NVP-AEW541

别名: AEW541

NVP-AEW541是一种有效的IGF-1R/InsR抑制剂,在无细胞试验中IC50为150 nM/140 nM,在细胞试验中对IGF-1R具有较高的作用和选择性。

NVP-AEW541 Chemical Structure

NVP-AEW541 Chemical Structure

CAS: 475489-16-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1875.51 现货
2mg 876.33 现货
5mg 1556.1 现货
10mg 2432.43 现货
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相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
CM Apoptosis assay ~5 μM induces Apoptosis 16601284
BON Apoptosis assay ~7.5 μM induces Apoptosis 16601284
CM Function assay ~5 μM induces cell cycle arrest 16601284
BON Function assay ~7.5 μM induces cell cycle arrest 16601284
CM Growth inhibitory assay ~5 μM IC50=3.3 μM 16601284
BON Growth inhibitory assay ~10 μM IC50=6.6 μM 16601284
BON Kinase assay ~6 μM induces dephosphorylation of IGF-1R 16601284
SK-Hep-1 Function assay ~10 μM Induces cell cycle arrest 16530734
Hep-G2 Function assay ~10 μM Induces cell cycle arrest 16530734
Huh-7 Function assay ~10 μM Induces cell cycle arrest 16530734
SK-Hep-1 Growth inhibitory assay ~10 μM IC50=6.9 μM 16530734
Hep-3B Growth inhibitory assay ~10 μM IC50=1.9 μM 16530734
Hep-G2 Growth inhibitory assay ~10 μM IC50=1.8 μM 16530734
Huh-7 Growth inhibitory assay ~10 μM IC50=1.4 μM 16530734
OVCAR-3 Function assay ~15 μM Decreases phosphorylation of AKT 16300820
OVCAR-4 Apoptosis assay ~15 μM induces apoptosis 16300820
OVCAR-3 Apoptosis assay ~15 μM induces apoptosis 16300820
OVCAR-4 Growth inhibitory assay ~15 μM inhibits cell proliferation 16300820
OVCAR-3 Growth inhibitory assay ~15 μM inhibits cell proliferation 16300820
RD/18 Growth inhibitory assay ~7 μM IC50<4 μM 15867386
CCA Growth inhibitory assay ~7 μM IC50<2 μM 15867386
RMZ-RC2 Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
IOR/RCH Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
IOR/NGR Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
IOR/CAR Growth inhibitory assay ~7 μM IC50<1 μM 15867386
IOR/BRZ Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
LAP35 Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
IOR/OS14 Growth inhibitory assay ~7 μM IC50<4 μM 15867386
IOR/OS10 Growth inhibitory assay ~7 μM IC50<5 μM 15867386
IOR/OS9 Growth inhibitory assay ~7 μM IC50<6 μM 15867386
IOR/OS7 Growth inhibitory assay ~7 μM IC50<1 μM 15867386
MOS Growth inhibitory assay ~7 μM IC50<4 μM 15867386
SARG Growth inhibitory assay ~7 μM IC50<3 μM 15867386
6647 Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
SJ-Rh 4 Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
SJ-Rh 30 Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
RD-ES Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
SK-N-MC Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
SK-ES-1 Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
U-2OS Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
Saos-2 Growth inhibitory assay ~7 μM IC50<3 μM 15867386
TC-71 Growth inhibitory assay ~7 μM IC50<0.5 μM 15867386
TC-71 Growth inhibitory assay ~1 μM inhibits insulin-like growth factor-I–mediated growth 15867386
32D-Bcr-Abl Kinase assay ~10 μM inhibits Bcr-Abl p210 with IC50 of >10 μM 15050915
GIST882 Kinase assay ~10 μM inhibits c-Kit with IC50 of >5 μM 15050915
A31  Kinase assay ~10 μM inhibits PDGFR with IC50 of >10 μM 15050915
