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产品名称 | JAK1 ↓ ↑ | JAK2 ↓ ↑ | JAK3 ↓ ↑ | Tyk2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Decernotinib |
+++
JAK1, IC50: 11 nM JAK1, Ki: 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 (V617F), Ki: 0.245 nM JAK2, IC50: 0.288 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 |
RET,FLT3 | 99%+ | ||||||||||||||||
WP1066 |
+
JAK2, IC50: 2.3 μM |
98% | |||||||||||||||||
Curcumol | ✔ | 98% | |||||||||||||||||
AZ960 |
++++
JAK2, IC50: <3 nM JAK2, Ki: 0.45 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 |
VEGFR,EGFR,Src | 98% | ||||||||||||||||
BMS-911543 |
++++
JAK2, IC50: 1.1 nM |
+
JAK3, IC50: 75 nM |
++
TYK2, IC50: 66 nM |
95% | |||||||||||||||
TG101209 |
+++
JAK2, IC50: 6 nM |
+
JAK3, IC50: 169 nM |
RET,FLT3 | 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。 |
靶点 |
|
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] |
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. |
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 |
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 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,2-8°C |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |