JAK2-IN-7

Research use only, not for human use.

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.

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.(In Vitro):JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2V617F cells.JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase.JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells.(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.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.

JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2V617F cells.JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase.JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells. Cell Cycle Analysis Cell Line:SET-2 cells Concentration:10-160 nM Incubation Time:24 hours Result:Induced cell arrest in the G0/G1 phase in a concentration-dependent manner.Apoptosis Analysis Cell Line:SET-2 cells Concentration:0.05-1.6 μM Incubation Time:2 hours Result:Induced apoptosis in SET-2 cells.

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.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. Animal Model:SET-2 cell-inoculated xenograft NOD/SCID mouse model 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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Angiogenesis

JAK

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2593402-36-7

459.59

C26H33N7O

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (543.96 mM)

CC(C)n1ncc(-c2c(C)cnc(Nc3cc(CCN(C4)C(/C=C/CN(C)C)=O)c4cc3)n2)c1

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(-20℃)

With Ice Pack

≥ 2 years