NVP-AEW541

Catalog No.S1034

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.

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NVP-AEW541 Chemical Structure

NVP-AEW541 Chemical Structure
Molecular Weight: 439.55

Validation & Quality Control

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Quality Control & MSDS

IGF-1R Inhibitors with Unique Features

  • Pan IGF-1R Inhibitor

    GSK1904529A Dual IGF-1R/IR inhibitor, IC50=27 nM/25 nM.

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  • IGF-1R Inhibitor in Clinical Trial

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  • Newest IGF-1R Inhibitor

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Product Information

  • Compare IGF-1R Inhibitors
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  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

Description 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)

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IC50 0.14 μM 0.15 μM 0.42 μM 0.53 μM
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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
NWT-21NX;2OFNPU2mwYYPlJIF{e2G7M{HB[Z4yOOLCit88US=>MXHEUXNQNIi5WYhqdmirYnn0d{BKT0ZvSWKge4l1cCCLQ{WwJI9nKDBwMEi2JOKyKDBwMEK4JO69VQ>?Mn3LNVUxPTB7MUW=
A14M17we2tqdmG|ZTDhd5NigQ>?M{LQRZ4yOOLCit88US=>NVvL[Fk5TE2VTx?=NFX5S3JqdmirYnn0d{BKdnOUIIfpeIghUUN3MDDv[kAzNjNiwsGgNE4yPjNizszNNWW2UW5NOTVyNUC5NVU>
A431 NYHHSYIxU2mwYYPlJIF{e2G7NVfuO4lohjFy4pEK{txONFjBeplFVVORMX3pcohq[mm2czDISXIyKHerdHigTWM2OCCxZjC+NVAh|ryPNWO1XYptOTVyNUC5NVU>
A31 NYXteFJmU2mwYYPlJIF{e2G7MVX+NVDjiIsQvF2=MkXPSG1UVw>?M1X2TYlvcGmkaYTzJHBFT0[UIIfpeIghUUN3MDDv[kA,OTBizszNNWe0ToNwOTVyNUC5NVU>
GIST882MkO4T4lv[XOnIHHzd4F6M4j5e54yOOLCit88US=>Mm\6SG1UVw>?NFzr[nFqdmirYnn0d{BkNUurdDD3bZRpKEmFNUCgc4YhRjVizszNM1L0elE2ODVyOUG1
32D-Bcr-AblNVPYSFhIU2mwYYPlJIF{e2G7NHP0U5l,OTEkgJtOwG0>M3zTcmROW09?MVTpcohq[mm2czDCZ5IuSWKuIICyNVAhf2m2aDDJR|UxKG:oIE6xNEDPxE1?NUKzcWNNOTVyNUC5NVU>
MCF-7 Ml;kR5l1d3irY3n0fUBie3OjeR?=NXO1Rot1TE2VTx?=MnPFTWM2OD1zLk[0JO69VQ>?M{\4c|E2ODVyOUG1
NWT-21MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?NG\iSHNFVVORMYjJR|UxRTBwMU[zJO69VQ>?NUW2S4g{OTVyNUC5NVU>
TC-71NYTJbpV1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=NEfXSYZ,OSEQvF2=MUHEUXNQMm\XbY5pcWKrdIOgbY5{fWyrbj3sbYtmKGe{b4f0bEBn[WO2b4KtTgKBm22nZHnheIVlKGe{b4f0bC=>MWCxOVg3PzN6Nh?=
TC-71NF7pbnhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=MmrOglfjiIsQvF2=NEPEfnVFVVORM{\VZ2lEPTB:MD61JO69VQ>?Mn:yNVU5Pjd|OE[=
Saos-2Mnj6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?NWfqVnZNhjgkgJtOwG0>Mk[wSG1UVw>?NGroWlZKSzVyPEOg{txOM3vKVVE2QDZ5M{i2
U-2OSM2i4VWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7NUHYTFlJhjgkgJtOwG0>MoXYSG1UVw>?M4fEcGlEPTB:MD61JO69VQ>?NWLVeGZwOTV6NkezPFY>
SK-ES-1NX3GNWVFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=M{PIcp446oDMzszNNFrDeW9FVVORNInDfGVKSzVyPECuOUDPxE1?NFj3TmYyPTh4N{O4Oi=>
SK-N-MCNV[0T|RUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=NInPcFV,P+LCit88US=>MYfEUXNQNWfuNXY{UUN3MEywMlUh|ryPNIjSS5MyPTh4N{O4Oi=>
RD-ESMonUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?MXP+O-KBks7:TR?=MnHPSG1UVw>?M1nKbmlEPTB:MD61JO69VQ>?MmTpNVU5Pjd|OE[=
SJ-Rh 30M4m0V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7NE[zNlJ,P+LCit88US=>MnrESG1UVw>?M3PFTmlEPTB:MD61JO69VQ>?M{ns[VE2QDZ5M{i2
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MOSM{XROGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7M{fpZ5446oDMzszNNHradZBFVVORNEn1bmlKSzVyPESg{txOMVKxOVg3PzN6Nh?=
IOR/OS7M{LYbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7NVHkdIJ7hjgkgJtOwG0>MXfEUXNQMUnJR|UxRDFizszNM{XWTlE2QDZ5M{i2
IOR/OS9MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?MmL4glfjiIsQvF2=MULEUXNQM3rLWGlEPTB:NjFOwG0>NInPV3AyPTh4N{O4Oi=>
IOR/OS10NUHtcYJXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=M1faZ5446oDMzszNMVPEUXNQMUfJR|UxRDVizszNMYKxOVg3PzN6Nh?=
