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FLLL32

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Chemical Structure| 1226895-15-3 同义名 : JAK2 Inhibitor X
CAS号 : 1226895-15-3
货号 : A315345
分子式 : C28H32O6
纯度 : 99%+
分子量 : 464.55
MDL号 : MFCD27976793
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(226.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • JAK2

    JAK2, IC50:<5 μM
描述 FLLL32 is a STAT3 inhibitor and also inhibits JAK2 kinase activity. FLLL32 inhibited STAT3 phosphorylation at 5μM, DNA-binding activity at 10μM, and transactivation at 5 or 10μMin vitro, leading to the impediment of multiple oncogenic processes and the induction of apoptosis in pancreatic and breast cancer cell lines. It also inhibited colony formation in soft agar and cell invasion and exhibit synergy with the anticancer drug doxorubicin against breast cancer cells. Administration of 50mg/kg FLLL32, i.p., daily, reduced tumor growth in mouse xenograft MDA-MB-231 breast cancer cells[2].
作用机制 FLLL32 selectively binds to Janus kinase 2 and the STAT3 Src homology-2 domain, which serve crucial roles in STAT3 dimerization and signal transduction.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.53mL

4.31mL

2.15mL
参考文献

[1]Lin L, Hutzen B, et al. Novel STAT3 phosphorylation inhibitors exhibit potent growth-suppressive activity in pancreatic and breast cancer cells. Cancer Res. 2010 Mar 15;70(6):2445-54.

[2]Lin L, Hutzen B, Zuo M, Ball S, Deangelis S, Foust E, Pandit B, Ihnat MA, Shenoy SS, Kulp S, Li PK, Li C, Fuchs J, Lin J. Novel STAT3 phosphorylation inhibitors exhibit potent growth-suppressive activity in pancreatic and breast cancer cells. Cancer Res. 2010 Mar 15;70(6):2445-54. doi: 10.1158/0008-5472.CAN-09-2468. Epub 2010 Mar 9. PMID: 20215512; PMCID: PMC2843552.