST), and glioma. Crenolanib is an orally bioavailable benzamidazole that selectively and potently inhibits signaling of wild-type and mutant isoforms of class III receptor tyrosine kinases (RTK) FLT3 (FMS-like Tyrosine Kinase 3), PDGFR α (Platelet-Derived Growth Factor Receptor), and PDGFR β. Unlike most RTK inhibitors, crenolanib is a type I mutant-specific inhibitor that preferentially binds to phosphorylated active kinases with the ‘DFG in’ conformation motif.
Type III Receptor tyrosine kinase, including FLT3, PDGFRα and PDGFRβ, have been directly implicated in the pathogenesis of epithelial, mesenchymal, and hematological malignancies.
Mutations of FLT3 comprise one of the most frequently identified types of genetic alterations in Angiomyolipoma. Approximately one-third of AML patients present with a mutation in this gene. The majority of these mutations result in constitutive activation of downstream signaling pathways and aberrant cell growth. Mutations in FLT3 have also been reported in acute lymphoblastic leukemia (ALL) and myelodysplastic syndrome (MDS).
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