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 33 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 MmfnT4lv[XOnIHHzd4F6 NETT[Fh,OTEkgJtOwG0> NIjhOZNFVVOR NEXpNYRqdmirYnn0d{BKT0ZvSWKge4l1cCCLQ{WwJI9nKDBwMEi2JOKyKDBwMEK4JO69VQ>? MlTYNVUxPTB7MUW=
A14 MXzLbY5ie2ViYYPzZZk> MXL+NVDjiIsQvF2= MWXEUXNQ NWW5OJBjcW6qaXLpeJMhUW6|UjD3bZRpKEmFNUCgc4YhOi5|INMxJFAvOTZ|IN88US=> NVftNJMyOTVyNUC5NVU>
A431  NHzVXndMcW6jc3WgZZN{[Xl? NH7R[HZ,OTEkgJtOwG0> Mn;GSG1UVw>? MofFbY5pcWKrdIOgTGVTOSC5aYToJGlEPTBib3[gQlExKM7:TR?= NXTk[GtEOTVyNUC5NVU>
A31  Mmj2T4lv[XOnIHHzd4F6 MkTJglEx6oDMzszN MWnEUXNQ NYe2Um86cW6qaXLpeJMhWESJRmKge4l1cCCLQ{WwJI9nKD5zMDFOwG0> M1npdFE2ODVyOUG1
GIST882 MYHLbY5ie2ViYYPzZZk> MVr+NVDjiIsQvF2= NYC0S2l1TE2VTx?= NXvX[XN2cW6qaXLpeJMh[y2NaYSge4l1cCCLQ{WwJI9nKD53IN88US=> Ml32NVUxPTB7MUW=
32D-Bcr-Abl MVnLbY5ie2ViYYPzZZk> NGfq[Y9,OTEkgJtOwG0> NWm1PVV[TE2VTx?= M4L6SolvcGmkaYTzJGJkei2DYnygdFIyOCC5aYToJGlEPTBib3[gQlExKM7:TR?= MWCxOVA2ODlzNR?=
MCF-7  MnL2R5l1d3irY3n0fUBie3OjeR?= NWm4OZk5TE2VTx?= MorNTWM2OD1zLk[0JO69VQ>? MXqxOVA2ODlzNR?=
NWT-21 NGjyRVhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3\pXGROW09? MUjJR|UxRTBwMU[zJO69VQ>? MUOxOVA2ODlzNR?=
TC-71 NX;Id3J1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEPnclR,OSEQvF2= NXz6cnd5TE2VTx?= MUPpcohq[mm2czDpcpN2dGmwLXzpb4Uh\3Kxd4ToJIZi[3Sxcj3J5qCUdWWmaXH0[YQh\3Kxd4To MX[xOVg3PzN6Nh?=
TC-71 NILHZnVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1rLR5446oDMzszN MXTEUXNQ Ml3hTWM2ODxyLkWg{txO MknXNVU5Pjd|OE[=
Saos-2 M4DDfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmjHglfjiIsQvF2= MWPEUXNQ MUXJR|UxRDNizszN MlzJNVU5Pjd|OE[=
U-2OS NF7OclVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2fUWp446oDMzszN NHq4UItFVVOR M33ZVmlEPTB:MD61JO69VQ>? NFuwVJIyPTh4N{O4Oi=>
SK-ES-1 M1\JO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3fDfZ446oDMzszN NILQO5VFVVOR NH7HeXhKSzVyPECuOUDPxE1? NY\oV4hwOTV6NkezPFY>
SK-N-MC NV;WPHdVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1m2cJ446oDMzszN M{XyeWROW09? NUK4SHlKUUN3MEywMlUh|ryP Mln5NVU5Pjd|OE[=
RD-ES NX;GNm1WT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFX1SFB,P+LCit88US=> NYm3fGFFTE2VTx?= MXvJR|UxRDBwNTFOwG0> M4HXN|E2QDZ5M{i2
SJ-Rh 30 MmjjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlG0glfjiIsQvF2= Mkn5SG1UVw>? M1LuW2lEPTB:MD61JO69VQ>? MmrUNVU5Pjd|OE[=
SJ-Rh 4 M4rSSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVr+O-KBks7:TR?= NWfmZnVuTE2VTx?= MUjJR|UxRDBwNTFOwG0> MUOxOVg3PzN6Nh?=
6647 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4PmVp446oDMzszN M1:4VmROW09? NYLhVoN4UUN3MEywMlUh|ryP NGfBfJYyPTh4N{O4Oi=>
SARG NVjsWnFbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlToglfjiIsQvF2= NWrNPYk{TE2VTx?= Mn3vTWM2ODx|IN88US=> MYKxOVg3PzN6Nh?=
MOS M3LZRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M17kPJ446oDMzszN NETaOJJFVVOR NX7KbpRWUUN3MEy0JO69VQ>? M{e0bFE2QDZ5M{i2
