货号:A157761
同义名:
磷酸鲁索利替尼
/ INCB018424 phosphate; Ruxolitinib (phosphate)
Ruxolitinib phosphate is a potent and selective JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, > 130-fold selectivity for JAK1/2 versus JAK3.
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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, 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 |
95% | ||||||||||||||
Peficitinib | ✔ | 98% | |||||||||||||||||
Go6976 | ✔ | FLT3 | 99%+ | ||||||||||||||||
AZD-1480 |
++++
JAK2, IC50: 0.26 nM |
99%+ | |||||||||||||||||
Fedratinib |
+++
JAK2, IC50: 3 nM JAK2 (V617F), IC50: 3 nM |
FLT3,RET | 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 |
EGFR,VEGFR,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 |
FLT3,RET | 99%+ | |||||||||||||||
AT9283 |
++++
JAK2, IC50: 1.2 nM |
++++
JAK3, IC50: 1.1 nM |
99%+ | ||||||||||||||||
Pacritinib |
++
JAK2, IC50: 23 nM JAK2 (V617F), IC50: 19 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 | Ruxolitinib (INCB018424) specifically and potently inhibits signaling and proliferation mediated by JAK2V617F. It inhibits the growth of HEL cells with an EC50 of 186 nM, significantly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell systems, and inhibits proliferation of hematopoietic progenitor cells from primary MPN patient samples[1]. |
Animal study | At a dose of 180 mg/kg administered orally, Ruxolitinib reduces tumor burden in mice injected with JAK2V617F-expressing cells without inducing anemia or lymphopenia[1]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03616184 | Graft-versus-host-disease (GVH... 展开 >>D) 收起 << | Phase 2 | Recruiting | April 2024 | United States, Nebraska ... 展开 >> University of Nebraska Medical Center Recruiting Omaha, Nebraska, United States, 68198 Contact: Penny Nurse Coordinator, RN 402-559-4596 收起 << |
NCT03386214 | Myelofibroses | Phase 1 | Recruiting | March 31, 2021 | United States, Missouri ... 展开 >> Washington University School of Medicine Recruiting Saint Louis, Missouri, United States, 63110 Contact: Stephen Oh, M.D., Ph.D. 314-747-7960 stoh@wustl.edu Principal Investigator: Stephen Oh, M.D., Ph.D. Sub-Investigator: Amy Zhou, M.D. 收起 << |
NCT00674479 | Acute Myeloid Leukemia ... 展开 >> Acute Lymphocytic Leukemia Myelodysplastic Syndrome Chronic Myelogenous Leukemia 收起 << | Phase 2 | Completed | - | United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.37mL 2.47mL 1.24mL |
24.73mL 4.95mL 2.47mL |
CAS号 | 1092939-17-7 |
分子式 | C17H21N6O4P |
分子量 | 404.36 |
SMILES Code | N#CC[C@@H](N1N=CC(C2=C3C(NC=C3)=NC=N2)=C1)C4CCCC4.O=P(O)(O)O |
MDL No. | MFCD18452860 |
别名 | 磷酸鲁索利替尼 ;INCB018424 phosphate; Ruxolitinib (phosphate); INCB 018424 (phosphate); INC 424 (phosphate); INC424; INCB018424 |
运输 | 蓝冰 |
InChI Key | JFMWPOCYMYGEDM-XFULWGLBSA-N |
Pubchem ID | 25127112 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, 2-8°C |