Quizartinib dihydrochloride (Synonyms: AC220 dihydrochloride)

Name: Quizartinib dihydrochloride
Brand: MedChemExpress
SKU: HY-14217
Rating: 5.0 (45 reviews)

Cat. No.: HY-14217 Purity: 99.81%: Data Sheet
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Quizartinib (AC220) dihydrochloride is an orally active, potent and selective FLT3 inhibitor. Quizartinib dihydrochloride inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib dihydrochloride inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib dihydrochloride can be used for the research of cancer.

For research use only. We do not sell to patients.

CAS No. : 1132827-21-4

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 45 publication(s) in Google Scholar

Other Forms of Quizartinib dihydrochloride:

Quizartinib In-stock

45 Publications Citing Use of MCE Quizartinib dihydrochloride

: Quizartinib dihydrochloride purchased from MedChemExpress. Usage Cited in: J Med Chem. 2017 Oct 26;60(20):8407-8424. [Abstract]; Doseresponsive immunoblotting of the signaling pathway with the cells extracted from tumor tissues of the experimental animal after the 14 and 7 (AC220) treatments.

: Quizartinib dihydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jul 26;7(30):47018-47032. [Abstract]; A. The established 32D cells are treated with Quizartinib for 2h, followed by 10 ng/mL FL stimulation for 10 minutes. Wt-FLT3 and mutant FLT3 are immunoprecipitated by each tag as indicated and subjected to Western blot. Phosphorylation levels of FLT3, STAT5, AKT and MAPK are examined. B. 32D cells are treated with Quizartinib at the indicated concentrations in the presence or absence of 10 ng/mL FL for 2 hours. Phosphorylation levels of FLT3, STAT5, AKT and MAPK are detected by Western blot.

: Quizartinib dihydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2014 Feb 10;25(2):226-42. [Abstract]; Western blot for indicated proteins on lysates from FLT3-ITD-positive primary murine cells expressing either wild-type (WT) or constitutive active (SYK-TEL) SYK and treated for eight hours with indicated doses of AC220.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
K562	GI₅₀	> 20 μM Compound: 1, AC220	Cytotoxicity against human FLT3-negative K562 cells harboring wild type BCR/ABL after 72 hrs by MTS assay Cytotoxicity against human FLT3-negative K562 cells harboring wild type BCR/ABL after 72 hrs by MTS assay	[PMID: 23618709]
MOLM-13	GI₅₀	0.004 μM Compound: 1, AC220	Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay	[PMID: 23618709]
MV4-11	GI₅₀	0.003 μM Compound: 1, AC220	Cytotoxicity against human MV4-11 cells harboring FLT3/ITD mutant after 72 hrs by MTS assay Cytotoxicity against human MV4-11 cells harboring FLT3/ITD mutant after 72 hrs by MTS assay	[PMID: 23618709]
RS4-11	GI₅₀	2.2 μM Compound: 1, AC220	Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by MTS assay Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by MTS assay	[PMID: 23618709]
Sf9	IC₅₀	0.069 μM Compound: 1, AC220	Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis	[PMID: 23618709]
Sf9	IC₅₀	0.43 μM Compound: 1, AC220	Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis	[PMID: 23618709]
Sf9	IC₅₀	> 10 μM Compound: 1, AC220	Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis	[PMID: 23618709]
U-937	GI₅₀	> 20 μM Compound: 1, AC220	Cytotoxicity against human FLT3 negative U937 cells after 72 hrs by MTS assay Cytotoxicity against human FLT3 negative U937 cells after 72 hrs by MTS assay	[PMID: 23618709]

In Vitro

Quizartinib (0-10,000 nM; 48 h) dihydrochloride potently inhibits proliferation of leukemia cell lines dependent on FLT3^ITD, FIP1L1-PDGFRA, or select KIT mutations (V560G, N822K, D814Y) with IC₅₀ values ranging from <1 nM to 77 nM^[1].
Quizartinib (0-10,000 nM; 48 h) dihydrochloride potently inhibits proliferation and induces apoptosis in isogenic Ba/F3 cells expressing FLT3^WT, FLT3^ITD, FLT3^K663Q, FLT3^D835Y, KIT^WT, or KIT^D816Y with IC₅₀ values ranging from <1 nM to 474 nM^[1].
Quizartinib (0-1000 nM; 90 min) dihydrochloride selectively inhibits autophosphorylation of mutant KIT^D816Y, KIT and FLT3^ITD, FLT3^D835Y isoforms in isogenic Ba/F3 cells, while KIT^D816V and FLT3^D835V are largely resistant to dephosphorylation^[1].
Quizartinib (0-5000 nM; 48 h) dihydrochloride inhibits proliferation of native AML blasts with wild-type KIT, FLT3 amplification, or select FLT3 ITD mutations, while FLT3 ITD-beta1-positive blasts are insensitive^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	isogenic Ba/F3 cells stably transfected with mutant KIT (D816V, D816Y, D816F) or FLT3 (ITD, D835V, D835Y)
Concentration:	0, 10, 100, 1000 nM
Incubation Time:	90 min
Result:	Inhibited autophosphorylation of KIT^D816Y and KIT^D816F in the nanomolar range. Caused dephosphorylation of both glycosylated and intracellular isoforms of KIT^D816Y, while dephosphorylation of KIT^D816F was restricted to the glycosylated isoform. Showed no significant reduction in phosphorylation of KIT^D816V. Inhibited autophosphorylation of FLT3 ITD and FLT3^D835Y. Caused minimal inhibition of FLT3^D835V phosphorylation.

Molecular Weight

633.59

Formula

C₂₉H₃₄Cl₂N₆O₄S

CAS No.

1132827-21-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C2=CN3C(SC4=CC(OCCN5CCOCC5)=CC=C34)=N2)C=C1)NC6=NOC(C(C)(C)C)=C6.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (52.60 mM; ultrasonic and adjust pH to 12 with 1 M NaOH; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5783 mL	7.8915 mL	15.7831 mL
5 mM	0.3157 mL	1.5783 mL	3.1566 mL
10 mM	0.1578 mL	0.7892 mL	1.5783 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Purity & Documentation

Purity: 99.81%

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Data Sheet (274 KB) SDS (393 KB)

COA (245 KB) HNMR (284 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Kampa-Schittenhelm KM, et al. 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;12:19. Published 2013 Mar 7. [Content Brief]

[2]. Cortes J, et al. Quizartinib, an FLT3 inhibitor, as monotherapy in patients with relapsed or refractory acute myeloid leukaemia: an open-label, multicentre, single-arm, phase 2 trial. Lancet Oncol. 2018;19(7):889-903. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5783 mL	7.8915 mL	15.7831 mL	39.4577 mL
	5 mM	0.3157 mL	1.5783 mL	3.1566 mL	7.8915 mL
	10 mM	0.1578 mL	0.7892 mL	1.5783 mL	3.9458 mL
	15 mM	0.1052 mL	0.5261 mL	1.0522 mL	2.6305 mL
	20 mM	0.0789 mL	0.3946 mL	0.7892 mL	1.9729 mL
	25 mM	0.0631 mL	0.3157 mL	0.6313 mL	1.5783 mL
	30 mM	0.0526 mL	0.2631 mL	0.5261 mL	1.3153 mL
	40 mM	0.0395 mL	0.1973 mL	0.3946 mL	0.9864 mL
	50 mM	0.0316 mL	0.1578 mL	0.3157 mL	0.7892 mL

Quizartinib dihydrochloride Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Quizartinib dihydrochloride (Synonyms: AC220 dihydrochloride)

Customer Review

Other Forms of Quizartinib dihydrochloride:

Quizartinib dihydrochloride Related Antibodies

45 Publications Citing Use of MCE Quizartinib dihydrochloride

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View All PDGFR Isoform Specific Products:

Biological Activity

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References

Customer Review

Quizartinib dihydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Quizartinib dihydrochloride Related Classifications

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