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 国内在庫あり

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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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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. This compound is more selective and shows 27-fold more potent than InsR at the cellular level. It 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. This chemical also reduces the level of phospho-IGF-1R and phospho-PKB in NWT-21 cells. [1] It shows growth inhibitory effect on TC-71 musculoskeletal sarcoma cells in low-serum medium as well as in 10% FBS–containing medium. This compound 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] It 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. This compound-driven inhibition of IGF-1R causes a reduction of phosphorylation of Akt, but not of Erk1 and Erk2 in neuroblastoma cells. [3] It inhibits glioma cell growth and disrupts the autocrine loop initiated by HIF1α stabilization. [4] A recent study shows that this chemical suppresses the proliferation and viability of PC3, DU145, and 22Rv1 prostate cancer cells, without necessarity of associated cell death. It 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 this compound with essential Akt. This compound-induced radiosensization is dependent on Akt activation status. It 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 this compound 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 this compound 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] This compound (50 mg/kg) causes tumor shrinkage in both HTLA-230 and SK-N-BE2c xenografts, without signs of systemic toxicity. It 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
  • https://pubmed.ncbi.nlm.nih.gov/15050915/
  • https://pubmed.ncbi.nlm.nih.gov/15867386/
  • https://pubmed.ncbi.nlm.nih.gov/17121898/
  • https://pubmed.ncbi.nlm.nih.gov/20488164/
  • http://www.ncbi.nlm.nih.gov/m/pubmed/21816290/

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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