NVP-AEW541

Catalog No.S1034 Synonyms: AEW541

NVP-AEW541 Chemical Structure

Molecular Weight(MW): 439.55

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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Cited by 23 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 NHXVfo1McW6jc3WgZZN{[Xl? M{T4Sp4yOOLCit88US=> MXnEUXNQ MVrpcohq[mm2czDJS2YuUVJid3n0bEBKSzVyIH;mJFAvODh4INMxJFAvODJ6IN88US=> M3fZbVE2ODVyOUG1
A14 MmP0T4lv[XOnIHHzd4F6 MXL+NVDjiIsQvF2= M3\udmROW09? MUDpcohq[mm2czDJcpNTKHerdHigTWM2OCCxZjCyMlMhyrFiMD6xOlMh|ryP NFrmeG4yPTB3MEmxOS=>
A431  MkPnT4lv[XOnIHHzd4F6 NGn4e5h,OTEkgJtOwG0> NVrlUYxxTE2VTx?= Ml3UbY5pcWKrdIOgTGVTOSC5aYToJGlEPTBib3[gQlExKM7:TR?= Ml:2NVUxPTB7MUW=
A31  MkjGT4lv[XOnIHHzd4F6 MoLUglEx6oDMzszN NFzqOWFFVVOR Ml32bY5pcWKrdIOgVGRITlJid3n0bEBKSzVyIH;mJF4yOCEQvF2= MYWxOVA2ODlzNR?=
GIST882 NU\0fFJXU2mwYYPlJIF{e2G7 M2\iXJ4yOOLCit88US=> MVLEUXNQ NIr0NGdqdmirYnn0d{BkNUurdDD3bZRpKEmFNUCgc4YhRjVizszN MVSxOVA2ODlzNR?=
32D-Bcr-Abl MV\LbY5ie2ViYYPzZZk> NF\hTo1,OTEkgJtOwG0> M3myOWROW09? NYXhfVBbcW6qaXLpeJMhSmO{LVHicEBxOjFyIIfpeIghUUN3MDDv[kA,OTBizszN MYmxOVA2ODlzNR?=
MCF-7  MVXDfZRwgGmlaYT5JIF{e2G7 M{nW[2ROW09? MXPJR|UxRTFwNkSg{txO NE\uWZIyPTB3MEmxOS=>
NWT-21 MmPPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3f2c2ROW09? MoPjTWM2OD1yLkG2N{DPxE1? MlzBNVUxPTB7MUW=
TC-71 NXfLUFdkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFvMWG1,OSEQvF2= MXzEUXNQ MmLybY5pcWKrdIOgbY5{fWyrbj3sbYtmKGe{b4f0bEBn[WO2b4KtTgKBm22nZHnheIVlKGe{b4f0bC=> MkjjNVU5Pjd|OE[=
TC-71 NU\FS3BST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3ToWp446oDMzszN Moi5SG1UVw>? NFy5e4pKSzVyPECuOUDPxE1? NYT1flZEOTV6NkezPFY>
Saos-2 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGT1XHh,P+LCit88US=> M2mwd2ROW09? MknjTWM2ODx|IN88US=> MmjkNVU5Pjd|OE[=
U-2OS M2XtNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlTIglfjiIsQvF2= M3HlbGROW09? MmXmTWM2ODxyLkWg{txO NYjJbVlKOTV6NkezPFY>
SK-ES-1 NWfhNVhuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2jYcJ446oDMzszN MoPhSG1UVw>? NGTBWYpKSzVyPECuOUDPxE1? M1TyRlE2QDZ5M{i2
SK-N-MC MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUT+O-KBks7:TR?= NIruRlBFVVOR NUTLOWUzUUN3MEywMlUh|ryP MV2xOVg3PzN6Nh?=
RD-ES MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXHrN2c4hjgkgJtOwG0> M32wOGROW09? NE\6VVFKSzVyPECuOUDPxE1? M1zKO|E2QDZ5M{i2
SJ-Rh 30 MlvVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M323ep446oDMzszN MWHEUXNQ NIDSfGFKSzVyPECuOUDPxE1? Mm\PNVU5Pjd|OE[=
SJ-Rh 4 MlPrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVvzdYRYhjgkgJtOwG0> MVvEUXNQ MUHJR|UxRDBwNTFOwG0> M2jHe|E2QDZ5M{i2
6647 NFjk[IRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYP+O-KBks7:TR?= MljhSG1UVw>? NGXxbYJKSzVyPECuOUDPxE1? M3PNdVE2QDZ5M{i2
SARG M3LJWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUP+O-KBks7:TR?= Mk\4SG1UVw>? Mln3TWM2ODx|IN88US=> MX:xOVg3PzN6Nh?=
MOS NV\FS5JvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYf+O-KBks7:TR?= MoP5SG1UVw>? MX\JR|UxRDRizszN MXOxOVg3PzN6Nh?=
