FT113
目录号: PL14889 纯度: ≥99%
CAS No. :1630808-89-7
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中文名称
FT113
英文名称
FT113
英文别名
FT113;BCP31017;BCP30637;ZB1585;s6666;(4-(4-(6-fluorobenzo[d]oxazol-2-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone;[4-(6-Fluoro-1,3-benzoxazol-2-yl)phenyl]-[4-(1-hydroxycyclopropanecarbonyl)piperazin-1-yl]methanone
Cas No.
1630808-89-7
分子式
C22H20FN3O4
分子量
409.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
FT113 是一种有效、可口服的脂肪酸合酶 (fatty acid synthase (FASN)) 抑制剂,对全长重组人 FASN 酶的 IC50 值为 213 nM。在 BT474 细胞中,FT113 抑制 FASN 的活性,IC50 值为 90 nM。FT113 具有抗增殖作用,在体内和体外实验中,都具有抗癌作用。
生物活性
FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC 50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC 50 , 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo.
性状
Solid
IC50 & Target[1][2]
IC50: 213 nM (FASN), 90 nM (FASN, in BT474 cell)
体外研究(In Vitro)
FT113 shows anti-proliferative activity against PC3 and MV-411 cells with IC50s of 47 and 26 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
FT113 (5 mg/kg, p.o.) exhibits potent oral bioavailability of 95% and 84% in mice and rats, respectively.
FT113 (5, 25, or 50 mg/kg, p.o., twice daily for 16 days) increases malonyl-CoA concentration in tumors, inhibits tumor growth in a dose-dependent manner in mice. 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]. Martin MW, et al. Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN). Bioorg Med Chem Lett. 2019 Apr 15;29(8):1001-1006.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (152.66 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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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