NVP-AEW541

For research use only.

Catalog No.S1034 Synonyms: AEW541

42 publications

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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Selleck's NVP-AEW541 has been cited by 42 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 Mn:3T4lv[XOnIHHzd4F6 NEjuUXR,OTEkgJtOwG0> NYrKWG1mTE2VTx?= MkPpbY5pcWKrdIOgTWdHNUmUIIfpeIghUUN3MDDv[kAxNjB6NjFCtUAxNjB{ODFOwG0> MUWxOVA2ODlzNR?=
A14 NWDHVZJyU2mwYYPlJIF{e2G7 MofsglEx6oDMzszN MVnEUXNQ M1PRTYlvcGmkaYTzJGlve1Jid3n0bEBKSzVyIH;mJFIvOyEEsTCwMlE3OyEQvF2= NYGwPYRDOTVyNUC5NVU>
A431  MlLTT4lv[XOnIHHzd4F6 MV3+NVDjiIsQvF2= MVLEUXNQ MlnXbY5pcWKrdIOgTGVTOSC5aYToJGlEPTBib3[gQlExKM7:TR?= MYKxOVA2ODlzNR?=
A31  MknST4lv[XOnIHHzd4F6 NVn0NlB1hjFy4pEK{txO NUjCWmQyTE2VTx?= NGm4OIdqdmirYnn0d{BRTEeIUjD3bZRpKEmFNUCgc4YhRjFyIN88US=> NFP3PGQyPTB3MEmxOS=>
GIST882 MV\LbY5ie2ViYYPzZZk> NFHZTYd,OTEkgJtOwG0> Ml\ZSG1UVw>? Ml\mbY5pcWKrdIOgZ{1McXRid3n0bEBKSzVyIH;mJF42KM7:TR?= MoezNVUxPTB7MUW=
32D-Bcr-Abl Mln3T4lv[XOnIHHzd4F6 M2HZdZ4yOOLCit88US=> MlyzSG1UVw>? NInaeoJqdmirYnn0d{BD[3JvQXLsJJAzOTBid3n0bEBKSzVyIH;mJF4yOCEQvF2= M4rB[lE2ODVyOUG1
MCF-7  MWTDfZRwgGmlaYT5JIF{e2G7 M1q0VGROW09? M2LyUWlEPTB;MT62OEDPxE1? MYWxOVA2ODlzNR?=
NWT-21 NUjx[WxuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWDEUXNQ MkPVTWM2OD1yLkG2N{DPxE1? NUeweZJCOTVyNUC5NVU>
TC-71 M1Xn[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWTEemdmhjFizszN NVvVXGtNTE2VTx?= NGKydIdqdmirYnn0d{BqdnO3bHnuMYxqc2ViZ4Lve5RpKG[jY4Tvdk1K6oDVbXXkbYF1\WRiZ4Lve5Rp MXyxOVg3PzN6Nh?=
TC-71 M2O4Wmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH\ZNlB,P+LCit88US=> MX\EUXNQ NHm4d|BKSzVyPECuOUDPxE1? NVO3ZVU5OTV6NkezPFY>
Saos-2 NXjIeWUxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWL+O-KBks7:TR?= NEjT[VJFVVOR NYP3cppJUUN3MEyzJO69VQ>? M2[wVlE2QDZ5M{i2
U-2OS MlLiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFr1Tll,P+LCit88US=> NY\FclNyTE2VTx?= M{Xwe2lEPTB:MD61JO69VQ>? NGX0R|gyPTh4N{O4Oi=>
SK-ES-1 M4rlfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1iyUZ446oDMzszN M1\WT2ROW09? NXfoTWx5UUN3MEywMlUh|ryP NV60ephpOTV6NkezPFY>
SK-N-MC MnftS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoPPglfjiIsQvF2= NVizU4dTTE2VTx?= MY\JR|UxRDBwNTFOwG0> M1e4[FE2QDZ5M{i2
RD-ES NUC1dpI4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV;+O-KBks7:TR?= M3\TTmROW09? M3\ISWlEPTB:MD61JO69VQ>? M3fQ[lE2QDZ5M{i2
SJ-Rh 30 NU\6TGw{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXH+O-KBks7:TR?= MlSxSG1UVw>? M4nkfWlEPTB:MD61JO69VQ>? M1z2ZVE2QDZ5M{i2
SJ-Rh 4 NVLITYVET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn60glfjiIsQvF2= MVzEUXNQ NEXP[|NKSzVyPECuOUDPxE1? M1v5[FE2QDZ5M{i2
6647 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3vBeJ446oDMzszN M33CZmROW09? MXrJR|UxRDBwNTFOwG0> NVT4bldJOTV6NkezPFY>
SARG MlPaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnfQglfjiIsQvF2= M36xU2ROW09? MYPJR|UxRDNizszN NILUd3YyPTh4N{O4Oi=>
MOS M1fhc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH;jeJR,P+LCit88US=> MYfEUXNQ NHT1fmhKSzVyPESg{txO NGjFNYgyPTh4N{O4Oi=>
IOR/OS7 Mk\QS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUf+O-KBks7:TR?= MUfEUXNQ NIHIdJdKSzVyPEGg{txO MV2xOVg3PzN6Nh?=
IOR/OS9 NWTGW4JlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV\+O-KBks7:TR?= MorxSG1UVw>? M3\zbWlEPTB:NjFOwG0> MnXsNVU5Pjd|OE[=
IOR/OS10 NETjbZVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUjONodChjgkgJtOwG0> Mnf1SG1UVw>? NGKwZnlKSzVyPEWg{txO M1fXZ|E2QDZ5M{i2
IOR/OS14 NUjrcHlsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGDtWIN,P+LCit88US=> NGTXSHJFVVOR NELGfFlKSzVyPESg{txO M{PS[lE2QDZ5M{i2
LAP35 M1X6emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoiyglfjiIsQvF2= NXzFOGdzTE2VTx?= NUDaRmdyUUN3MEywMlUh|ryP NFPJZZIyPTh4N{O4Oi=>
IOR/BRZ MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV3+O-KBks7:TR?= MVTEUXNQ M4XRT2lEPTB:MD61JO69VQ>? MlHQNVU5Pjd|OE[=
IOR/CAR M4TmZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV;+O-KBks7:TR?= NFywb2tFVVOR NV\Me21rUUN3MEyxJO69VQ>? M4[4NFE2QDZ5M{i2
IOR/NGR NHfJUXJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYL+O-KBks7:TR?= NF3XZ3RFVVOR NXjUblRCUUN3MEywMlUh|ryP MWCxOVg3PzN6Nh?=
IOR/RCH NGnvRWtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3HMe5446oDMzszN MXjEUXNQ NVrB[2V{UUN3MEywMlUh|ryP M1HQVVE2QDZ5M{i2
RMZ-RC2 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV;+O-KBks7:TR?= NWLDU|FPTE2VTx?= NXrmZ3VVUUN3MEywMlUh|ryP MXexOVg3PzN6Nh?=
CCA MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFfiUVV,P+LCit88US=> NVPVflM5TE2VTx?= NHXFU49KSzVyPEKg{txO MVyxOVg3PzN6Nh?=
RD/18 MmXJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU\+O-KBks7:TR?= MVzEUXNQ NXjvPIFZUUN3MEy0JO69VQ>? M3rYc|E2QDZ5M{i2
OVCAR-3 NIHOSVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYX+NVXjiIsQvF2= NHTtSI1FVVOR M1v5UolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NWDMXYtkOTZ|MEC4NlA>
OVCAR-4 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEDMOFh,OTYkgJtOwG0> NIqzOYJFVVOR M1nkZolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NFfHS4IyPjNyMEiyNC=>
OVCAR-3 M2nmemFxd3C2b4Ppd{Bie3OjeR?= MXv+NVXjiIsQvF2= NXrsbpVjTE2VTx?= NYHIXG1[cW6mdXPld{BieG:ydH;zbZM> MV2xOlMxODh{MB?=
OVCAR-4 NHLFW2NCeG:ydH;zbZMh[XO|YYm= MnPGglE26oDMzszN MWXEUXNQ MkPDbY5lfWOnczDhdI9xfG:|aYO= MUixOlMxODh{MB?=
OVCAR-3 M1vvUGZ2dmO2aX;uJIF{e2G7 Ml;KglE26oDMzszN NGC4cnRFVVOR Mn3BSIVkemWjc3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? MYCxOlMxODh{MB?=
Huh-7 NWDvbXhHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUXKSmlIhjFy4pEK{txO NFvp[oZFVVOR MYHJR|UxRTFwNDFOwG0> M1\DNVE3PTNyN{O0
Hep-G2 NFjDNZpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUn+NVDjiIsQvF2= NIGzOZZFVVOR MknKTWM2OD1zLkig{txO Mn\SNVY2OzB5M{S=
Hep-3B MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXS1cGtHhjFy4pEK{txO M2riR2ROW09? M3;D[mlEPTB;MT65JO69VQ>? MWqxOlU{ODd|NB?=
SK-Hep-1 MnLLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mo\RglEx6oDMzszN NG\GW4JFVVOR NWCyfHJkUUN3ME22Mlkh|ryP M2TEZlE3PTNyN{O0
Huh-7 MUXGeY5kfGmxbjDhd5NigQ>? MUH+NVDjiIsQvF2= MX7EUXNQ M1LL[Wlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= Mn23NVY2OzB5M{S=
Hep-G2 Mn36SpVv[3Srb36gZZN{[Xl? MmjwglEx6oDMzszN NVHBeGFsTE2VTx?= Mk\iTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NHnSU4wyPjV|MEezOC=>
SK-Hep-1 M4DUTWZ2dmO2aX;uJIF{e2G7 MUf+NVDjiIsQvF2= MmHuSG1UVw>? NEPkb5ZKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NEnycJAyPjV|MEezOC=>
BON Ml7ET4lv[XOnIHHzd4F6 NVjyOHRnhjZizszN MWTEUXNQ NWK4RVZCcW6mdXPld{Bl\XCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXI> MmnHNVY3ODF{OES=
BON NYrIc2lMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnLUglEx6oDMzszN MoHQSG1UVw>? MkPNTWM2OD14Lk[g{txO NGq4OIUyPjZyMUK4OC=>
CM NITEb2ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXX+OgKBks7:TR?= NX3KU3Q6TE2VTx?= NEnwRnRKSzVyPUOuN{DPxE1? Mn6zNVY3ODF{OES=
BON NF6xZpdHfW6ldHnvckBie3OjeR?= MnrIglcvPeLCit88US=> MUDEUXNQ MkL1bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MVGxOlYxOTJ6NB?=
CM MVTGeY5kfGmxbjDhd5NigQ>? M1z2bZ426oDMzszN NYHONGtOTE2VTx?= M2DNcolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M{POcFE3PjBzMki0
BON NHzRU3RCeG:ydH;zbZMh[XO|YYm= NFHUO5V,Py534pEK{txO NVjrW2pCTE2VTx?= Mki4bY5lfWOnczDBdI9xfG:|aYO= M4PBTFE3PjBzMki0
CM NWnvVmhzSXCxcITvd4l{KGG|c3H5 NUXMV2tYhjYkgJtOwG0> Mor6SG1UVw>? NIDWTHFqdmS3Y3XzJGFxd3C2b4Ppdy=> MlzENVY3ODF{OES=
HT-29 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYj+NVDjiIsQvF2= MW\EUXNQ NIrkZWFKSzVyPUGuO{DPxE1? MoHQNVcxODdyMUW=
HCT-116 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlrFglEx6oDMzszN MkTZSG1UVw>? M3vOb2lEPTB;Mj61JO69VQ>? NEHiZ5UyPzByN{CxOS=>
primary colorectal cancer cells MXLGeY5kfGmxbjDhd5NigQ>? M{i4UZ426oDMzszN NUn0ZlhkTE2VTx?= MUjhcJRmenNidHjlJI1wenCqb3zv[5khd2ZidHjlJJJmdWGrbnnu[{Bk\Wyucx?= MWSxO|AxPzBzNR?=
HTLA-230 MV3GeY5kfGmxbjDhd5NigQ>? MV;+PEDPxE1? MWDEUXNQ M4PQN4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MkD1NVcyOjF6OUi=
KCNR NVu5T4pLTnWwY4Tpc44h[XO|YYm= NXHNTZRyhjhizszN MV\EUXNQ MYTpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MknZNVcyOjF6OUi=
SK-N-BE2c MlzUSpVv[3Srb36gZZN{[Xl? MWX+PEDPxE1? M3LleGROW09? MmLQbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MWOxO|EzOTh7OB?=
SK-N-BE MkXMSpVv[3Srb36gZZN{[Xl? Mlr4glgh|ryP MVnEUXNQ NHzOOG5qdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NGrhcmwyPzF{MUi5PC=>
LAN-5 NHjReFFHfW6ldHnvckBie3OjeR?= M4TacJ45KM7:TR?= MYjEUXNQ MoDobY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NVX4NJpbOTdzMkG4PVg>
GI-CA-N NYHoNHBmTnWwY4Tpc44h[XO|YYm= M3\nTZ45KM7:TR?= NYPDNFZoTE2VTx?= MYfpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NWjzOpVyOTdzMkG4PVg>
SH-EP MoH0SpVv[3Srb36gZZN{[Xl? MUP+PEDPxE1? Mmq3SG1UVw>? MVnpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= M1v1RlE4OTJzOEm4
SK-N-AS MkmzSpVv[3Srb36gZZN{[Xl? NIfiTHd,QCEQvF2= NUixTZFFTE2VTx?= M2L1XolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MUmxO|EzOTh7OB?=
RN-GA Mn7iSpVv[3Srb36gZZN{[Xl? MU\+PEDPxE1? M1LhNWROW09? NXnIWnRScW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 NX7ObGJnOTdzMkG4PVg>
SY-5Y(N) MX;GeY5kfGmxbjDhd5NigQ>? MWj+PEDPxE1? M2CwVmROW09? MkKybY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NXLQcJM2OTdzMkG4PVg>
GI-CA-N NI\Xbm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mli5glgh|ryP MlTjSG1UVw>? MkDkTWM2OD1iNj64JO69VQ>? NUTSdpU5OTdzMkG4PVg>
SH-EP NWLmXGRbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUX+PEDPxE1? MXzEUXNQ NGLB[FdKSzVyPTCzJO69VQ>? M4rZfVE4OTJzOEm4
HTLA-230 NYXRWoI2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3T2TJ45KM7:TR?= M4\0SmROW09? M1POeGlEPTB;IECuOUDPxE1? MXWxO|EzOTh7OB?=
SK-N-BE2c MoK2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1rWZ545KM7:TR?= NYTEVHUzTE2VTx?= NEP1N3FKSzVyPTCxMlEh|ryP M3naWFE4OTJzOEm4
SK-N-BE2 NH;WO5dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnXFglgh|ryP NUWxeod3TE2VTx?= MWfJR|UxRSB|IN88US=> MkDZNVcyOjF6OUi=
SY-5Y (N) MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4K5W545KM7:TR?= M37G[GROW09? M{TQNmlEPTB;IEKuOEDPxE1? MUWxO|EzOTh7OB?=
LAN-5 NEXKSXpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NG\wTlB,QCEQvF2= M1XE[WROW09? MVfJR|UxRSByLkSg{txO NFqyO2EyPzF{MUi5PC=>
KCNR NUXscIhxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mm\aglgh|ryP MX;EUXNQ MlnmTWM2OD1iMD60JO69VQ>? M2CyVVE4OTJzOEm4
RN-GA MkfKS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUDSOXhqhjhizszN M2jufmROW09? MlXTTWM2OD1iMT6zJO69VQ>? NVjXRpo3OTdzMkG4PVg>
SK-N-AS MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYr+PEDPxE1? M1;iNGROW09? NF65OZlqdmS3Y3XzJIFxd3C2b4Ppdy=> NVnNVod[OTdzMkG4PVg>
KCNR NES3[nNCeG:ydH;zbZMh[XO|YYm= MkT6glgh|ryP M1f4PGROW09? MnXJbY5lfWOnczDhdI9xfG:|aYO= MmezNVcyOjF6OUi=
GI-CA-N M1uzcmFxd3C2b4Ppd{Bie3OjeR?= MnTKglgh|ryP NWjpfFd4TE2VTx?= NEjjcIlqdmS3Y3XzJIFxd3C2b4Ppdy=> MWqxO|EzOTh7OB?=
HTLA-230 M{HwWGFxd3C2b4Ppd{Bie3OjeR?= Ml\uglgh|ryP Mn;NSG1UVw>? MnrIbY5lfWOnczDhdI9xfG:|aYO= MXKxO|EzOTh7OB?=
SK-N-BE2c MXPBdI9xfG:|aYOgZZN{[Xl? MW\+PEDPxE1? MXXEUXNQ NYS5U4RrcW6mdXPld{BieG:ydH;zbZM> MWqxO|EzOTh7OB?=
SY-5Y (N) MkW1RZBweHSxc3nzJIF{e2G7 M2G4[545KM7:TR?= MkH2SG1UVw>? MkS4bY5lfWOnczDhdI9xfG:|aYO= MVexO|EzOTh7OB?=
HL60AR NVXKdoI6TnWwY4Tpc44h[XO|YYm= MUGxOlAhdk1? NXrMc3BO\W6qYX7j[ZMhfGinIHzleoVteyCxZjDwNldMcXBz NXf2SZhOOTd|NkGyNlU>
HL60AR MYDBdI9xfG:|aYOgZZN{[Xl? M1LEfp4zODBibl2= NWKxcG1YcW6mdXPld{BieG:ydH;zbZM> M1TFXVE4OzZzMkK1
HPAF-II MkXlT4lv[XOnIHHzd4F6 NU\yTGZYhjFizszN MnTUSG1UVw>? NX7nOIVOcW6qaXLpeJMhUUeILVmtcYVlcWG2ZXSgd4lodmGubHnu[y=> NWDEW2NyOTh2NEW1NlA>
HPAF-II MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX\+NkDPxE1? NHfpN5VFVVOR NYnFWJpjcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M3\OTlE5PDR3NUKw
HPAF-II M3LJVmZ2dmO2aX;uJIF{e2G7 M1PuVp4zKM7:TR?= NWHCW2ZyTE2VTx?= M1\YTYlvcGmkaYTzJIJie2GuIHHu[EBKT0ZvST3t[YRq[XSnZDDwZY5kemWjdHnjJINidmOncjDj[YxtKG2rZ4LheIlwdg>? Ml;kNVg1PDV3MkC=
TFK-1 NX73PVVkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX7+NlUxKG6P NVfkOXozTE2VTx?= MkjNTWM2OD1yLkK2JO69VQ>? M165OVIxODZ4N{O0
EGI-1 M1jrc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmX3glI2OCCwTR?= MVzEUXNQ MVPJR|UxRTBwMkig{txO NH\DflQzODB4NkezOC=>
CC-LP-1 NFr3WIhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmjKglI2OCCwTR?= NGXvVVFFVVOR NGHhUlRKSzVyPUCuNVUh|ryP Ml63NlAxPjZ5M{S=
CC-SW-1 M1G3Z2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYD4fnIyhjJ3MDDuUS=> M2\tXmROW09? NH3iTmJKSzVyPUCuOVQh|ryP NXrscIxiOjByNk[3N|Q>
Sk-ChA-1 NHPK[pNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4DXTp4zPTBibl2= Mn;1SG1UVw>? NF;MNZlKSzVyPUCuNkDPxE1? MXqyNFA3Pjd|NB?=
Mz-ChA-1 NHXmTW9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV7ybYxGhjJ3MDDuUS=> NHXUbHBFVVOR NXL1cFdvUUN3ME2xMlM6KM7:TR?= MlzRNlAxPjZ5M{S=
Mz-ChA-2 M1rodGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{LZOZ4zPTBibl2= MUPEUXNQ MkXsTWM2OD1yLkezJO69VQ>? MYWyNFA3Pjd|NB?=
ECC-1 NHu4N|BMcW6jc3WgZZN{[Xl? MnTPglExKM7:TR?= M4Xjc2ROW09? MnXTbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQThn MXGyNVI6PTN|NR?=
Ishikawa MmLrT4lv[XOnIHHzd4F6 NFPBPWR,OTBizszN MV3EUXNQ NXvER2RYcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOUOl NXrRNWdyOjF{OUWzN|U>
USPC-1 M4rx[mtqdmG|ZTDhd5NigQ>? MonnglExKM7:TR?= MV7EUXNQ NIOyc3RqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSBzMECl MVSyNVI6PTN|NR?=
USPC-2 NXnn[G5FU2mwYYPlJIF{e2G7 Mk[xglExKM7:TR?= NV3vVnlmTE2VTx?= NHyzTpNqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSB7NjW= NE\xemQzOTJ7NUOzOS=>
ECC-1 M2f6V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MljjglExKM7:TR?= M{PBcGROW09? NGnWeFRl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MYWyNVI6PTN|NR?=
Ishikawa Mn6zS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2TlOp4yOCEQvF2= NGXsZnBFVVOR NYCzZWRk\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NETWXpIzOTJ7NUOzOS=>
USPC-1 M4HWXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXLKUIJ5hjFyIN88US=> M1GySmROW09? M{XCe4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NEKycG8zOTJ7NUOzOS=>
USPC-2 M4jDNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVvFUnI2hjFyIN88US=> MkTHSG1UVw>? MVvk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MVmyNVI6PTN|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

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

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).

Dilution Calculator

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).

The Serial Dilution Calculator Equation

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  • Computed Result

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Molecular Weight Calculator

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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