MedKoo Cat#: 206700 | Name: Quizartinib free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Quizartinib, also known as AC220 and AC010220, is a highly potent FMS-like receptor tyrosine kinase-3 (FLT3) inhibitor. Quizartinib free base inhibits FLT3 activity and displays antitumor properties in a mouse MV4-11 tumor xenograft model.

Chemical Structure

Quizartinib free base
Quizartinib free base
CAS#950769-58-1 (free base)

Theoretical Analysis

MedKoo Cat#: 206700

Name: Quizartinib free base

CAS#: 950769-58-1 (free base)

Chemical Formula: C29H32N6O4S

Exact Mass: 560.2206

Molecular Weight: 560.67

Elemental Analysis: C, 62.13; H, 5.75; N, 14.99; O, 11.41; S, 5.72

Price and Availability

Size Price Availability Quantity
50mg USD 400.00 2 weeks
100mg USD 650.00 2 weeks
200mg USD 950.00 2 weeks
500mg USD 1,950.00 2 weeks
1g USD 2,950.00 2 weeks
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Synonym
AC220; AC 220; AC-220; AC010220; AC-010220; AC 010220; AC010220; Quizartinib.
IUPAC/Chemical Name
1-(5-(tert-butyl)isoxazol-3-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea
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(C2=CN3C(SC4=CC(OCCN5CCOCC5)=CC=C34)=N2)C=C1)NC6=NOC(C(C)(C)C)=C6
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
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
Shelf Life
>2 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).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
Quizartinib is an orally available FLT3 / STK1 inhibitor (Kd = 1.6 nM, IC50 = 0.56 nM in MV4-11 cell proliferation assay). Displays >10-fold selectivity for FLT3 over panel of 400 kinases.
In vitro activity:
FLT3 inhibitors have been developed to treat patients with FLT3-ITD acute myeloid leukemia (AML); however, when used alone, their efficacy is insufficient. Homoharringtonine synergizes with quizartinib to inhibit cell growth/viability and induce cell-cycle arrest and apoptosis in FLT3-ITD AML cells in vitro. Homoharringtonine combined with quizartinib may be a promising treatment strategy for patients with FLT3-ITD AML, improving positive progonisis. Reference: Biochem Pharmacol. 2021 Jun;188:114538. https://pubmed.ncbi.nlm.nih.gov/33831397/
In vivo activity:
AML is a heterogeneous hematopoietic malignancy with poor outcomes. This study investigated the preclinical efficacy of the combination of quizartinib with the pan PI3K inhibitor BAY-806946 in FLT3-ITD cell lines and primary cells from AML patients. BAY-806946 enhanced quizartinib cytotoxicity and this combination increased the ability of quizartinib to kill CD34+ CD38-leukemia stem cells while sparing normal hematopoietic stem cells. Reference: Adv Biol Regul. 2023 May 23;89:100974. https://pubmed.ncbi.nlm.nih.gov/37245251/
Solvent mg/mL mM
Solubility
DMSO 56.1 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 560.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Wang F, Huang J, Guo T, Zheng Y, Zhang L, Zhang D, Wang F, Naren D, Cui Y, Liu X, Qu Y, Luo H, Yang Y, Wei H, Guo Y. Homoharringtonine synergizes with quizartinib in FLT3-ITD acute myeloid leukemia by targeting FLT3-AKT-c-Myc pathway. Biochem Pharmacol. 2021 Jun;188:114538. doi: 10.1016/j.bcp.2021.114538. Epub 2021 Apr 6. PMID: 33831397. 2. 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. PMID: 23412931. 3. Darici S, Jørgensen HG, Huang X, Serafin V, Antolini L, Barozzi P, Luppi M, Forghieri F, Marmiroli S, Zavatti M. Improved efficacy of quizartinib in combination therapy with PI3K inhibition in primary FLT3-ITD AML cells. Adv Biol Regul. 2023 May 23;89:100974. doi: 10.1016/j.jbior.2023.100974. Epub ahead of print. PMID: 37245251. 4. Swaminathan M, Kantarjian HM, Levis M, Guerra V, Borthakur G, Alvarado Y, DiNardo CD, Kadia T, Garcia-Manero G, Ohanian M, Daver N, Konopleva M, Pemmaraju N, Ferrajoli A, Andreeff M, Jain N, Estrov Z, Jabbour EJ, Wierda WG, Pierce S, Pinsoy MR, Xiao L, Ravandi F, Cortes JE. A phase I/II study of the combination of quizartinib with azacitidine or low-dose cytarabine for the treatment of patients with acute myeloid leukemia and myelodysplastic syndrome. Haematologica. 2021 Aug 1;106(8):2121-2130. doi: 10.3324/haematol.2020.263392. PMID: 33853292; PMCID: PMC8327731.
