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NVP-AEW541
別名: AEW541
NVP-AEW541是一種有效的IGF-1R/InsR抑制劑，在無細胞試驗中IC50為150 nM/140 nM，在細胞試驗中對IGF-1R具有較高的作用和選擇性。
NVP-AEW541 Chemical Structure
CAS: 475489-16-8
產(chǎn)品質(zhì)控
批次：
純度：
99.61%
99.61
NVP-AEW541相關(guān)產(chǎn)品
| 相關(guān)靶點 | Insulin Receptor | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Linsitinib (OSI-906) BMS-754807 Picropodophyllin (PPP) GSK1904529A BMS-536924 AG-1024 NVP-ADW742 NT157 PQ 401 | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 細胞周期化合物庫 血管生成相關(guān)化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | NVP-AEW541是一種有效的IGF-1R/InsR抑制劑，在無細胞試驗中IC50為150 nM/140 nM，在細胞試驗中對IGF-1R具有較高的作用和選擇性。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在純化的激酶/重組激酶域?qū)嶒炛?，NVP-AEW541也抑制InsR, Tek, Flt1 和 Flt3，IC50分別為140 nM, 530 nM, 600 nM 和 420 nM。在細胞水平，NVP-AEW541選擇性更高，比InsR選擇性高27倍。NVP-AEW541抑制IGF-I調(diào)節(jié)的生存，軟瓊脂，和MCF-7細胞增殖，IC50分別為0.162 μM, 0.105 μM 和 1.64 μM。NVP-AEW541作用于NWT-21細胞，也降低 p-IGF-IR 和 p-PKB 水平。[1] NVP-AEW541 作用于培養(yǎng)在低血清培養(yǎng)基和含10% FBS的培養(yǎng)基中的TC-71肌肉骨骼肉瘤細胞，抑制生長。NVP-AEW541作用于肉瘤細胞系(TC-71, SK-N-MC, SaoS-2, RD/18 和 RH4)，抑制細胞周期進展和誘導細胞周期在G1期停頓。 [2]NVP-AEW541可抑制神經(jīng)母細胞瘤細胞生長,IC50為0.4-6.8 μM。在這些細胞中可以檢測到亞二倍體片段增多及 S和 G2-M 期細胞消耗。在神經(jīng)母細胞瘤細胞中，NVP-AEW541驅(qū)動的 IGF-IR 受抑制，可降低 Akt磷酸化,而不是Erk1和Erk2磷酸化。[3] NVP-AEW541 抑制神經(jīng)膠質(zhì)瘤細胞生長，且破壞HIF1α 穩(wěn)定化啟動的自分泌環(huán)。[4]最新研究顯示NVP-AEW541抑制 PC3, DU145, 和22Rv1 前列腺癌細胞增殖和活性。NVP-AEW541 作用于22Rv1和 DU415 細胞而不是PC3細胞，降低 p-Akt水平，不會影響整體Akt水平，說明PTEN狀態(tài)可決定NVP-AEW541的有效性。NVP-AEW541誘導的放射敏感度決定于Akt 激活狀態(tài)。NVP-AEW541作用于PC3, DU145, 和 22Rv1細胞，可提高H2AX 磷酸化。[5] | |||
|---|---|---|---|---|
| 激酶實驗 | 體外酶法測定 | |||
| NVP-AEW541溶解在DMSO(10 mM) 中，儲存在-20oC下。稀釋液在1:1的DMSO/水中現(xiàn)配。在酶法測定中DMSO的最終濃度<0.5 %。蛋白激酶實驗在96孔板上進行，加入20 μl 125 mM EDTA終止反應。隨后, 30 μl (c-Abl, c-Src, IGF-1R) 反應混合物轉(zhuǎn)移到Immobilon-P轉(zhuǎn)印膜上，加入甲醇預浸泡5分鐘,用水沖洗, 然后加入0.5 % H3PO4浸泡5分鐘，然后裝在真空管中。識別所有樣本后，用200 μl 0.5 % H3PO4沖洗每孔。分離膜，在攪拌器上用1.0 % H3PO4沖洗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, 膜計數(shù)。通過線性回歸分析NVP-AEW541在四種不同濃度(0.01, 0.1, 1, 和10 μM)下的抑制百分數(shù)來計算IC50值。37oC下，每分鐘，每毫克蛋白中，[γ33P]ATP轉(zhuǎn)化到底物蛋白中的1 nM 33P表示蛋白激酶活性。 | ||||
| 細胞實驗 | 細胞系 | MCF-7細胞 | ||
| 濃度 | 30到300 nM | |||
| 孵育時間 | 30分鐘 | |||
| 方法 | NVP-AEW541直接加到瓊脂培養(yǎng)基中，最終濃度為30到300 nM。MCF7生長培養(yǎng)基中下層包括每孔0.5 ml 細菌瓊脂。包被培養(yǎng)板，儲存在孵育器中(37oC, 5% CO2)至少30分鐘，固定培養(yǎng)基，然后加入上層瓊脂。在生長培養(yǎng)基的0.5ml上層0.4%瓊脂中每孔接種5×103個MCF-7細胞。在37oC, 5% CO2環(huán)境下溫育3周后, 細胞混合, 用結(jié)晶紫染色,計數(shù)陽性菌落(直徑>40 μm),使用KS-400圖像分析系統(tǒng)測定轉(zhuǎn)化效率。 | |||
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | NVP-AEW541(50 mg/kg, 口服處理)作用于NWT-21移植瘤，導致基礎(chǔ)型和IGF-I誘導型受體的廢除，也抑制 PKB和MAPK磷酸化，T/C 值為14%。[1]NVP-AEW541(50 mg/kg) 作用于HTLA-230和 SK-N-BE2c移植瘤，引起腫瘤縮小，沒有全身毒性跡象。NVP-AEW541作用于Matrigel包被的細胞和HTLA-230移植瘤，可以抑制腫瘤入侵。[3] | |
|---|---|---|
| 動物實驗 | Animal Models | 攜帶NWT-21細胞的Harlan無胸腺裸鼠，體重為18-25 g |
| Dosages | 20, 30,或50 mg/kg; 10 ml/kg | |
| Administration | 每天口服處理2次，每周處理7天 | |
化學信息&溶解度
| 分子量 | 439.55 | 分子式 | C27H29N5O |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 88 mg/mL ( (200.2 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 24 mg/mL (54.6 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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