| Identification | Back Directory | [Name]
JAK2-IN-7 | [CAS]
2593402-36-7 | [Synonyms]
JAK2-IN-7
JAK2IN7,JAK-2-IN-7,JAK2 IN 7
(E)-4-(dimethylamino)-1-(6-(4-(1-isopropyl-1H-pyrazol-4-yl)-5-methylpyrimidin-2-ylamino)-3,4-dihydroisoquinolin-2(1H)-yl)but-2-en-1-one | [Molecular Formula]
C26H33N7O | [MOL File]
2593402-36-7.mol | [Molecular Weight]
459.6 |
| Hazard Information | Back Directory | [Uses]
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities[1]. | [in vivo]
JAK2-IN-7 (15-60 mg/kg; p.o.; daily for 16 days) shows potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model[1].
JAK2-IN-7 (30-60 mg/kg; p.o.; q.d. for 16 day) significantly ameliorates the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib[1]. | Animal Model: | SET-2 cell-inoculated xenograft NOD/SCID mouse model[1] | | Dosage: | 15, 30, and 60 mg/kg | | Administration: | Orally daily for 16 days | | Result: | Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.
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| [IC 50]
JAK1: 42 nM (IC50); JAK2: 3 nM (IC50); JAK3: 94 nM (IC50); Tyk2: 75 nM (IC50); FLT3: 62 nM (IC50) | [References]
[1] Yang T, et al. N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms [published online ahead of print, 2020 Nov 30]. J Med Chem. 2020;10.1021/acs.jmedchem.0c01488. DOI:10.1021/acs.jmedchem.0c01488 |
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