计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
鲁索替尼, Janus 激酶 1 抑制剂;Janus 激酶 2 抑制剂;Janus 激酶 3 抑制剂;酪氨酸激酶 2 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
S-Ruxolitinib (INCB018424)是第一个应用到临床的，有效的，选择性JAK1/2抑制剂，IC50为3.3 nM/2.8 nM，作用于JAK1/2比作用于JAK3选择性高130倍以上。 Phase 3。
Information
S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective,JAK1/2inhibitor to enter the clinic withIC50of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3.
In vitro
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 Data
cell lines：
Concentrations：3 μM
Incubation Time：48 hours
Powder Purity:≥99%
规格
英文别名
1H-Pyrazole-1-propanenitrile, β-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (βS)-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
S-Ruxolitinib (INCB018424)
生化机理
S-Ruxolitinib 是 INCB018424 的手性，它是第一个进入临床的强效、选择性 JAK1/2 抑制剂，IC50 为 3.3 nM/2.8 nM，对 JAK1/2 相对于 JAK3 的选择性大于 130 倍。第 3 阶段。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
Janus 激酶 1 抑制剂;Janus 激酶 2 抑制剂;Janus 激酶 3 抑制剂;酪氨酸激酶 2 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CCC(C1)[C@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
PubChem CID
分子量
306.37
技术文档
高级数据
关联靶点（人）
JAK2
Tclin
酪氨酸蛋白激酶JAK2(Tyrosine-protein kinase JAK2)
(2 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 45 mg/mL (199.74 mM); Ethanol: 19 mg/mL (84.33 mM); Water: Insoluble;
熔点
138-143ºC
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 A2311027 |
分析证书 | S408648 |
溶液计算器
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