A431  Kinase assay ~10 μM inhibits HER1 with IC50 of >10 μM 15050915
A14 Kinase assay ~10 μM inhibits InsR with IC50 of 2.3 ± 0.163 μM 15050915
NWT-21 Kinase assay ~10 μM inhibits IGF-IR with IC50 of 0.086 ± 0.028 μM 15050915
HT-29 Growth inhibitory assay ~10 μM IC50=1.7 μM 17007015
HCT-116 Growth inhibitory assay ~10 μM IC50=2.5 μM 17007015
primary colorectal cancer cells Function assay ~5 μM alters the morphology of the remaining cells 17007015
HTLA-230 Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
KCNR Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
SK-N-BE2c Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
SK-N-BE Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
LAN-5 Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
GI-CA-N Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
SH-EP Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
SK-N-AS Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
RN-GA Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
SY-5Y(N) Function assay ~8 μM inhibits IGF-II-mediated stimulation of IGF-IR and Akt 17121898
GI-CA-N Growth inhibitory assay ~8 μM IC50= 6.8 μM 17121898
SH-EP Growth inhibitory assay ~8 μM IC50= 3 μM 17121898
HTLA-230 Growth inhibitory assay ~8 μM IC50= 0.5 μM 17121898
SK-N-BE2c Growth inhibitory assay ~8 μM IC50= 1.1 μM 17121898
SK-N-BE2 Growth inhibitory assay ~8 μM IC50= 3 μM 17121898
SY-5Y (N) Growth inhibitory assay ~8 μM IC50= 2.4 μM 17121898
LAN-5 Growth inhibitory assay ~8 μM IC50= 0.4 μM 17121898
KCNR Growth inhibitory assay ~8 μM IC50= 0.4 μM 17121898
RN-GA Growth inhibitory assay ~8 μM IC50= 1.3 μM 17121898
SK-N-AS Growth inhibitory assay ~8 μM induces apoptosis 17121898
KCNR Apoptosis assay ~8 μM induces apoptosis 17121898
GI-CA-N Apoptosis assay ~8 μM induces apoptosis 17121898
HTLA-230 Apoptosis assay ~8 μM induces apoptosis 17121898
SK-N-BE2c Apoptosis assay ~8 μM induces apoptosis 17121898
SY-5Y (N) Apoptosis assay ~8 μM induces apoptosis 17121898
HL60AR Function assay 160 nM enhances the levels of p27Kip1 17361225
HL60AR Apoptosis assay ~200 nM induces apoptosis 17361225
HPAF-II Kinase assay ~1 μM inhibits IGF-I-mediated signalling 18445520
HPAF-II Growth inhibitory assay ~2 μM inhibits cell proliferation 18445520
HPAF-II Function assay ~2 μM inhibits basal and IGF-I-mediated pancreatic cancer cell migration 18445520
TFK-1 Growth inhibitory assay ~250 nM IC50=0.26 μM 20066734
EGI-1 Growth inhibitory assay ~250 nM IC50=0.28 μM 20066734
CC-LP-1 Growth inhibitory assay ~250 nM IC50=0.15 μM 20066734
CC-SW-1 Growth inhibitory assay ~250 nM IC50=0.54 μM 20066734
Sk-ChA-1 Growth inhibitory assay ~250 nM IC50=0.2 μM 20066734
Mz-ChA-1 Growth inhibitory assay ~250 nM IC50=1.39 μM 20066734
Mz-ChA-2 Growth inhibitory assay ~250 nM IC50=0.73 μM 20066734
ECC-1 Kinase assay ~10 μM inhibits IGF-IR activation by 98% 21295335
Ishikawa Kinase assay ~10 μM inhibits IGF-IR activation by 93% 21295335
USPC-1 Kinase assay ~10 μM inhibits IGF-IR activation by 100% 21295335
USPC-2 Kinase assay ~10 μM inhibits IGF-IR activation by 96% 21295335
ECC-1 Growth inhibitory assay ~10 μM decreases cell proliferation 21295335
Ishikawa Growth inhibitory assay ~10 μM decreases cell proliferation 21295335
USPC-1 Growth inhibitory assay ~10 μM decreases cell proliferation 21295335
USPC-2 Growth inhibitory assay ~10 μM decreases cell proliferation 21295335
HEK293 Function assay 60 mins Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50=0.065μM 26951753
HEK293 Function assay 60 mins Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50=0.892μM 26951753
NWT-21 Growth inhibitory assay IC50=0.163 μM 15050915
MCF-7  Cytoxicity assay IC50=1.64 μM 15050915
Ba/F3 Function assay Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50=0.02μM 26951753
HEK293 Function assay Displacement of [3H]-dofetilide from human ERG channel expressed in HEK293 cells, IC50=0.13μM 26951753
Ba/F3 Function assay Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50=0.244μM 26951753
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 NVP-AEW541是一种有效的IGF-1R/InsR抑制剂,在无细胞试验中IC50为150 nM/140 nM,在细胞试验中对IGF-1R具有较高的作用和选择性。
靶点
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
Tek [1]
(Cell-free assay)
FLT1 [1]
(Cell-free assay)
点击更多
0.14 μM 0.15 μM 0.42 μM 0.53 μM 0.6 μM
体外研究(In Vitro)
体外研究活性 在纯化的激酶/重组激酶域实验中,NVP-AEW541也抑制InsR, Tek, Flt1 和 Flt3,IC50分别为140 nM, 530 nM, 600 nM 和 420 nM。在细胞水平,NVP-AEW541选择性更高,比InsR选择性高27倍。NVP-AEW541抑制IGF-I调节的生存,软琼脂,和MCF-7细胞增殖,IC50分别为0.162 μM, 0.105 μM 和 1.64 μM。NVP-AEW541作用于NWT-21细胞,也降低 p-IGF-IR 和 p-PKB 水平。[1] NVP-AEW541 作用于培养在低血清培养基和含10% FBS的培养基中的TC-71肌肉骨骼肉瘤细胞,抑制生长。NVP-AEW541作用于肉瘤细胞系(TC-71, SK-N-MC, SaoS-2, RD/18 和 RH4),抑制细胞周期进展和诱导细胞周期在G1期停顿。 [2]NVP-AEW541可抑制神经母细胞瘤细胞生长,IC50为0.4-6.8 μM。在这些细胞中可以检测到亚二倍体片段增多及 S和 G2-M 期细胞消耗。在神经母细胞瘤细胞中,NVP-AEW541驱动的 IGF-IR 受抑制,可降低 Akt磷酸化,而不是Erk1和Erk2磷酸化。[3] NVP-AEW541 抑制神经胶质瘤细胞生长,且破坏HIF1α 稳定化启动的自分泌环。[4]最新研究显示NVP-AEW541抑制 PC3, DU145, 和22Rv1 前列腺癌细胞增殖和活性。NVP-AEW541 作用于22Rv1和 DU415 细胞而不是PC3细胞,降低 p-Akt水平,不会影响整体Akt水平,说明PTEN状态可决定NVP-AEW541的有效性。NVP-AEW541诱导的放射敏感度决定于Akt 激活状态。NVP-AEW541作用于PC3, DU145, 和 22Rv1细胞,可提高H2AX 磷酸化。[5]
激酶实验 体外酶法测定
NVP-AEW541溶解在DMSO(10 mM) 中,储存在-20oC下。稀释液在1:1的DMSO/水中现配。在酶法测定中DMSO的最终浓度<0.5 %。蛋白激酶实验在96孔板上进行,加入20 μl 125 mM EDTA终止反应。随后, 30 μl (c-Abl, c-Src, IGF-1R) 反应混合物转移到Immobilon-P转印膜上,加入甲醇预浸泡5分钟,用水冲洗, 然后加入0.5 % H3PO4浸泡5分钟,然后装在真空管中。识别所有样本后,用200 μl 0.5 % H3PO4冲洗每孔。分离膜,在搅拌器上用1.0 % H3PO4冲洗4次,其中一次加入乙醇。烘干后,建立Packard TopCount 96孔框架,每孔加入10 μl Microscint, 膜计数。通过线性回归分析NVP-AEW541在四种不同浓度(0.01, 0.1, 1, 和10 μM)下的抑制百分数来计算IC50值。37oC下,每分钟,每毫克蛋白中,[γ33P]ATP转化到底物蛋白中的1 nM 33P表示蛋白激酶活性。
细胞实验 细胞系 MCF-7细胞
浓度 30到300 nM
孵育时间 30分钟
方法 NVP-AEW541直接加到琼脂培养基中,最终浓度为30到300 nM。MCF7生长培养基中下层包括每孔0.5 ml 细菌琼脂。包被培养板,储存在孵育器中(37oC, 5% CO2)至少30分钟,固定培养基,然后加入上层琼脂。在生长培养基的0.5ml上层0.4%琼脂中每孔接种5×103个MCF-7细胞。在37oC, 5% CO2环境下温育3周后, 细胞混合, 用结晶紫染色,计数阳性菌落(直径>40 μm),使用KS-400图像分析系统测定转化效率。
体内研究(In Vivo)
体内研究活性 NVP-AEW541(50 mg/kg, 口服处理)作用于NWT-21移植瘤,导致基础型和IGF-I诱导型受体的废除,也抑制 PKB和MAPK磷酸化,T/C 值为14%。[1]NVP-AEW541(50 mg/kg) 作用于HTLA-230和 SK-N-BE2c移植瘤,引起肿瘤缩小,没有全身毒性迹象。NVP-AEW541作用于Matrigel包被的细胞和HTLA-230移植瘤,可以抑制肿瘤入侵。[3]
动物实验 Animal Models 携带NWT-21细胞的Harlan无胸腺裸鼠,体重为18-25 g
Dosages 20, 30,或50 mg/kg; 10 ml/kg
Administration 每天口服处理2次,每周处理7天

化学信息&溶解度

分子量 439.55 分子式

C27H29N5O

CAS号 475489-16-8 SDF Download NVP-AEW541 SDF
Smiles C1CN(C1)CC2CC(C2)N3C=C(C4=C(N=CN=C43)N)C5=CC(=CC=C5)OCC6=CC=CC=C6
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 88 mg/mL ( (200.2 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 24 mg/mL (54.6 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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