货号:A1677663 同义名: Ndi-034858;TAK-279
Zasocitinib是一种高选择性Tyk2抑制剂,靶向Tyk2的JH2结构域,具有强效的抗炎和抗肿瘤活性,适用于免疫和癌症研究。
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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 |
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 |
Src,EGFR,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。 |
描述 | Zasocitinib (NDI-034858) is an inhibitor of TYK2, targeting the TYK2 JH2 domain with a binding constant Kd of <200 pM[1]. |
体外研究 | Zasocitinib, at a concentration of 10 μM, inhibits Tyk2 and JAK by targeting the Tyk2 JH1 and JAK JH1 domains, respectively, with inhibition rates of <50%[1]. Zasocitinib inhibits the induction of phosphorylation in the heterodimer complex Tyk2/JAK2-mediated IL-12 (1.7 ng/mL) effect, with an IC50 value of <0.1 μM in human peripheral blood mononuclear cells[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.86mL 2.17mL 1.09mL |
21.72mL 4.34mL 2.17mL |
CAS号 | 2272904-53-5 |
分子式 | C23H24N8O3 |
分子量 | 460.488 |
别名 | Ndi-034858;TAK-279 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 50 mg/mL(108.58 mM),配合低频超声,并水浴加热至45℃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 |