NVP-AEW541

For research use only.

Catalog No.S1034 Synonyms: AEW541

53 publications

NVP-AEW541 Chemical Structure

CAS No. 475489-16-8

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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Selleck's NVP-AEW541 has been cited by 53 publications

Purity & Quality Control

Choose Selective IGF-1R Inhibitors

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)
FLT1 [1]
(Cell-free assay)
0.14 μM 0.15 μM 0.42 μM 0.53 μM 0.6 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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NWT-21 MYXLbY5ie2ViYYPzZZk> MUX+NVDjiIsQvF2= MWfEUXNQ MVnpcohq[mm2czDJS2YuUVJid3n0bEBKSzVyIH;mJFAvODh4INMxJFAvODJ6IN88US=> NY\ITXNFOTVyNUC5NVU>
A14 M4HCdmtqdmG|ZTDhd5NigQ>? M37wO54yOOLCit88US=> MkXDSG1UVw>? NG\xWGhqdmirYnn0d{BKdnOUIIfpeIghUUN3MDDv[kAzNjNiwsGgNE4yPjNizszN MnnyNVUxPTB7MUW=
A431  MoXMT4lv[XOnIHHzd4F6 M4r3PJ4yOOLCit88US=> MWfEUXNQ MYfpcohq[mm2czDISXIyKHerdHigTWM2OCCxZjC+NVAh|ryP NWLt[5JUOTVyNUC5NVU>
A31  NIOzUWpMcW6jc3WgZZN{[Xl? NX3u[FBPhjFy4pEK{txO MWHEUXNQ MkTTbY5pcWKrdIOgVGRITlJid3n0bEBKSzVyIH;mJF4yOCEQvF2= MX[xOVA2ODlzNR?=
GIST882 NUPmb4h6U2mwYYPlJIF{e2G7 MWj+NVDjiIsQvF2= M2XNfWROW09? MoPobY5pcWKrdIOgZ{1McXRid3n0bEBKSzVyIH;mJF42KM7:TR?= NUDtSZZKOTVyNUC5NVU>
32D-Bcr-Abl NF\RcIlMcW6jc3WgZZN{[Xl? M3npdJ4yOOLCit88US=> NYTCSoM2TE2VTx?= MmLsbY5pcWKrdIOgRoNzNUGkbDDwNlExKHerdHigTWM2OCCxZjC+NVAh|ryP NWD1U4R{OTVyNUC5NVU>
MCF-7  NH76epBEgXSxeHnjbZR6KGG|c3H5 NUjWUZhnTE2VTx?= M1rx[mlEPTB;MT62OEDPxE1? M3fhVVE2ODVyOUG1
NWT-21 M3XLXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWDEUXNQ M{f4SWlEPTB;MD6xOlMh|ryP MVOxOVA2ODlzNR?=
TC-71 MmSzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFPBb2t,OSEQvF2= MWfEUXNQ MULpcohq[mm2czDpcpN2dGmwLXzpb4Uh\3Kxd4ToJIZi[3Sxcj3J5qCUdWWmaXH0[YQh\3Kxd4To NW\kTpViOTV6NkezPFY>
TC-71 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFPMbnh,P+LCit88US=> MoDySG1UVw>? MUHJR|UxRDBwNTFOwG0> M1PtWVE2QDZ5M{i2
Saos-2 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnX0glfjiIsQvF2= Mme1SG1UVw>? NFvyXmxKSzVyPEOg{txO NWL5WGVDOTV6NkezPFY>
U-2OS MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2DQWJ446oDMzszN MlTpSG1UVw>? MXfJR|UxRDBwNTFOwG0> NYGyRVlQOTV6NkezPFY>
SK-ES-1 NXfMXoZPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUn+O-KBks7:TR?= NGHxdm9FVVOR MoLKTWM2ODxyLkWg{txO MUexOVg3PzN6Nh?=
SK-N-MC MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHLmSXR,P+LCit88US=> MVnEUXNQ MmC3TWM2ODxyLkWg{txO MmC4NVU5Pjd|OE[=
RD-ES NHrkRW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3TqUp446oDMzszN MV;EUXNQ MV7JR|UxRDBwNTFOwG0> NYnVfFA1OTV6NkezPFY>
SJ-Rh 30 MkezS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXv+O-KBks7:TR?= NXrLe4J{TE2VTx?= MlH1TWM2ODxyLkWg{txO NXHlbZBWOTV6NkezPFY>
SJ-Rh 4 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MU\+O-KBks7:TR?= NFm2[lZFVVOR NGLHTGpKSzVyPECuOUDPxE1? M{DuXVE2QDZ5M{i2
6647 M{Lx[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVXlOlFthjgkgJtOwG0> MUfEUXNQ NWnSPWRqUUN3MEywMlUh|ryP MYmxOVg3PzN6Nh?=
