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Crenolanib

Crenolanib structure

Crenolanib 

structure
  • CAS No:

    670220-88-9

  • Formula:

    C26H29N5O2

  • Chemical Name:

    Crenolanib

  • Synonyms:

    4-Piperidinamine,1-[2-[5-[(3-methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-;1-[2-[5-[(3-Methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine;[1-[2-[5-(3-Methyloxetan-3-ylmethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-yl]amine;ARO 002;Crenolanib;CP 868596;1-[2-[5-[(3-Methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine;866109-23-1

  • Categories:

    Pharmaceutical Intermediates  >  Antineoplastics

Description

Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 2.1 nM/3.2 nM, 0.74 nM, respectively.

Crenolanib Basic Attributes

443.54076

443.54

Characteristics

78.4

3.7

1.4±0.1 g/cm3

363.0±34.3 °C

1.704

Crenolanib Use and Manufacturing

Crenolanib is an orally bioavailable, selective inhibitor of type III tyrosine kinases with nanomolar potencies against platelet-derived growth factor receptor α (PDGFRα) and PDGFRβ and Fms-related tyrosine kinase 3 (FLT3; IC50s = 11, 3.2, and 4 nM, respectively). It also inhibits medically-relevant mutant forms of these kinases, including the D842V-containing form of PDGFR and D835Y and internal tandem duplication mutations of FLT3, at nanomolar concentrations. Crenolanib is more than 100-fold selective for these kinases over other tyrosine and serine/threonine kinases. It is effective when used in cells and in vivo.[Cayman Chemical]

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