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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
CAS: 475489-16-8
产品质控
批次：
纯度：
99.61%
99.61
NVP-AEW541相关产品
| 相关靶点 | Insulin Receptor | 点击展开 |
|---|---|---|
| 相关产品 | Linsitinib (OSI-906) BMS-754807 Picropodophyllin (PPP) GSK1904529A BMS-536924 AG-1024 NVP-ADW742 NT157 PQ 401 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 细胞周期化合物库 血管生成相关化合物库 | 点击展开 |
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(PMID) |
|---|---|---|---|---|---|
| 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 |
|
| 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) | |||
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体外溶解度 |
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 |
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体内溶解配方 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
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
只
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，注：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：取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：取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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