Gilteritinib|1254053-43-4|(吉瑞替尼; 吉列替尼; ASP2215)-陌孚医药/Medlife

您当前的位置：

Gilteritinib (Synonyms: 吉瑞替尼; 吉列替尼; ASP2215)

目录号: PL02661 纯度: ≥99%

CAS No. :1254053-43-4

商品编号	规格	价格	会员价
PL02661-2mg	2mg	¥1285.00	请登录
PL02661-5mg	5mg	¥1607.00	请登录
PL02661-10mg	10mg	¥2571.00	请登录
PL02661-50mg	50mg	¥9000.00	请登录
PL02661-100mg	100mg	¥11411.00	请登录
PL02661-200mg	200mg	询价	询价
PL02661-500mg	500mg	询价	询价

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称	Gilteritinib
中文别名	Gilteritinib;Gilteritinib吉列替尼
英文名称	Gilteritinib
英文别名	Gilteritinib;6-Ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-2-pyrazinecarboxamide;ASP 2215;ASP2215;Xospata;6-Ethyl-3-((3-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-amino)-5-((tetrahydro-2H-pyran-4-yl)amino)pyrazine-2-carboxamide;66D92MGC8M;2-Pyrazinecarboxamide, 6-ethyl-3-((3-methoxy-4-(4-(4-methyl-1-piperazinyl)-1-piperidinyl)phenyl)amino)-5-((tetrahydro-2H-pyran-4-yl)amino)-;6-ethyl-3-[[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]amino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide;2-Pyrazinecar
Cas No.	1254053-43-4
分子式	C₂₉H₄₄N₈O₃
分子量	552.71
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情

Gilteritinib (ASP2215) 是一种有效的 ATP 竞争性的 FLT3/AXL 抑制剂，IC₅₀ 分别为 0.29 nM/0.73 nM。

生物活性

Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC 50 s of 0.29 nM/0.73 nM, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 0.29 nM (FLT3)
IC50: 0.35 nM (LTK), 0.73 nM (AXL), 1.2 nM (EML4-ALK), 230 nM (c-KIT)

体外研究(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. Gilteritinib inhibits the activity of eight of the 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. Gilteritinib inhibits FLT3 at an IC50 that is approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM). 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 wit

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. ASP2215, a novel FLT3/AXL inhibitor: Preclinical evaluation in acute myeloid leukemia (AML). 2014 ASCO Annual Meeting.
[2]. Mori M, et al. 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.

溶解度数据	In Vitro: Ethanol : 100 mg/mL (180.93 mM; ultrasonic and adjust pH to 2 with HCl)DMSO : 2 mg/mL (3.62 mM; Need ultrasonic)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation