NVP-AEW541

For research use only.

Catalog No.S1034 Synonyms: AEW541

54 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 54 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 MWPLbY5ie2ViYYPzZZk> NEm5TnZ,OTEkgJtOwG0> NEj0cGRFVVOR NVLaXGppcW6qaXLpeJMhUUeILVnSJJdqfGhiSVO1NEBw\iByLkC4OkDDuSByLkCyPEDPxE1? MlXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVyNUC5NVUoRjF3MEWwPVE2RC:jPh?=
A14 MmfPT4lv[XOnIHHzd4F6 NYP2eI53hjFy4pEK{txO MVLEUXNQ M1PLd4lvcGmkaYTzJGlve1Jid3n0bEBKSzVyIH;mJFIvOyEEsTCwMlE3OyEQvF2= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTB3MEmxOUc,OTVyNUC5NVU9N2F-
A431  M3\weGtqdmG|ZTDhd5NigQ>? MoX1glEx6oDMzszN MUHEUXNQ NXrjbFlPcW6qaXLpeJMhUEWUMTD3bZRpKEmFNUCgc4YhRjFyIN88US=> MmLtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVyNUC5NVUoRjF3MEWwPVE2RC:jPh?=
A31  M3;FcmtqdmG|ZTDhd5NigQ>? MWr+NVDjiIsQvF2= NYe1[oxYTE2VTx?= NX;tUmo6cW6qaXLpeJMhWESJRmKge4l1cCCLQ{WwJI9nKD5zMDFOwG0> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTB3MEmxOUc,OTVyNUC5NVU9N2F-
GIST882 M1r0bmtqdmG|ZTDhd5NigQ>? MkC2glEx6oDMzszN MXXEUXNQ NGPuPY9qdmirYnn0d{BkNUurdDD3bZRpKEmFNUCgc4YhRjVizszN NVzCfWtYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWwOVA6OTVpPkG1NFUxQTF3PD;hQi=>
32D-Bcr-Abl Mlz0T4lv[XOnIHHzd4F6 MkfCglEx6oDMzszN NFz1dppFVVOR MlTnbY5pcWKrdIOgRoNzNUGkbDDwNlExKHerdHigTWM2OCCxZjC+NVAh|ryP MljpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVyNUC5NVUoRjF3MEWwPVE2RC:jPh?=
MCF-7  MWfDfZRwgGmlaYT5JIF{e2G7 NF3NRVJFVVOR MXrJR|UxRTFwNkSg{txO M4nwdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MEWwPVE2Lz5zNUC1NFkyPTxxYU6=
NWT-21 NUD2Um1bT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXGyTlNGTE2VTx?= NXjsbYVCUUN3ME2wMlE3OyEQvF2= NHLu[4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUC1NFkyPSd-MUWwOVA6OTV:L3G+
TC-71 NUK1fnY{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1rVe54yKM7:TR?= MkT0SG1UVw>? MmDMbY5pcWKrdIOgbY5{fWyrbj3sbYtmKGe{b4f0bEBn[WO2b4KtTgKBm22nZHnheIVlKGe{b4f0bC=> Mkj3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
TC-71 MkK3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MknNglfjiIsQvF2= MWDEUXNQ M1HvW2lEPTB:MD61JO69VQ>? NE\IOpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUi2O|M5Pid-MUW4Olc{QDZ:L3G+
Saos-2 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MljaglfjiIsQvF2= Mk\TSG1UVw>? MkjQTWM2ODx|IN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
U-2OS M2TURmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlWwglfjiIsQvF2= NHn4R4xFVVOR NUPEbGM1UUN3MEywMlUh|ryP NX7sV5R6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
SK-ES-1 NYXBVosyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYD+O-KBks7:TR?= Mnz3SG1UVw>? NY\XPW1nUUN3MEywMlUh|ryP MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
SK-N-MC MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MU\+O-KBks7:TR?= NX3VNlE2TE2VTx?= MoLvTWM2ODxyLkWg{txO MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
RD-ES NVHROVEyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{O5VJ446oDMzszN NH;OUoZFVVOR M3rXPGlEPTB:MD61JO69VQ>? MnLTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
SJ-Rh 30 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml7tglfjiIsQvF2= NHyyVohFVVOR MlLmTWM2ODxyLkWg{txO NVfrNmlSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
SJ-Rh 4 NYjmb4ZrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVTMZnJbhjgkgJtOwG0> MmDFSG1UVw>? NIr0c2JKSzVyPECuOUDPxE1? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
