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 38 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 MXLLbY5ie2ViYYPzZZk> M1i0dp4yOOLCit88US=> NYL3XHVjTE2VTx?= MkfhbY5pcWKrdIOgTWdHNUmUIIfpeIghUUN3MDDv[kAxNjB6NjFCtUAxNjB{ODFOwG0> M4HHOFE2ODVyOUG1
A14 NHLQTFhMcW6jc3WgZZN{[Xl? NWXCcHhZhjFy4pEK{txO MVHEUXNQ MYnpcohq[mm2czDJcpNTKHerdHigTWM2OCCxZjCyMlMhyrFiMD6xOlMh|ryP NEH1SlkyPTB3MEmxOS=>
A431  M1P3UmtqdmG|ZTDhd5NigQ>? Ml;RglEx6oDMzszN M4fsdGROW09? M1;ZVYlvcGmkaYTzJGhGWjFid3n0bEBKSzVyIH;mJF4yOCEQvF2= M13ZcVE2ODVyOUG1
A31  MVrLbY5ie2ViYYPzZZk> NXTiOJlmhjFy4pEK{txO MWPEUXNQ MVXpcohq[mm2czDQSGdHWiC5aYToJGlEPTBib3[gQlExKM7:TR?= M{G5WVE2ODVyOUG1
GIST882 NIDo[W5McW6jc3WgZZN{[Xl? NWnWR3BphjFy4pEK{txO NXeyfYx4TE2VTx?= MmfFbY5pcWKrdIOgZ{1McXRid3n0bEBKSzVyIH;mJF42KM7:TR?= M3\UbVE2ODVyOUG1
32D-Bcr-Abl NVjZS4NWU2mwYYPlJIF{e2G7 MW\+NVDjiIsQvF2= MljxSG1UVw>? M3f6cIlvcGmkaYTzJGJkei2DYnygdFIyOCC5aYToJGlEPTBib3[gQlExKM7:TR?= MV6xOVA2ODlzNR?=
MCF-7  NXXQOZJtS3m2b4jpZ4l1gSCjc4PhfS=> MkD0SG1UVw>? NGjKNFhKSzVyPUGuOlQh|ryP M4ixcVE2ODVyOUG1
NWT-21 NXnYU4o3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1vPS2ROW09? NEXQN29KSzVyPUCuNVY{KM7:TR?= M4XrTFE2ODVyOUG1
TC-71 NXOzdXBZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGj5S5d,OSEQvF2= MomxSG1UVw>? MnHmbY5pcWKrdIOgbY5{fWyrbj3sbYtmKGe{b4f0bEBn[WO2b4KtTgKBm22nZHnheIVlKGe{b4f0bC=> NWT1UHlQOTV6NkezPFY>
TC-71 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHTqVFd,P+LCit88US=> MlPCSG1UVw>? M2DRU2lEPTB:MD61JO69VQ>? NGrqOVYyPTh4N{O4Oi=>
Saos-2 NYjhc2RFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4DmUJ446oDMzszN M{TE[GROW09? MX7JR|UxRDNizszN MmLINVU5Pjd|OE[=
U-2OS NWnMemx4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M13uWJ446oDMzszN M4TSe2ROW09? NUfJRnJnUUN3MEywMlUh|ryP MkTiNVU5Pjd|OE[=
SK-ES-1 Mof4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MorUglfjiIsQvF2= NVnxcIxMTE2VTx?= M{e0UmlEPTB:MD61JO69VQ>? NGrtT48yPTh4N{O4Oi=>
SK-N-MC MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWL+O-KBks7:TR?= MXPEUXNQ M4\WUWlEPTB:MD61JO69VQ>? MorTNVU5Pjd|OE[=
RD-ES NELTWI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnvFglfjiIsQvF2= NHTsZ|BFVVOR NVe2Tlc6UUN3MEywMlUh|ryP MVWxOVg3PzN6Nh?=
SJ-Rh 30 Ml\pS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVT+O-KBks7:TR?= MXTEUXNQ NGO1S41KSzVyPECuOUDPxE1? NIXIUmEyPTh4N{O4Oi=>
SJ-Rh 4 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX;XUHFbhjgkgJtOwG0> MlnqSG1UVw>? NI\KOmdKSzVyPECuOUDPxE1? NIW0U5QyPTh4N{O4Oi=>
6647 NILIdIJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4\UOJ446oDMzszN MlvpSG1UVw>? NFfmcIVKSzVyPECuOUDPxE1? NYHobGRlOTV6NkezPFY>
SARG MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIWwNWp,P+LCit88US=> Mne4SG1UVw>? NX;U[oFrUUN3MEyzJO69VQ>? NV7qWIl{OTV6NkezPFY>
