| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A409099-1ml |
1ml |
现货  |
|
| 英文别名 | (S)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | AZ 960 |
| 生化机理 | AZ 960 是一种新型 ATP 竞争性 JAK2 抑制剂，其 IC50 和Ki分别为 <3 nM 和 0.45 nM，AZ960 对 JAK2 的选择性是 JAK3 的 3 倍。AZ 960 可诱导细胞凋亡和生长停滞。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | Janus 激酶 2 抑制剂 |
| 产品介绍 |
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。 Information AZ 960 is a novel ATP competitiveJAK2inhibitor withIC50andKiof <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. AZ 960 inducesapoptosisand growth arrest. 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. In vivo
cell lines： Concentrations：0.016-10 μM Incubation Time：48-72 hours Powder Purity:≥99% |
| Ki Data | JAK2, Ki: 0.45 nM |
|---|---|
| IC50 | JAK2, IC50: <3 nM |
| ALogP | 4.495 |
| hba_count | 2 |
| HBD Count | 3 |
| Rotatable Bond | 5 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC(NC1=NC(=C(F)C=C1C#N)NC2=N[NH]C(=C2)C)C3=CC=C(F)C=C3 |
| 分子量 | 354.36 |
| Reaxy-Rn | 27406339 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27406339&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 44 mg/mL (197.86 mM); |
|---|---|
| DMSO(mg / mL) Max Solubility | 71 |
| DMSO(mM) Max Solubility | 200.36 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 27406339 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27406339&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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