| CAS NO: | 1334298-90-6 |
| 规格: | ≥98% |
| 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 |
| 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 |
| 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 Vivo | Itacitinib 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 model | Human pancreatic xenograft models in mice |
| Formulation & Dosage | N/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). |
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