Gilteritinib hemifumarate NEW
| Price | $34 | $80 | $122 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Gilteritinib hemifumarate | CAS No.: 1254053-84-3 |
| Purity: 98.07% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Gilteritinib hemifumarate |
| Description | Gilteritinib hemifumarate (ASP2215 hemifumarate) is a potent ATP-competitive dual FLT3 (IC50: 0.29 nM) and AXL (IC50: 0.73 nM) inhibitor for the treatment of relapsed or refractory FLT3 mutant AML. |
| In vitro | 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. It is approximately 800-fold more potent for FLT3 inhibition than for c-KIT[1]. In addition, Gilteritinib inhibits the activity of eight out of 78 tested kinases by over 50% at concentrations of either 1 nM (FLT3, LTK, ALK, and AXL) or 5 nM (TRKA, ROS, RET, and MER). The IC50s are 0.29 nM for FLT3 and 0.73 nM for AXL. The antiproliferative activity of Gilteritinib is evaluated against MV4-11 and MOLM-13 cells, which endogenously express FLT3-ITD. After 5 days of treatment, Gilteritinib inhibits the growth of MV4-11 and MOLM-13 cells with mean IC50s of 0.92 nM (95% CI: 0.23-3.6 nM) and 2.9 nM (95% CI: 1.4-5.8 nM), respectively. Growth suppression of MV4-11 cells is accompanied by the inhibition of FLT3 phosphorylation. Relative to vehicle control cells, phosphorylated FLT3 levels are 57%, 8%, and 1% after 2 h of treatment with 0.1 nM, 1 nM, and 10 nM Gilteritinib, respectively. Additionally, doses as low as 0.1 nM or 1 nM result in the suppression of phosphorylated ERK, STAT5, and AKT, all downstream targets of FLT3 activation. To investigate the effects of Gilteritinib on AXL inhibition, MV4-11 cells expressing exogenous AXL are treated with Gilteritinib. At concentrations of 1 nM, 10 nM, and 100 nM for 4 h, Gilteritinib treatment decreases phosphorylated AXL levels by 38%, 29%, and 22%, respectively[2]. |
| In vivo | With oral administration of Gilteritinib (ASP2215) at 10 mg/kg for 4 days in MV4-11 xenografted mice, the concentration of Gilteritinib in tumors is more than 20-fold higher than that in plasma. Treatment with Gilteritinib for 28 days results in dose-dependent inhibition of MV4-11 tumor growth, inducing complete tumor regression at doses higher than 6 mg/kg. Additionally, Gilteritinib decreases tumor burden in the bone marrow and prolongs the survival of mice intravenously transplanted with MV4-11 cells[1]. |
| Storage | Shipping with blue ice. |
| Solubility Information | DMSO : 3 mg/mL (4.91 mM), Sonication is recommended. H2O : 1 mg/mL (1.64 mM), Sonication is recommended. |
| Keywords | ASP-2215 Hemifumarate | ASP2215 | ASP 2215 Hemifumarate | Gilteritinib Hemifumarate | ASP2215 Hemifumarate | Gilteritinib | ASP-2215 | ASP 2215 |
| Inhibitors Related | Gilteritinib | Fedratinib | Nintedanib | Sunitinib Malate | Sorafenib | Tandutinib | Pexidartinib | Sorafenib tosylate | Cabozantinib S-malate |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Approved Drug Library | Kinase Inhibitor Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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