Quizartinib

Bezeichnung:Quizartinib

CAS-Nr950769-58-1

Englisch Name:Quizartinib

CBNumberCB52514647

SummenformelC29H32N6O4S

Molgewicht560.67

MOL-Datei950769-58-1.mol

Quizartinib physikalisch-chemischer Eigenschaften

Dichte	1.39±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (up to at least 25 mg/ml)
Aggregatzustand	White powder.
pka	12.59±0.70(Predicted)
Farbe	Off-white
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

Sicherheit

HS Code

2914500090

Gefahreninformationscode (GHS)

Quizartinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Quizartinib is an oral, highly potent, and selective next-generation FLT3 inhibitor (Kd= 1.6nM, IC50= 0.56 nM MV4-11 cells) with clinical antileukaemic activity in relapsed or refractory acute myeloid leukaemia. Quizartinib priming resulted in prevention of myelosuppression in mice treated with 5-FU and Gemcitabine. Quizartinib showed significant reversal of ABCG2-mediated multidrug resistance (@ 3 μM) via antagonism of drug efflux function.?
Verwenden
AC 220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Definition
ChEBI: Quizartinib is a member of the class of phenylureas that is urea in which one of the amino groups has been substituted by a 5-tert-butyl-1,2-oxazol-3-yl group while the other has been substituted by a phenyl group substituted at the para- position by an imidazo[2,1-b][1,3]benzothiazol-2-yl group that, in turn, is substituted at position 7 by a 2-(morpholin-4-yl)ethoxy group. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an antineoplastic agent and a necroptosis inhibitor. It is a benzoimidazothiazole, a member of morpholines, a member of isoxazoles and a member of phenylureas.
target
Flt3ITD
Lager
Store at -20°C
Einzelnachweise
[1] QI CHAO. Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor[J]. Journal of Medicinal Chemistry, 2009, 52 23: 7808-7816. DOI:10.1021/jm9007533.
[2] PATRICK P ZARRINKAR. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).[J]. ACS Nano, 2009: 2984-2992. DOI:10.1182/blood-2009-05-222034.
[3] AMIR T. FATHI Yi B C. The role of FLT3 inhibitors in the treatment of FLT3-mutated acute myeloid leukemia[J]. European Journal of Haematology, 2016, 98 4: 330-336. DOI:10.1111/ejh.12841.
[4] SAMUEL J TAYLOR Wallace Y L. Hitting the snooze button: Inducing quiescence with the FLT3 inhibitor quizartinib protects hematopoietic progenitors from chemotherapy.[J]. Molecular and Cellular Oncology, 2017, 4 6: e1378156. DOI:10.1080/23723556.2017.1378156.
[5] JUN LI. Quizartinib (AC220) reverses ABCG2-mediated multidrug resistance: In vitro and in vivo studies.[J]. Oncotarget, 2017: 93785-93799. DOI:10.18632/oncotarget.21078.
[6] JASJEET BHULLAR. The FLT3 inhibitor quizartinib inhibits ABCG2 at pharmacologically relevant concentrations, with implications for both chemosensitization and adverse drug interactions.[J]. ACS Applied Bio Materials, 2013: e71266. DOI:10.1371/journal.pone.0071266.
[7] JORGE CORTES. Quizartinib, an FLT3 inhibitor, as monotherapy in patients with relapsed or refractory acute myeloid leukaemia: an open-label, multicentre, single-arm, phase 2 trial.[J]. Journal of Agricultural and Food Chemistry, 2018: 889-903. DOI:10.1016/S1470-2045(18)30240-7.

Quizartinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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