24418-86-8

中文名稱 2-(3,4-二羥基亞芐基)苯并呋喃-3(2H)-酮

英文名稱 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 結(jié)構(gòu)式

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) 2-(3,4-二羥基亞芐基)苯并呋喃-3(2H)-酮價(jià)格(試劑級(jí)) 常見問題列表

基本信息

中文別名

化合物SKI V
2-(3,4-二羥基亞芐基)苯并呋喃-3(2H)-酮

英文別名

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

物理化學(xué)性質(zhì)

沸點(diǎn)493.2±45.0 °C(Predicted)

密度1.489±0.06 g/cm3(Predicted)

儲(chǔ)存條件Sealed in dry,2-8°C

溶解度DMSO: 250 mg/mL (983.32 mM)

酸度系數(shù)(pKa)8.99±0.10(Predicted)

形態(tài)Solid

顏色Light yellow to yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS) GHS hazard pictograms

GHS07

警示詞警告

危險(xiǎn)性描述H302-H315-H319

防范說明P280-P264-P305+P351+P338-P337+P313

2-(3,4-二羥基亞芐基)苯并呋喃-3(2H)-酮價(jià)格(試劑級(jí))

報(bào)價(jià)日期	產(chǎn)品編號(hào)	產(chǎn)品名稱	CAS號(hào)	包裝	價(jià)格
2024/11/08	HY-12895	2-(3,4-二羥基亞芐基)苯并呋喃-3(2H)-酮 SKI V	24418-86-8	5mg	1500元
2024/11/08	HY-12895	2-(3,4-二羥基亞芐基)苯并呋喃-3(2H)-酮 SKI V	24418-86-8	10mM * 1mLin DMSO	1650元
2024/11/08	HY-12895	2-(3,4-二羥基亞芐基)苯并呋喃-3(2H)-酮 SKI V	24418-86-8	10mg	2500元

常見問題列表

生物活性

SKI V 是一種非競(jìng)爭(zhēng)性的，有效的非脂質(zhì)鞘氨醇激酶 (SPHK; SK) 抑制劑，對(duì) GST-hSK 的 IC50 為 2 μM。 SKI V 有效抑制 PI3K，對(duì) hPI3k 的 IC50 為 6 μM。SKI V 減少有絲分裂的第二信使鞘氨醇-1-磷酸 (S1P) 的形成。SKI V 誘導(dǎo)細(xì)胞凋亡 (apoptosis) 并具有抗腫瘤活性。

靶點(diǎn)

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

體外研究

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.

體內(nèi)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.