IOR/OS7 NGDkdWlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NITU[ld,P+LCit88US=> NWmxU3BCTE2VTx?= MkPLTWM2ODxzIN88US=> NGjDOHYyPTh4N{O4Oi=>
IOR/OS9 M3uzVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkjHglfjiIsQvF2= MmDqSG1UVw>? MmHrTWM2ODx4IN88US=> MXGxOVg3PzN6Nh?=
IOR/OS10 MnLxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWj0ZmtvhjgkgJtOwG0> MX;EUXNQ NUPOcFRUUUN3MEy1JO69VQ>? MkDUNVU5Pjd|OE[=
IOR/OS14 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXn+O-KBks7:TR?= MYLEUXNQ MVHJR|UxRDRizszN M1fmdVE2QDZ5M{i2
LAP35 M364U2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{TqTJ446oDMzszN MmHzSG1UVw>? M{jm[mlEPTB:MD61JO69VQ>? MojGNVU5Pjd|OE[=
IOR/BRZ M2O5fGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVH+O-KBks7:TR?= NVv6W|RFTE2VTx?= MmPDTWM2ODxyLkWg{txO MmO0NVU5Pjd|OE[=
IOR/CAR M1XQ[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHXSO2R,P+LCit88US=> MXPEUXNQ MXfJR|UxRDFizszN M2fsdVE2QDZ5M{i2
IOR/NGR NX;wOIQ6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M17FbJ446oDMzszN NWrWbmNDTE2VTx?= NX3w[WlyUUN3MEywMlUh|ryP MVWxOVg3PzN6Nh?=
IOR/RCH NHL2VmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn\rglfjiIsQvF2= MV\EUXNQ NWH6[5R[UUN3MEywMlUh|ryP MljnNVU5Pjd|OE[=
RMZ-RC2 NHvsS4VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVX+O-KBks7:TR?= MnnWSG1UVw>? MkLhTWM2ODxyLkWg{txO M17yNFE2QDZ5M{i2
CCA M2jLSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEn5OW9,P+LCit88US=> MmnxSG1UVw>? NI\MT5pKSzVyPEKg{txO MYWxOVg3PzN6Nh?=
RD/18 NILMcGdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGPI[Zh,P+LCit88US=> M3TCW2ROW09? MlT3TWM2ODx2IN88US=> MlriNVU5Pjd|OE[=
OVCAR-3 MkTsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWj+NVXjiIsQvF2= NFrHSGJFVVOR MX\pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MlHiNVY{ODB6MkC=
OVCAR-4 NWi0XY41T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFHJSGV,OTYkgJtOwG0> M1nhUGROW09? NXnq[IFkcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MmLyNVY{ODB6MkC=
OVCAR-3 MUTBdI9xfG:|aYOgZZN{[Xl? NYL6dGs6hjF34pEK{txO M4nXPGROW09? MmDSbY5lfWOnczDhdI9xfG:|aYO= NEXKcJkyPjNyMEiyNC=>
OVCAR-4 NXfOcpM5SXCxcITvd4l{KGG|c3H5 MmX6glE26oDMzszN M{\0TmROW09? NITQOItqdmS3Y3XzJIFxd3C2b4Ppdy=> NFuyeIsyPjNyMEiyNC=>
OVCAR-3 M1G0OWZ2dmO2aX;uJIF{e2G7 NFvx[ot,OTYkgJtOwG0> NYnVPGhFTE2VTx?= MnHtSIVkemWjc3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? NIX0NnMyPjNyMEiyNC=>
Huh-7 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmriglEx6oDMzszN NYrtbGlUTE2VTx?= MYfJR|UxRTFwNDFOwG0> MWWxOlU{ODd|NB?=
Hep-G2 NH25bnNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2D2Z54yOOLCit88US=> NGn3bW1FVVOR MmLqTWM2OD1zLkig{txO Ml;4NVY2OzB5M{S=
Hep-3B M4[yd2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnHrglEx6oDMzszN NXftNldWTE2VTx?= MVLJR|UxRTFwOTFOwG0> MYSxOlU{ODd|NB?=