In vitro protocol:
1. Wang F, Huang J, Guo T, Zheng Y, Zhang L, Zhang D, Wang F, Naren D, Cui Y, Liu X, Qu Y, Luo H, Yang Y, Wei H, Guo Y. Homoharringtonine synergizes with quizartinib in FLT3-ITD acute myeloid leukemia by targeting FLT3-AKT-c-Myc pathway. Biochem Pharmacol. 2021 Jun;188:114538. doi: 10.1016/j.bcp.2021.114538. Epub 2021 Apr 6. PMID: 33831397. 2. 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. PMID: 23412931.
In vivo protocol:
1. Darici S, Jørgensen HG, Huang X, Serafin V, Antolini L, Barozzi P, Luppi M, Forghieri F, Marmiroli S, Zavatti M. Improved efficacy of quizartinib in combination therapy with PI3K inhibition in primary FLT3-ITD AML cells. Adv Biol Regul. 2023 May 23;89:100974. doi: 10.1016/j.jbior.2023.100974. Epub ahead of print. PMID: 37245251. 2. Swaminathan M, Kantarjian HM, Levis M, Guerra V, Borthakur G, Alvarado Y, DiNardo CD, Kadia T, Garcia-Manero G, Ohanian M, Daver N, Konopleva M, Pemmaraju N, Ferrajoli A, Andreeff M, Jain N, Estrov Z, Jabbour EJ, Wierda WG, Pierce S, Pinsoy MR, Xiao L, Ravandi F, Cortes JE. A phase I/II study of the combination of quizartinib with azacitidine or low-dose cytarabine for the treatment of patients with acute myeloid leukemia and myelodysplastic syndrome. Haematologica. 2021 Aug 1;106(8):2121-2130. doi: 10.3324/haematol.2020.263392. PMID: 33853292; PMCID: PMC8327731.
1: Xiao X, Wang P, Zhang W, Wang J, Cai M, Jiang H, Wu Y, Shan H. GNF-7, a novel FLT3 inhibitor, overcomes drug resistance for the treatment of FLT3‑ITD acute myeloid leukemia. Cancer Cell Int. 2023 Nov 30;23(1):302. doi: 10.1186/s12935-023-03142-y. PMID: 38037057; PMCID: PMC10691066. 2: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Quizartinib. 2023 Nov 15. PMID: 38051808. 3: Alshamleh I, Kurrle N, Makowka P, Bhayadia R, Kumar R, Süsser S, Seibert M, Ludig D, Wolf S, Koschade SE, Stoschek K, Kreitz J, Fuhrmann DC, Toenges R, Notaro M, Comoglio F, Schuringa JJ, Berg T, Brüne B, Krause DS, Klusmann JH, Oellerich T, Schnütgen F, Schwalbe H, Serve H. PDP1 is a key metabolic gatekeeper and modulator of drug resistance in FLT3-ITD-positive acute myeloid leukemia. Leukemia. 2023 Dec;37(12):2367-2382. doi: 10.1038/s41375-023-02041-5. Epub 2023 Nov 7. PMID: 37935978; PMCID: PMC10681906. 4: Zheng C, Guo H, Mo Y, Liu G. Integrating Bioinformatics and Drug Sensitivity Analyses to Identify Molecular Characteristics Associated with Targeting Necroptosis in Breast Cancer and their Clinical Prognostic Significance. Recent Pat Anticancer Drug Discov. 2023 Aug 31. doi: 10.2174/1574892819666230831112815. Epub ahead of print. PMID: 37653627. 5: Ge SS, Qiu QC, Dai HP, Shen XD, Wu TM, Du JH, Wan CL, Shen HJ, Wu DP, Xue SL, Liu SB. Mutation spectrum of FLT3 and significance of non-canonical FLT3 mutations in haematological malignancy. Br J Haematol. 2023 Aug;202(3):539-549. doi: 10.1111/bjh.18877. Epub 2023 May 28. PMID: 37246158. 6: Wang L, Jiang P, Li J, Huang Y, Wen J, Wu Z, Chen Y, Hu J. Loss of MiR-155 Sensitizes FLT3-ITD+AML to Chemotherapy and FLT3 Inhibitors via Glycolysis Blocking by Targeting PIK3R1. J Cancer. 2023 Jan 1;14(1):99-113. doi: 10.7150/jca.54775. PMID: 36605494; PMCID: PMC9809327. 7: Jiang X, Zhang K, Gao C, Ma W, Liu M, Guo X, Bao G, Han B, Hu H, Zhao Z. Activation of FMS-like tyrosine kinase 3 protects against isoprenaline-induced cardiac hypertrophy by improving autophagy and mitochondrial dynamics. FASEB J. 2022 Dec;36(12):e22672. doi: 10.1096/fj.202200419RR. PMID: 36440960. 8: Chen R, Wu W, Chen SY, Liu ZZ, Wen ZP, Yu J, Zhang LB, Liu Z, Zhang J, Luo P, Zeng WJ, Cheng Q. A Pan-Cancer Analysis Reveals CLEC5A as a Biomarker for Cancer Immunity and Prognosis. Front Immunol. 