Crenolanib

Crenolanib
Names
	IUPAC name 1-(2-{5-[(3-methyloxetan-3-yl)methoxy]-1H-benzimidazol-1-yl}quinolin-8-yl)piperidin-4-amine
	Other names CP-868,596; AR-868,596-26
Identifiers
CAS Number	670220-88-9 ;
3D model (JSmol)	Interactive image;
ChEBI	CHEBI:145365;
ChEMBL	ChEMBL2105728 ; ChEMBL2146086 ;
ChemSpider	8541584 ;
IUPHAR/BPS	7882;
KEGG	D10102 ;
PubChem CID	10366136;
UNII	LQF7I567TQ ;
CompTox Dashboard (EPA)	DTXSID50985873 ;
	InChI InChI=1S/C26H29N5O2/c1-26(14-32-15-26)16-33-20-6-7-22-21(13-20)28-17-31(22)24-8-5-18-3-2-4-23(25(18)29-24)30-11-9-19(27)10-12-30/h2-8,13,17,19H,9-12,14-16,27H2,1H3 Key: DYNHJHQFHQTFTP-UHFFFAOYSA-N ;
	SMILES O(c5cc4ncn(c1nc3c(cc1)cccc3N2CCC(N)CC2)c4cc5)CC6(COC6)C;
Properties
Chemical formula	C26H29N5O2
Molar mass	443.551 g·mol−1
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). verify (what is ?) Infobox references

Crenolanib besylate (CP-868,596-26 or AR-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),^[1]^[2] gastrointestinal stromal tumor (GIST),^[3] and glioma.^[4] Crenolanib is an orally bioavailable benzimidazole 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.^[5]

^ "A Phase II Study of Crenolanib in Relapsed/Refractory Acute Myeloid Leukemia Patients With FLT3 Activating Mutations - Full Text View". ClinicalTrials.gov. Retrieved 2014-04-08.
^ "Phase II Study of Crenolanib in Subjects With Relapsed/Refractory AML With FLT3 Activating Mutations - Full Text View". ClinicalTrials.gov. Retrieved 2014-04-08.
^ "Phase II Study of Crenolanib (CP-868,596), for the Treatment of Patients With Advanced Gastrointestinal Stromal Tumors With the D842-related Mutations and Deletions in the PDGFRA Gene - Full Text View". ClinicalTrials.gov. Retrieved 2014-04-08.
^ "PDGFR Inhibitor Crenolanib in Children/Young Adults With Diffuse Intrinsic Pontine Glioma or Recurrent High-Grade Glioma - Full Text View". ClinicalTrials.gov. Retrieved 2014-04-08.
^ A. Ramachandran; H. Marshall; V. Jain. "CRENOLANIB, A NOVEL TYPE I, MUTANT -SPECIFIC INHIBITOR OF CLASS III RECEPTOR TYROSINE KINASES, PREFERENTIALLY BINDS TO PHOSPHORYLATED KINASES" (PDF). gistsupport.org. Retrieved 2014-04-08.

[1] "A Phase II Study of Crenolanib in Relapsed/Refractory Acute Myeloid Leukemia Patients With FLT3 Activating Mutations - Full Text View". ClinicalTrials.gov. Retrieved 2014-04-08.

[2] "Phase II Study of Crenolanib in Subjects With Relapsed/Refractory AML With FLT3 Activating Mutations - Full Text View". ClinicalTrials.gov. Retrieved 2014-04-08.

[3] "Phase II Study of Crenolanib (CP-868,596), for the Treatment of Patients With Advanced Gastrointestinal Stromal Tumors With the D842-related Mutations and Deletions in the PDGFRA Gene - Full Text View". ClinicalTrials.gov. Retrieved 2014-04-08.

[4] "PDGFR Inhibitor Crenolanib in Children/Young Adults With Diffuse Intrinsic Pontine Glioma or Recurrent High-Grade Glioma - Full Text View". ClinicalTrials.gov. Retrieved 2014-04-08.

[5] A. Ramachandran; H. Marshall; V. Jain. "CRENOLANIB, A NOVEL TYPE I, MUTANT -SPECIFIC INHIBITOR OF CLASS III RECEPTOR TYROSINE KINASES, PREFERENTIALLY BINDS TO PHOSPHORYLATED KINASES" (PDF). gistsupport.org. Retrieved 2014-04-08.

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