NVP-AEW541

Catalog No.S1034 Synonyms: AEW541

For research use only.

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 Chemical Structure

CAS No. 475489-16-8

Selleck's NVP-AEW541 has been cited by 58 publications

Purity & Quality Control

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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)
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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 Mo\ET4lv[XOnIHHzd4F6 NF;H[Xd,OTEkgJtOwG0> NYe5VGFtTE2VTx?= NFfmVWVqdmirYnn0d{BKT0ZvSWKge4l1cCCLQ{WwJI9nKDBwMEi2JOKyKDBwMEK4JO69VQ>? MnvjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVyNUC5NVUoRjF3MEWwPVE2RC:jPh?=
A14 MWnLbY5ie2ViYYPzZZk> M4rRW54yOOLCit88US=> NGmxOpVFVVOR MnrkbY5pcWKrdIOgTY5{WiC5aYToJGlEPTBib3[gNk4{KMLzIECuNVY{KM7:TR?= M{P3VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MEWwPVE2Lz5zNUC1NFkyPTxxYU6=
A431  NHTuW3BMcW6jc3WgZZN{[Xl? MYr+NVDjiIsQvF2= MXLEUXNQ MXvpcohq[mm2czDISXIyKHerdHigTWM2OCCxZjC+NVAh|ryP M1nITVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MEWwPVE2Lz5zNUC1NFkyPTxxYU6=
A31  M1nYWWtqdmG|ZTDhd5NigQ>? NH;rUFV,OTEkgJtOwG0> NXLxeo1nTE2VTx?= NIHibGRqdmirYnn0d{BRTEeIUjD3bZRpKEmFNUCgc4YhRjFyIN88US=> M2mwV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MEWwPVE2Lz5zNUC1NFkyPTxxYU6=
GIST882 M2\VeGtqdmG|ZTDhd5NigQ>? M3Tldp4yOOLCit88US=> Ml76SG1UVw>? MYDpcohq[mm2czDjMWtqfCC5aYToJGlEPTBib3[gQlUh|ryP NXXhPI1wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWwOVA6OTVpPkG1NFUxQTF3PD;hQi=>
32D-Bcr-Abl MWDLbY5ie2ViYYPzZZk> MnnZglEx6oDMzszN NEftUIdFVVOR Mnr0bY5pcWKrdIOgRoNzNUGkbDDwNlExKHerdHigTWM2OCCxZjC+NVAh|ryP NGPY[Yc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUC1NFkyPSd-MUWwOVA6OTV:L3G+
MCF-7  MlzpR5l1d3irY3n0fUBie3OjeR?= MmjKSG1UVw>? MnXNTWM2OD1zLk[0JO69VQ>? NY\SbXdHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWwOVA6OTVpPkG1NFUxQTF3PD;hQi=>
NWT-21 M1jIUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVXEUXNQ M3fpW2lEPTB;MD6xOlMh|ryP MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTB3MEmxOUc,OTVyNUC5NVU9N2F-
TC-71 MmW5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF3lXo5,OSEQvF2= MmfKSG1UVw>? NVnQTpE1cW6qaXLpeJMhcW6|dXzpck1tcWunIHfyc5d1cCCoYXP0c5IuUeLCk33l[IlifGWmIHfyc5d1cA>? MlrxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
TC-71 MmDGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGLKXXl,P+LCit88US=> MoT6SG1UVw>? M2LhTGlEPTB:MD61JO69VQ>? NEDHO|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUi2O|M5Pid-MUW4Olc{QDZ:L3G+
Saos-2 M2rzUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHLidlJ,P+LCit88US=> MVnEUXNQ NV;WbZdMUUN3MEyzJO69VQ>? MlzzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
U-2OS M1r2b2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFzmbml,P+LCit88US=> M4\yN2ROW09? M2fKZ2lEPTB:MD61JO69VQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
SK-ES-1 NX\DRoViT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWjV[o82hjgkgJtOwG0> MWLEUXNQ MofBTWM2ODxyLkWg{txO Mmf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
SK-N-MC M3rBVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MojwglfjiIsQvF2= MULEUXNQ NUP0fVRFUUN3MEywMlUh|ryP NX;HN2x4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
RD-ES NWXF[G4xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFy4TW1,P+LCit88US=> NF;6W|lFVVOR NI\IblhKSzVyPECuOUDPxE1? NYW1NXhRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
SJ-Rh 30 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{L3UZ446oDMzszN MVfEUXNQ MWXJR|UxRDBwNTFOwG0> MoXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
SJ-Rh 4 NU\tPZZMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojCglfjiIsQvF2= MlW0SG1UVw>? NUnDcVdXUUN3MEywMlUh|ryP Mn75QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
6647 M1;SbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHPWO|B,P+LCit88US=> M4KwSGROW09? MljiTWM2ODxyLkWg{txO MoPJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
SARG NF\HW2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYLCfYhZhjgkgJtOwG0> MlfYSG1UVw>? NXnJb2ZYUUN3MEyzJO69VQ>? NF\VdmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUi2O|M5Pid-MUW4Olc{QDZ:L3G+
MOS M3HZWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWi5UXNbhjgkgJtOwG0> Mn62SG1UVw>? NVvvOJBJUUN3MEy0JO69VQ>? NUPheWZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
IOR/OS7 NUPmbHpkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWm5W45EhjgkgJtOwG0> MY\EUXNQ MX3JR|UxRDFizszN MkLrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