2022 Aug 1;13:831542. doi: 10.3389/fimmu.2022.831542. PMID: 35979347; PMCID: PMC9376251. 9: Cai B, Liu Y, Chong Y, Mori SF, Matsunaga A, Zhang H, Fang X, Chang CS, Cowell JK, Hu T. A truncated derivative of FGFR1 kinase cooperates with FLT3 and KIT to transform hematopoietic stem cells in syndromic and de novo AML. Mol Cancer. 2022 Jul 29;21(1):156. doi: 10.1186/s12943-022-01628-3. PMID: 35906694; PMCID: PMC9336057. 10: Powell RM, Peeters MJW, Rahbech A, Aehnlich P, Seremet T, Thor Straten P. Small Molecule Inhibitors of MERTK and FLT3 Induce Cell Cycle Arrest in Human CD8+ T Cells. Vaccines (Basel). 2021 Nov 8;9(11):1294. doi: 10.3390/vaccines9111294. PMID: 34835225; PMCID: PMC8617686. 11: Yamawaki K, Shiina I, Murata T, Tateyama S, Maekawa Y, Niwa M, Shimonaka M, Okamoto K, Suzuki T, Nishida T, Abe R, Obata Y. FLT3-ITD transduces autonomous growth signals during its biosynthetic trafficking in acute myelogenous leukemia cells. Sci Rep. 2021 Nov 22;11(1):22678. doi: 10.1038/s41598-021-02221-2. PMID: 34811450; PMCID: PMC8608843. 12: Wachholz V, Mustafa AM, Zeyn Y, Henninger SJ, Beyer M, Dzulko M, Piée-Staffa A, Brachetti C, Haehnel PS, Sellmer A, Mahboobi S, Kindler T, Brenner W, Nikolova T, Krämer OH. Inhibitors of class I HDACs and of FLT3 combine synergistically against leukemia cells with mutant FLT3. Arch Toxicol. 2022 Jan;96(1):177-193. doi: 10.1007/s00204-021-03174-1. Epub 2021 Oct 19. PMID: 34665271; PMCID: PMC8748367. 13: Yang X, Wan M, Yu F, Wu X. Histone methyltransferase EZH2 epigenetically affects CCNA1 expression in acute myeloid leukemia. Cell Signal. 2021 Nov;87:110144. doi: 10.1016/j.cellsig.2021.110144. Epub 2021 Sep 9. PMID: 34509612. 14: Lu X, Han L, Busquets J, Collins M, Lodi A, Marszalek JR, Konopleva M, Tiziani S. The Combined Treatment With the FLT3-Inhibitor AC220 and the Complex I Inhibitor IACS-010759 Synergistically Depletes Wt- and FLT3-Mutated Acute Myeloid Leukemia Cells. Front Oncol. 2021 Aug 20;11:686765. doi: 10.3389/fonc.2021.686765. PMID: 34490088; PMCID: PMC8417744. 15: Liu SB, Dong HJ, Wang J, Qiu QC, Xue SL, Li L. [Effect of FLT3-ITD Length on 32D Cell Proliferation, Apoptosis and Sensitivity to FLT3 Inhibitor]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2021 Aug;29(4):1034-1038. Chinese. doi: 10.19746/j.cnki.issn.1009-2137.2021.04.004. PMID: 34362479. 16: Wang P, Xiao X, Zhang Y, Zhang B, Li D, Liu M, Xie X, Liu C, Liu P, Ren R. A dual inhibitor overcomes drug-resistant FLT3-ITD acute myeloid leukemia. J Hematol Oncol. 2021 Jul 3;14(1):105. doi: 10.1186/s13045-021-01098-y. PMID: 34217323; PMCID: PMC8255005. 17: Guo D, Zhao Y, Wang N, You N, Zhu W, Zhang P, Ren Q, Yin J, Cheng T, Ma X. GADD45g acts as a novel tumor suppressor, and its activation suggests new combination regimens for the treatment of AML. Blood. 2021 Aug 12;138(6):464-479. doi: 10.1182/blood.2020008229. PMID: 33945602. 18: Liu Y, Wei J, Liu J, Ma W, Duan Y, Liu D. Novel AXL-targeted agents overcome FLT3 inhibitor resistance in FLT3-ITD+ acute myeloid leukemia cells. Oncol Lett. 2021 May;21(5):397. doi: 10.3892/ol.2021.12658. Epub 2021 Mar 18. PMID: 33777220; PMCID: PMC7988696. 19: An X, Liu J, Wang N, Wang D, Huang L, Zhang L, Cai J, Wery JP, Zhou D, Zhou J, Li QX. Corrigendum to "AC220 and AraC cause differential inhibitory dynamics in patient-derived M5-AML with FLT3-ITD and, thus, ultimately distinct therapeutic outcomes" [Experimental Hematology 2017;45:36-44]. Exp Hematol. 2021 Jan;93:85. doi: 10.1016/j.exphem.2020.10.004. Epub 2020 Nov 12. Erratum for: Exp Hematol. 2017 Jan;45:36-44.e2. doi: 10.1016/j.exphem.2016.09.004. PMID: 33189657. 20: Garcia-Horton A, Yee KW. Quizartinib for the treatment of acute myeloid leukemia. Expert Opin Pharmacother. 2020 Dec;21(17):2077-2090. doi: 10.1080/14656566.2020.1801637. Epub 2020 Aug 9. PMID: 32772726.