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酪氨酸磷酸化抑制剂A23

EGFR/ErbB1 Selective Inhibitors | Activators
规格或纯度: 10mM in DMSO
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
A408794-1ml
1ml 期货 Stock Image

基本描述

规格或纯度 10mM in DMSO
英文名称 AG-18
英文别名 RG-50810, Tyrphostin A23, TX 825;Propanedinitrile, 2-[(3,4-dihydroxyphenyl)methylene]-
生化机理 AG-18 (RG-50810, Tyrphostin A23, TX 825) inhibits EGFR with IC50 of 35 μM.
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍

Information

AG-18 (RG-50810, Tyrphostin A23, TX 825) inhibitsEGFRwithIC50of 35 μM.
In?vitro

AG 18 inhibits EGFR and IR with Ki of 11 μM and 12 mM. AG 18 inhibits EGF-induced EGFR autophoshporylation with IC50 of 15 μM in A431 cells. AG 18 (10 μM) inhibits EGF-induced proliferation of GH3 cells. AG 18 (10 μM) causes significant inhibition of the cell proliferation induced by 10 nM and 1 μM ghrelin. AG 18 (10 μM) blocks the ghrelin-stimulated increase in ERK 1/2 phosphorylation in GH3 cells. [2]AG 18 inhibits the volume-sensitive release of [3H]taurine in primary astrocyte cultures in a dose-dependent manner. AG 18 activates swelling-induced volume-dependent D-[3H]aspartate release from primary astrocytic cultures. AG 18 (300 μM) inhibits TPA-induced stimulation of ICAM-1 expression in a dose dependent manner in A549 epithelial cells. AG 18 (300 μM) also inhibits TPA stimulated NF-kappaB DNA-protein binding and ICAM-1 promoter activity in A549 epithelial cells. AG 18 (300 μM) inhibits TNF-alpha-induced NF-kappaB DNA-protein binding and ICAM-1 promoter activity in a dose dependent manner in A549 epithelial cells. IKK activity is stimulated by both TNF-alpha and TPA, and these effects are inhibited by AG 18 (100 μM) in A549 epithelial cells. AG 18 (10 μM) decreases the potency of 5-HT 4-fold and reduces the maximal contraction to 5-HT in the carotid artery. AG 18 (10 μM) shifts KCl-induced contraction 2-fold and causes the maximum significantly inhibition.

In?vivo


Cell?Data

cell?lines:

Concentrations:10 μM

Incubation?Time:0.5 hour

Powder?Purity:≥99%

Information

AG-18 (RG-50810, Tyrphostin A23, TX 825) inhibitsEGFRwithIC50of 35 μM.
In?vitro

AG 18 inhibits EGFR and IR with Ki of 11 μM and 12 mM. AG 18 inhibits EGF-induced EGFR autophoshporylation with IC50 of 15 μM in A431 cells. AG 18 (10 μM) inhibits EGF-induced proliferation of GH3 cells. AG 18 (10 μM) causes significant inhibition of the cell proliferation induced by 10 nM and 1 μM ghrelin. AG 18 (10 μM) blocks the ghrelin-stimulated increase in ERK 1/2 phosphorylation in GH3 cells. [2]AG 18 inhibits the volume-sensitive release of [3H]taurine in primary astrocyte cultures in a dose-dependent manner. AG 18 activates swelling-induced volume-dependent D-[3H]aspartate release from primary astrocytic cultures. AG 18 (300 μM) inhibits TPA-induced stimulation of ICAM-1 expression in a dose dependent manner in A549 epithelial cells. AG 18 (300 μM) also inhibits TPA stimulated NF-kappaB DNA-protein binding and ICAM-1 promoter activity in A549 epithelial cells. AG 18 (300 μM) inhibits TNF-alpha-induced NF-kappaB DNA-protein binding and ICAM-1 promoter activity in a dose dependent manner in A549 epithelial cells. IKK activity is stimulated by both TNF-alpha and TPA, and these effects are inhibited by AG 18 (100 μM) in A549 epithelial cells. AG 18 (10 μM) decreases the potency of 5-HT 4-fold and reduces the maximal contraction to 5-HT in the carotid artery. AG 18 (10 μM) shifts KCl-induced contraction 2-fold and causes the maximum significantly inhibition.

In?vivo


Cell?Data

cell?lines:

Concentrations:10 μM

Incubation?Time:0.5 hour

Powder?Purity:≥99%

产品属性

IC50 EGFR, IC50: 35 μM

名称和标识符

Canonical SMILES OC1=C(O)C=C(C=C1)C=C(C#N)C#N
分子量 186.17

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 51 mg/mL (197.46 mM); ? ?

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