Luxeptinib (Synonyms: CG-806)
目录号: PL03847 纯度: ≥99%
CAS No. :1616428-23-9
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中文名称
Luxeptinib
英文名称
Luxeptinib
英文别名
Luxeptinib;CG806;TQ6PBX1JU0;CG026806;Luxeptinib [USAN];US9758508, Compound 7;GTPL11671;BDBM340031;example 7 [US9758508B2];NSC791692;WHO 11799;D96116;1-[3-fluoro-4-[7-(5-methyl-1H-imidazol-2-yl)-1-oxo-2,3-dihydroisoindol-4-yl]phenyl]-3-(2,4,6-trifluorophenyl)urea;1-{3-fluoro-4-[7-(5-methyl-1H-imidazol-2- yl)-1-oxo-2,3-dihydro-1H-isoindol-4-yl]- phenyl}-3-(2,4,6-trifluoro-phenyl)-urea;3-{3-FLUORO-4-[7-(4-METHYL-1H-IMID
Cas No.
1616428-23-9
分子式
C25H17F4N5O2
分子量
495.43
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Luxeptinib (CG-806) 是一种具有口服活性、可逆的、一流的非共价的有效 pan-FLT3/pan-BTK 抑制剂。Luxeptinib 诱导急性髓系白血病细胞周期阻滞、凋亡或自噬。
生物活性
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.
性状
Solid
IC50 & Target[1][2]
Pan-FLT3/Pan-BTK
体外研究(In Vitro)
Luxeptinib (MEC-1 CLL cells; 0.1~10 μM; 72 hours) inhibits cells proliferation with an IC50 of 32 nM.
Luxeptinib inhibits BCR signaling-induced phosphorylation of BTK, PLCg2, AKT, ERK1/2, S6 ribosomal protein and strongly suppresses SYK phosphorylation in primary chronic lymphocytic leukemia (CLL) cells. Luxeptinib (MV4-11 cells; 500 pM; 1 hour) completely inhibits phosphorylation of FLT3 and STAT5. 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
ClinicalTrial
参考文献
[1]. Ekaterina Kim MS, et al. CG-806, a First-in-Class Pan-FLT3/Pan-BTK Inhibitor, Exhibits Broad Signaling Inhibition in Chronic Lymphocytic Leukemia Cells. bloodjournal Blood blood (2019). 134 (Supplement_1) : 3051.
[2]. Abstract 44: CG′806, a first-in-class FLT3/BTK inhibitor, exhibits potent activity against AML patient samples with mutant or wild type FLT3, as well as other hematologic malignancy subtypes
溶解度数据
In Vitro: DMSO : 50 mg/mL (100.92 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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