SARG NGT1UGJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3fuSJ446oDMzszN NI\ZeWxFVVOR NVjYWXVsUUN3MEyzJO69VQ>? NIPjbHIyPTh4N{O4Oi=>
MOS M3ewOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4\qZp446oDMzszN Mof5SG1UVw>? MkPoTWM2ODx2IN88US=> MoH2NVU5Pjd|OE[=
IOR/OS7 NEfLPXpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH\CRY9,P+LCit88US=> Mor2SG1UVw>? NFjqe|VKSzVyPEGg{txO MmPLNVU5Pjd|OE[=
IOR/OS9 MoTIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlvHglfjiIsQvF2= NVfoNnQxTE2VTx?= MYHJR|UxRDZizszN MkTRNVU5Pjd|OE[=
IOR/OS10 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4jQdJ446oDMzszN MUHEUXNQ Ml\hTWM2ODx3IN88US=> MUSxOVg3PzN6Nh?=
IOR/OS14 NULM[IJST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1vz[p446oDMzszN MnLzSG1UVw>? MWXJR|UxRDRizszN MkjmNVU5Pjd|OE[=
LAP35 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{LJVp446oDMzszN NX\Memo1TE2VTx?= MXHJR|UxRDBwNTFOwG0> MkHQNVU5Pjd|OE[=
IOR/BRZ NX3kO3lYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXjzU3NQhjgkgJtOwG0> NYTvVpZKTE2VTx?= MU\JR|UxRDBwNTFOwG0> M3Xv[|E2QDZ5M{i2
IOR/CAR MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYX+O-KBks7:TR?= MlrBSG1UVw>? NES3[49KSzVyPEGg{txO NE\GVlQyPTh4N{O4Oi=>
IOR/NGR NX\p[nVXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGTteoF,P+LCit88US=> NVfzSWZ7TE2VTx?= NGfO[ppKSzVyPECuOUDPxE1? MnrMNVU5Pjd|OE[=
IOR/RCH M4XMd2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoD6glfjiIsQvF2= M{K3e2ROW09? M1;aU2lEPTB:MD61JO69VQ>? NVPwOXVHOTV6NkezPFY>
RMZ-RC2 NFTEN4RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NILVfYN,P+LCit88US=> NVjXSmRETE2VTx?= M3n6[WlEPTB:MD61JO69VQ>? NUjxbJFkOTV6NkezPFY>
CCA NXe2b|dZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXz+O-KBks7:TR?= NUO1OHpSTE2VTx?= Mn;5TWM2ODx{IN88US=> M2i1WFE2QDZ5M{i2
RD/18 NF3scW9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXn+O-KBks7:TR?= MVTEUXNQ Mnf3TWM2ODx2IN88US=> MX6xOVg3PzN6Nh?=
OVCAR-3 NWS2flg4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGnWXm5,OTYkgJtOwG0> NEn6SVlFVVOR NX6wNo1[cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M4rmR|E3OzByOEKw
OVCAR-4 MoXHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVHEPWpyhjF34pEK{txO NUexNJhyTE2VTx?= NXfqbYpucW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v Mof1NVY{ODB6MkC=
OVCAR-3 NYLT[HdISXCxcITvd4l{KGG|c3H5 Mk\yglE26oDMzszN M{LZ[2ROW09? M{[xXIlv\HWlZYOgZZBweHSxc3nz MYixOlMxODh{MB?=
OVCAR-4 NFvV[2lCeG:ydH;zbZMh[XO|YYm= MlX0glE26oDMzszN MWTEUXNQ NWXxN293cW6mdXPld{BieG:ydH;zbZM> M3zGVlE3OzByOEKw
OVCAR-3 MYfGeY5kfGmxbjDhd5NigQ>? NVu5UWt6hjF34pEK{txO M2LZZ2ROW09? MXzE[YNz\WG|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? M373PFE3OzByOEKw
Huh-7 NFr2doZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFzaXmh,OTEkgJtOwG0> MUnEUXNQ MlW3TWM2OD1zLkSg{txO NXHsVIE4OTZ3M{C3N|Q>
Hep-G2 MnjNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWT+NVDjiIsQvF2= M2LYN2ROW09? MYrJR|UxRTFwODFOwG0> M2PsZ|E3PTNyN{O0
Hep-3B Mlq3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHjHZ4J,OTEkgJtOwG0> M3zUPWROW09? NEPIXXVKSzVyPUGuPUDPxE1? MYCxOlU{ODd|NB?=
