Quizartinib

Quizartinib

Names
IUPAC name 1-(5-(tert-Butyl)isoxazol-3-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea
Other names AC220
Identifiers
CAS Number	950769-58-1 Y
ChEBI	CHEBI:90217 N
ChEMBL	ChEMBL576982 N
ChemSpider	24640357 N
IUPHAR/BPS	5658
Jmol 3D model	Interactive image
UNII	7LA4O6Q0D3 Y
InChI InChI=1S/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36) N Key: CVWXJKQAOSCOAB-UHFFFAOYSA-N N InChI=1/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36) Key: CVWXJKQAOSCOAB-UHFFFAOYAF
SMILES CC(C)(C)c1cc(no1)NC(=O)Nc2ccc(cc2)c3cn4c5ccc(cc5sc4n3)OCCN6CCOCC6
Properties
Chemical formula	C29H32N6O4S
Molar mass	560.67 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
N verify (what is YN ?)
Infobox references

Quizartinib (AC220) is a small molecule receptor tyrosine kinase inhibitor that is currently under development by Ambit Biosciences for the treatment of acute myeloid leukaemia. Its molecular target is FLT3, also known as CD135 which is a proto-oncogene.^[1]

Flt3 mutations are among the most common mutations in acute myeloid leukaemia due to internal tandem duplication of Flt3. The presence of this mutation is a marker of adverse outcome.

Mechanism[edit]

Specifically, Quizartinib selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs).^{[citation needed]}

Mutations cause constitutive action of Flt3 resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis.^{[citation needed]}

Clinical trials[edit]

It had good results in a phase II clinical trial for refractory AML - particularly in patients who went on to have a stem cell transplant.^[2]

References[edit]