| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A409020-1ml |
1ml |
现货  |
|
| 英文别名 | 1-cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)urea |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | AT9283 |
| 生化机理 | AT9283 是一种强效的 JAK2/3 抑制剂，在无细胞实验中的 IC50 为 1.2 nM/1.1 nM；对 Aurora A/B、Abl1(T315I) 也有效。第二阶段 |
| 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 | 酪氨酸蛋白激酶 JAK3 抑制剂 |
| 产品介绍 |
AT9283是多靶点抑制剂，对Bcr-Abl(T3151)，Jak2，Jak3，aurora A和B的IC50分别为4，1.2，1.1，3 nM和3 nM。 Information AT9283 is a potentJAK2/3inhibitor withIC50of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2. AT9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC50 of 30 nM. Furthermore, AT9283 also produces the potent inhibition on HCT116 colony formation. In vivo In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, AT9283 also exhibits a significantly longer half-life in tumors(2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice (Fp.o. = 24%). cell lines： Concentrations：1 nM - 10 μM Incubation Time：72 hours Powder Purity:≥99% |
| ALogP | 0.5 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1CC1NC(=O)NC2=C(NN=C2)C3=NC4=C(N3)C=C(C=C4)CN5CCOCC5 |
| 分子量 | 381.43 |
| Reaxy-Rn | 36407987 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=36407987&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 44 mg/mL (199.77 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
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