SK-Hep-1 MlrrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnzLglEx6oDMzszN NXXZOFRPTE2VTx?= M4XFRWlEPTB;Nj65JO69VQ>? NGG1VYUyPjV|MEezOC=>
Huh-7 MoPSSpVv[3Srb36gZZN{[Xl? NWTicWE5hjFy4pEK{txO Moe0SG1UVw>? NEG4b4JKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M1;KXFE3PTNyN{O0
Hep-G2 MknQSpVv[3Srb36gZZN{[Xl? MoSxglEx6oDMzszN MkTCSG1UVw>? NFfuZ2JKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MXOxOlU{ODd|NB?=
SK-Hep-1 NEG2RnFHfW6ldHnvckBie3OjeR?= M1nPcZ4yOOLCit88US=> MXzEUXNQ MVLJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NEnJO|QyPjV|MEezOC=>
BON MYnLbY5ie2ViYYPzZZk> M4C2Wp43KM7:TR?= MkXySG1UVw>? MoPNbY5lfWOnczDk[ZBpd3OyaH;yfYxifGmxbjDv[kBKT0ZvMWK= NHTXWmwyPjZyMUK4OC=>
BON NFn0VGJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlfSglEx6oDMzszN M3H4SGROW09? M2fRXWlEPTB;Nj62JO69VQ>? NXKwfoZjOTZ4MEGyPFQ>
CM Mn\BS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH6yeYp,PeLCit88US=> M2LQZ2ROW09? M4\FVWlEPTB;Mz6zJO69VQ>? MmCyNVY3ODF{OES=
BON MYPGeY5kfGmxbjDhd5NigQ>? NVHjO2FKhjdwNfMAju69VQ>? NF;MUXhFVVOR M2D5[Ylv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NHPqb5kyPjZyMUK4OC=>
CM NHnpXINHfW6ldHnvckBie3OjeR?= M33hOZ426oDMzszN NV\FemRVTE2VTx?= NGjve|JqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MmXkNVY3ODF{OES=
BON MVzBdI9xfG:|aYOgZZN{[Xl? MlvNglcvPeLCit88US=> MlzQSG1UVw>? NEnKb4NqdmS3Y3XzJGFxd3C2b4Ppdy=> MVKxOlYxOTJ6NB?=
CM NGmxWIRCeG:ydH;zbZMh[XO|YYm= MV7+OgKBks7:TR?= NUfEeIVUTE2VTx?= M1nze4lv\HWlZYOgRZBweHSxc3nz NVv1[JJCOTZ4MEGyPFQ>
HT-29 NILKZ41Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1TrVJ4yOOLCit88US=> NHXEepBFVVOR MkDhTWM2OD1zLkeg{txO NX\ITJlkOTdyMEewNVU>
HCT-116 NYCwPW9xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{TFfZ4yOOLCit88US=> MXPEUXNQ M1rh[2lEPTB;Mj61JO69VQ>? NGm1dYwyPzByN{CxOS=>
primary colorectal cancer cells NGfPbpNHfW6ldHnvckBie3OjeR?= M{i1U5426oDMzszN NHi4TlFFVVOR MX3hcJRmenNidHjlJI1wenCqb3zv[5khd2ZidHjlJJJmdWGrbnnu[{Bk\Wyucx?= NV2wXGtlOTdyMEewNVU>
HTLA-230 NHznOXRHfW6ldHnvckBie3OjeR?= MkHyglgh|ryP M1XKTGROW09? NXzGUoJvcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 M3L4UlE4OTJzOEm4
KCNR M3T4TGZ2dmO2aX;uJIF{e2G7 MVn+PEDPxE1? NUTidFRzTE2VTx?= M2O4O4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MYixO|EzOTh7OB?=
SK-N-BE2c M4TjbWZ2dmO2aX;uJIF{e2G7 MVz+PEDPxE1? MYnEUXNQ NEjybY1qdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NWPxWWg6OTdzMkG4PVg>
SK-N-BE M2H4OWZ2dmO2aX;uJIF{e2G7 Mmjjglgh|ryP Mn3FSG1UVw>? Mn35bY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MonVNVcyOjF6OUi=
LAN-5 NYfxfppsTnWwY4Tpc44h[XO|YYm= NWHD[GNrhjhizszN NFXo[XNFVVOR MUnpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= M2PSZVE4OTJzOEm4
GI-CA-N NHHhNndHfW6ldHnvckBie3OjeR?= NGjxd|F,QCEQvF2= M2XNVGROW09? NX\h[YlpcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MnXwNVcyOjF6OUi=
SH-EP MnTmSpVv[3Srb36gZZN{[Xl? NGHKd3d,QCEQvF2= NWXMTo5GTE2VTx?= NYHnVHk1cW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 M1rDSlE4OTJzOEm4