SK-Hep-1 MlzhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYL+NVDjiIsQvF2= Mm\PSG1UVw>? MWDJR|UxRTZwOTFOwG0> MlnqNVY2OzB5M{S=
Huh-7 NYPIeY5STnWwY4Tpc44h[XO|YYm= NFr3SYZ,OTEkgJtOwG0> NILZRYVFVVOR NYrK[HRHUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MYOxOlU{ODd|NB?=
Hep-G2 MmD2SpVv[3Srb36gZZN{[Xl? NIfMbHh,OTEkgJtOwG0> MWTEUXNQ NHHRdo5KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NWqxU5R5OTZ3M{C3N|Q>
SK-Hep-1 M33yb2Z2dmO2aX;uJIF{e2G7 Ml;iglEx6oDMzszN NEfkXYZFVVOR Ml6yTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NFjTcHMyPjV|MEezOC=>
BON M3;ydGtqdmG|ZTDhd5NigQ>? NIXocHJ,PiEQvF2= MWfEUXNQ NGLBWplqdmS3Y3XzJIRmeGixc4Doc5J6dGG2aX;uJI9nKEmJRj2xVi=> MorjNVY3ODF{OES=
BON MnXhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnrYglEx6oDMzszN NYH0d4I6TE2VTx?= MmLrTWM2OD14Lk[g{txO NYrjUJRqOTZ4MEGyPFQ>
CM MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlvaglXjiIsQvF2= NWXOWWZ7TE2VTx?= MUjJR|UxRTNwMzFOwG0> NV7nRmFWOTZ4MEGyPFQ>
BON NUPqZmRJTnWwY4Tpc44h[XO|YYm= NXrDPW9FhjdwNfMAju69VQ>? NUX1R5lJTE2VTx?= M1HFN4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MWCxOlYxOTJ6NB?=
CM Mm\1SpVv[3Srb36gZZN{[Xl? M2TMcZ426oDMzszN M3zaeWROW09? NVy0NpNlcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NYDqSJgyOTZ4MEGyPFQ>
BON NYjhSmNrSXCxcITvd4l{KGG|c3H5 M2DRW544NjYkgJtOwG0> NGHEcXBFVVOR NUPseoF7cW6mdXPld{BCeG:ydH;zbZM> NVXWfWprOTZ4MEGyPFQ>
CM NUjZeWZOSXCxcITvd4l{KGG|c3H5 Mm\sglXjiIsQvF2= MUDEUXNQ MlrHbY5lfWOnczDBdI9xfG:|aYO= Mn:xNVY3ODF{OES=
HT-29 MlOwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NE\HU2R,OTEkgJtOwG0> MkDSSG1UVw>? MYLJR|UxRTFwNzFOwG0> MYixO|AxPzBzNR?=
HCT-116 M2jGV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHnk[|J,OTEkgJtOwG0> M33SUGROW09? MlftTWM2OD1{LkWg{txO MVexO|AxPzBzNR?=
primary colorectal cancer cells MWTGeY5kfGmxbjDhd5NigQ>? MV\+OgKBks7:TR?= MXrEUXNQ M{\ZSYFtfGW{czD0bIUhdW:{cHjvcI9ogSCxZjD0bIUhemWvYXnubY5oKGOnbHzz M2XlflE4ODB5MEG1
HTLA-230 NEPuXnlHfW6ldHnvckBie3OjeR?= NWP0flFjhjhizszN M4\5dmROW09? NY\JUIYycW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MYixO|EzOTh7OB?=
KCNR MonHSpVv[3Srb36gZZN{[Xl? NYj3W|NphjhizszN MmnSSG1UVw>? MWHpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= M2HoT|E4OTJzOEm4
SK-N-BE2c MX7GeY5kfGmxbjDhd5NigQ>? M2jqfp45KM7:TR?= NXPrS|B6TE2VTx?= MULpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NXfWXmdDOTdzMkG4PVg>
SK-N-BE MUnGeY5kfGmxbjDhd5NigQ>? MVr+PEDPxE1? NFH5WXhFVVOR Mn;rbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NWX6fnVrOTdzMkG4PVg>
LAN-5 MnjSSpVv[3Srb36gZZN{[Xl? NEf1Uml,QCEQvF2= NUHUdXh7TE2VTx?= M3fENolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> M3\JclE4OTJzOEm4
GI-CA-N MkWzSpVv[3Srb36gZZN{[Xl? M33mc545KM7:TR?= M{[z[2ROW09? MYTpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NXzLdlM5OTdzMkG4PVg>
SH-EP M175c2Z2dmO2aX;uJIF{e2G7 MlPoglgh|ryP M3nK[2ROW09? NHK1SlZqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M1v5PVE4OTJzOEm4
SK-N-AS MVzGeY5kfGmxbjDhd5NigQ>? Mnixglgh|ryP NH[1RpNFVVOR MlfIbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 M4PETVE4OTJzOEm4
RN-GA M2TDVGZ2dmO2aX;uJIF{e2G7 NXzvTmNUhjhizszN M4nyU2ROW09? NVX1UXRqcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MkjTNVcyOjF6OUi=
SY-5Y(N) NHW1WIhHfW6ldHnvckBie3OjeR?= MXz+PEDPxE1? NE\SVI5FVVOR NYLyXIcxcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MUKxO|EzOTh7OB?=
GI-CA-N M{H1OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1\MfJ45KM7:TR?= M4\jZWROW09? M333R2lEPTB;IE[uPEDPxE1? MnjJNVcyOjF6OUi=
SH-EP MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVn+PEDPxE1? MV;EUXNQ MofRTWM2OD1iMzFOwG0> MorzNVcyOjF6OUi=
HTLA-230 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYH+PEDPxE1? MmL2SG1UVw>? M4rPeGlEPTB;IECuOUDPxE1? MWGxO|EzOTh7OB?=
SK-N-BE2c NGnPdYVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mkjjglgh|ryP MWHEUXNQ M3LHRWlEPTB;IEGuNUDPxE1? Mo[1NVcyOjF6OUi=
SK-N-BE2 NXnVUoNpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MY\+PEDPxE1? NETi[o9FVVOR MX;JR|UxRSB|IN88US=> M2LXcVE4OTJzOEm4
SY-5Y (N) M3jnXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlG1glgh|ryP MmD1SG1UVw>? MXvJR|UxRSB{LkSg{txO NXLETpF{OTdzMkG4PVg>
LAN-5 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWXP[|BLhjhizszN MYDEUXNQ M2XTS2lEPTB;IECuOEDPxE1? M2XpOFE4OTJzOEm4
KCNR NW\oNoVHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmPjglgh|ryP NUDwO3VuTE2VTx?= NYP0c3M6UUN3ME2gNE41KM7:TR?= NILmU|IyPzF{MUi5PC=>
RN-GA M13lZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVT+PEDPxE1? MYXEUXNQ MmT3TWM2OD1iMT6zJO69VQ>? MXWxO|EzOTh7OB?=
SK-N-AS NYrCe5ptT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYD+PEDPxE1? Ml25SG1UVw>? NVjZXpNscW6mdXPld{BieG:ydH;zbZM> M3;VZ|E4OTJzOEm4
KCNR NHHhfGlCeG:ydH;zbZMh[XO|YYm= M1XFWp45KM7:TR?= MXXEUXNQ M2TPPYlv\HWlZYOgZZBweHSxc3nz NYXMN2tnOTdzMkG4PVg>
GI-CA-N M2LVXWFxd3C2b4Ppd{Bie3OjeR?= NYnqR3lChjhizszN NXTObI5KTE2VTx?= MkP1bY5lfWOnczDhdI9xfG:|aYO= MnniNVcyOjF6OUi=
HTLA-230 M4fSPGFxd3C2b4Ppd{Bie3OjeR?= M1fRdZ45KM7:TR?= NInjNYNFVVOR M3vwbolv\HWlZYOgZZBweHSxc3nz NUPNOJFrOTdzMkG4PVg>
SK-N-BE2c Ml23RZBweHSxc3nzJIF{e2G7 MUT+PEDPxE1? NH;Je5NFVVOR Mme2bY5lfWOnczDhdI9xfG:|aYO= NWLKTpBsOTdzMkG4PVg>
SY-5Y (N) M{j6bWFxd3C2b4Ppd{Bie3OjeR?= NWnud5V2hjhizszN MVTEUXNQ MULpcoR2[2W|IHHwc5B1d3Orcx?= MWmxO|EzOTh7OB?=
HL60AR MWrGeY5kfGmxbjDhd5NigQ>? MoHtNVYxKG6P NXTMS4Vs\W6qYX7j[ZMhfGinIHzleoVteyCxZjDwNldMcXBz NV3CcZd5OTd|NkGyNlU>
HL60AR NUHse3BTSXCxcITvd4l{KGG|c3H5 NH\PeJR,OjByIH7N M2HjbIlv\HWlZYOgZZBweHSxc3nz NGHrNWkyPzN4MUKyOS=>
HPAF-II NX;Wd|VKU2mwYYPlJIF{e2G7 MXj+NUDPxE1? MmnKSG1UVw>? M{WxfIlvcGmkaYTzJGlITi2LLX3l[IlifGWmIIPp[45idGyrbne= M4jHVlE5PDR3NUKw
HPAF-II M2LhOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3nzWZ4zKM7:TR?= NHrUOnJFVVOR NV;iWWk4cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MnzBNVg1PDV3MkC=
HPAF-II MojLSpVv[3Srb36gZZN{[Xl? M2HTWp4zKM7:TR?= NIDMXJlFVVOR NVfhSGVOcW6qaXLpeJMh[mG|YXygZY5lKEmJRj3JMY1m\GmjdHXkJJBidmO{ZXH0bYMh[2GwY3XyJINmdGxibXnndoF1cW:w MW[xPFQ1PTV{MB?=