MOS NYH0[mR6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV;5Spl5hjgkgJtOwG0> MXzEUXNQ NGrzbo9KSzVyPESg{txO NHjpUWIyPTh4N{O4Oi=>
IOR/OS7 Mo\BS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX6weYx1hjgkgJtOwG0> Ml\SSG1UVw>? MWfJR|UxRDFizszN MVGxOVg3PzN6Nh?=
IOR/OS9 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWr+O-KBks7:TR?= NHvTOXJFVVOR M37U[mlEPTB:NjFOwG0> NY[xWllROTV6NkezPFY>
IOR/OS10 NV74doo4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWXrUGRzhjgkgJtOwG0> M4PG[2ROW09? MnrnTWM2ODx3IN88US=> M3rK[lE2QDZ5M{i2
IOR/OS14 NHLPV5FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHOyfHl,P+LCit88US=> Ml:3SG1UVw>? MXXJR|UxRDRizszN NI\JeXQyPTh4N{O4Oi=>
LAP35 NFvXSVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4\wV5446oDMzszN NXrXemZQTE2VTx?= Mnv3TWM2ODxyLkWg{txO MmL4NVU5Pjd|OE[=
IOR/BRZ NFXie2pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mnq2glfjiIsQvF2= NH3yNmdFVVOR MYDJR|UxRDBwNTFOwG0> MUGxOVg3PzN6Nh?=
IOR/CAR MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUH+O-KBks7:TR?= M1XIWmROW09? NXe5WXpCUUN3MEyxJO69VQ>? MU[xOVg3PzN6Nh?=
IOR/NGR MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHPveHd,P+LCit88US=> NV3QWY1[TE2VTx?= MYLJR|UxRDBwNTFOwG0> Mk\jNVU5Pjd|OE[=
IOR/RCH NF62UXBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlfSglfjiIsQvF2= MnnxSG1UVw>? MnKzTWM2ODxyLkWg{txO NHHJNYYyPTh4N{O4Oi=>
RMZ-RC2 NU\wWYtMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXj+O-KBks7:TR?= NV7qNIVmTE2VTx?= NFjNSYpKSzVyPECuOUDPxE1? NWi3b4ZROTV6NkezPFY>
CCA MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX;+O-KBks7:TR?= NHu5VJJFVVOR NFX4RWNKSzVyPEKg{txO NW\lVlNGOTV6NkezPFY>
RD/18 NUS1eno5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4DuPJ446oDMzszN NVTZc5JzTE2VTx?= M4nHOWlEPTB:NDFOwG0> MYixOVg3PzN6Nh?=
OVCAR-3 NHO3S2hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXH+NVXjiIsQvF2= NWXqcXU3TE2VTx?= MoLWbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u Mn;oNVY{ODB6MkC=
OVCAR-4 NWHLd4txT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVL+NVXjiIsQvF2= MVnEUXNQ NHnzfW9qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NUTMS5p5OTZ|MEC4NlA>
OVCAR-3 NX2zOVdRSXCxcITvd4l{KGG|c3H5 MUT+NVXjiIsQvF2= NVq0[XJnTE2VTx?= MknEbY5lfWOnczDhdI9xfG:|aYO= NHnLNFIyPjNyMEiyNC=>
OVCAR-4 NUXCelhVSXCxcITvd4l{KGG|c3H5 MYX+NVXjiIsQvF2= MYfEUXNQ NWjvcZZ5cW6mdXPld{BieG:ydH;zbZM> MkXZNVY{ODB6MkC=
OVCAR-3 NWrMWYhKTnWwY4Tpc44h[XO|YYm= M1\UTJ4yPeLCit88US=> NGDMT2ZFVVOR NFvJWo1F\WO{ZXHz[ZMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NXvr[2NKOTZ|MEC4NlA>
Huh-7 NVvWb|BuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYXpfJM3hjFy4pEK{txO MWnEUXNQ NHuwTFBKSzVyPUGuOEDPxE1? NIXzS5oyPjV|MEezOC=>
Hep-G2 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoqxglEx6oDMzszN NXnhOWlETE2VTx?= MV\JR|UxRTFwODFOwG0> NUjZ[Y9oOTZ3M{C3N|Q>