IOR/OS7 Mo\IS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX\+O-KBks7:TR?= NH7XTm5FVVOR NHvxZpJKSzVyPEGg{txO NInTbmkyPTh4N{O4Oi=>
IOR/OS9 Mn3XS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NED6OGx,P+LCit88US=> NEXDSohFVVOR MUTJR|UxRDZizszN MmHuNVU5Pjd|OE[=
IOR/OS10 NHPzS3ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGDj[|h,P+LCit88US=> MonkSG1UVw>? NWTSPFRwUUN3MEy1JO69VQ>? M1LnRVE2QDZ5M{i2
IOR/OS14 NFLsTZNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHyzToN,P+LCit88US=> MkSxSG1UVw>? M4PU[GlEPTB:NDFOwG0> NVjJOmhqOTV6NkezPFY>
LAP35 NV;mPGU4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH;ifWN,P+LCit88US=> NFPmWmVFVVOR MmjVTWM2ODxyLkWg{txO NFvvPGMyPTh4N{O4Oi=>
IOR/BRZ NWOzNnY2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVTqeHY5hjgkgJtOwG0> NWXiZZY{TE2VTx?= M321WGlEPTB:MD61JO69VQ>? NV2yXVBoOTV6NkezPFY>
IOR/CAR MnKxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIfXOmN,P+LCit88US=> NHu4NI1FVVOR MYnJR|UxRDFizszN NWnzNm9wOTV6NkezPFY>
IOR/NGR NXzX[Ix3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHrMToN,P+LCit88US=> MmqxSG1UVw>? MWfJR|UxRDBwNTFOwG0> MkLWNVU5Pjd|OE[=
IOR/RCH NGTnWZpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVL+O-KBks7:TR?= NFTpZ|JFVVOR NXewS3doUUN3MEywMlUh|ryP MVKxOVg3PzN6Nh?=
RMZ-RC2 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnnBglfjiIsQvF2= NE\lbJdFVVOR Mk\5TWM2ODxyLkWg{txO NYXTeGhQOTV6NkezPFY>
CCA NEC1U5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYT+O-KBks7:TR?= M1;mbmROW09? NX[0WIVWUUN3MEyyJO69VQ>? MoGxNVU5Pjd|OE[=
RD/18 NELMUlRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYL+O-KBks7:TR?= MlrSSG1UVw>? NUTKUW84UUN3MEy0JO69VQ>? NIP1PVIyPTh4N{O4Oi=>
OVCAR-3 M4TsTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlfFglE26oDMzszN MX\EUXNQ M{DxOolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MmnzNVY{ODB6MkC=
OVCAR-4 M3TEbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkXtglE26oDMzszN MlTjSG1UVw>? M17tW4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> Ml\CNVY{ODB6MkC=
OVCAR-3 M1vzeGFxd3C2b4Ppd{Bie3OjeR?= MXT+NVXjiIsQvF2= MoKwSG1UVw>? NU\ZN49qcW6mdXPld{BieG:ydH;zbZM> MnzENVY{ODB6MkC=
OVCAR-4 NGLVdo5CeG:ydH;zbZMh[XO|YYm= NFXONpZ,OTYkgJtOwG0> NI\lbmpFVVOR MmXQbY5lfWOnczDhdI9xfG:|aYO= MUOxOlMxODh{MB?=
OVCAR-3 MmPhSpVv[3Srb36gZZN{[Xl? NGCxXlh,OTYkgJtOwG0> NWrjcm9QTE2VTx?= MVnE[YNz\WG|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MWGxOlMxODh{MB?=
Huh-7 NXfxVWhkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2fmOZ4yOOLCit88US=> MXXEUXNQ MUTJR|UxRTFwNDFOwG0> M{DwO|E3PTNyN{O0
Hep-G2 MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHTJbm5,OTEkgJtOwG0> NYjBbYRUTE2VTx?= MlXlTWM2OD1zLkig{txO Mo\ENVY2OzB5M{S=
Hep-3B NWnhPFRIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnvYglEx6oDMzszN MXPEUXNQ NHPhWGZKSzVyPUGuPUDPxE1? MmS4NVY2OzB5M{S=
SK-Hep-1 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXMglEx6oDMzszN MUfEUXNQ M13Rd2lEPTB;Nj65JO69VQ>? NY\MfXhCOTZ3M{C3N|Q>