IOR/OS9 NF:yZ|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1TXTp446oDMzszN NWfkUJBtTE2VTx?= MUfJR|UxRDZizszN NVHL[3hWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
IOR/OS10 MoDGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M37WOp446oDMzszN NGTpTpVFVVOR M3vtRmlEPTB:NTFOwG0> NELQW5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUi2O|M5Pid-MUW4Olc{QDZ:L3G+
IOR/OS14 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoK3glfjiIsQvF2= NFXaTI1FVVOR MXrJR|UxRDRizszN NVrmOm9ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
LAP35 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYr+O-KBks7:TR?= NHPmRWxFVVOR MWLJR|UxRDBwNTFOwG0> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
IOR/BRZ MnjsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEnKWlB,P+LCit88US=> Mn\aSG1UVw>? NEP5d4tKSzVyPECuOUDPxE1? NV3C[lNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
IOR/CAR NXTzb4F1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUj3O485hjgkgJtOwG0> NEXiV3NFVVOR NITwNXVKSzVyPEGg{txO MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
IOR/NGR NV;HSW5RT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIrsfVR,P+LCit88US=> NFfXc49FVVOR M3nQS2lEPTB:MD61JO69VQ>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
IOR/RCH MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVL+O-KBks7:TR?= MXLEUXNQ MlXKTWM2ODxyLkWg{txO MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
RMZ-RC2 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXP+O-KBks7:TR?= NFXOPFNFVVOR M3nKNGlEPTB:MD61JO69VQ>? NHzwS3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUi2O|M5Pid-MUW4Olc{QDZ:L3G+
CCA NFr0e|dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV33Omp6hjgkgJtOwG0> MVXEUXNQ MkLtTWM2ODx{IN88US=> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
RD/18 NI\4XXRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3n2Zp446oDMzszN MlXvSG1UVw>? NUXtZVZPUUN3MEy0JO69VQ>? M1X5TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OE[3N|g3Lz5zNUi2O|M5PjxxYU6=
OVCAR-3 NGjObYNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlX4glE26oDMzszN MUHEUXNQ M4\zfYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjNyMEiyNEc,OTZ|MEC4NlA9N2F-
OVCAR-4 M4XqSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGHid3p,OTYkgJtOwG0> Mn7LSG1UVw>? NUPod|gycW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NHPveJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkOwNFgzOCd-MU[zNFA5OjB:L3G+
OVCAR-3 NFHKbpdCeG:ydH;zbZMh[XO|YYm= NUH5e5RzhjF34pEK{txO NUD0fGRkTE2VTx?= NFP4O|ZqdmS3Y3XzJIFxd3C2b4Ppdy=> NHXvSY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkOwNFgzOCd-MU[zNFA5OjB:L3G+
OVCAR-4 MX\BdI9xfG:|aYOgZZN{[Xl? Mn3vglE26oDMzszN NXPtUnY6TE2VTx?= NFLoR3pqdmS3Y3XzJIFxd3C2b4Ppdy=> NVjjUlF5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[zNFA5OjBpPkG2N|AxQDJyPD;hQi=>
OVCAR-3 M4\uS2Z2dmO2aX;uJIF{e2G7 MXr+NVXjiIsQvF2= MkL6SG1UVw>? MVfE[YNz\WG|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjNyMEiyNEc,OTZ|MEC4NlA9N2F-
Huh-7 NInETXRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUL+NVDjiIsQvF2= MVTEUXNQ NG\LbZdKSzVyPUGuOEDPxE1? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjV|MEezOEc,OTZ3M{C3N|Q9N2F-
Hep-G2 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGnubJB,OTEkgJtOwG0> NUn5UVU1TE2VTx?= NFq1[nNKSzVyPUGuPEDPxE1? M4TPOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4NUOwO|M1Lz5zNkWzNFc{PDxxYU6=
Hep-3B MlTwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWT+NVDjiIsQvF2= NGnVO|RFVVOR MlvrTWM2OD1zLkmg{txO MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjV|MEezOEc,OTZ3M{C3N|Q9N2F-
SK-Hep-1 MnXVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1\MUJ4yOOLCit88US=> MXrEUXNQ MUjJR|UxRTZwOTFOwG0> MljtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ3M{C3N|QoRjF4NUOwO|M1RC:jPh?=
Huh-7 MlXkSpVv[3Srb36gZZN{[Xl? MmTPglEx6oDMzszN NVfOc29OTE2VTx?= M3jo[Glv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjV|MEezOEc,OTZ3M{C3N|Q9N2F-
Hep-G2 NETPVIJHfW6ldHnvckBie3OjeR?= M{jL[54yOOLCit88US=> NHzNb5VFVVOR M2DVbWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NGTXVIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkWzNFc{PCd-MU[1N|A4OzR:L3G+
SK-Hep-1 NXzp[Yo1TnWwY4Tpc44h[XO|YYm= NWHXTFJnhjFy4pEK{txO NXP3RZFGTE2VTx?= NH;Nb2dKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NX3ld4xjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[1N|A4OzRpPkG2OVMxPzN2PD;hQi=>
BON NYDmc5ZjU2mwYYPlJIF{e2G7 NXLWcWJJhjZizszN Mmi4SG1UVw>? MXHpcoR2[2W|IHTldIhwe3Cqb4L5cIF1cW:wIH;mJGlITi1zUh?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjZyMUK4OEc,OTZ4MEGyPFQ9N2F-
