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4-羟基苯亚甲基丙二腈

4-羟基苯亚甲基丙二腈用途

酪磷蛋白8是一种酪氨酸激酶,EGFR激酶的IC50为560μM。酪磷蛋白8也是GTPase抑制剂。酪磷蛋白8可抑制蛋白丝氨酸/苏氨酸磷酸酶钙调神经磷酸酶(IC50=21μM)[1][2][3]。

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4-羟基苯亚甲基丙二腈名称

[ CAS 号 ]:
3785-90-8

[ 中文名 ]:
4-羟基苯亚甲基丙二腈

[ 英文名 ]:
Tyrphostin 8

[英文别名 ]:

4-(HYDROXYBENZYLIDENE)-MALONONITRILE
4-Hydroxybenzylidenemalononitrile
(4-Hydroxybenzylidene)malonitrile
EINECS 223-253-0
2-[(4-hydroxyphenyl)methylidene]propanedinitrile
MFCD00020189

4-羟基苯亚甲基丙二腈生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> JAK/STAT信号通路 >> EGFR

信号通路 >> 代谢酶/蛋白酶 >> 磷酸酶

信号通路 >> 蛋白酪氨酸激酶 >> EGFR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 拉斯

研究领域 >> 代谢疾病

[ 靶点 ]

EGFR:560 μM (IC50)

calcineuin phosphatase:21 μM (IC50)

[体外研究]

酪磷蛋白8(10-100μM；预处理20分钟)阻断了卡巴胆碱引发的腮腺腺泡细胞PKCδ酪氨酸磷酸化和ERK1/2激活[1]。Tyrphostin 8(10-100μM)使腮腺腺泡的基础O2消耗量快速而大幅增加[1]。酪磷素8(10-100μM)可通过以下方式降低腮腺ATP含量：∼浓度为100μM时为90%[1]。酪磷蛋白8通过增强滤器生长的Caco-2细胞单层中转铁蛋白受体介导的细胞转运,增加胰岛素-转铁蛋白结合物从顶端到基底外侧的转运[2]。westernblot分析[1]细胞系：腮腺腺泡细胞浓度：10100μM孵育时间：预处理20min结果：减少卡巴胆碱引起的PKCδ酪氨酸磷酸化的增加。减少卡巴胆碱对ERK1/2的激活。

[体内研究]

酪磷蛋白8改善链脲佐菌素诱导的糖尿病大鼠胰岛素转铁蛋白的降糖效果[2]。

[参考文献]

[1]. Soltoff SP. Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling. J Biol Chem. 2004 Mar 19;279(12):10910-8.

[2]. Xia CQ, et, al. Tyrphostin-8 enhances transferrin receptor-mediated transcytosis in Caco-2- cells and inreases hypoglycemic effect of orally administered insulin-transferrin conjugate in diabetic rats. Pharm Res. 2001 Feb;18(2):191-5.

[3]. Martin BL. Inhibition of calcineurin by the tyrphostin class of tyrosine kinase inhibitors. Biochem Pharmacol. 1998 Aug 15;56(4):483-8.

4-羟基苯亚甲基丙二腈物理化学性质

[ 密度 ]:
1.29 g/cm3

[ 沸点 ]:
354.3ºC at 760 mmHg

[ 熔点 ]:
186-189 °C

[ 分子式 ]:
C₁₀H₆N₂O

[ 分子量 ]:
170.17

[ 闪点 ]:
168.1ºC

[ 精确质量 ]:
170.04800

[ PSA ]:
67.81000

[ LogP ]:
1.82276

[ 外观性状 ]:
黄色固体

[ 折射率 ]:
1.653

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
ethanol: 20 mg/mL, clear

4-羟基苯亚甲基丙二腈MSDS

详细MSDS(安全技术说明书)

4-羟基苯亚甲基丙二腈毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OO4200000

CHEMICAL NAME :: Malononitrile, (p-hydroxybenzylidene)-

CAS REGISTRY NUMBER :: 3785-90-8

BEILSTEIN REFERENCE NO. :: 2209079

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C10-H6-N2-O

MOLECULAR WEIGHT :: 170.18

WISWESSER LINE NOTATION :: QR D1UYCN&CN

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 14,1325,1965

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 65 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NATUAS Nature. (Nature Subscription Dept., POB 1018, Manasguan, NJ 08736) V.1- 1869- Volume(issue)/page/year: 228,1315,1970

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4-羟基苯亚甲基丙二腈安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H319

[ 警示性声明 ]:
P301 + P310-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
25

[ 安全声明 (欧洲) ]:
S45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
OO4200000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2926909090

4-羟基苯亚甲基丙二腈合成路线

详细合成路线

4-羟基苯亚甲基丙二腈上下游产品

4-羟基苯亚甲基丙二腈上游产品

4-羟基苯亚甲基丙二腈下游产品

4-羟基苯亚甲基丙二腈海关

[ 海关编码 ]: 2926909090

[ 中文概述 ]:
2926909090 其他腈基化合物. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
HS:2926909090 other nitrile-function compounds VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

4-羟基苯亚甲基丙二腈文献

Effect of combined changes in delayed extraction time and potential gradient on the mass resolution and ion discrimination in the analysis of polydisperse polymers and polymer blends by delayed extraction matrix-assisted laser desorption/ionization time-of-flight mass spectrometry

Rapid Commun. Mass Spectrom. 13(24) , 2511-7, (1999)

Data reported here show that, in the delayed extraction matrix-assisted laser desorption/ionization time-of-flight (DE-MALDI-TOF) mass spectrometric analysis of synthetic polydisperse polymers, differ...

[Prevalence of Aeromonas spp. pediatric gastroenteritis].

CMAJ 138(8) , 714-7, (1988)

A selective medium and biochemical tests were used to search for Aeromonas spp. in the stools of 536 children, more than 90% of whom had "gastroenteritis", seen at Sainte-Justine Hospital, Montreal, i...

Characterization and modulation of the transferrin receptor on brain capillary endothelial cells.

Pharm. Res. 21(5) , 761-9, (2004)

The expression level of the transferrin receptor (TfR) on brain capillary endothelial cells (BCECs) and the endocytosis of 125I-transferrin (125I-Tf) by this receptor was investigated. Furthermore, th...

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