Huh-7 NXrBeGZnTnWwY4Tpc44h[XO|YYm= Mk\rglEx6oDMzszN MYnEUXNQ NHHzfppKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MWGxOlU{ODd|NB?=
Hep-G2 NHfybIJHfW6ldHnvckBie3OjeR?= NVPFbHdbhjFy4pEK{txO MojvSG1UVw>? NGfleFVKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MmHZNVY2OzB5M{S=
SK-Hep-1 NYfpcXV2TnWwY4Tpc44h[XO|YYm= MlfPglEx6oDMzszN MnfrSG1UVw>? NWnwXIVJUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M1:xcVE3PTNyN{O0
BON NXKzdVBuU2mwYYPlJIF{e2G7 MXP+OkDPxE1? NIDt[WZFVVOR M4XVT4lv\HWlZYOg[IVxcG:|cHjvdplt[XSrb36gc4YhUUeILUHS M3;tRVE3PjBzMki0
BON NE\CWVFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUD+NVDjiIsQvF2= Mor5SG1UVw>? M{mwbGlEPTB;Nj62JO69VQ>? MkX1NVY3ODF{OES=
CM M{DmVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NU[3O5hIhjYkgJtOwG0> NFTXd3NFVVOR MUjJR|UxRTNwMzFOwG0> MUSxOlYxOTJ6NB?=
BON MnfHSpVv[3Srb36gZZN{[Xl? MXP+O{426oDMzszN M{TmNGROW09? MkHqbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NH3tVFQyPjZyMUK4OC=>
CM NELzcWFHfW6ldHnvckBie3OjeR?= MljMglXjiIsQvF2= NH\HWm1FVVOR Mnv0bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NUDMNYx5OTZ4MEGyPFQ>
BON M13IWGFxd3C2b4Ppd{Bie3OjeR?= MlnCglcvPeLCit88US=> M1\KPGROW09? NIXoTnpqdmS3Y3XzJGFxd3C2b4Ppdy=> NVP3[YF6OTZ4MEGyPFQ>
CM M2DhWmFxd3C2b4Ppd{Bie3OjeR?= NFrWU4V,PeLCit88US=> M3vPd2ROW09? MYjpcoR2[2W|IFHwc5B1d3Orcx?= M3LmeFE3PjBzMki0
HT-29 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYP5O2xxhjFy4pEK{txO MnTpSG1UVw>? NYm5cXJ5UUN3ME2xMlch|ryP MknJNVcxODdyMUW=
HCT-116 NHPGVm9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoTBglEx6oDMzszN MWnEUXNQ NEfMPJJKSzVyPUKuOUDPxE1? MmnyNVcxODdyMUW=
primary colorectal cancer cells MVfGeY5kfGmxbjDhd5NigQ>? MkX3glXjiIsQvF2= M3zBUWROW09? NGPlbpBidHSncoOgeIhmKG2xcoDoc4xw\3lib3[geIhmKHKnbXHpcolv\yClZXzsdy=> MXqxO|AxPzBzNR?=
HTLA-230 M1LnSmZ2dmO2aX;uJIF{e2G7 MlrNglgh|ryP NUi5W|lXTE2VTx?= M{XIN4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NIHGPJgyPzF{MUi5PC=>
KCNR NGnqPFhHfW6ldHnvckBie3OjeR?= NXq5TIduhjhizszN NWfqdGN1TE2VTx?= NGPVV5pqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> MkfjNVcyOjF6OUi=
SK-N-BE2c MoDmSpVv[3Srb36gZZN{[Xl? NInsVo9,QCEQvF2= NVjVW2ExTE2VTx?= MnvLbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NEnNfo0yPzF{MUi5PC=>
SK-N-BE NVzCNXdNTnWwY4Tpc44h[XO|YYm= MU\+PEDPxE1? MojqSG1UVw>? NEf2SW9qdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M{jEc|E4OTJzOEm4
LAN-5 NUThZVJkTnWwY4Tpc44h[XO|YYm= M{fIfJ45KM7:TR?= M{PEbWROW09? MXPpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NUDqOmhDOTdzMkG4PVg>
GI-CA-N NEHFfmdHfW6ldHnvckBie3OjeR?= NUjrOWhLhjhizszN Mke0SG1UVw>? MUnpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= Ml7ENVcyOjF6OUi=
SH-EP NHXyPHhHfW6ldHnvckBie3OjeR?= M4faR545KM7:TR?= NX3QUoJxTE2VTx?= NInvVIZqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NXPVWmwxOTdzMkG4PVg>
SK-N-AS MV\GeY5kfGmxbjDhd5NigQ>? Mn\rglgh|ryP NEjzRXNFVVOR MUHpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MnPxNVcyOjF6OUi=
