Molecular Formula | C18H16F2N6 |
Molar Mass | 354.36 |
Density | 1.37±0.1 g/cm3(Predicted) |
Boling Point | 515.2±50.0 °C(Predicted) |
pKa | 13.42±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | AZ 960 inhibited JAK2 enzyme activity with K I at 0.45 nM and IC50<3 nM. In addition, 0.1 μm AZ960 also inhibited 31 of 83 kinases, such as JAK3(IC50 of 9 nM), TrkA, Aurora, and ark5. AZ 960 inhibits STAT5 phosphorylation in TEL-JAK2 cells with an average IC50 of 15 nM, and acts on TEL-JAK2-driven STAT5 phosphorylation than on other JAK kinase family members (TEL-JAK1, -JAK3, and-TYK2) driven Cell Line selectivity is 15 to 30 fold higher. AZ 960 potently inhibited TEL-JAK2, -JAK1, -JAK3, and-Tyk2 cell proliferation with GI50 of 25 nM, 230 nM, 279 nM, and 214 nM, respectively. And, AZ 960 also effectively inhibited SET-2 cell proliferation by reducing STAT3 and STAT5 phosphorylation levels, with an average GI50 of 33 nM. AZ 960 causes growth arrest and apoptosis of human T-cell lymphotropic Virus type 1 (HTLV-1) infected T cells (MT-1 and MT-2), and the anti-proliferative effect of AZ 960 on MT-1 cells was enhanced by small interfering RNA, while the inhibition was Bcl-xL. Recent studies have shown that AZ 960 significantly inhibits the clonal growth of newly isolated AML cells from patients and induces apoptosis. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.822 ml | 14.11 ml | 28.22 ml |
5 mM | 0.564 ml | 2.822 ml | 5.644 ml |
10 mM | 0.282 ml | 1.411 ml | 2.822 ml |
5 mM | 0.056 ml | 0.282 ml | 0.564 ml |
biological activity | AZ 960 is a new type of ATP competitive JAK2 inhibitor. IC50 and Ki are lower than 3 nM and 0.45 nM respectively, and the selectivity of JAK2 is 3 times higher than that of JAK3. AZ 960 can induce apoptosis and growth arrest. |
target | TargetValue JAK2 0.45 nM(Ki) JAK2 <3 nM |
Target | Value |
JAK2 | 0.45 nM(Ki) <3 nM |
in vitro study | AZ 960 inhibits JAK2 enzyme activity, K I is 0.45 nM,IC50<3 nM. In addition, 0.1 μM AZ960 also inhibits 31 of 83 kinases, such as JAK3(IC50 is 9 nM), TrkA, Aurora, and ARK5. AZ 960 acts on TEL-JAK2 cells and inhibits STAT5 phosphorylation with an average IC50 of 15 nM. TEL-JAK2-driven STAT5 phosphorylation is 15 to 30 times more selective than cell lines driven by other JAK kinase family members (TEL-JAK1, -JAK3, and-TYK2). AZ 960 effectively inhibited TEL-JAK2, -JAK1, -JAK3, and-Tyk2 cell proliferation with GI50 of 25 nM, 230 nM, 279 nM, and 214 nM, respectively. Moreover, AZ 960 also effectively inhibited SET-2 cell proliferation by reducing STAT3 and STAT5 phosphorylation levels, with an average GI50 of 33 nM. AZ 960 causes growth arrest and apoptosis of T cells (MT-1 and MT-2) infected by human T-cell lymphoid lymphocyte virus type 1 (HTLV-1), and enhances the anti-proliferation effect of AZ 960 on MT-1 cells through small interfering RNA, thus inhibiting Bcl-xL. The latest research shows that AZ 960 significantly inhibits the clonal growth of newly isolated AML cells and induces apoptosis. |