MedKoo Cat#: 200072 Name: Quizartinib HCl CAS#: 1132827-21-4 (2HCl salt) Chemical Formula: C29H34Cl2N6O4S Exact Mass: Molecular Weight: 633.589 Elemental Analysis: C, 54.98; H, 5.41; Cl, 11.19; N, 13.26; O, 10.10; S, 5.06
Related CAS #: 1132827-21-4 (2HCl) 950769-58-1 (free base)
Synonym: AC220; AC 220; AC-220; AC010220; AC-010220; AC 010220; AC010220.2HCl; Quizartinib; Quizartinib HCl; Quizartinib dihydrochloride..
IUPAC/Chemical Name: 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
InChi Key: CVWXJKQAOSCOAB-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(NC1=CC=C(C(N=C2SC3=C4)=CN2C3=CC=C4OCCN5CCOCC5)C=C1)NC6=NOC(C(C)(C)C)=C6
Technical Data
Appearance: Yellow to orange solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Certificate of Analysis: View CoA: current batch, Lot#BBC61215
QC Data: View QC data: current batch, Lot#BBC61215
Safety Data Sheet (MSDS): View Material Safety Data Sheet (MSDS)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not soluble in water.
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
Additional Information
References
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2: Zorn JA, Wang Q, Fujimura E, Barros T, Kuriyan J. Crystal structure of the FLT3 kinase domain bound to the inhibitor Quizartinib (AC220). PLoS One. 2015 Apr 2;10(4):e0121177. doi: 10.1371/journal.pone.0121177. eCollection 2015. PubMed PMID: 25837374; PubMed Central PMCID: PMC4383440.
3: Altman K, Sharata H. Catastrophic eruptive keratoacanthomas and squamous cell cancers after treatment with an FLT3 inhibitor quizartinib (AC220). Dermatol Surg. 2015 Apr;41(4):530-1. doi: 10.1097/DSS.0000000000000316. PubMed PMID: 25775444.
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5: Wander SA, Levis MJ, Fathi AT. The evolving role of FLT3 inhibitors in acute myeloid leukemia: quizartinib and beyond. Ther Adv Hematol. 2014 Jun;5(3):65-77. doi: 10.1177/2040620714532123. Review. PubMed PMID: 24883179; PubMed Central PMCID: PMC4031904.
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7: Levis M. Quizartinib in acute myeloid leukemia. Clin Adv Hematol Oncol. 2013;11(9):586-8. Review. PubMed PMID: 24518522.
8: Schaab C, Oppermann FS, Klammer M, Pfeifer H, Tebbe A, Oellerich T, Krauter J, Levis M, Perl AE, Daub H, Steffen B, Godl K, Serve H. Global phosphoproteome analysis of human bone marrow reveals predictive phosphorylation markers for the treatment of acute myeloid leukemia with quizartinib. Leukemia. 2014 Mar;28(3):716-9. doi: 10.1038/leu.2013.347. Epub 2013 Nov 19. PubMed PMID: 24247654; PubMed Central PMCID: PMC3948157.
9: Ostronoff F, Estey E. The role of quizartinib in the treatment of acute myeloid leukemia. Expert Opin Investig Drugs. 2013 Dec;22(12):1659-69. doi: 10.1517/13543784.2013.842973. Epub 2013 Sep 26. Review. PubMed PMID: 24070241.
10: Cortes JE, Kantarjian H, Foran JM, Ghirdaladze D, Zodelava M, Borthakur G, Gammon G, Trone D, Armstrong RC, James J, Levis M. Phase I study of quizartinib administered daily to patients with relapsed or refractory acute myeloid leukemia irrespective of FMS-like tyrosine kinase 3-internal tandem duplication status. J Clin Oncol. 2013 Oct 10;31(29):3681-7. doi: 10.1200/JCO.2013.48.8783. Epub 2013 Sep 3. PubMed PMID: 24002496; PubMed Central PMCID: PMC3804291.
11: Bhullar J, Natarajan K, Shukla S, Mathias TJ, Sadowska M, Ambudkar SV, Baer MR. The FLT3 inhibitor quizartinib inhibits ABCG2 at pharmacologically relevant concentrations, with implications for both chemosensitization and adverse drug interactions. PLoS One. 2013 Aug 14;8(8):e71266. doi: 10.1371/journal.pone.0071266. eCollection 2013. PubMed PMID: 23967177; PubMed Central PMCID: PMC3743865.
12: Kampa-Schittenhelm KM, Heinrich MC, Akmut F, Döhner H, Döhner K, Schittenhelm MM. Quizartinib (AC220) is a potent second generation class III tyrosine kinase inhibitor that displays a distinct inhibition profile against mutant-FLT3, -PDGFRA and -KIT isoforms. Mol Cancer. 2013 Mar 7;12:19. doi: 10.1186/1476-4598-12-19. PubMed PMID: 23497317; PubMed Central PMCID: PMC3637582.
13: Gunawardane RN, Nepomuceno RR, Rooks AM, Hunt JP, Ricono JM, Belli B, Armstrong RC. Transient exposure to quizartinib mediates sustained inhibition of FLT3 signaling while specifically inducing apoptosis in FLT3-activated leukemia cells. Mol Cancer Ther. 2013 Apr;12(4):438-47. doi: 10.1158/1535-7163.MCT-12-0305. Epub 2013 Feb 14. PubMed PMID: 23412931.
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