| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R409244-1ml |
1ml |
现货  |
|
| 英文别名 | (3R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Ruxolitinib (INCB018424) |
| 生化机理 | Ruxolitinib（INCB018424）是首个进入临床的强效、选择性 JAK1/2 抑制剂，在无细胞实验中的 IC50 为 3.3 nM/2.8 nM，对 JAK1/2 的选择性大于 JAK3 的 130 倍。Ruxolitinib 通过毒性有丝分裂杀死肿瘤细胞。Ruxolitinib可诱导自噬并促进细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
Ruxolitinib (INCB018424)是第一个应用于临床的、有效的、选择性的JAK1/2抑制剂，IC50为3.3 nM/2.8 nM。作用于JAK1， JAK2与 作用于JAK3相比，选择性强130倍多。An inhibitor of JAK1, JAK2, and JAK3. Information Ruxolitinib (INCB018424) is the first potent, selective,JAK1/2inhibitor to enter the clinic withIC50of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib indu INCB018424 potently and selectively inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. INCB018424 markedly increases apoptosis in a dose dependent manner in Ba/F3 cells. INCB018424 (64 nM) results in a doubling of cells with depolarized mitochondria in Ba/F3 cells. INCB018424 inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC50 of 407 nM and 223 nM, respectively. INCB018424 demonstrates remarkable potency against erythroid colony formation with IC50 of 67nM. In vivo INCB018424 (180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 in a JAK2V617F-driven mouse model. INCB018424 (180 mg/kg, orally, twice a day) markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects in a JAK2V617F-driven mouse model. The primary end point is reached in 41.9% of patients in the Ruxolitinib group as compared with 0.7% in the placebo group in the double-blind trial of myelofibrosis. Ruxolitinib results in maintaining of reduction in spleen volume and improvement of 50% or more in the total symptom score. A total of 28% of the patients in the Ruxolitinib (15 mg twice daily) group has at least a 35% reduction in spleen volume at week 48 in patients with myelofibrosis, as compared with 0% in the group receiving the best available therapy. The mean palpable spleen length has decreased by 56% with Ruxolitinib but has increased by 4% with the best available therapy at week 48. Patients in the ruxolitinib group has an improvement in overall quality-of-life measures and a reduction in symptoms associated with myelofibrosis. cell lines：NSCLC and Ba/F3 cells Concentrations：3 μM Incubation Time：48 hours Powder Purity:≥98% |
| Isomeric SMILES | C1CCC(C1)[C@@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 |
|---|---|
| PubChem CID | 25126798 |
| 分子量 | 306.37 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 45 mg/mL (201.54 mM); Ethanol: 45 mg/mL (201.54 mM); Water: Insoluble; |
|---|
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