吉列替尼|T4409|TargetMol

Gilteritinib
1254053-43-4

￥358 1mg 起订

￥519 2mg 起订

￥828 5mg 起订

上海更新日期：2024-09-23

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产品详情:

中文名称：: 吉列替尼

英文名称：: Gilteritinib

CAS号：: 1254053-43-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.74%

产品类别：: 抑制剂

货号：: T4409

Product Introduction

Bioactivity

Name	Gilteritinib
Description	Gilteritinib (ASP2215) is a FLT3 inhibitor (IC50=0.29 nM) and an AXL inhibitor (IC50=0.73 nM) with ATP-competitive, selective, and oral activity. Gilteritinib exhibits antitumor activity and can be used to treat FLT3 mutation-positive AML.
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
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)
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
In vitro	方法：人急性髓细胞白血病细胞 MV4-11 和 MOLM-13 用 Gilteritinib (0.01-100 nM) 处理 5 天，使用 CellTiter-Glo 检测细胞增殖。结果：Gilteritinib 抑制 MV4-11 和 MOLM-13 细胞的生长，平均 IC50 值分别为 0.92 nM 和 2.9 nM。[1] 方法：人急性髓细胞白血病细胞 Molm14 用 Gilteritinib (5-20 nM) 处理 1-24 h，使用 Western Blot 检测靶点蛋白表达水平。结果：当与 Molm14 细胞孵育 1 h 时，Gilteritinib 有效地抑制了 FLT3 及其下游信号通路的活性。但是到 24 h，尽管 FLT3 持续受到抑制，但 ERK 信号传导反弹，如 pERK 上调。[2]
In vivo	方法：为测试体内抗肿瘤活性，将 Gilteritinib (1-10 mg/kg) 口服给药给携带人急性髓细胞白血病肿瘤 MV4-11 的 Nude 小鼠，每天一次，持续二十八天。结果：在 1 mg/kg/天 (63%)和 3 mg/kg/天 (80%) 剂量下观察到 MV4-11 肿瘤的显着生长抑制。并且在 6 mg/kg/天 (93%) 和 10 mg/kg/天 (100%) 剂量下观察到肿瘤几乎完全消退。[1]
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 1 mg/mL Ethanol : 4 mg/mL (7.2 mM) H2O : Insoluble 10% DMSO+90% Saline : 0.2 mg/mL (0.36 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Keywords	FLT3 \| TAM Receptor \| CD135 \| Axl \| inhibit \| Gilteritinib \| Mer \| ASP-2215 \| Tyro3 \| Fms like tyrosine kinase 3 \| Cluster of differentiation antigen 135 \| ASP 2215 \| Inhibitor
Inhibitors Related	Sorafenib
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Kinase Inhibitor Library \| FDA-Approved Drug Library \| Membrane Protein-targeted Compound Library \| Tyrosine Kinase Inhibitor Library \| Anti-Cancer Drug Library

吉列替尼|||ASP2215|TargetMol

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