6647 NHXuZm9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYn+O-KBks7:TR?= M13DPWROW09? NHPjc5pKSzVyPECuOUDPxE1? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
SARG MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFXwSJF,P+LCit88US=> NX3le5l{TE2VTx?= M3vuNGlEPTB:MzFOwG0> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
MOS MnX4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFXkRmV,P+LCit88US=> M1n5eWROW09? NUTNVIdNUUN3MEy0JO69VQ>? M3v0PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OE[3N|g3Lz5zNUi2O|M5PjxxYU6=
IOR/OS7 M165[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlnBglfjiIsQvF2= NFvxPZhFVVOR NULZe3lxUUN3MEyxJO69VQ>? M3H2WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OE[3N|g3Lz5zNUi2O|M5PjxxYU6=
IOR/OS9 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NILRNZN,P+LCit88US=> MU\EUXNQ MVLJR|UxRDZizszN M3HoPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OE[3N|g3Lz5zNUi2O|M5PjxxYU6=
IOR/OS10 M2LrN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWD+O-KBks7:TR?= NUT2PG1VTE2VTx?= NIXIeG5KSzVyPEWg{txO M372VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OE[3N|g3Lz5zNUi2O|M5PjxxYU6=
IOR/OS14 M1TMT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{LSPZ446oDMzszN NUmxb4x5TE2VTx?= NEf1bZhKSzVyPESg{txO M{HHclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OE[3N|g3Lz5zNUi2O|M5PjxxYU6=
LAP35 NHvJT2lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVH+O-KBks7:TR?= NFrhcVZFVVOR NFvrNGdKSzVyPECuOUDPxE1? NWnnTnZyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
IOR/BRZ M3;Vbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXj0SXJUhjgkgJtOwG0> MkKzSG1UVw>? Mo\3TWM2ODxyLkWg{txO NITKSJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUi2O|M5Pid-MUW4Olc{QDZ:L3G+
IOR/CAR NEKzfmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXoNY1ChjgkgJtOwG0> NYj5cpBtTE2VTx?= NILWbYdKSzVyPEGg{txO MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh4N{O4Okc,OTV6NkezPFY9N2F-
IOR/NGR MnjqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkPYglfjiIsQvF2= NH7zNY9FVVOR MoiwTWM2ODxyLkWg{txO NV;5V21lRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4Olc{QDZpPkG1PFY4Ozh4PD;hQi=>
IOR/RCH NHfsSVlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoW3glfjiIsQvF2= M37QeGROW09? MkLFTWM2ODxyLkWg{txO NGjV[HM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUi2O|M5Pid-MUW4Olc{QDZ:L3G+
RMZ-RC2 Mlq5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVrWZWpPhjgkgJtOwG0> NUPzUIFYTE2VTx?= MVPJR|UxRDBwNTFOwG0> Mn7YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
CCA NWW3WoNMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmixglfjiIsQvF2= NEf1TYZFVVOR NGfROYJKSzVyPEKg{txO Ml\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV6NkezPFYoRjF3OE[3N|g3RC:jPh?=
RD/18 M3vTWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVfwUHFXhjgkgJtOwG0> NFrrc|FFVVOR M{LmOWlEPTB:NDFOwG0> M4fENlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OE[3N|g3Lz5zNUi2O|M5PjxxYU6=
OVCAR-3 MmTlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXHDZpR{hjF34pEK{txO NF7XTYlFVVOR MofjbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NGjXZlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkOwNFgzOCd-MU[zNFA5OjB:L3G+
OVCAR-4 Mor3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWXY[XhXhjF34pEK{txO MnHMSG1UVw>? MmrrbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NEHLcFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkOwNFgzOCd-MU[zNFA5OjB:L3G+
