TL02-59|1315330-17-6|-陌孚医药/Medlife

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TL02-59

目录号: PL02119 纯度: ≥99%

CAS No. :1315330-17-6

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中文名称	TL02-59
英文名称	TL02-59
英文别名	3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methylbenzamide;3-((6,7-Dimethoxyquinazolin-4-yl)oxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide;3-(6,7-dimethoxyquinazolin-4-yl)oxy-N-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-4-methylbenzamide;3-(6,7-Dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-;3-(6,7-Dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-;3-(6,7-Dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide;3-(6,7-dimethoxyquinazolin-4-yl)oxy-N-[4-[(4-ethylpiperazin-1-;TL02-59
Cas No.	1315330-17-6
分子式	C₃₂H₃₄F₃N₅O₄
分子量	609.64
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TL02-59 是一种具有口服活性，选择性的 Src-家族激酶 Fgr 抑制剂，IC₅₀ 为 0.03 nM。TL02-59 抑制 Src-家族激酶 Lyn 和 Hck，IC₅₀ 分别为 0.1 nM 和 160 nM。TL02-59 有效抑制急性髓性白血病 (AML) 细胞生长。
生物活性	TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC 50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC 50 s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth.
性状	Solid
IC50 & Target[1][2]	IC50: 0.03 nM (Fgr), 0.1 nM (Lyn) and 160 nM (Hck)
体外研究(In Vitro)	TL02-59 (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation in TF-1 cells, with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range. TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. TL02-59 induces growth arrest in primary AML bone marrow samples. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	TL02-59 (oral administration; 1 and 10 mg/kg; for three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement. TL02-59 has a t 1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively. 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	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Weir MC, et al. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 Jun 15;13(6):1551-1559.

溶解度数据	In Vitro: DMSO : 125 mg/mL (205.04 mM; Need ultrasonic)配制储备液

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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。

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