JAK2-IN-7,2593402-36-7

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JAK2-IN-7

CAS No. : 2593402-36-7

MCE 国际站：JAK2-IN-7

产品活性：JAK2-IN-7 是一种选择性 JAK2 抑制剂，对 JAK2，SET-2 和 Ba/F3^V617F 细胞的 IC₅₀ 为 3、11.7 和 41 nM。 JAK2-IN-7 的选择性是 JAK1, JAK3，FLT3 的 14 倍以上。JAK2-IN-7 刺激细胞周期停滞在 G0/G1 期，并诱导肿瘤细胞凋亡 (apoptosis)。抗肿瘤活性。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt  |  Apoptosis

作用靶点：JAK  |  FLT3  |  Apoptosis

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-JAK2^V617F 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.

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