OVCAR-3 NFXOWHpCeG:ydH;zbZMh[XO|YYm= NV7tVHQyhjF34pEK{txO NFXx[4xFVVOR M1jLbolv\HWlZYOgZZBweHSxc3nz M2j1fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4M{CwPFIxLz5zNkOwNFgzODxxYU6=
OVCAR-4 M2jaXmFxd3C2b4Ppd{Bie3OjeR?= NVTEZoNxhjF34pEK{txO MXPEUXNQ NFvTc|VqdmS3Y3XzJIFxd3C2b4Ppdy=> Ml;aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ|MEC4NlAoRjF4M{CwPFIxRC:jPh?=
OVCAR-3 Ml7SSpVv[3Srb36gZZN{[Xl? MYX+NVXjiIsQvF2= MmPhSG1UVw>? NWX1cHh2TGWlcnXhd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= Mn\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ|MEC4NlAoRjF4M{CwPFIxRC:jPh?=
Huh-7 MoW4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3zQUZ4yOOLCit88US=> M2HoWmROW09? Ml7KTWM2OD1zLkSg{txO M2W2[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4NUOwO|M1Lz5zNkWzNFc{PDxxYU6=
Hep-G2 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGCxfW5,OTEkgJtOwG0> NU[wNZFxTE2VTx?= MY\JR|UxRTFwODFOwG0> MkLiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ3M{C3N|QoRjF4NUOwO|M1RC:jPh?=
Hep-3B MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGewV2F,OTEkgJtOwG0> Ml3xSG1UVw>? NGrtdpVKSzVyPUGuPUDPxE1? MnzWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ3M{C3N|QoRjF4NUOwO|M1RC:jPh?=
SK-Hep-1 NV\JdIlLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYj+NVDjiIsQvF2= NWXLfFdoTE2VTx?= MV7JR|UxRTZwOTFOwG0> NH3UO3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkWzNFc{PCd-MU[1N|A4OzR:L3G+
Huh-7 NXzvfIplTnWwY4Tpc44h[XO|YYm= M4HMRp4yOOLCit88US=> NEi2XpFFVVOR Mn;oTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M{jNfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4NUOwO|M1Lz5zNkWzNFc{PDxxYU6=
Hep-G2 MmHhSpVv[3Srb36gZZN{[Xl? MlvpglEx6oDMzszN M1;KcGROW09? NI\xUo9KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 Ml\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ3M{C3N|QoRjF4NUOwO|M1RC:jPh?=
SK-Hep-1 NUfCcYk4TnWwY4Tpc44h[XO|YYm= NEP0Zph,OTEkgJtOwG0> NYP0O|dRTE2VTx?= MlzkTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MkfVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ3M{C3N|QoRjF4NUOwO|M1RC:jPh?=
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ECC-1 NUfOSmlwU2mwYYPlJIF{e2G7 M{PGdJ4yOCEQvF2= M2nlcmROW09? NXTINIljcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOUil M{\ERlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkm1N|M2Lz5{MUK5OVM{PTxxYU6=
Ishikawa MUjLbY5ie2ViYYPzZZk> M1rJ[Z4yOCEQvF2= MoDjSG1UVw>? M2fkOYlvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl|JR?= M4W1OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkm1N|M2Lz5{MUK5OVM{PTxxYU6=
USPC-1 NWPpdXlRU2mwYYPlJIF{e2G7 NFzlZ2N,OTBizszN M1iwSmROW09? NXHMO5Z2cW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliMUCwKS=> NW\IdIF1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPVU{OzVpPkKxNlk2OzN3PD;hQi=>
USPC-2 NWTP[XlHU2mwYYPlJIF{e2G7 NWLRb2E3hjFyIN88US=> NVX1V4ZNTE2VTx?= NUW4PYJocW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOU[l NECy[2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK5OVM{PSd-MkGyPVU{OzV:L3G+
ECC-1 MnLHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mnz6glExKM7:TR?= NFL6c|dFVVOR M3y4TYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ7NUOzOUc,OjF{OUWzN|U9N2F-
Ishikawa MmPVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFO1dI9,OTBizszN MXLEUXNQ NF7LeWdl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v NWS3fJhMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPVU{OzVpPkKxNlk2OzN3PD;hQi=>
