Ruxolitinib (INCB018424)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ruxolitinib dihydrochloride是一种特异性的Janus相关激酶（JAK1和JAK2）小分子抑制剂，其分子式为C17H21N6O4P，分子量为404。Ruxolitinib phosphate是ATP竞争性的环戊基丙腈衍生物，抑制JAK1和JAK2。Ruxolitinib抑制JAK1/2，STAT5和ERK1 / 2的磷酸化，从而减少细胞增殖。
参考文献：
Ruxolitinib inhibits transforming JAK2 fusion proteins in vitro and induces complete cytogenetic remission in t (8; 9)(p22; p24)/PCM1-JAK2–positive chronic.
E Lierman, D Selleslag, S Smits, J Billiet. Blood. 20122. Ruxolitinib for the treatment of myelofibrosis. A Ostojic, R Vrhovac, S Verstovsek. Ther Clin Risk Manag. 2011
- 1. Lin Du, YolandaWong Ying Yip, et al. "Ruxolitinib Alleviates Uveitis Caused by Salmonella typhimurium Endotoxin." Microorganisms. 2021 Jul 11;9(7):1481. PMID:34361917
- 2. Jinqiang Zhang, Hui He, et al. "Priming of microglia with IFN ‐γ impairs adult hippocampal neurogenesis and leads to depression‐like behaviors and cognitive defects." Glia. 2020 Dec;68(12):2674-2692. PMID:32652855
- 3. Gibbs KD, Washington EJ, et al. "The Salmonella Secreted Effector SarA/SteE Mimics Cytokine Receptor Signaling to Activate STAT3." Cell Host Microbe. 2020 Jan 8;27(1):129-139.e4. PMID:31901521
- 4. Li L, Shang L, et al. "Janus kinase inhibitor ruxolitinib blocks thymic regeneration after acute thymus injury." Biochem Pharmacol. 2019 Nov 11:113712. PMID:31726048
- 5. Hermans MAW, Schrijver B, et al. "The JAK1/JAK2- inhibitor ruxolitinib inhibits mast cell degranulation and cytokine release." Clin Exp Allergy. 2018 Jun 25. PMID:29939445
- 6. Zhang S, Li Z, et al. "Interleukin-4 Enhances the Sensitivity of Human Monocytes to Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Through Upregulation of Death Receptor 4." J Interferon Cytokine Res. 2018 Apr;38(4):186-194. PMID:29638207
- 7. Hall BM, Balan V, et al. "p16(Ink4a) and senescence-associated β-galactosidase can be induced in macrophages as part of a reversible response to physiological stimuli." Aging (Albany NY). 2017 Aug 2;9(8):1867-1884. PMID:28768895
- 8. Radhakrishnan H, Ilm K, et al. "MACC1 regulates Fas mediated apoptosis through STAT1/3-Mcl-1 signaling in solid cancers." Cancer Lett. 2017 Jun 23. pii: S0304-3835(17)30402-0. PMID:28649004
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 306.37 |
| Cas No. | 941678-49-5 |
| Formula | C17H18N6 |
| Synonyms | Ruxolitinib, INCB018424, INCB-018424 |
| Solubility | insoluble in H2O; ≥15.32 mg/mL in DMSO; ≥17.53 mg/mL in EtOH |
| Chemical Name | (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile |
| SDF | Download SDF |
| Canonical SMILES | C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
PV患者或正常对照者体内分离的原代单核细胞 |
|
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
IC50：红系祖细胞：正常捐献者 407 nM，PV捐献者 223 nM。 髓系祖细胞：正常捐献者 511 nM，PV捐献者 444 nM。时间：14天 |
|
应用 |
在逐渐增加浓度的INCB018424存在时，红系（BFU-E）和骨髓来源（CFU-M）克隆祖细胞的生长用集落形成实验进行评估。INCB018424剂量依赖地抑制红系和髓系祖细胞的生长，其对正常捐献者和PV患者来源的红系祖细胞的平均IC50值分别为407 nM和223 nM。而对对照和PV样品来源的髓系祖细胞（CFU-M）的IC50值分别为511 nM和444 nM。 |
| 动物实验[2]： | |
|
动物模型 |
C57BL/6N小鼠 |
|
剂量 |
75 mg/kg；口服给药 |
|
应用 |
小鼠在注射OVA/CpG之前或之后6 h口服给药75 mg/kg的ruxolitinib或对照，并分析CD11c 1CD81脾DCs活化标志物的表达水平。在ruxolitinib治疗小鼠中，CD40、CD80、CD86以及MHC I和II分子的表达水平均降低。小鼠在注射OVA/CpG和转入CFSE标记的OT-I细胞之前6小时或之后6小时和18小时口服给药ruxolitinib或对照，在ruxolitinib预处理小鼠中，对转入的CFSE标记OT-I细胞的分析表明，ruxolitinib减少细胞增殖、CD25的表达以及IFN的产生。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Quintás-Cardama A, Vaddi K, Liu P, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15): 3109-3117. [2] Heine A, Held S A E, Daecke S N, et al. The JAK-inhibitor ruxolitinib impairs dendritic cell function in vitro and in vivo. Blood, 2013, 122(7): 1192-1202. |
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| 描述 | Ruxolitinib (INCB018424)是第一个用于临床的、有效的和选择性的JAK1/2抑制剂，IC50值为3.3 nM/2.8 nM，比对JAK3的选择性高130多倍。 | |||||
| 靶点 | JAK1 | JAK2 | ||||
| IC50 | 3.3 nM | 2.8 nM | ||||
质量控制和MSDS
- 批次:
化学结构
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