计算溶液所需的质量、体积或浓度。
为什么选择此级别
，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
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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
Information
NVP-BSK805 2HCl is a potent and selective ATP-competitiveJAK2inhibitor withIC50of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2.
In vitro
NVP-BSK805 is found to potently inhibit JAK2, whereas displaying more than 20-fold selectivity towards JAK1, JAK3, and TYK2. NVP-BSK805 causes half-maximal inhibition of full-length JAK2V617F and JAK2 wild-type enzymes at 0.5 nM. NVP-BSK805 blocks the growth of JAK2V617F cells (Ba/F3) and induces apoptosis with a GI50 at concentrations ＜100 nM. As constitutive STAT5 phosphorylation in dependent on JAK2, NVP-BSK805 is found to potently suppress STAT5 phophorylation at ≥ 100 nM concentrations in the JAK2 V617F -mutant cell lines, like MB-02. Incubation of SET-2 cells with 150 nM and 1µM of NVP-BSK805, which corresponds to concentration yielding 75% and 95% growth inhibition, respectively, for 24, 48, and 72 hours lead to concentration- and time- dependent induction of apoptosis. These results are evidenced by the detection of cleaved PARP, reduced Bcl-xL expression, and a strong increase in the number of cells with less than 2N DNA content. NVP-BSK805 triggered cell death requires activation of caspase cascades and is overcome by caspase inhibition in both SET-2 and MB-02 cells. NVP-BSK805 modulates the post-translational modification of Bim and levels of Mcl-1 in JAK2V617F cells, SET-2 and MB-02 cells.
In vivo
Oral bioavailability of NVP-BSK805 in mice is estimated to be 45%, while it is 50% in rats. Oral administration of NVP-BSK805 at 150 mg/kg suppresses STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell–driven mouse model. NVP-BSK805 suppresses rhEpo-induced STAT5 phosphorylation as well as rhEpo-mediated polycythemia and splenomegaly in BALB/c mice at doses of 25, 50, and 100 mg/kg orally.
Cell Data
cell lines：DU-145, H1581, and VCaP cells
Concentrations：100 nM
Incubation Time：72 hours
Powder Purity:≥97%
规格
英文别名
BSK805 | 8-(3,5-difluoro-4-(morpholinomethyl)phenyl)-2-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxaline
规格或纯度
10mM in DMSO
英文名称
NVP-BSK805 2HCl
生化机理
NVP-BSK805 2HCl 是一种强效的选择性 ATP 竞争性 JAK2 抑制剂，IC50 为 0.5 nM，对 JAK1、JAK3 和 TYK2 的选择性大于 20 倍。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CNCCC1N2C=C(C=N2)C3=NC4=C(C=CC=C4N=C3)C5=CC(=C(C(=C5)F)CN6CCOCC6)F.Cl.Cl
PubChem CID
分子量
563.47
技术文档
高级数据
产品属性
| IC50 | JAK3, IC50: 18.68 nM |
|---|---|
| ALogP | 3.92 |
| HBD Count | 1 |
| Rotatable Bond | 5 |
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 44 mg/mL (198.9 mM); Water: 44 mg/mL (198.9 mM); Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility
113
DMSO(mM) Max Solubility
200.5430635
Water(mg / mL) Max Solubility
3
Water(mM) Max Solubility
5.324152129
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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