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24418-86-8

中文名称 2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
英文名称 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V
CAS 24418-86-8
分子式 C15H10O4
分子量 254.24
MOL 文件 24418-86-8.mol
更新日期 2024/12/23 09:08:09
24418-86-8 结构式 24418-86-8 结构式

基本信息

中文别名
化合物SKI V
2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
英文别名
SKI V
Sphingosine Kinase Inhibitor V
2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one
2-(3,4-Dihydroxybenzylidene)benzofuran-3(2H)-one
3(2H)-Benzofuranone, 2-[(3,4-dihydroxyphenyl)methylene]-
(2Z)-2-(3,4-dihydroxybenzylidene)-1-benzofuran-3(2H)-one
(2E)-2-[(3,4-dihydroxyphenyl)methylidene]-1-benzofuran-3-one
2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V

物理化学性质

沸点493.2±45.0 °C(Predicted)
密度1.489±0.06 g/cm3(Predicted)
储存条件Sealed in dry,2-8°C
溶解度DMSO: 250 mg/mL (983.32 mM)
酸度系数(pKa)8.99±0.10(Predicted)
形态Solid
颜色Light yellow to yellow

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS07
警示词警告
危险性描述H302-H315-H319
2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/11/08HY-128952-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
SKI V
24418-86-85mg1500元
2024/11/08HY-128952-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
SKI V
24418-86-810mM * 1mLin DMSO1650元
2024/11/08HY-128952-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
SKI V
24418-86-810mg2500元

常见问题列表

生物活性
SKI V 是一种非竞争性的,有效的非脂质鞘氨醇激酶 (SPHK; SK) 抑制剂,对 GST-hSK 的 IC50 为 2 μM。 SKI V 有效抑制 PI3K,对 hPI3k 的 IC50 为 6 μM。SKI V 减少有丝分裂的第二信使鞘氨醇-1-磷酸 (S1P) 的形成。SKI V 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。
靶点

IC50: 2 μM (GST-hSK), 6 μM (hPI3k) and 80 μM (ERK2)

体外研究

SKI V has weak activity toward ERK2 ( IC 50 of 80 μM for hERK2) and does not inhibit PKC-α.
SKI V (10 μM; for 24 hours) inhibits cancer cell proliferation and induces apoptosis.
SKI V (0.2, 1, 5 μM; pretreated for 1 hour) decreases phospho-Akt and phospho-MEK levels. Near-confluent cultures of JC cells are serum-starved for 16 hours, followed by pretreatment SKI V for 1 hour.
SKI V has IC 50 s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of ∼2 μM.
SKI V (20 μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells.
SKI V (0.2, 1, 5 μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion.

Cell Proliferation Assay

Cell Line: T24 tumor cells
Concentration: 10 μM
Incubation Time: For 24 hours
Result: Inhibited cancer cell proliferation.

Apoptosis Analysis

Cell Line: T24 tumor cells
Concentration: 10 μM
Incubation Time: For 24 hours
Result: Induced apoptosis.

Western Blot Analysis

Cell Line: JC cells
Concentration: 0.2, 1, 5 μM
Incubation Time: Pretreated for 1 hour
Result: Decreased phospho-Akt and phospho-MEK levels.
体内研究

SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals.

Animal Model: 6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells
Dosage: 75 mg/kg
Administration: IP; days 1, 5, 9, 15
Result: Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.
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