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FLLL32 {[allProObj[0].p_purity_real_show]}

货号:A315345 同义名: JAK2 Inhibitor X

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

FLLL32 化学结构 CAS号:1226895-15-3
FLLL32 化学结构
CAS号:1226895-15-3
FLLL32 3D分子结构
CAS号:1226895-15-3
FLLL32 化学结构 CAS号:1226895-15-3
FLLL32 3D分子结构 CAS号:1226895-15-3
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FLLL32 纯度/质量文件 产品仅供科研

货号:A315345 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 JAK1 JAK2 JAK3 Tyk2 其他靶点 纯度
Decernotinib +++

JAK1, Ki: 11 nM

JAK1, IC50: 11 nM

+++

JAK2, Ki: 13 nM

++++

JAK3, Ki: 2.5 nM

+++

TYK2, Ki: 13 nM

99%+
ZM39923 HCl +

JAK1, pIC50: 4.4

+

JAK3, pIC50: 7.1

EGFR 97%
Cerdulatinib +++

JAK1, IC50: 12 nM

+++

JAK2, IC50: 6 nM

+++

JAK3, IC50: 8 nM

++++

TYK2, IC50: 0.5 nM

99%+
Momelotinib +++

JAK1, IC50: 11 nM

++

JAK2, IC50: 18 nM

+

JAK3, IC50: 155 nM

99%+
XL019 +

JAK1, IC50: 134.3 nM

++++

JAK2, IC50: 2.2 nM

+

JAK3, IC50: 214.2 nM

FLT3 99%+
Ruxolitinib +++

JAK1, IC50: 3.3 nM

++++

JAK2, IC50: 2.8 nM

98%
Tofacitinib +

JAK1, IC50: 112 nM

++

JAK2, IC50: 20 nM

++++

JAK3, IC50: 1 nM

98%
Ruxolitinib (S enantiomer) +++

JAK1, IC50: 3.3 nM

++++

JAK2, IC50: 2.8 nM

++

TYK2, IC50: 19 nM

98%
Filgotinib +++

JAK1, IC50: 10 nM

++

JAK2, IC50: 28 nM

+

JAK3, IC50: 810 nM

+

TYK2, IC50: 116 nM

99%
Baricitinib +++

JAK1, IC50: 5.9 nM

+++

JAK2, IC50: 5.7 nM

++

TYK2, IC50: 53 nM

99%
Gandotinib ++

JAK1, IC50: 19.8 nM

++++

JAK2, IC50: 0.288 nM

JAK2 (V617F), Ki: 0.245 nM

++

JAK3, IC50: 48.0 nM

++

TYK2, IC50: 44 nM

FLT3 99%+
Oclacitinib maleate +++

JAK1, IC50: 10nM

++

JAK2, IC50: 18nM

+

JAK3, IC50: 99nM

+

TYK2, IC50: 84nM

98+%
NVP-BSK805 2HCl ++

JAK1, IC50: 31.63 nM

++++

JAK2, IC50: ~0.5 nM

++

JAK3, IC50: 18.68 nM

+++

TYK2, IC50: 10.76 nM

99+%
Peficitinib 98%
Go6976 FLT3 99%+
AZD-1480 ++++

JAK2, IC50: 0.26 nM

99%+
Fedratinib +++

JAK2 (V617F), IC50: 3 nM

JAK2, IC50: 3 nM

FLT3,RET 99%+
WP1066 +

JAK2, IC50: 2.3 μM

98%
Curcumol 98%
AZ960 ++++

JAK2, Ki: 0.45 nM

JAK2, IC50: <3 nM

97%
GLPG0634 analog 99%+
CEP-33779 ++++

JAK2, IC50: 1.8 nM

99%+
FLLL32 +

JAK2, IC50: <5 μM

99%+
WHI-P154 +

JAK3, IC50: 1.8 μM

EGFR,Src,VEGFR 98%
BMS-911543 ++++

JAK2, IC50: 1.1 nM

+

JAK3, IC50: 75 nM

++

TYK2, IC50: 66 nM

98%
TG101209 +++

JAK2, IC50: 6 nM

+

JAK3, IC50: 169 nM

FLT3,RET 99%+
AT9283 ++++

JAK2, IC50: 1.2 nM

++++

JAK3, IC50: 1.1 nM

99%+
Pacritinib ++

JAK2 (V617F), IC50: 19 nM

JAK2, IC50: 23 nM

+

JAK3, IC50: 520 nM

++

TYK2, IC50: 50 nM

FLT3 97%
Tofacitinib citrate ++

JAK2, IC50: 20 nM

++++

JAK3, IC50: 1 nM

99%
FM-381 ++++

JAK3, IC50: 127 pM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

FLLL32 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]

FLLL32 动物研究

Dose Mice: 25 mg/kg, 50 mg/kg[2] (p.o.); 50 mg/kg[1] (i.p.); 15 mg/kg[3] (i.v.)
Administration p.o., i.p., i.v.

FLLL32 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.

FLLL32 实验方案

计算器
存储液制备 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

FLLL32 技术信息

CAS号1226895-15-3
分子式C28H32O6
分子量 464.55
别名 JAK2 Inhibitor X
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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
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