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Ishikawa MW\LbY5ie2ViYYPzZZk> MkHDglExKM7:TR?= MYrEUXNQ NFjNXlNqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSB7MzW= NWH2doRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPVU{OzVpPkKxNlk2OzN3PD;hQi=>
USPC-1 NFjVS4RMcW6jc3WgZZN{[Xl? M4f3Zp4yOCEQvF2= NXvQXppTTE2VTx?= NYrXOWZxcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliMUCwKS=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ7NUOzOUc,OjF{OUWzN|U9N2F-
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ECC-1 NHfOV29Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn7mglExKM7:TR?= MmfXSG1UVw>? M2LPfIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NWfPZZd{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPVU{OzVpPkKxNlk2OzN3PD;hQi=>
Ishikawa MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2jLe54yOCEQvF2= NHztN|hFVVOR M2W5T4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> M1jSW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkm1N|M2Lz5{MUK5OVM{PTxxYU6=
USPC-1 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4DrPJ4yOCEQvF2= NF;lfJRFVVOR NVzjRoZz\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? MnTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OUWzN|UoRjJzMkm1N|M2RC:jPh?=
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Ba/F3 M3LJXmZ2dmO2aX;uJIF{e2G7 NWXWO5Z3UW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBKT0ZvMTDy[YNmeHSxcjCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKEKjL1[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxicILvcIln\XKjdHnvckwhUUN3ME2wMlAz|ryP MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl3MUe1N{c,OjZ7NUG3OVM9N2F-
HEK293 M3ftTmZ2dmO2aX;uJIF{e2G7 MmXWOlAhdWmwcx?= MnvOTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDJS2YuOSC{ZXPldJRweiBqdX7rco94diCxcnnnbY4qKGG3dH;wbI9{eGixconsZZRqd25idILhcpNn\WO2ZXSgbY4hUEWNMkmzJINmdGy|IIDy[ZRz\WG2ZXSg[o9zKDZyIH3pcpMh\m:ubH;3[YQh[nliSVfGMVEhe3SrbYXsZZRqd25ibXXhd5Vz\WRiYX\0[ZIhOTBibXnud{BjgSCzdXHueIl1[XSrdnWgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVAvODZ3zszN NVixTHBMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5OVE4PTNpPkK2PVUyPzV|PD;hQi=>
HEK293 NIf1ZpVHfW6ldHnvckBie3OjeR?= MoriSIl{eGyjY3Xt[Y51KG:oIGuzTH0u\G:oZYTpcIll\SCocn;tJIh2dWGwIFXSS{BkcGGwbnXsJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOsJGlEPTB;MD6xN:69VQ>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl3MUe1N{c,OjZ7NUG3OVM9N2F-
Ba/F3 M1rVemZ2dmO2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIHnud5VtcW5icnXj[ZB1d3JiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBD[S:IMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MD6yOFTPxE1? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl3MUe1N{c,OjZ7NUG3OVM9N2F-
HEK293 M3jRfGZ2dmO2aX;uJIF{e2G7 NED5OGg3OCCvaX7z M1X2WmlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigbY5{fWyrbjDy[YNmeHSxcjCoeY5sdm:5bjDvdolocW5rIHH1eI9xcG:|cHjvdplt[XSrb36geJJidnOoZXP0[YQhcW5iSFXLNlk{KGOnbHzzJJBz\XS{ZXH0[YQh\m:{IE[wJI1qdnNiZn;scI94\WRiYomgTWdHNTFic4TpcZVt[XSrb36gcYVie3W{ZXSgZYZ1\XJiMUCgcYlveyCkeTDxeYFvfGm2YYTpeoUhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDJR|UxRTBwOEmy{txO NHrNc4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm1NVc2Oyd-Mk[5OVE4PTN:L3G+
TC32 NVHj[ItJeUiWUzDhd5NigQ>? M4jMXJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| M2DVNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NG\ZSIFyUFSVIHHzd4F6 NG\zXWtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> MkTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MlrxdWhVWyCjc4PhfS=> NGSwZ4JyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz Mo\NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 NV\HfYtSeUiWUzDhd5NigQ>? MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NGXiT3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 MVLxTHRUKGG|c3H5 M365eZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NVvkTGZ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD M2TWPJFJXFNiYYPzZZk> NHnZO49yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MoH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 MXnxTHRUKGG|c3H5 MYHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? MoL3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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 (from 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 Research:[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 Research:[1]
  • 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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 439.55
Formula

C27H29N5O

CAS No. 475489-16-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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