SK-N-AS M4\QOGZ2dmO2aX;uJIF{e2G7 Moryglgh|ryP NGD4NWxFVVOR NWDtOpFncW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 NF[4ZnoyPzF{MUi5PC=>
RN-GA MYTGeY5kfGmxbjDhd5NigQ>? NF;I[4R,QCEQvF2= M{TuO2ROW09? NWfPb|h3cW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MofNNVcyOjF6OUi=
SY-5Y(N) NWW1fIc1TnWwY4Tpc44h[XO|YYm= MWT+PEDPxE1? NF\4VVZFVVOR NU\RUJc2cW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 Mn\CNVcyOjF6OUi=
GI-CA-N NHHaXVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mmfkglgh|ryP MVXEUXNQ NYnuPZBDUUN3ME2gOk45KM7:TR?= MXKxO|EzOTh7OB?=
SH-EP MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHO3R|N,QCEQvF2= NF;NfVBFVVOR MlvUTWM2OD1iMzFOwG0> NFTobXMyPzF{MUi5PC=>
HTLA-230 NX\BcVRDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnfMglgh|ryP NUfRZlkzTE2VTx?= NELzPVBKSzVyPTCwMlUh|ryP MVyxO|EzOTh7OB?=
SK-N-BE2c Mk\ZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIOxR|l,QCEQvF2= MknPSG1UVw>? NU\udmRmUUN3ME2gNU4yKM7:TR?= NEPFTWsyPzF{MUi5PC=>
SK-N-BE2 MmfkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHPJdop,QCEQvF2= NHfIOYhFVVOR MmOxTWM2OD1iMzFOwG0> NV;YUFhtOTdzMkG4PVg>
SY-5Y (N) MmHQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFvZd4p,QCEQvF2= M{TRTGROW09? MY\JR|UxRSB{LkSg{txO MX:xO|EzOTh7OB?=
LAN-5 MlLXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4XBPZ45KM7:TR?= M1\kNWROW09? MnPYTWM2OD1iMD60JO69VQ>? MnTkNVcyOjF6OUi=
KCNR MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVrHbYM{hjhizszN NImwb2pFVVOR M1ThbWlEPTB;IECuOEDPxE1? MYqxO|EzOTh7OB?=
RN-GA MljUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVT+PEDPxE1? MWHEUXNQ MkTNTWM2OD1iMT6zJO69VQ>? NF3VXJkyPzF{MUi5PC=>
SK-N-AS NFnqbXRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVXyNYJ7hjhizszN Ml7MSG1UVw>? MXvpcoR2[2W|IHHwc5B1d3Orcx?= NH;lUXgyPzF{MUi5PC=>
KCNR M333bWFxd3C2b4Ppd{Bie3OjeR?= Ml3Iglgh|ryP NUjnWYViTE2VTx?= NWP3OXpVcW6mdXPld{BieG:ydH;zbZM> M3TMU|E4OTJzOEm4
GI-CA-N M{ftfWFxd3C2b4Ppd{Bie3OjeR?= MkTHglgh|ryP M4rMbmROW09? MVTpcoR2[2W|IHHwc5B1d3Orcx?= M2fmS|E4OTJzOEm4
HTLA-230 NVjtdGFRSXCxcITvd4l{KGG|c3H5 MYD+PEDPxE1? M{XD[mROW09? NYjPSZg{cW6mdXPld{BieG:ydH;zbZM> M3;xflE4OTJzOEm4
SK-N-BE2c MVvBdI9xfG:|aYOgZZN{[Xl? MmDQglgh|ryP Mn\USG1UVw>? Mkn1bY5lfWOnczDhdI9xfG:|aYO= MkTINVcyOjF6OUi=
SY-5Y (N) MlG3RZBweHSxc3nzJIF{e2G7 M1K4Sp45KM7:TR?= NIDQcYdFVVOR M4eydYlv\HWlZYOgZZBweHSxc3nz NVXvNWw{OTdzMkG4PVg>
HL60AR NFfIdJRHfW6ldHnvckBie3OjeR?= MnPYNVYxKG6P NXPIZ2po\W6qYX7j[ZMhfGinIHzleoVteyCxZjDwNldMcXBz MmnpNVc{PjF{MkW=
HL60AR M3myeWFxd3C2b4Ppd{Bie3OjeR?= NVHy[3hwhjJyMDDuUS=> M2\vSIlv\HWlZYOgZZBweHSxc3nz Mm\INVc{PjF{MkW=
HPAF-II NWrsNI1pU2mwYYPlJIF{e2G7 MWn+NUDPxE1? Ml3oSG1UVw>? NHnWe5FqdmirYnn0d{BKT0ZvST3t[YRq[XSnZDDzbYdv[WyuaX7n MXqxPFQ1PTV{MB?=
