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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(wú)細(xì)胞試驗(yàn)中IC50為150 nM/140 nM，在細(xì)胞試驗(yàn)中對(duì)IGF-1R具有較高的作用和選擇性。

NVP-AEW541 Chemical Structure

NVP-AEW541 Chemical Structure

CAS: 475489-16-8

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 1875.51 現(xiàn)貨
2mg 876.33 現(xiàn)貨
5mg 1556.1 現(xiàn)貨
10mg 2432.43 現(xiàn)貨
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NVP-AEW541相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

IGF-1R Signaling Pathways

IGF-1R信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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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(wú)細(xì)胞試驗(yàn)中IC50為150 nM/140 nM，在細(xì)胞試驗(yàn)中對(duì)IGF-1R具有較高的作用和選擇性。
靶點(diǎn)
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)		 點(diǎn)擊更多
0.14 μM 0.15 μM 0.42 μM 0.53 μM 0.6 μM
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?yàn)中，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(xì)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(xì)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(xì)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(xì)胞，抑制生長(zhǎng)。NVP-AEW541作用于肉瘤細(xì)胞系(TC-71, SK-N-MC, SaoS-2, RD/18 和 RH4)，抑制細(xì)胞周期進(jìn)展和誘導(dǎo)細(xì)胞周期在G1期停頓。 [2]NVP-AEW541可抑制神經(jīng)母細(xì)胞瘤細(xì)胞生長(zhǎng),IC50為0.4-6.8 μM。在這些細(xì)胞中可以檢測(cè)到亞二倍體片段增多及 S和 G2-M 期細(xì)胞消耗。在神經(jīng)母細(xì)胞瘤細(xì)胞中，NVP-AEW541驅(qū)動(dòng)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(xì)胞生長(zhǎng)，且破壞HIF1α 穩(wěn)定化啟動(dòng)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(xì)胞增殖和活性。NVP-AEW541 作用于22Rv1和 DU415 細(xì)胞而不是PC3細(xì)胞，降低 p-Akt水平，不會(huì)影響整體Akt水平，說(shuō)明PTEN狀態(tài)可決定NVP-AEW541的有效性。NVP-AEW541誘導(dǎo)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(xì)胞，可提高H2AX 磷酸化。[5]
激酶實(shí)驗(yàn) 體外酶法測(cè)定
NVP-AEW541溶解在DMSO(10 mM) 中，儲(chǔ)存在-20oC下。稀釋液在1:1的DMSO/水中現(xiàn)配。在酶法測(cè)定中DMSO的最終濃度<0.5 %。蛋白激酶實(shí)驗(yàn)在96孔板上進(jìn)行，加入20 μl 125 mM EDTA終止反應(yīng)。隨后, 30 μl (c-Abl, c-Src, IGF-1R) 反應(yīng)混合物轉(zhuǎn)移到Immobilon-P轉(zhuǎn)印膜上，加入甲醇預(yù)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(shí)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(jì)數(shù)。通過(guò)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?jǐn)?shù)來(lái)計(jì)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(xì)胞實(shí)驗(yàn) 細(xì)胞系 MCF-7細(xì)胞
濃度 30到300 nM
孵育時(shí)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(zhǎng)培養(yǎng)基中下層包括每孔0.5 ml 細(xì)菌瓊脂。包被培養(yǎng)板，儲(chǔ)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(zhǎng)培養(yǎng)基的0.5ml上層0.4%瓊脂中每孔接種5×103個(gè)MCF-7細(xì)胞。在37oC, 5% CO2環(huán)境下溫育3周后, 細(xì)胞混合, 用結(jié)晶紫染色,計(jì)數(shù)陽(yáng)性菌落(直徑>40 μm),使用KS-400圖像分析系統(tǒng)測(cè)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(dǎo)致基礎(chǔ)型和IGF-I誘導(dǎo)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(méi)有全身毒性跡象。NVP-AEW541作用于Matrigel包被的細(xì)胞和HTLA-230移植瘤，可以抑制腫瘤入侵。[3]
動(dòng)物實(shí)驗(yàn) Animal Models 攜帶NWT-21細(xì)胞的Harlan無(wú)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(xué)信息&溶解度

分子量 439.55 分子式

C27H29N5O
CAS號(hào) 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(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 88 mg/mL ( (200.2 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 24 mg/mL (54.6 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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(jìn)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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