Gilteritinib hemifumarate

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
250mg	$850	Check With Us
500mg	$1180	Check With Us
1g	$1770	Check With Us

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Cat #: V3135 CAS #: 1254053-84-3 Purity ≥ 99%

Description: Gilteritinib hemifumarate (ASP2215; ASP-2215 hemifumarate; Xospata), the hemifumarate salt of Gilteritinib (ASP2215), is a marketed anti-AML drug acting as a dual inhibitor of FLT3/AXL with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL respectively.

References: ASP2215, a novel FLT3/AXL inhibitor: Preclinical evaluation in acute myeloid leukemia (AML). 2014 ASCO Annual Meeting.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	610.75
Molecular Formula	C29H44N8O3 ₀.₅C₄H₄O₄
CAS No.	1254053-84-3
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 2 mg/mLr
	Water: N/Ar
	Ethanol: N/A
SMILES Code	OC(/C=C/C(O)=O)=O.NC(C1=NC(CC)=C(NC2CCOCC2)N=C1NC3=CC(OC)=C(N4CCC(N5CCN(C)CC5)CC4)C=C3)=O.[0.5]
Synonyms	ASP2215 hemifumarate; ASP-2215 hemifumarate; ASP 2215 hemifumarate; Gilteritinib hemifumarate; Trade name: Xospata

Protocol	In Vitro	Of the 78 tyrosine kinases tested, Gilteritinib (ASP2215) inhibits FLT3, leukocyte tyrosine kinase (LTK), anaplastic lymphoma kinase (ALK), and AXL kinases by over 50% at 1 nM with an IC50 value of 0.29 nM for FLT3, approximately 800-fold more potent than for c-KIT.
Protocol	In Vivo	In MV4-11 xenografted-mice, the concentration of Gilteritinib (ASP2215) in tumors is more than 20-fold higher than that in plasma with oral administration of Gilteritinib at 10 mg/kg for 4 days. Treatment of Gilteritinib for 28 days results in dose-dependent inhibition of MV4-11 tumor growth and induces complete tumor regression at more than 6 mg/kg. Further, Gilteritinib decreases tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.6373 mL	8.1867 mL	16.3733 mL	32.7466 mL
5mM	0.3275 mL	1.6373 mL	3.2747 mL	6.5493 mL
10mM	0.1637 mL	0.8187 mL	1.6373 mL	3.2747 mL
20mM	0.0819 mL	0.4093 mL	0.8187 mL	1.6373 mL

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.