IOR/OS14NXOySIlET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=M3zjVJ446oDMzszNM1rzcGROW09?M2Xud2lEPTB:NDFOwG0>NXflXpQ1OTV6NkezPFY>
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primary colorectal cancer cellsNH7JV4xHfW6ldHnvckBie3OjeR?=NUHSWWZjhjYkgJtOwG0>MoTMSG1UVw>?NY\BPJR1[Wy2ZYLzJJRp\SCvb4LwbI9td2e7IH;mJJRp\SC{ZX3hbY5qdmdiY3XscJM>M2K4[FE4ODB5MEG1
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SK-N-BENUDMcoNpTnWwY4Tpc44h[XO|YYm=NXuyXGtkhjhizszNNVewZnp3TE2VTx?=MXfpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S=M2fKPFE4OTJzOEm4
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SK-N-ASMmn1SpVv[3Srb36gZZN{[Xl?NIXLOol,QCEQvF2=NF3nNGlFVVORNXO2coFScW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1MYKxO|EzOTh7OB?=
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SY-5Y(N)NXKxb5lSTnWwY4Tpc44h[XO|YYm=M1HreZ45KM7:TR?=NVXwZ|Z6TE2VTx?=NYLLT5dycW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1NG\qVWwyPzF{MUi5PC=>
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SK-N-BE2cM1PldGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7M4TrNZ45KM7:TR?=NIW4dFRFVVORMYrJR|UxRSBzLkGg{txONHnUcHoyPzF{MUi5PC=>
SK-N-BE2MlS3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?NF6zS4x,QCEQvF2=NInUTXJFVVORNVT4U|IyUUN3ME2gN{DPxE1?M{CyN|E4OTJzOEm4
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RN-GAM{HDOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7MWf+PEDPxE1?NEHFN2pFVVORM1XHbWlEPTB;IEGuN{DPxE1?NFnGRXYyPzF{MUi5PC=>
SK-N-ASMYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?Mnizglgh|ryPMVfEUXNQM1y5V4lv\HWlZYOgZZBweHSxc3nzMnjvNVcyOjF6OUi=
KCNRMmnlRZBweHSxc3nzJIF{e2G7NXPqd4VkhjhizszNM3zGW2ROW09?M3fYXolv\HWlZYOgZZBweHSxc3nzM1vNTVE4OTJzOEm4
GI-CA-NM1\GVGFxd3C2b4Ppd{Bie3OjeR?=NEDRd2x,QCEQvF2=M{n1OmROW09?Mo\wbY5lfWOnczDhdI9xfG:|aYO=NXHUTnU5OTdzMkG4PVg>
HTLA-230MWDBdI9xfG:|aYOgZZN{[Xl?NIr0VY9,QCEQvF2=MUjEUXNQMV;pcoR2[2W|IHHwc5B1d3Orcx?=MYCxO|EzOTh7OB?=
SK-N-BE2cNF\1VlJCeG:ydH;zbZMh[XO|YYm=MlvLglgh|ryPMlfCSG1UVw>?MXXpcoR2[2W|IHHwc5B1d3Orcx?=M33IflE4OTJzOEm4
SY-5Y (N)MnvIRZBweHSxc3nzJIF{e2G7NH7heVZ,QCEQvF2=NUe4W5g3TE2VTx?=NYXrTIx1cW6mdXPld{BieG:ydH;zbZM>NXfub2IzOTdzMkG4PVg>
HL60ARMXLGeY5kfGmxbjDhd5NigQ>?MUCxOlAhdk1?MV3lcohidmOnczD0bIUhdGW4ZXzzJI9nKHB{N1vpdFE>M2LhcVE4OzZzMkK1
HL60ARMVHBdI9xfG:|aYOgZZN{[Xl?MkHQglIxOCCwTR?=NV3iOZhEcW6mdXPld{BieG:ydH;zbZM>NEnzeYMyPzN4MUKyOS=>
HPAF-IIMX7LbY5ie2ViYYPzZZk>M1\IXJ4yKM7:TR?=MWnEUXNQNH\re3JqdmirYnn0d{BKT0ZvST3t[YRq[XSnZDDzbYdv[WyuaX7nNWPJSVI3OTh2NEW1NlA>
HPAF-IIMlW0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?Mnj4glIh|ryPMnPoSG1UVw>?MVvpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36=NH\sVHoyQDR2NUWyNC=>
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... Click to View More Cell Line Experimental Data

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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Cell Assay: [1]

Cell lines MCF-7 cells
Concentrations ~ 10 μM
Incubation Time 72 hours
Method 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.

Animal Study: [1]

Animal Models Female Harlan athymic nude mice weighing 18-25 g with NWT-21 cells
Formulation Dissolved in 25 mM L(+)-tartaric acid
Dosages 20, 30, or 50 mg/kg
Administration Administered via p.o. twice daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] García-Echeverría C, et al. Cancer Cell. 2004, 5(3), 231-239.

[2] Scotlandi K, et al. Cancer Res, 2005, 65(9), 3868-3876.

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Chemical Information

Download NVP-AEW541 SDF
Molecular Weight (MW) 439.55
Formula

C27H29N5O

CAS No. 475489-16-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms AEW541
Solubility (25°C) * In vitro DMSO 88 mg/mL (200.2 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 20 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 7-((1s,3s)-3-(azetidin-1-ylmethyl)cyclobutyl)-5-(3-(benzyloxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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