| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G409108-1ml |
1ml |
现货  |
|
| 别名 | 甘多替尼 (LY2784544) |
|---|---|
| 英文别名 | 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Gandotinib (LY2784544) |
| 生化机理 | 甘多替尼（LY2784544）是一种强效的 JAK2 抑制剂，IC50 为 3 nM，对 JAK2V617F 有效，对 JAK1 和 JAK3 的选择性分别为 8 倍和 20 倍。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 JAK2 抑制剂 |
| 产品介绍 |
LY2784544是一种有效的JAK2抑制剂，IC50为3 nM，作用于JAK2V617F有效，比作用于JAK1和JAK3选择性高8和20倍。Phase 2。A selective inhibitor of JAK2 mutant V617F. Information Gandotinib (LY2784544) is a potentJAK2inhibitor withIC50of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2. LY2784544 also inhibits IL-3-activated wild type JAK2 with IC50 of 2.26 μM. Similarly in the proliferation assay, LY2784544 shows antiproliferation activity in JAK2 V617F-driven cells with IC50 of 68 nM, compared to 1.36 μM in wild type JAK2-driven cells and 0.94 μM in JAK3-driven cells. Though biochemical assays do not reveal selectivity of LY2784544 for mutant JAK2V617F, LY2784544 shows higher selectivity for inhibition of JAK2-mediated signaling and induction of apoptosis in Ba/F3 cells expressing JAK2V617F than wild-type cells. In vivo LY2784544 significantly inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts with a Threshold Effective Dose 50 (TED50) of 12.7 mg/kg. LY2784544 also reduces Ba/F3-JAK2 V617F-GFP tumor burden in the JAK2 V617F-induced MPN model with a TED50 of 13.7 mg/kg after oral treatment. LY2784544 has no effect on CD71/Ter119 positive erythroid progenitors in spleens of SCID mice after oral treatment. cell lines： Concentrations： Incubation Time： Powder Purity:≥98% |
| Ki Data | JAK2 (V617F), Ki: 0.245 nM; JAK2, Ki: 0.288 nM |
|---|---|
| IC50 | JAK2, IC50: 3 nM |
| ALogP | 3.938 |
| hba_count | 4 |
| HBD Count | 2 |
| Rotatable Bond | 6 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC1=N[NH]C(=C1)NC2=N[N]3C(=C(C)N=C3C(=C2)CN4CCOCC4)CC5=CC=C(Cl)C=C5F |
| 分子量 | 469.94 |
| Reaxy-Rn | 25492983 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25492983&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 44 mg/mL (198.87 mM); Ethanol: 44 mg/mL (198.87 mM); Water: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 94 |
| DMSO(mM) Max Solubility | 200.03 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 25492983 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25492983&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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