1226895-15-3|FLLL32|CsnPharm

CAS No.: 1226895-15-3

FLLL32 Catalog No. CSN18801

Synonyms: JAK2 Inhibitor X

FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of < 5 μM.

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实验方案

技术信息

生物活性

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]
动物研究
剂量
Mice: 25 mg/kg, 50 mg/kg^[2] (p.o.); 50 mg/kg^[1] (i.p.); 15 mg/kg^[3] (i.v.)

给药途径
p.o., i.p., i.v.
参考文献

动物研究
剂量	Mice: 25 mg/kg, 50 mg/kg^[2] (p.o.); 50 mg/kg^[1] (i.p.); 15 mg/kg^[3] (i.v.)
给药途径	p.o., i.p., i.v.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1526 mL
- 10.7631 mL
- 21.5262 mL
- 5 mM
- 0.4305 mL
- 2.1526 mL
- 4.3052 mL
- 10 mM
- 0.2153 mL
- 1.0763 mL
- 2.1526 mL

技术信息

CAS号

1226895-15-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H32O6

运输

蓝冰

分子量

464.55

别名

JAK2 Inhibitor X

溶解度

DMSO	91.0 mg/mL (195.9 mM)
Water	Insoluble
Ethanol	25.0 mg/mL (53.8 mM) warming

动物实验配方

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