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Itacitinib(INCB-039110)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Itacitinib(INCB-039110)图片
CAS NO:1334298-90-6
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 553.51
Formula C26H23F4N9O
CAS No. 1334298-90-6 (free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: >90 mg/mL
Water: <1 mg/mL
Ethanol: >90 mg/mL
Chemical Name 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(1-(3-fluoro-2-(trifluoromethyl)isonicotinoyl) piperidin-4-yl)azetidin-3-yl)acetonitrile
Synonyms Itacitinib; INCB039110; INCB-039110; INCB 039110; INCB39110; INCB 39110; INCB-39110
SMILES Code N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(C5CCN(C(C6=C(F)C(C(F)(F)F)=NC=C6)=O)CC5)C1
实验参考方法
In Vitro

In vitro activity: Itacitinib (also known as INCB39110) is a potent, selective and orally bioavailable inhibitor of JAK1 (Janus-associated kinase 1) with>20-fold selectivity for JAK1 over JAK2 and>100-fold over JAK3 and TYK2 (IC50 for JAK1, 2, 3, and TYK2 are 2, 63,>2000, and 795 nM, respectively). It has potential antineoplastic activity and is currently in Phase II clinical trials for the treatment of myelofibrosis, rheumatoid arthritis and plaque psoriasis. Janus kinases (JAKs) are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling and are strongly linked to both cancer and inflammatory diseases.


Kinase Assay: Itacitinib has>20-fold selectivity for JAK1 over JAK2 and>100-fold over JAK3 and TYK2 (IC50 for JAK1, 2, 3, and TYK2 are 2, 63,>2000, and 795 nM, respectively).

In VivoItacitinib is able to inhibit tumor growth in human pancreatic xenograft models in mice at clinically relevant doses, both as monotherapy and in combination with cytotoxic agents such as gemcitabine.
Animal modelHuman pancreatic xenograft models in mice
Formulation & DosageN/A
References Haematologica. 2017 Feb;102(2):327-335; Expert Opin Ther Pat. 2017 Feb;27(2):127-143; AACR; Cancer Res. 2015, 75(15 Suppl).