USPC-1 M{HuPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXvsflRuhjFyIN88US=> MUnEUXNQ MofN[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> MmP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OUWzN|UoRjJzMkm1N|M2RC:jPh?=
USPC-2 MlHpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH7rSmd,OTBizszN NV7vR4RtTE2VTx?= NU[z[5py\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NV70VFFVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyPVU{OzVpPkKxNlk2OzN3PD;hQi=>
Ba/F3 Mn[wSpVv[3Srb36gZZN{[Xl? MkDETY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDJS2YuOSC{ZXPldJRweiBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJGJiN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwheHKxbHnm[ZJifGmxbjygTWM2OD1yLkCy{txO NHfQbWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm1NVc2Oyd-Mk[5OVE4PTN:L3G+
HEK293 NFXPUFBHfW6ldHnvckBie3OjeR?= M1HaW|YxKG2rboO= NHTwW|NKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJGlITi1zIILlZ4VxfG:{IDj1cotvd3ewIH;ybYdqdiliYYX0c5Bpd3OyaH;yfYxifGmxbjD0doFve2[nY4Tl[EBqdiCKRVuyPVMh[2WubIOgdJJmfHKnYYTl[EBnd3JiNkCgcYlveyCob3zsc5dm\CCkeTDJS2YuOSC|dHnteYxifGmxbjDt[YF{fXKnZDDh[pRmeiBzMDDtbY5{KGK7IIH1ZY51cXSjdHn2[UBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNuIFnDOVA:OC5yNkZOwG0> MmPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7NUG3OVMoRjJ4OUWxO|U{RC:jPh?=
HEK293 Mn\FSpVv[3Srb36gZZN{[Xl? MVjEbZNxdGGlZX3lcpQhd2ZiW{PIYU1ld2[ndHnsbYRmKG[{b32gbJVu[W5iRWLHJINp[W6wZXyg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczygTWM2OD1yLkGz{txO MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl3MUe1N{c,OjZ7NUG3OVM9N2F-
Ba/F3 MYfGeY5kfGmxbjDhd5NigQ>? NIHCXZdKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJIlve3WuaX6gdoVk\XC2b4KgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCEYT;GN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9NE4zPDUQvF2= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl3MUe1N{c,OjZ7NUG3OVM9N2F-
HEK293 M2HWTmZ2dmO2aX;uJIF{e2G7 NIfIWXI3OCCvaX7z MYjJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIHnud5VtcW5icnXj[ZB1d3JiKIXub45wf25ib4Lp[4lvMSCjdYTvdIhwe3Cqb4L5cIF1cW:wIITyZY5{\mWldHXkJIlvKEiHS{K5N{Bk\WyuczDwdoV1emWjdHXkJIZweiB4MDDtbY5{KG[xbHzve4VlKGK7IFnHSk0yKHO2aX31cIF1cW:wIH3lZZN2emWmIHHmeIVzKDFyIH3pcpMh[nlicYXhcpRqfGG2aY\lJHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0xNjh7Mt88US=> NELTeVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm1NVc2Oyd-Mk[5OVE4PTN:L3G+
TC32 MYnxTHRUKGG|c3H5 NEO2Z3JyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?= Ml;2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 Mn\idWhVWyCjc4PhfS=> MkX2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= NVHOZYIxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NVfFflRXeUiWUzDhd5NigQ>? M2mzTJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= MkPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 NXriOYh[eUiWUzDhd5NigQ>? M{fPS5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= NInYeW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 NV3BVnlGeUiWUzDhd5NigQ>? MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NWnyOFVQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD Ml\GdWhVWyCjc4PhfS=> MnvHdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NEe0PXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 NH7TTIpyUFSVIHHzd4F6 M17iSJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| NWrSSms5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

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

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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