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AZ 960
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产品介绍
产品介绍
产品信息
抗原名称
JAK2,JAK2
商品描述
AZ 960是一种新型的，ATP竞争性的JAK2抑制剂，IC50和Ki分别低于3 nM和0.45 nM，作用于JAK2比作用于JAK3选择性高3倍。AZ 960抑制JAK2酶活性，Ki为0.45 nM，IC50<3 nM。此外, 0.1 μM AZ960也抑制 83 种激酶中的31种，如 JAK3(IC50为9 nM), TrkA, Aurora, 和 ARK5。AZ 960作用于TEL-JAK2细胞，抑制STAT5磷酸化，平均IC50为15 nM，作用于 TEL-JAK2驱动的STAT5磷酸化比作用于其他 JAK 激酶家族成员(TEL-JAK1, -JAK3, 和 -TYK2)驱动的细胞系选择性高15到30倍。
分子量
354.36
纯度
98%
可溶性
Ethanol ：3 mg/mL (8.46 mM)
DMSO ：66 mg/mL (186.3 mM)
DMSO ：66 mg/mL (186.3 mM)
In vitro(体外研究)
AZ960 also inhibits many kinases less than 50% at a concentration of 0.1 μM such as JAK3 (IC50=9 nM), TrkA, Aurora, and ARK5. In cells, AZ 960 inhibits the phosphorylation of STAT5 in TEL-JAK2 cells with an average IC50 of 15 nM and exhibits 15-30 -fold sensitivity for TEL-JAK2-driven STAT5 phosphorylation compared with cell lines driven by other JAK kinase family members (TEL-JAK1, -JAK3, and -TYK2). AZ 960 shows potent activity in inhibiting the proliferation of the TEL-JAK2, -JAK1, -JAK3, and -Tyk2 cell lines with GI50 values of 25 nM, 230 nM, 279 nM, and 214 nM, respectively. Moreover, AZ 960 also potently inhibits SET-2 cell proliferation with an average GI50 of 33 nM by reducing both STAT3 and STAT5 phosphorylation levels. AZ 960 causes growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1pe 1, HTLV-1LV-1osis of human T-cSET-2 cell proliferation witBcl-xL by small interfering RNA potentiates anti-proliferative effects of AZ 960 in MT-1 cells. A recent study shows that AZ 960 leads to significant inhibition of the clonogenic growth and induction of apoptosis of freshly isolated AML cells from patients.
背景
别名
AZ-960
分子式
C18H16F2N6
CAS号
905586-69-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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