RN-GA NECxSIdHfW6ldHnvckBie3OjeR?= Mn[0glgh|ryP M4PpdmROW09? MW\pcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MXWxO|EzOTh7OB?=
SY-5Y(N) NVHFS|l1TnWwY4Tpc44h[XO|YYm= NFuzNoJ,QCEQvF2= NGnkXZVFVVOR MnnubY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NY[5cGJrOTdzMkG4PVg>
GI-CA-N NULGUIhlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYf+PEDPxE1? M2TIcmROW09? Ml35TWM2OD1iNj64JO69VQ>? NVvUXnRtOTdzMkG4PVg>
SH-EP NV;ue|J3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWf+PEDPxE1? NFXHN2RFVVOR MVvJR|UxRSB|IN88US=> MV:xO|EzOTh7OB?=
HTLA-230 M2XDTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;WbYRmhjhizszN MoLWSG1UVw>? NWC1bpJ[UUN3ME2gNE42KM7:TR?= MWGxO|EzOTh7OB?=
SK-N-BE2c M{m2OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUn+PEDPxE1? NYHZNJE4TE2VTx?= NHHufJZKSzVyPTCxMlEh|ryP MnO2NVcyOjF6OUi=
SK-N-BE2 NXnRV3VjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4\i[J45KM7:TR?= MUnEUXNQ M37IPWlEPTB;IEOg{txO MX:xO|EzOTh7OB?=
SY-5Y (N) NGjaNY5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MY\+PEDPxE1? NYrxeVY3TE2VTx?= NELpdoJKSzVyPTCyMlQh|ryP NUW4PWhMOTdzMkG4PVg>
LAN-5 M4LrRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUL+PEDPxE1? MXPEUXNQ Mn61TWM2OD1iMD60JO69VQ>? NXr5So97OTdzMkG4PVg>
KCNR NH\w[lJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUj+PEDPxE1? NHu2WodFVVOR MUjJR|UxRSByLkSg{txO MVGxO|EzOTh7OB?=
RN-GA MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHHUS2l,QCEQvF2= NHHEVHVFVVOR MnGwTWM2OD1iMT6zJO69VQ>? NYrPXGdmOTdzMkG4PVg>
SK-N-AS MoDXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUjnSHJVhjhizszN MmS5SG1UVw>? NGnoT3pqdmS3Y3XzJIFxd3C2b4Ppdy=> MmfQNVcyOjF6OUi=
KCNR NV23UXkxSXCxcITvd4l{KGG|c3H5 MoO0glgh|ryP M3fyVWROW09? MXXpcoR2[2W|IHHwc5B1d3Orcx?= NUnUeYI2OTdzMkG4PVg>
GI-CA-N NU\HcY1CSXCxcITvd4l{KGG|c3H5 MXX+PEDPxE1? M4jUN2ROW09? NGjhTmZqdmS3Y3XzJIFxd3C2b4Ppdy=> M4\Z[lE4OTJzOEm4
HTLA-230 MWDBdI9xfG:|aYOgZZN{[Xl? M3fwcZ45KM7:TR?= NX3TSmF[TE2VTx?= NX;hc4hLcW6mdXPld{BieG:ydH;zbZM> NHvORm8yPzF{MUi5PC=>
SK-N-BE2c MVzBdI9xfG:|aYOgZZN{[Xl? MWP+PEDPxE1? NHPWTXlFVVOR MnTIbY5lfWOnczDhdI9xfG:|aYO= NHGwSHUyPzF{MUi5PC=>
SY-5Y (N) NY\BeXNMSXCxcITvd4l{KGG|c3H5 MoLoglgh|ryP NEW1XWJFVVOR MWTpcoR2[2W|IHHwc5B1d3Orcx?= NYTMe4JSOTdzMkG4PVg>
HL60AR M3rBUGZ2dmO2aX;uJIF{e2G7 MkjjNVYxKG6P NXfaVFls\W6qYX7j[ZMhfGinIHzleoVteyCxZjDwNldMcXBz M3LSXVE4OzZzMkK1
HL60AR NGHBUFRCeG:ydH;zbZMh[XO|YYm= MmXYglIxOCCwTR?= NWfKUXF1cW6mdXPld{BieG:ydH;zbZM> M{\5Z|E4OzZzMkK1
HPAF-II NXLRcGNVU2mwYYPlJIF{e2G7 NYnUZWdEhjFizszN NYjBSINiTE2VTx?= M3rGdolvcGmkaYTzJGlITi2LLX3l[IlifGWmIIPp[45idGyrbne= M1qwVlE5PDR3NUKw
HPAF-II MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkTnglIh|ryP MofzSG1UVw>? NXTLcZVwcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MX:xPFQ1PTV{MB?=
HPAF-II NYXsdlBiTnWwY4Tpc44h[XO|YYm= M1fjVZ4zKM7:TR?= NFfhcItFVVOR M2n2OYlvcGmkaYTzJIJie2GuIHHu[EBKT0ZvST3t[YRq[XSnZDDwZY5kemWjdHnjJINidmOncjDj[YxtKG2rZ4LheIlwdg>? MU[xPFQ1PTV{MB?=