TFK-1 M{TQXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGexTlJ,OjVyIH7N NHzKSlNFVVOR M4HUe2lEPTB;MD6yOkDPxE1? NGLu[HAzODB4NkezOC=>
EGI-1 NEXmUmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkjBglI2OCCwTR?= NYjjXphSTE2VTx?= NGTzWnVKSzVyPUCuNlgh|ryP M3PlXVIxODZ4N{O0
CC-LP-1 NG[yeXJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUPzZoozhjJ3MDDuUS=> NFqwcoRFVVOR NGrFWGtKSzVyPUCuNVUh|ryP MXGyNFA3Pjd|NB?=
CC-SW-1 Mle0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVX+NlUxKG6P MoXuSG1UVw>? M2LlOWlEPTB;MD61OEDPxE1? M1n0WVIxODZ4N{O0
Sk-ChA-1 NVLUVnByT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlnNglI2OCCwTR?= NXv0eHJkTE2VTx?= Ml;JTWM2OD1yLkKg{txO MX6yNFA3Pjd|NB?=
Mz-ChA-1 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1W2cJ4zPTBibl2= NInvTYZFVVOR MkPETWM2OD1zLkO5JO69VQ>? MVSyNFA3Pjd|NB?=
Mz-ChA-2 NXzSSnhMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVL+NlUxKG6P M3\hZWROW09? NYPHS|BqUUN3ME2wMlc{KM7:TR?= MmPBNlAxPjZ5M{S=
ECC-1 NHnJeVZMcW6jc3WgZZN{[Xl? M2[5NZ4yOCEQvF2= M2TxUGROW09? MYTpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6QCV? Mn;NNlEzQTV|M{W=
Ishikawa Mme4T4lv[XOnIHHzd4F6 M4ntOp4yOCEQvF2= NHnMVlhFVVOR MlXXbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQTNn MW[yNVI6PTN|NR?=
USPC-1 MnLTT4lv[XOnIHHzd4F6 MVT+NVAh|ryP M4fq[WROW09? M1Tvc4lvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDFyMDW= NGH0N5AzOTJ7NUOzOS=>
USPC-2 Mn7aT4lv[XOnIHHzd4F6 M4Doc54yOCEQvF2= NX3NOVRETE2VTx?= NWKycGI2cW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOU[l MXWyNVI6PTN|NR?=
ECC-1 NXvrUmNDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoLqglExKM7:TR?= MVTEUXNQ NFfnfodl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v NVjCNmxnOjF{OUWzN|U>
Ishikawa M4rWeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIDHc3F,OTBizszN M{jpb2ROW09? M4HmO4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NYLGelFMOjF{OUWzN|U>
USPC-1 NXvWWnVxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHzYUpJ,OTBizszN NEnQUmNFVVOR NFftNpNl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MXyyNVI6PTN|NR?=
USPC-2 Ml;US5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnrUglExKM7:TR?= NE\6O|FFVVOR MYfk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MVWyNVI6PTN|NR?=

... 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]

Protocol

Kinase Assay:[1]
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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 Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female Harlan athymic nude mice weighing 18-25 g with NWT-21 cells
  • Dosages: 20, 30, or 50 mg/kg
  • Administration: Administered via p.o. twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (200.2 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
20 mg/mL

* 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 Information

Molecular Weight 439.55
Formula

C27H29N5O

CAS No. 475489-16-8
Storage powder
in solvent
Synonyms AEW541
Smiles C1CN(C1)CC2CC(C2)N3C=C(C4=C(N=CN=C43)N)C5=CC(=CC=C5)OCC6=CC=CC=C6

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID