SML3784
AZ960
≥98% (HPLC)
别名:
(S)-5-Fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile, 5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile, AZ 960, AZ-960
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
Fc1c(nc(c(c1)C#N)N[C@@H](C)c3ccc(cc3)F)Nc2[nH]nc(c2)C
InChI
1S/C18H16F2N6/c1-10-7-16(26-25-10)23-18-15(20)8-13(9-21)17(24-18)22-11(2)12-3-5-14(19)6-4-12/h3-8,11H,1-2H3,(H3,22,23,24,25,26)/t11-/m0/s1
InChI key
SUNXHXDJOIXABJ-NSHDSACASA-N
相关类别
生化/生理作用
ATP-competitive, potent and selective Janus-associated kinase 2 (JAK2) inhibitor.
AZ960 is an ATP-competitive, potent and selective Janus-associated kinase 2 inhibitor (JAK2 Ki = 0.45 nM with 15 μM ATP, 96% inhibition at 10 nM) with additional lower potency against TrkA/Aurora-A/ARK5 (91/73/65% inhibition at 10 nM; IC50 >100 nM against 72 other kinases). AZ960 exhibits JAK2-selective anti-proliferation potency (GI50 = 25, 214, 230, 279 nM using cells expression TEL-JAK2, -Tyk2, -JAK1, -JAK3, respectively) and inhibits cellular STAT5 phosphorylation in TEL-JAK2-expressing cells (IC50 = 15 nM) at a 15–30-fold potency than the TEL-JAK1, -JAK3, and -Tyk2 transfectants.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
Identifying a confused cell identity for esophageal squamous cell carcinoma
Signal transduction and targeted therapy, 7(1), 122-122 (2022)
AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells
Molecular Cancer Therapeutics, 9(12), 3386-3395 (2010)
Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor
Bioorganic & Medicinal Chemistry, 24(19), 4647-4651 (2016)
Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2
The Journal of Biological Chemistry, 283(47), 32334-32343 (2008)
FAT10 stimulates the development of osteosarcoma by regulating the JAK/STAT signaling pathway
Journal of B.U.ON. : Official Journal of the Balkan Union of Oncology, 26(5), 2090-2096 (2021)
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