Hep-3B NFXFNXJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVewcmc4hjFy4pEK{txO M4PyRWROW09? NEfvdG5KSzVyPUGuPUDPxE1? NYfSXIhSOTZ3M{C3N|Q>
SK-Hep-1 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1X6ZZ4yOOLCit88US=> M{DDbGROW09? NXr5WoxDUUN3ME22Mlkh|ryP NGHldHEyPjV|MEezOC=>
Huh-7 M2rMTmZ2dmO2aX;uJIF{e2G7 NYnFOGtjhjFy4pEK{txO MWnEUXNQ MmjiTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M4TaelE3PTNyN{O0
Hep-G2 MYXGeY5kfGmxbjDhd5NigQ>? NIDxS3F,OTEkgJtOwG0> NYTFeYJHTE2VTx?= MoX3TY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MljINVY2OzB5M{S=
SK-Hep-1 NFnsS5JHfW6ldHnvckBie3OjeR?= MmmzglEx6oDMzszN NWrOdYxbTE2VTx?= NUC3UYVjUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MlTrNVY2OzB5M{S=
BON MYXLbY5ie2ViYYPzZZk> MnLYglYh|ryP M17uNGROW09? M{PFOolv\HWlZYOg[IVxcG:|cHjvdplt[XSrb36gc4YhUUeILUHS MlP6NVY3ODF{OES=
BON NWCwV2d{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn71glEx6oDMzszN NWO3UGpETE2VTx?= MkO3TWM2OD14Lk[g{txO MkLaNVY3ODF{OES=
CM MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXX+OgKBks7:TR?= MkDZSG1UVw>? MW\JR|UxRTNwMzFOwG0> M{XNWlE3PjBzMki0
BON M4XKXWZ2dmO2aX;uJIF{e2G7 Mom5glcvPeLCit88US=> MV7EUXNQ NYDKN|Y3cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MoH2NVY3ODF{OES=
CM NHTEeGZHfW6ldHnvckBie3OjeR?= NUjEdIxNhjYkgJtOwG0> NVTuTXFMTE2VTx?= M2S2Oolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NV\lWJhNOTZ4MEGyPFQ>
BON M3iwUGFxd3C2b4Ppd{Bie3OjeR?= Mkf1glcvPeLCit88US=> MkXySG1UVw>? M2Dp[Ilv\HWlZYOgRZBweHSxc3nz NUn6dlI{OTZ4MEGyPFQ>
CM MnrURZBweHSxc3nzJIF{e2G7 NVvjeoN4hjYkgJtOwG0> M1\EWGROW09? NWTzNnFEcW6mdXPld{BCeG:ydH;zbZM> NUHtT2U{OTZ4MEGyPFQ>
HT-29 NF;tR3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX\+NVDjiIsQvF2= MVnEUXNQ M4PZUGlEPTB;MT63JO69VQ>? Mm\tNVcxODdyMUW=
HCT-116 NXSwe25vT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYeyTmNshjFy4pEK{txO MYXEUXNQ MnuxTWM2OD1{LkWg{txO NYfTboRHOTdyMEewNVU>
primary colorectal cancer cells M{jxSWZ2dmO2aX;uJIF{e2G7 MmDuglXjiIsQvF2= MYPEUXNQ MljEZYx1\XK|IITo[UBud3KyaH;sc4d6KG:oIITo[UBz\W2jaX7pcoch[2WubIO= NUWxUnVNOTdyMEewNVU>
HTLA-230 M1Lo[2Z2dmO2aX;uJIF{e2G7 M3\kT545KM7:TR?= NY[4cot7TE2VTx?= MmTubY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NIriR|EyPzF{MUi5PC=>
KCNR M2nGcWZ2dmO2aX;uJIF{e2G7 MWj+PEDPxE1? MnLlSG1UVw>? MoDabY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 M2rWXlE4OTJzOEm4
SK-N-BE2c MUXGeY5kfGmxbjDhd5NigQ>? Mly3glgh|ryP MmTFSG1UVw>? MWHpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MWWxO|EzOTh7OB?=
SK-N-BE NVnoc4d2TnWwY4Tpc44h[XO|YYm= M4TOZZ45KM7:TR?= M17YdWROW09? MWXpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NFPYUYgyPzF{MUi5PC=>
LAN-5 M{X6d2Z2dmO2aX;uJIF{e2G7 MX7+PEDPxE1? NWDGcXQ{TE2VTx?= NWHwXFBHcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 M4Pt[|E4OTJzOEm4
GI-CA-N MmnqSpVv[3Srb36gZZN{[Xl? MoK1glgh|ryP NH;LPWJFVVOR NFTzVoRqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NXGwdpVnOTdzMkG4PVg>
SH-EP NWK0XnBiTnWwY4Tpc44h[XO|YYm= M4LWVp45KM7:TR?= MXnEUXNQ MkftbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NFfyRlEyPzF{MUi5PC=>
SK-N-AS M3jYbmZ2dmO2aX;uJIF{e2G7 MkTuglgh|ryP MoHlSG1UVw>? MV\pcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NH;2PYEyPzF{MUi5PC=>
RN-GA NFjGSXdHfW6ldHnvckBie3OjeR?= NVfJfmE1hjhizszN Mk\zSG1UVw>? MYjpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NHTYWVUyPzF{MUi5PC=>
SY-5Y(N) NHXuW3JHfW6ldHnvckBie3OjeR?= NEK2XGh,QCEQvF2= MoXxSG1UVw>? M2iwU4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NYXaTlhPOTdzMkG4PVg>
GI-CA-N NUnReXNoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2HPUZ45KM7:TR?= MWPEUXNQ M4\JeWlEPTB;IE[uPEDPxE1? NVLPTXNTOTdzMkG4PVg>
SH-EP NHf3VllIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVznW5huhjhizszN MX3EUXNQ MlHMTWM2OD1iMzFOwG0> NYjDN2l2OTdzMkG4PVg>
HTLA-230 M{XLcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIrMfJl,QCEQvF2= MnfpSG1UVw>? NH\6PFdKSzVyPTCwMlUh|ryP M1rTOVE4OTJzOEm4
SK-N-BE2c M1TMdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1X6fp45KM7:TR?= MmKxSG1UVw>? MorLTWM2OD1iMT6xJO69VQ>? MVexO|EzOTh7OB?=
SK-N-BE2 M4fiO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHP6PZR,QCEQvF2= MVTEUXNQ NIDxepZKSzVyPTCzJO69VQ>? M3OxZ|E4OTJzOEm4
SY-5Y (N) NFXDZVNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHruR3F,QCEQvF2= NV3BfnFtTE2VTx?= MojyTWM2OD1iMj60JO69VQ>? MknjNVcyOjF6OUi=
LAN-5 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MknYglgh|ryP M1TvSGROW09? MUHJR|UxRSByLkSg{txO M{XhblE4OTJzOEm4
KCNR NFHJVIZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MonFglgh|ryP NYX1[JJETE2VTx?= MkXPTWM2OD1iMD60JO69VQ>? M{XqNVE4OTJzOEm4
RN-GA MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{PnSZ45KM7:TR?= MUHEUXNQ NFTqb3lKSzVyPTCxMlMh|ryP M1PsbVE4OTJzOEm4
SK-N-AS NIHR[m1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYXESYRwhjhizszN NGj0R4dFVVOR Mmq0bY5lfWOnczDhdI9xfG:|aYO= NWT5OJFKOTdzMkG4PVg>
KCNR NVLXTGN[SXCxcITvd4l{KGG|c3H5 NGXIfW9,QCEQvF2= Mn3NSG1UVw>? NESzc3BqdmS3Y3XzJIFxd3C2b4Ppdy=> MlS1NVcyOjF6OUi=
GI-CA-N M3zL[GFxd3C2b4Ppd{Bie3OjeR?= M{i2UZ45KM7:TR?= NFzvcoRFVVOR NVrTNoF[cW6mdXPld{BieG:ydH;zbZM> MoTlNVcyOjF6OUi=
HTLA-230 NI\nSFBCeG:ydH;zbZMh[XO|YYm= MlHSglgh|ryP NIHYfHlFVVOR NWLTTYhNcW6mdXPld{BieG:ydH;zbZM> MY[xO|EzOTh7OB?=
SK-N-BE2c MmLTRZBweHSxc3nzJIF{e2G7 MmjJglgh|ryP NYXBdlUyTE2VTx?= NX;2foRDcW6mdXPld{BieG:ydH;zbZM> MVqxO|EzOTh7OB?=
SY-5Y (N) Mm\rRZBweHSxc3nzJIF{e2G7 NIDCUW5,QCEQvF2= NHT1eGlFVVOR NUe4enEzcW6mdXPld{BieG:ydH;zbZM> NV3nUIg3OTdzMkG4PVg>
HL60AR M2nJe2Z2dmO2aX;uJIF{e2G7 MmnaNVYxKG6P NEnpeW9mdmijbnPld{B1cGVibHX2[Yx{KG:oIICyO2tqeDF? MYGxO|M3OTJ{NR?=
HL60AR NF\O[otCeG:ydH;zbZMh[XO|YYm= Mkm0glIxOCCwTR?= M4DkOIlv\HWlZYOgZZBweHSxc3nz NFPoNGYyPzN4MUKyOS=>
HPAF-II MVXLbY5ie2ViYYPzZZk> NYXwNXVShjFizszN NYPmUXpNTE2VTx?= NVXTSpl2cW6qaXLpeJMhUUeILVmtcYVlcWG2ZXSgd4lodmGubHnu[y=> M2LOZ|E5PDR3NUKw
HPAF-II MkL5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2Dhdp4zKM7:TR?= MYDEUXNQ M3\FcYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NHfmZmUyQDR2NUWyNC=>
HPAF-II MorySpVv[3Srb36gZZN{[Xl? NXLhZotohjJizszN MXjEUXNQ MlXSbY5pcWKrdIOgZoF{[WxiYX7kJGlITi2LLX3l[IlifGWmIIDhcoNz\WG2aXOgZ4Fv[2W{IHPlcIwhdWmpcnH0bY9v MoPJNVg1PDV3MkC=
TFK-1 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIH4TFR,OjVyIH7N MmPHSG1UVw>? NHrHfopKSzVyPUCuNlYh|ryP MVSyNFA3Pjd|NB?=
EGI-1 M{XtWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYS3OolwhjJ3MDDuUS=> M3\IU2ROW09? NIDrR21KSzVyPUCuNlgh|ryP NVS2eI1zOjByNk[3N|Q>
CC-LP-1 NYC5SohST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWn+NlUxKG6P M2HORmROW09? MWDJR|UxRTBwMUWg{txO NGrWXIYzODB4NkezOC=>
CC-SW-1 M33WT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoPvglI2OCCwTR?= MojaSG1UVw>? NFzUbo1KSzVyPUCuOVQh|ryP M33JbVIxODZ4N{O0
Sk-ChA-1 M4robGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWe1OG1HhjJ3MDDuUS=> M2rTW2ROW09? MX;JR|UxRTBwMjFOwG0> NHSxS|YzODB4NkezOC=>
Mz-ChA-1 NYPGc|R6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUf+NlUxKG6P NGP0bmFFVVOR NXnHTok6UUN3ME2xMlM6KM7:TR?= NX31bWd5OjByNk[3N|Q>
Mz-ChA-2 MlXMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MljYglI2OCCwTR?= NXfLPVRHTE2VTx?= MmHsTWM2OD1yLkezJO69VQ>? M37BNFIxODZ4N{O0
ECC-1 MY\LbY5ie2ViYYPzZZk> M1:xSp4yOCEQvF2= M4j1bGROW09? M1:zRYlvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl6JR?= MXeyNVI6PTN|NR?=
Ishikawa NHfi[nVMcW6jc3WgZZN{[Xl? NV:5d5Z1hjFyIN88US=> M3q2VWROW09? NGP2NYFqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSB7MzW= NIC5NWEzOTJ7NUOzOS=>
USPC-1 NYP5cIhZU2mwYYPlJIF{e2G7 NEXHNm5,OTBizszN MYPEUXNQ NHiz[WxqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSBzMECl NGnO[WUzOTJ7NUOzOS=>
USPC-2 Mn\TT4lv[XOnIHHzd4F6 MnLFglExKM7:TR?= MlnrSG1UVw>? NVvqUGpqcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOU[l NEGzUmQzOTJ7NUOzOS=>
ECC-1 NF\jZ5RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmPSglExKM7:TR?= M2\KemROW09? NH6xTZJl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v NEXOWG8zOTJ7NUOzOS=>
Ishikawa NYfPVJhzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXP+NVAh|ryP MVjEUXNQ NX;l[JJU\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NHG3VoMzOTJ7NUOzOS=>
USPC-1 NYLSTFVWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV3+NVAh|ryP MV;EUXNQ M{HROoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> MWmyNVI6PTN|NR?=
USPC-2 M3rlUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlzoglExKM7:TR?= MmP3SG1UVw>? M1jqUYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NUjOZ2RFOjF{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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID