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Gilteritinib

Catalog No. T4409 CAS 1254053-43-4

Synonyms: ASP2215

Gilteritinib (ASP2215) is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preClinicalal studies, gilteritinib showed strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 Clinicalal trials for acute myeloid leukemia.

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Gilteritinib, CAS 1254053-43-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 82.00
10 mg	In stock	$ 123.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 291.00
100 mg	In stock	$ 457.00
500 mg	In stock	$ 1,060.00
1 g	In stock	$ 1,430.00

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Purity: 99.74%

Purity: 99.72%

Purity: 99.68%

Purity: 99.32%

Purity: 97.75%

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Description	Gilteritinib (ASP2215) is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preClinicalal studies, gilteritinib showed strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 Clinicalal trials for acute myeloid leukemia.
Targets&IC50	FLT3:0.29 nM, c-Kit:230 nM, TYK1/LTK:0.35 nM, EML4-ALK:1.2 nM, Axl:0.73 nM
In vitro	Gilteritinib (ASP2215) has been tested against 78 tyrosine kinases, demonstrating strong inhibitory effects on FLT3, leukocyte tyrosine kinase (LTK), anaplastic lymphoma kinase (ALK), and AXL kinases, reducing their activity by over 50% at a concentration of 1 nM. Particularly, Gilteritinib exhibits an IC50 of 0.29 nM for FLT3, making it approximately 800 times more effective against FLT3 than against c-KIT, for which the IC50 is 230 nM. Furthermore, it significantly inhibits eight out of the tested kinases at concentrations up to 5 nM, including TRKA, ROS, RET, and MER, in addition to those previously mentioned. In cell-based assays, Gilteritinib effectively suppresses the growth of MV4-11 and MOLM-13 cells, which naturally express FLT3-ITD mutations, with mean IC50 values of 0.92 nM and 2.9 nM, respectively, upon 5-day treatment. This antiproliferative effect correlates with the reduction of FLT3 phosphorylation and the downstream inhibition of ERK, STAT5, and AKT phosphorylation. A study exploring its impact on AXL inhibition in MV4-11 cells that express exogenous AXL revealed dose-dependent decreases in phosphorylated AXL levels following 4 hours of treatment, highlighting Gilteritinib's potent inhibitory action on both FLT3 and AXL signaling pathways.
In vivo	In MV4-11 xenografted mice, administration of Gilteritinib (ASP2215) orally at 10 mg/kg for four days markedly elevates its tumor concentration, achieving levels over 20-fold higher than in plasma. A 28-day course of Gilteritinib treatment demonstrates dose-dependent suppression of MV4-11 tumor growth, with complete regression observed at dosages exceeding 6 mg/kg. Additionally, Gilteritinib significantly reduces tumor presence in the bone marrow and extends the survival of mice that have undergone intravenous transplant with MV4-11 cells.
Kinase Assay	The kinase inhibitory activity of Gilteritinib is tested against a panel of 78 tested kinases using ATP concentrations that are approximately equal to the Km value for each kinase in a TK-ELISA or off-chip mobility shift assay. Initially, two concentrations of Gilteritinib (1 nM and 5 nM) are tested to assess each compound's inhibitory effect on TK activity. Further studies are then conducted using a dose range of Gilteritinib to determine IC50 values for kinases in which activity is inhibited by >50% with 1 nM Gilteritinib as well as for c-KIT. TK-ELISA and MSA assays are used to conduct IC50 studies for FLT3, LTK, AXL, and c-KIT; the HTRF KinEASE-TK assay is performed to assess the IC50 value of echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK)
Cell Research	Gilteritinib is dissolved in DMSO and stored, and then diluted with appropriate media before use.The effect of Gilteritinib on MV4-11 and MOLM-13 cells is assessed using the CellTiter-Glo Luminescent Cell Viability Assay. Subsequent studies are conducted to examine the effect of Gilteritinib and Quizartinib on Ba/F3 cells expressing either FLT3-ITD, FLT3-D835Y, FLT3-ITD-D835Y, FLT3-ITD-F691 L, or FLT3-ITD-F691I. MV4-11 and MOLM-13 cells are treated with DMSO or increasing concentrations of Gilteritinib (0.01, 0.1, 1, 10, and 100 nM) for 5 days, and cell viability is measured using CellTiter-Glo
Animal Research	MiceAntitumor activity is evaluated in nude mice transplanted with MV4-11 AML cells. The pharmacokinetics in xenografted mice is also investigated. MV4-11 xenografted-mice are treated 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

Synonyms	ASP2215
Molecular Weight	552.71
Formula	C29H44N8O3
CAS No.	1254053-43-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 2 mg/mL

Ethanol: 4 mg/mL(7.2 mM)

H2O: Insoluble

References and Literature

1. Mori M,etal.Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia.Invest New Drugs. 2017 Oct;35(5):556-565. 2. Lee LY,etal.PreClinicalal studies of gilteritinib, a next-generation FLT3 inhibitor.Blood. 2017 Jan 12;129(2):257-260.

Citations

1. Zhang Y, Wang P, Wang Y, et al.Sitravatinib as a potent FLT3 inhibitor can overcome gilteritinib resistance in acute myeloid leukemia.Biomarker Research.2023, 11(1): 1-16. 2. Huang F, Liang J, Lin Y, et al.Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis.Communications Biology.2023, 6(1): 972.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Kinase Inhibitor Library FDA-Approved Kinase Inhibitor Library EMA Approved Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library

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Keywords

Gilteritinib 1254053-43-4 Angiogenesis Tyrosine Kinase/Adaptors c-Kit TAM Receptor FLT FLT3 CD135 Axl inhibit Mer ASP-2215 Tyro3 Fms like tyrosine kinase 3 Cluster of differentiation antigen 135 ASP 2215 ASP2215 Inhibitor inhibitor

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