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SPHINX31
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SPHINX31图片
CAS NO:1818389-84-2
包装:5mg, 25mg
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品名称
SPHINX-31
产品介绍

生物活性

SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1) with IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 treatment results in inhibition of SRSF1 phosphorylation at 300 nM in PC3 prostate cancer cells. Metabolic stability in mouse liver microsomes shows that SPHINX31 had medium clearance with a T1/2 of 95.79 min.

In vivo, SPHINX31 exerts a dose dependent inhibition of choroidal neovascularisation in mouse model. SPHINX31 inhibits blood vessel growth and macrophage infiltration. SPHINX31 treatment prolongs survival of immunocompromised mice transplanted with MLL-rearranged AML cells.


化学数据

分子量507.51
分子式C27H24F3N5O2
CAS号1818389-84-2
纯度>99%
溶解性(25°C)DMSO 18 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系THP-1 cells
方法For synergy studies between SPHINX31 and iBET, THP-1 cells were seeded in 96-well plates at 10,000 cells per well and treated with SPHINX31 (dose range of 0.039–5 μM) and iBET (dose range of 9.8–312.5 nM) in an 8 by 6 matrix. Each treatment was carried out in triplicate. Cells were treated for 72 h, and cell viability was determined using CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay (Promega) in order to calculate the relative cell proliferation. Cell viability for each treatment was normalized against the DMSO control group. A Bliss independence model was employed to evaluate combination effects and calculate the Bliss independence score. All the compounds were dissolved in DMSO.
浓度0.039-5 μM
处理时间72 h

动物实验
动物模型DBA2J mice
配制dissolved in 20%(w/v) 2-hydroxyproply beta-cyclodextrin vehicle
剂量0.8 mg/kg
给药处理i.p.

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM1.9704 mL9.852 mL19.704 mL
5 mM0.3941 mL1.9704 mL3.9408 mL
10 mM0.197 mL0.9852 mL1.9704 mL