ホームページ Protein Tyrosine Kinase IGF-1R inhibitor NVP-AEW541 For research use only.

NVP-AEW541

別名：AEW541

NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, greater potency and selectivity for IGF-1R in a cell-based assay.

NVP-AEW541化学構造

CAS No. 475489-16-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 37900 国内在庫あり
JPY 20400 国内在庫あり
JPY 32300 国内在庫あり
JPY 47700 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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NVP-AEW541関連製品

シグナル伝達経路

IGF-1R Signaling Pathways

IGF-1Rシグナル伝達経路

IGF-1R阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
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生物活性

製品説明 NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, greater potency and selectivity for IGF-1R in a cell-based assay.
Targets
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)		 もっとクリックする
0.14 μM 0.15 μM 0.42 μM 0.53 μM 0.6 μM
In Vitro
In vitro NVP-AEW541 also inhibits InsR, Tek, Flt1 and Flt3 with IC50 of 140 nM, 530 nM, 600 nM and 420 nM in purified kinases/recombinant kinase domains assay. NVP-AEW541 is more selective and shows 27-fold more potent than InsR at the cellular level. NVP-AEW541 suppresses the IGF-I-mediated survival, soft agar and proliferation of MCF-7 cells with IC50 of 0.162 μM, 0.105 μM and 1.64 μM, respectively. NVP-AEW541 also reduces the level of phospho-IGF-1R and phospho-PKB in NWT-21 cells. [1] NVP-AEW541 shows growth inhibitory effect on TC-71 musculoskeletal sarcoma cells in low-serum medium as well as in 10% FBS–containing medium. NVP-AEW541 inhibits cell cycle progression and induces specific G1 arrest in sarcoma cell lines (TC-71, SK-N-MC, SaoS-2, RD/18 and RH4). [2] NVP-AEW541 could inhibit the growth of human neuroblastoma cells with IC50 of 0.4-6.8 μM. An increase in the hypodiploid fraction and the depletion of the S and G2-M compartments could be detected in these cell lines. NVP-AEW541-driven inhibition of IGF-1R causes a reduction of phosphorylation of Akt, but not of Erk1 and Erk2 in neuroblastoma cells. [3] NVP-AEW541 inhibits glioma cell growth and disrupts the autocrine loop initiated by HIF1α stabilization. [4] A recent study shows that NVP-AEW541 suppresses the proliferation and viability of PC3, DU145, and 22Rv1 prostate cancer cells, without necessarity of associated cell death. NVP-AEW541 decreases phospho-Akt levels in 22Rv1 and DU415 cells but not PC3 cells, without affecting total Akt levels, which shows that PTEN status could determine the effectiveness of NVP-AEW541 with essential Akt. NVP-AEW541-induced radiosensization is dependent on Akt activation status. NVP-AEW541 could increase the H2AX phosphorylation (a measure of DSBs) in PC3, DU145, and 22Rv1 cells. [5]
Kinase Assay In vitro kinase assays
NVP-AEW541 is dissolved in DMSO (10 mM) and stored at -20 °C. Dilutions are freshly made in DMSO/water 1:1. The final concentration of DMSO in the enzyme assays is <0.5 %. The protein kinase assays are carried out in 96-well plates at RT and terminated by the addition of 20 μL of 125 mM EDTA. Subsequently, 30 μL (c-Abl, c-Src, IGF-1R) of the reaction mixture are transferred onto Immobilon-PVDF presoaked for 5 min with methanol, rinsed with water, then soaked for 5 min with 0.5 % H3PO4 and mounted on vacuum manifold. After spotting all samples, vacuum is connected and each well rinsed with 200 μL 0.5 % H3PO4. Membranes are removed and washed 4× on a shaker with 1.0 % H3PO4, once with ethanol. After drying, mounting in Packard TopCount 96-well frame, and adding of 10 μL/well of Microscint, membranes are counted. IC50 values are calculated by linear regression analysis of the percentage inhibition of NVP-AEW541 in duplicate, at four concentrations (usually 0.01, 0.1, 1, and 10 μM). One unit of protein kinase activity is defined as 1 nmol of 33P transferred from [γ33P]ATP to the substrate protein per minute per mg of protein at 37 °C.
細胞実験 細胞株 MCF-7 cells
濃度 ~ 10 μM
反応時間 72 hours
実験の流れ Between 3 × 103 and 6 × 103 cells/well are seeded in 96-well plates with a total media volume of 100 μL/well. Increasing concentrations of NVP-AEW541 is added 24 hours thereafter in quadruplicate. 72 hours later, cells are fixed by addition of 25 μL/well Glutaraldehyde (20%) and incubation for 10 min at RT. Cells are then washed 2× with 200 μL/well H2O and 100 μL Methylene Blue (0.05%) is added. After incubation for 10 min at RT, cells are washed 3× with 200 μL/well H2O. 200 μL/well HCl (3%) is added, and following incubation for 30 min at RT on a plate shaker, absorbance is measured at 650 nm.
In Vivo
In Vivo NVP-AEW541 (50 mg/kg, p.o.) results in abrogation of basal and IGF-I-induced receptor, and PKB and MAPK phosphorylation, with T/C value of 14% in the NWT-21 tumor xenograft. [1] NVP-AEW541 (50 mg/kg) causes tumor shrinkage in both HTLA-230 and SK-N-BE2c xenografts, without signs of systemic toxicity. NVP-AEW541 could inhibit tumor invasion both in Matrigel-coated chambers and in HTLA-230 xenografts. [3]
動物実験 動物モデル Female Harlan athymic nude mice weighing 18-25 g with NWT-21 cells
投与量 20, 30, or 50 mg/kg
投与経路 Administered via p.o. twice daily

化学情報

分子量 439.55 化学式

C27H29N5O
CAS No. 475489-16-8 SDF Download NVP-AEW541 SDFをダウンロードする
Smiles C1CN(C1)CC2CC(C2)N3C=C(C4=C(N=CN=C43)N)C5=CC(=CC=C5)OCC6=CC=CC=C6
保管

In vitro
Batch:

DMSO : 88 mg/mL ( (200.2 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 24 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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