TFK-1 NITmbWNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGDK[VB,OjVyIH7N MnWwSG1UVw>? MlTDTWM2OD1yLkK2JO69VQ>? NUj3ZWl5OjByNk[3N|Q>
EGI-1 M17LNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVH+NlUxKG6P MVvEUXNQ MVHJR|UxRTBwMkig{txO NVXJZlZHOjByNk[3N|Q>
CC-LP-1 NWLxUmpqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUX+NlUxKG6P M{PUWGROW09? M2GxUWlEPTB;MD6xOUDPxE1? Ml;jNlAxPjZ5M{S=
CC-SW-1 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2Dscp4zPTBibl2= M{Hxd2ROW09? MkDETWM2OD1yLkW0JO69VQ>? MYGyNFA3Pjd|NB?=
Sk-ChA-1 Mn;OS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYT0bVc4hjJ3MDDuUS=> MlP2SG1UVw>? MWfJR|UxRTBwMjFOwG0> MVKyNFA3Pjd|NB?=
Mz-ChA-1 NIf0T5RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFLnTlN,OjVyIH7N M2XJZWROW09? MXPJR|UxRTFwM{mg{txO Mk\kNlAxPjZ5M{S=
Mz-ChA-2 MlzmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUT+NlUxKG6P NET1[ZZFVVOR Mm\TTWM2OD1yLkezJO69VQ>? MWKyNFA3Pjd|NB?=
ECC-1 M3PjbmtqdmG|ZTDhd5NigQ>? NXHkWYRHhjFyIN88US=> NEnrNZJFVVOR MX7pcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6QCV? MkLzNlEzQTV|M{W=
Ishikawa MWDLbY5ie2ViYYPzZZk> NHfpWW1,OTBizszN MVXEUXNQ NXjMOZhpcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOUOl NGXCSpUzOTJ7NUOzOS=>
USPC-1 M3e5dWtqdmG|ZTDhd5NigQ>? NHHzXo9,OTBizszN M3HxTmROW09? NHjld3JqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSBzMECl NFvLOIszOTJ7NUOzOS=>
USPC-2 M4rFfmtqdmG|ZTDhd5NigQ>? MWL+NVAh|ryP MVfEUXNQ NXrDfmZlcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOU[l MYeyNVI6PTN|NR?=
ECC-1 NGnCSoRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX23TWVnhjFyIN88US=> NWTSZXlmTE2VTx?= MWTk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MV:yNVI6PTN|NR?=
Ishikawa NUnXT3hzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXjSdHE1hjFyIN88US=> NFqzdm9FVVOR MVLk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MUWyNVI6PTN|NR?=
USPC-1 M1XIUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXPqdVA4hjFyIN88US=> M{jHPGROW09? M1XKcoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NWL5cYFSOjF{OUWzN|U>
USPC-2 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIDVc3l,OTBizszN NHLv[pZFVVOR NYrK[oJk\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? M17adFIyOjl3M{O1

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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
    (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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

Mass (g) = Concentration (mol/L) × Volume (L) × 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:

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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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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

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

If you have any other enquiries, please leave a message.

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IGF-1R Signaling Pathway Map

IGF-1R Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID