AZ960是高效选择性的JAK2激酶抑制剂,Ki值为0.45 nM。 应用: 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 可诱导凋亡和生长阻滞。对其它JAKs家族成员,例如 JAK1、JAK3和TYK2以及其它激酶,包括TrkA、Aurora A和FAK的抑制作用较小,IC50大约为0.1 μmol/L。最近的研究表明AZ960对成人T细胞白血病(ATL),CD4+ T淋巴细胞侵略性恶性肿瘤具有一定的抗癌活性,主要是通过诱导人类T细胞嗜淋巴细胞病毒1型(HTLV-1)感染的T细胞的生长停滞和细胞凋亡发挥作用。
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AZ 960
CAS number:905586-69-8 molecular formula:C18H16F2N6
overview
compound introduction
Specs
| Chinese alias | 5-氟-2-[[(1S)-1-(4-氟苯基)乙基]氨基]-6-[(5-甲基-1H-吡唑-3-基)氨基]-3-吡啶腈,AZ-960,AZ960) | ||
| English alias | (S)-5-fluoro-2-((1-(4-fluorophenyl)ethyl)amino)-6-((5-methyl-1H-pyrazol-3-yl)amino)nicotinonitrile | NCGC00346581-01 | AZ 960;AZ960 | (S)-5-Fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile | 3-(3-(((Dimethylamino)me | ||
| CAS number | 905586-69-8 | molecular formula | C18H16F2N6 |
| molecular weight | 354.36 g/mol | Exact mass | - |
| PSA | 89.400 Ų | logp | 4.400 |
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