HPAF-II NF6zNZRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXH+NkDPxE1? MVfEUXNQ NVXWbWJPcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M{LPN|E5PDR3NUKw
HPAF-II NWG2R494TnWwY4Tpc44h[XO|YYm= M4PGXJ4zKM7:TR?= M2T6VWROW09? MWHpcohq[mm2czDiZZNidCCjbnSgTWdHNUlvbXXkbYF1\WRicHHuZ5Jm[XSrYzDjZY5k\XJiY3XscEBucWe{YYTpc44> NICxWFYyQDR2NUWyNC=>
TFK-1 NX3oblY2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojpglI2OCCwTR?= M3jPO2ROW09? MXfJR|UxRTBwMk[g{txO NH\NcZIzODB4NkezOC=>
EGI-1 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2LoeJ4zPTBibl2= NH7uPJVFVVOR NYDY[FFHUUN3ME2wMlI5KM7:TR?= NYrGWnY1OjByNk[3N|Q>
CC-LP-1 M3zRcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGPOZ5l,OjVyIH7N NWq5WWtVTE2VTx?= NU[1ZlI{UUN3ME2wMlE2KM7:TR?= MmXWNlAxPjZ5M{S=
CC-SW-1 MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2C1ep4zPTBibl2= NW\LUJBETE2VTx?= MoSwTWM2OD1yLkW0JO69VQ>? MlHJNlAxPjZ5M{S=
Sk-ChA-1 MoPUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYLjR4c4hjJ3MDDuUS=> NIXpVlBFVVOR Ml7STWM2OD1yLkKg{txO M36yUVIxODZ4N{O0
Mz-ChA-1 MnHiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVTUUHhthjJ3MDDuUS=> NFyydnNFVVOR NHm4RXpKSzVyPUGuN|kh|ryP NV;LdYNROjByNk[3N|Q>
Mz-ChA-2 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIDhXJJ,OjVyIH7N NXzPTYFUTE2VTx?= MoDxTWM2OD1yLkezJO69VQ>? NEHkb|MzODB4NkezOC=>
ECC-1 MnTBT4lv[XOnIHHzd4F6 NEXXZmZ,OTBizszN NFXY[mtFVVOR MWHpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6QCV? Ml;2NlEzQTV|M{W=
Ishikawa M{Hi[WtqdmG|ZTDhd5NigQ>? NWLUV4xOhjFyIN88US=> NUfvbIlpTE2VTx?= Mo\ubY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQTNn NG\qVVMzOTJ7NUOzOS=>
USPC-1 M4PXbmtqdmG|ZTDhd5NigQ>? MXf+NVAh|ryP M{f5[mROW09? Mn:0bY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhOTByJR?= M1;4d|IyOjl3M{O1
USPC-2 MYnLbY5ie2ViYYPzZZk> NFWwWpR,OTBizszN NHLmW2FFVVOR MVLpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6PiV? MYWyNVI6PTN|NR?=
ECC-1 M4[w[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWn+NVAh|ryP NGe3XIhFVVOR M1;0eIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NEC4c|IzOTJ7NUOzOS=>
Ishikawa MnHwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1S2Xp4yOCEQvF2= NGi5UJpFVVOR MlvQ[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> M1WwcVIyOjl3M{O1
USPC-1 NV3FVWlRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWjhZYZWhjFyIN88US=> MXnEUXNQ Mnvp[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NXixWlY1OjF{OUWzN|U>
USPC-2 MlezS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2C5UJ4yOCEQvF2= M{\JR2ROW09? NVu1NYF4\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NWDzZVN5OjF{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]
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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
  • 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 (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).

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID