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 30 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 NH7sUWhMcW6jc3WgZZN{[Xl? MWD+NVDjiIsQvF2= NYizNG5JTE2VTx?= M1LoU4lvcGmkaYTzJGlITi2LUjD3bZRpKEmFNUCgc4YhOC5yOE[gxtEhOC5yMkig{txO M{e0e|E2ODVyOUG1
A14 NUHtZ5M{U2mwYYPlJIF{e2G7 NFSzXlR,OTEkgJtOwG0> NHS2R5dFVVOR NU\6fItJcW6qaXLpeJMhUW6|UjD3bZRpKEmFNUCgc4YhOi5|INMxJFAvOTZ|IN88US=> NGrSc4kyPTB3MEmxOS=>
A431  NYHqTHBTU2mwYYPlJIF{e2G7 NV7ue3FrhjFy4pEK{txO MXnEUXNQ MYXpcohq[mm2czDISXIyKHerdHigTWM2OCCxZjC+NVAh|ryP MXSxOVA2ODlzNR?=
A31  M3;md2tqdmG|ZTDhd5NigQ>? MnLsglEx6oDMzszN MoHVSG1UVw>? MXvpcohq[mm2czDQSGdHWiC5aYToJGlEPTBib3[gQlExKM7:TR?= NF7VeYgyPTB3MEmxOS=>
GIST882 NGq2cWxMcW6jc3WgZZN{[Xl? Mk[3glEx6oDMzszN NHS0ZlhFVVOR M4D5colvcGmkaYTzJIMuU2m2IIfpeIghUUN3MDDv[kA,PSEQvF2= MYOxOVA2ODlzNR?=
32D-Bcr-Abl NHTmeGFMcW6jc3WgZZN{[Xl? MoH1glEx6oDMzszN MUTEUXNQ NUWwTY1rcW6qaXLpeJMhSmO{LVHicEBxOjFyIIfpeIghUUN3MDDv[kA,OTBizszN NHz1R2UyPTB3MEmxOS=>
MCF-7  MknOR5l1d3irY3n0fUBie3OjeR?= NEn5b5JFVVOR NV\UR4VRUUN3ME2xMlY1KM7:TR?= M3OzeVE2ODVyOUG1
NWT-21 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVLEUXNQ M3XZdGlEPTB;MD6xOlMh|ryP MWGxOVA2ODlzNR?=
TC-71 M4[zN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnHWglEh|ryP NFWxbmVFVVOR MUTpcohq[mm2czDpcpN2dGmwLXzpb4Uh\3Kxd4ToJIZi[3Sxcj3J5qCUdWWmaXH0[YQh\3Kxd4To NUTYPWpOOTV6NkezPFY>
TC-71 NWPvZ5ZMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4HkWZ446oDMzszN NUP5cYhYTE2VTx?= NF\KO2FKSzVyPECuOUDPxE1? NVzTUGxIOTV6NkezPFY>
Saos-2 NXz6TJJOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkD5glfjiIsQvF2= MUXEUXNQ NHXVNJZKSzVyPEOg{txO M{TobFE2QDZ5M{i2
U-2OS M1\wRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUX+O-KBks7:TR?= MUfEUXNQ NUDCfHhPUUN3MEywMlUh|ryP NHTTdG8yPTh4N{O4Oi=>
SK-ES-1 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1rje5446oDMzszN M{P1TWROW09? M{fFfmlEPTB:MD61JO69VQ>? NIHCW2IyPTh4N{O4Oi=>
SK-N-MC M3nPdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXTOdZVHhjgkgJtOwG0> NGi5TmJFVVOR M1\w[WlEPTB:MD61JO69VQ>? M{n5c|E2QDZ5M{i2
RD-ES MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnjBglfjiIsQvF2= NFzJR3dFVVOR NEPCdFlKSzVyPECuOUDPxE1? M4Hxc|E2QDZ5M{i2
SJ-Rh 30 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVX+O-KBks7:TR?= M3:zUWROW09? MV7JR|UxRDBwNTFOwG0> NITl[IsyPTh4N{O4Oi=>
SJ-Rh 4 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYf+O-KBks7:TR?= NIjUfY1FVVOR M36xZWlEPTB:MD61JO69VQ>? MXyxOVg3PzN6Nh?=
6647 NHfRTY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NULzWoFmhjgkgJtOwG0> M4nxeWROW09? NEO1d4pKSzVyPECuOUDPxE1? MVixOVg3PzN6Nh?=
SARG MkXqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVH+O-KBks7:TR?= MVzEUXNQ NETjcnRKSzVyPEOg{txO MYmxOVg3PzN6Nh?=
MOS NFTwNGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHS1e3Z,P+LCit88US=> NW\tdFNNTE2VTx?= MVjJR|UxRDRizszN NFXqd|IyPTh4N{O4Oi=>
IOR/OS7 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3i0fJ446oDMzszN MX7EUXNQ M{\HUWlEPTB:MTFOwG0> MWmxOVg3PzN6Nh?=
IOR/OS9 M4i3V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXf+O-KBks7:TR?= MVfEUXNQ M{jF[WlEPTB:NjFOwG0> Mn\QNVU5Pjd|OE[=
IOR/OS10 M4\JPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEPlXY5,P+LCit88US=> M1vSTGROW09? M4OwWWlEPTB:NTFOwG0> NEPM[HEyPTh4N{O4Oi=>
IOR/OS14 NGHWfGdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUntfZdRhjgkgJtOwG0> NH;3[JJFVVOR MnnhTWM2ODx2IN88US=> MXyxOVg3PzN6Nh?=
LAP35 Mmm2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\CNp446oDMzszN NF3tUXZFVVOR MXvJR|UxRDBwNTFOwG0> MU[xOVg3PzN6Nh?=
IOR/BRZ NEfReXpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoKxglfjiIsQvF2= NIrkW3dFVVOR MnLtTWM2ODxyLkWg{txO MX2xOVg3PzN6Nh?=
IOR/CAR M4PMUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mom2glfjiIsQvF2= MmTiSG1UVw>? NFq3Z3dKSzVyPEGg{txO NWnXUm5uOTV6NkezPFY>
IOR/NGR NEjaW2FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmDqglfjiIsQvF2= M1X1N2ROW09? MX3JR|UxRDBwNTFOwG0> NF7NN4UyPTh4N{O4Oi=>
IOR/RCH NWfEcXhsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYH+O-KBks7:TR?= M2fl[2ROW09? MXrJR|UxRDBwNTFOwG0> MnvENVU5Pjd|OE[=
RMZ-RC2 NF\TeVFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHrncFJ,P+LCit88US=> M3LTZ2ROW09? NXG1bJZjUUN3MEywMlUh|ryP MXGxOVg3PzN6Nh?=
CCA MlzRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlHMglfjiIsQvF2= NHX5[4ZFVVOR M{DpcGlEPTB:MjFOwG0> NYDNc5VJOTV6NkezPFY>
RD/18 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUXhO2g4hjgkgJtOwG0> NVfuXYxKTE2VTx?= MVTJR|UxRDRizszN NXzlU4RDOTV6NkezPFY>
OVCAR-3 MoLnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3HLXZ4yPeLCit88US=> M{TiNmROW09? NEDOW5dqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MoX3NVY{ODB6MkC=
OVCAR-4 NVHwSWlkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2\uSp4yPeLCit88US=> MYjEUXNQ MXPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NVPJTWMzOTZ|MEC4NlA>
OVCAR-3 NG\OPYlCeG:ydH;zbZMh[XO|YYm= MUj+NVXjiIsQvF2= NYfXWmFOTE2VTx?= NESxbnRqdmS3Y3XzJIFxd3C2b4Ppdy=> M1;FTFE3OzByOEKw
OVCAR-4 MkXERZBweHSxc3nzJIF{e2G7 M{i3Np4yPeLCit88US=> MnnvSG1UVw>? NGX5PGZqdmS3Y3XzJIFxd3C2b4Ppdy=> M4e3W|E3OzByOEKw
OVCAR-3 M3u0VmZ2dmO2aX;uJIF{e2G7 NUHrVHdXhjF34pEK{txO M4DOR2ROW09? Mlu4SIVkemWjc3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? M2TaOlE3OzByOEKw
Huh-7 NEe2S|hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NETadIV,OTEkgJtOwG0> MWXEUXNQ MXTJR|UxRTFwNDFOwG0> MmnmNVY2OzB5M{S=
Hep-G2 MmLzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYL+NVDjiIsQvF2= NUPzcWRkTE2VTx?= NYG4[pdUUUN3ME2xMlgh|ryP NF;3SVgyPjV|MEezOC=>
Hep-3B MnvzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3S3Np4yOOLCit88US=> NWnFdZk6TE2VTx?= NUWyRYl2UUN3ME2xMlkh|ryP MXOxOlU{ODd|NB?=
SK-Hep-1 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1y0VJ4yOOLCit88US=> NW\DZo9UTE2VTx?= NGDG[YlKSzVyPU[uPUDPxE1? Mk\tNVY2OzB5M{S=
Huh-7 NWHObm9bTnWwY4Tpc44h[XO|YYm= MU\+NVDjiIsQvF2= NFjmZ2RFVVOR MVfJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 Mn3YNVY2OzB5M{S=
Hep-G2 MkizSpVv[3Srb36gZZN{[Xl? MoDsglEx6oDMzszN MUDEUXNQ MYPJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 M1;HblE3PTNyN{O0
SK-Hep-1 MmKySpVv[3Srb36gZZN{[Xl? NGT3R2Z,OTEkgJtOwG0> MUDEUXNQ MoqzTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M13meFE3PTNyN{O0
BON NUTrZ|ZjU2mwYYPlJIF{e2G7 M{fLbJ43KM7:TR?= Mn\ESG1UVw>? MVHpcoR2[2W|IHTldIhwe3Cqb4L5cIF1cW:wIH;mJGlITi1zUh?= MmnrNVY3ODF{OES=
BON Mm[0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWjBdpdChjFy4pEK{txO MmnKSG1UVw>? NXTiWmQ4UUN3ME22MlYh|ryP NXLSTlhbOTZ4MEGyPFQ>
CM Mke0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEf3UWx,PeLCit88US=> MUjEUXNQ NGrZTHVKSzVyPUOuN{DPxE1? M1v1RVE3PjBzMki0
BON NUOwdZhkTnWwY4Tpc44h[XO|YYm= NVf3UHM4hjdwNfMAju69VQ>? M2DEdWROW09? NGDj[nlqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NUT2NlJjOTZ4MEGyPFQ>
CM M1fObGZ2dmO2aX;uJIF{e2G7 NEXqWlh,PeLCit88US=> NV7SWng5TE2VTx?= NFzPRoRqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MmjsNVY3ODF{OES=
BON MX\BdI9xfG:|aYOgZZN{[Xl? MVX+O{426oDMzszN M2nNbWROW09? M135[4lv\HWlZYOgRZBweHSxc3nz MnLDNVY3ODF{OES=
CM Ml;XRZBweHSxc3nzJIF{e2G7 MkDZglXjiIsQvF2= M3;HcGROW09? MVnpcoR2[2W|IFHwc5B1d3Orcx?= NGXRVGgyPjZyMUK4OC=>
HT-29 MkDNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIjibIx,OTEkgJtOwG0> MlH5SG1UVw>? MoXqTWM2OD1zLkeg{txO NFLNNmkyPzByN{CxOS=>
HCT-116 M3[zeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1;TOJ4yOOLCit88US=> M4j1S2ROW09? M1LjdWlEPTB;Mj61JO69VQ>? NXLOfFY3OTdyMEewNVU>
primary colorectal cancer cells MUDGeY5kfGmxbjDhd5NigQ>? Mn7mglXjiIsQvF2= M2\JemROW09? MX3hcJRmenNidHjlJI1wenCqb3zv[5khd2ZidHjlJJJmdWGrbnnu[{Bk\Wyucx?= MUCxO|AxPzBzNR?=
HTLA-230 NVHoNI5XTnWwY4Tpc44h[XO|YYm= MUn+PEDPxE1? NHTEO2JFVVOR NV7HXVBKcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MYSxO|EzOTh7OB?=
KCNR MnPTSpVv[3Srb36gZZN{[Xl? NYXPXVJthjhizszN M3XLdWROW09? NGfG[WtqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NGfHc5oyPzF{MUi5PC=>
SK-N-BE2c MorFSpVv[3Srb36gZZN{[Xl? Mnz5glgh|ryP NVzneppxTE2VTx?= NHrHcGZqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M3mxflE4OTJzOEm4
SK-N-BE MVjGeY5kfGmxbjDhd5NigQ>? MmPLglgh|ryP MYnEUXNQ NIjXbnZqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NULDSFQzOTdzMkG4PVg>
LAN-5 MWnGeY5kfGmxbjDhd5NigQ>? NH31dJl,QCEQvF2= NWDiNFU5TE2VTx?= NFXvRW9qdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> MnLLNVcyOjF6OUi=
GI-CA-N NGrRTHJHfW6ldHnvckBie3OjeR?= MUL+PEDPxE1? NGDRZ5ZFVVOR MlvQbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MWqxO|EzOTh7OB?=
SH-EP MXXGeY5kfGmxbjDhd5NigQ>? NWXkRlN1hjhizszN MnPLSG1UVw>? NECxfpBqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M2LGUlE4OTJzOEm4
SK-N-AS M4HYbWZ2dmO2aX;uJIF{e2G7 NYXEWJd7hjhizszN M4r5U2ROW09? MlPmbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MXKxO|EzOTh7OB?=
RN-GA NWGwTol1TnWwY4Tpc44h[XO|YYm= M{fQdp45KM7:TR?= NGjYc4pFVVOR NV3BOW84cW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MXOxO|EzOTh7OB?=
SY-5Y(N) NEfoUHlHfW6ldHnvckBie3OjeR?= NXzvbmRJhjhizszN NYC1NWtTTE2VTx?= M2\IbolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> M37yOlE4OTJzOEm4
GI-CA-N M2TsdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV;C[IdLhjhizszN M4\K[WROW09? NIezRWNKSzVyPTC2Mlgh|ryP NYPYd|A6OTdzMkG4PVg>
SH-EP MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUn+PEDPxE1? MmjSSG1UVw>? Mnn0TWM2OD1iMzFOwG0> NF21WGQyPzF{MUi5PC=>
HTLA-230 MmPQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEXBRpJ,QCEQvF2= NVLxZ|lnTE2VTx?= MWPJR|UxRSByLkWg{txO MojoNVcyOjF6OUi=
SK-N-BE2c MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mnfpglgh|ryP NEDUOpZFVVOR M4nvW2lEPTB;IEGuNUDPxE1? M2mxNVE4OTJzOEm4
SK-N-BE2 MoftS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoHxglgh|ryP M4L1eWROW09? NEjyPG9KSzVyPTCzJO69VQ>? NXfUcnRROTdzMkG4PVg>
SY-5Y (N) NIniNGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYTsWYtLhjhizszN NE\SXGpFVVOR M1jyZmlEPTB;IEKuOEDPxE1? M{DPNVE4OTJzOEm4
LAN-5 M2\ONmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVj+PEDPxE1? MXLEUXNQ MUfJR|UxRSByLkSg{txO NV7r[otrOTdzMkG4PVg>
KCNR NFHtO2RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGTIc2t,QCEQvF2= M{W2[GROW09? NHjwUYtKSzVyPTCwMlQh|ryP MmqwNVcyOjF6OUi=
RN-GA NWnW[Y5NT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmTqglgh|ryP NX;WSlFtTE2VTx?= NEHlTHFKSzVyPTCxMlMh|ryP NUf0eZFLOTdzMkG4PVg>
SK-N-AS M1rq[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MW\+PEDPxE1? MWDEUXNQ M3;4eYlv\HWlZYOgZZBweHSxc3nz MoPsNVcyOjF6OUi=
KCNR Moi5RZBweHSxc3nzJIF{e2G7 NX3DNZR3hjhizszN MWnEUXNQ MXjpcoR2[2W|IHHwc5B1d3Orcx?= M3PwW|E4OTJzOEm4
GI-CA-N M2Dqd2Fxd3C2b4Ppd{Bie3OjeR?= M1TVU545KM7:TR?= M2TxbmROW09? NVrHNIIycW6mdXPld{BieG:ydH;zbZM> NYnGco02OTdzMkG4PVg>
HTLA-230 NFHYUlVCeG:ydH;zbZMh[XO|YYm= M3LHVZ45KM7:TR?= MlXwSG1UVw>? NIXhWJpqdmS3Y3XzJIFxd3C2b4Ppdy=> MnftNVcyOjF6OUi=
SK-N-BE2c Mom0RZBweHSxc3nzJIF{e2G7 NEnNWJh,QCEQvF2= NIjJVmZFVVOR M{CwRolv\HWlZYOgZZBweHSxc3nz NFTSR5IyPzF{MUi5PC=>
SY-5Y (N) NG\aSmZCeG:ydH;zbZMh[XO|YYm= MVP+PEDPxE1? NHPyelNFVVOR NUGyVYxKcW6mdXPld{BieG:ydH;zbZM> MVWxO|EzOTh7OB?=
HL60AR MWPGeY5kfGmxbjDhd5NigQ>? MlTjNVYxKG6P MnT6[Y5p[W6lZYOgeIhmKGyndnXsd{Bw\iCyMkfLbZAy M{ThXFE4OzZzMkK1
HL60AR M3XS[2Fxd3C2b4Ppd{Bie3OjeR?= NWfKXWJXhjJyMDDuUS=> M3WxT4lv\HWlZYOgZZBweHSxc3nz NVv2fIxGOTd|NkGyNlU>
HPAF-II MXHLbY5ie2ViYYPzZZk> NV72ZYJlhjFizszN NIH4OVhFVVOR NGHWdVRqdmirYnn0d{BKT0ZvST3t[YRq[XSnZDDzbYdv[WyuaX7n M3H0SFE5PDR3NUKw
HPAF-II NGLGZpZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYn+NkDPxE1? MkPPSG1UVw>? MVvpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NWqzdmw5OTh2NEW1NlA>
HPAF-II NHT6[pVHfW6ldHnvckBie3OjeR?= NFv6[ox,OiEQvF2= NHfWNZVFVVOR MV\pcohq[mm2czDiZZNidCCjbnSgTWdHNUlvbXXkbYF1\WRicHHuZ5Jm[XSrYzDjZY5k\XJiY3XscEBucWe{YYTpc44> M3:yOlE5PDR3NUKw
TFK-1 MonZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFnFXVZ,OjVyIH7N MXTEUXNQ M2PnSmlEPTB;MD6yOkDPxE1? MkTZNlAxPjZ5M{S=
EGI-1 NVzQeZNMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFTDdpJ,OjVyIH7N NVnJOFhCTE2VTx?= M3W2OWlEPTB;MD6yPEDPxE1? NFTWS2QzODB4NkezOC=>
CC-LP-1 Ml3MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGjN[ml,OjVyIH7N M1\X[mROW09? Mmn3TWM2OD1yLkG1JO69VQ>? NWLaeWUzOjByNk[3N|Q>
CC-SW-1 NGrVdm9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGf0[XZ,OjVyIH7N MX7EUXNQ MmLYTWM2OD1yLkW0JO69VQ>? MVyyNFA3Pjd|NB?=
Sk-ChA-1 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkfiglI2OCCwTR?= M37lbGROW09? M2\2XWlEPTB;MD6yJO69VQ>? NG\h[nMzODB4NkezOC=>
Mz-ChA-1 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2DY[54zPTBibl2= MWfEUXNQ MWrJR|UxRTFwM{mg{txO MnnqNlAxPjZ5M{S=
Mz-ChA-2 Mmf3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFHafXR,OjVyIH7N M1ywVmROW09? MlnyTWM2OD1yLkezJO69VQ>? NHO3TGkzODB4NkezOC=>
ECC-1 NF[3TIVMcW6jc3WgZZN{[Xl? MnjwglExKM7:TR?= MWHEUXNQ M{XLTIlvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl6JR?= MkXINlEzQTV|M{W=
Ishikawa NE[3UWVMcW6jc3WgZZN{[Xl? NHnBe2Z,OTBizszN M3vHS2ROW09? MXnpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6OyV? M4LEclIyOjl3M{O1
USPC-1 M3XDVGtqdmG|ZTDhd5NigQ>? NHrleXN,OTBizszN NFO3[JVFVVOR NUXTVIdrcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliMUCwKS=> NWXJfnU4OjF{OUWzN|U>
USPC-2 MoPtT4lv[XOnIHHzd4F6 NWO4ZXVyhjFyIN88US=> NU\0eIdrTE2VTx?= M4LySYlvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl4JR?= NIDQ[2szOTJ7NUOzOS=>
ECC-1 NVy1ZYw1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYf+NVAh|ryP NHe3R3BFVVOR MXfk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u Mn\INlEzQTV|M{W=
Ishikawa NWLLOHNpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnK0glExKM7:TR?= MY\EUXNQ Mnju[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> MnnVNlEzQTV|M{W=
USPC-1 NI[1NolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYP+NVAh|ryP MXPEUXNQ NYSwbnI{\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NInG[XAzOTJ7NUOzOS=>
USPC-2 NYXjOZA3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVL+NVAh|ryP MkfPSG1UVw>? NIPlO|Zl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v NYDDbWRoOjF{OUWzN|U>

... 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

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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID