NVP-AEW541

For research use only.

Catalog No.S1034 Synonyms: AEW541

50 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 50 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 NImxPY5McW6jc3WgZZN{[Xl? NXvPenVWhjFy4pEK{txO NUDObVRJTE2VTx?= NIXGfZBqdmirYnn0d{BKT0ZvSWKge4l1cCCLQ{WwJI9nKDBwMEi2JOKyKDBwMEK4JO69VQ>? NYi0cY9rOTVyNUC5NVU>
A14 M4H2cWtqdmG|ZTDhd5NigQ>? M4XI[54yOOLCit88US=> MkXhSG1UVw>? NUHmdWNNcW6qaXLpeJMhUW6|UjD3bZRpKEmFNUCgc4YhOi5|INMxJFAvOTZ|IN88US=> M4S2[FE2ODVyOUG1
A431  MVnLbY5ie2ViYYPzZZk> NF;iOHh,OTEkgJtOwG0> M3:yfmROW09? NFjKOphqdmirYnn0d{BJTVJzIIfpeIghUUN3MDDv[kA,OTBizszN Mn3KNVUxPTB7MUW=
A31  M1X2fGtqdmG|ZTDhd5NigQ>? MmKxglEx6oDMzszN NIKzWpFFVVOR MkDibY5pcWKrdIOgVGRITlJid3n0bEBKSzVyIH;mJF4yOCEQvF2= NFrJeWQyPTB3MEmxOS=>
GIST882 NUPGWFFCU2mwYYPlJIF{e2G7 Mkf1glEx6oDMzszN NUHBeHY3TE2VTx?= NEjkRYlqdmirYnn0d{BkNUurdDD3bZRpKEmFNUCgc4YhRjVizszN MVGxOVA2ODlzNR?=
32D-Bcr-Abl NES0b2JMcW6jc3WgZZN{[Xl? NYPkVVdyhjFy4pEK{txO MlLQSG1UVw>? NFq2[opqdmirYnn0d{BD[3JvQXLsJJAzOTBid3n0bEBKSzVyIH;mJF4yOCEQvF2= NEXOU|IyPTB3MEmxOS=>
MCF-7  NXfwSoJ{S3m2b4jpZ4l1gSCjc4PhfS=> M3PDTGROW09? NIjoSG9KSzVyPUGuOlQh|ryP M3zyOVE2ODVyOUG1
NWT-21 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1e2PWROW09? NYq0ZZhvUUN3ME2wMlE3OyEQvF2= MV[xOVA2ODlzNR?=
TC-71 NWOxdYd5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NITzcpV,OSEQvF2= MkXmSG1UVw>? NGrzdo5qdmirYnn0d{BqdnO3bHnuMYxqc2ViZ4Lve5RpKG[jY4Tvdk1K6oDVbXXkbYF1\WRiZ4Lve5Rp MVqxOVg3PzN6Nh?=
TC-71 M{TxNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnvVglfjiIsQvF2= NFzBbVdFVVOR M1LnVGlEPTB:MD61JO69VQ>? M1H6[|E2QDZ5M{i2
Saos-2 MnXMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mo[3glfjiIsQvF2= MUfEUXNQ NV;SfXJ3UUN3MEyzJO69VQ>? M2XZVlE2QDZ5M{i2
U-2OS M3H1cmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIGzUWt,P+LCit88US=> NILhdIhFVVOR NVL1RpZPUUN3MEywMlUh|ryP NILsU|UyPTh4N{O4Oi=>
SK-ES-1 M2ryVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4\pXZ446oDMzszN NX25Nm1pTE2VTx?= NXz2XXJVUUN3MEywMlUh|ryP MlfVNVU5Pjd|OE[=
SK-N-MC NV\ReoFTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH\rdZF,P+LCit88US=> MYXEUXNQ MWfJR|UxRDBwNTFOwG0> NGDydYMyPTh4N{O4Oi=>
RD-ES NIfKelNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV\MU5dihjgkgJtOwG0> M37COWROW09? NELoVYdKSzVyPECuOUDPxE1? MmXWNVU5Pjd|OE[=
SJ-Rh 30 Mke4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4frdZ446oDMzszN MYrEUXNQ MVfJR|UxRDBwNTFOwG0> M4j3elE2QDZ5M{i2
SJ-Rh 4 NHy2[5pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHfHc3B,P+LCit88US=> NHP0NVFFVVOR MUPJR|UxRDBwNTFOwG0> NWPMPG0zOTV6NkezPFY>
6647 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mo\JglfjiIsQvF2= NXTp[olkTE2VTx?= MmfQTWM2ODxyLkWg{txO MXmxOVg3PzN6Nh?=
SARG NV\pb4ZJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXr+O-KBks7:TR?= MVXEUXNQ MnfqTWM2ODx|IN88US=> MlL2NVU5Pjd|OE[=
MOS MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWnme2QxhjgkgJtOwG0> MYrEUXNQ NYGyNIFjUUN3MEy0JO69VQ>? NW\BZZhsOTV6NkezPFY>
IOR/OS7 MkDkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Moq3glfjiIsQvF2= MkXLSG1UVw>? NGqwXIdKSzVyPEGg{txO NV;UcYVWOTV6NkezPFY>
IOR/OS9 NGDZ[WpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV;+O-KBks7:TR?= M4TDdGROW09? MkLFTWM2ODx4IN88US=> NGX2booyPTh4N{O4Oi=>
IOR/OS10 NF3SOm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUf+O-KBks7:TR?= M1LDN2ROW09? MoHyTWM2ODx3IN88US=> Ml\zNVU5Pjd|OE[=
IOR/OS14 NYXWS|Y5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWP+O-KBks7:TR?= MVrEUXNQ MVvJR|UxRDRizszN M4TpSFE2QDZ5M{i2
LAP35 NF;Ve3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mlm0glfjiIsQvF2= NIiw[VdFVVOR NVTkZZVGUUN3MEywMlUh|ryP MW[xOVg3PzN6Nh?=
IOR/BRZ M2r5bGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWD+O-KBks7:TR?= MYrEUXNQ MoXITWM2ODxyLkWg{txO NVmwdJRYOTV6NkezPFY>
IOR/CAR M4L1SWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXr+O-KBks7:TR?= M{ftfGROW09? NYrSSVlnUUN3MEyxJO69VQ>? NYfN[Y1UOTV6NkezPFY>
IOR/NGR MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHvBdHl,P+LCit88US=> NFTOS3hFVVOR Ml;xTWM2ODxyLkWg{txO MkH2NVU5Pjd|OE[=
IOR/RCH NGLMN5lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXTVTFdLhjgkgJtOwG0> NWm5[YhZTE2VTx?= NUjtXo5LUUN3MEywMlUh|ryP NF;sXZgyPTh4N{O4Oi=>
RMZ-RC2 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXH+O-KBks7:TR?= MnLNSG1UVw>? NHXoVGhKSzVyPECuOUDPxE1? MVuxOVg3PzN6Nh?=
CCA MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1zufJ446oDMzszN NW\JXZN5TE2VTx?= NF:xO3pKSzVyPEKg{txO Mm\aNVU5Pjd|OE[=
RD/18 NHnnbFJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVn+O-KBks7:TR?= MYPEUXNQ M{nJV2lEPTB:NDFOwG0> M3HZXFE2QDZ5M{i2
OVCAR-3 M1XzPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYrLNIVWhjF34pEK{txO Mk\OSG1UVw>? M2rQ[olvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NV3lVoJkOTZ|MEC4NlA>
OVCAR-4 Ml3XS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmC5glE26oDMzszN M2\ycGROW09? NIPRbJRqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NX3YTFZKOTZ|MEC4NlA>
OVCAR-3 NUHIdW1lSXCxcITvd4l{KGG|c3H5 MVL+NVXjiIsQvF2= M1\sW2ROW09? M3LXUolv\HWlZYOgZZBweHSxc3nz NFvX[IEyPjNyMEiyNC=>
OVCAR-4 NUXJWIxSSXCxcITvd4l{KGG|c3H5 MUX+NVXjiIsQvF2= NVXkNYpSTE2VTx?= NYmzZ2E5cW6mdXPld{BieG:ydH;zbZM> NV;JZ3psOTZ|MEC4NlA>
OVCAR-3 NXvTTlNoTnWwY4Tpc44h[XO|YYm= NUTBbYV1hjF34pEK{txO NV;oe4dETE2VTx?= NW[yPYxvTGWlcnXhd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= NGL2W4MyPjNyMEiyNC=>
Huh-7 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkjMglEx6oDMzszN NGTNUXVFVVOR MmT5TWM2OD1zLkSg{txO NH7vZ5AyPjV|MEezOC=>
Hep-G2 MlTNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4LzfZ4yOOLCit88US=> M1TiUmROW09? M{PTVmlEPTB;MT64JO69VQ>? NYn6SZd3OTZ3M{C3N|Q>
Hep-3B MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIO3bo1,OTEkgJtOwG0> MlL4SG1UVw>? NH7GRllKSzVyPUGuPUDPxE1? NE\pW|QyPjV|MEezOC=>
SK-Hep-1 M3fHTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV\+NVDjiIsQvF2= M3jtTWROW09? NFXNSXVKSzVyPU[uPUDPxE1? NW\PTWYzOTZ3M{C3N|Q>
Huh-7 M3H5bGZ2dmO2aX;uJIF{e2G7 M1XFN54yOOLCit88US=> MkPQSG1UVw>? M3vTRWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NY\6V4p[OTZ3M{C3N|Q>
Hep-G2 MUfGeY5kfGmxbjDhd5NigQ>? MXv+NVDjiIsQvF2= MXLEUXNQ NGrucIlKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NYj5[lZCOTZ3M{C3N|Q>
SK-Hep-1 MljHSpVv[3Srb36gZZN{[Xl? MWX+NVDjiIsQvF2= NITLZoJFVVOR NFjKZVlKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 Mn7TNVY2OzB5M{S=
BON MlHJT4lv[XOnIHHzd4F6 NID1c4p,PiEQvF2= MYDEUXNQ M4TiXolv\HWlZYOg[IVxcG:|cHjvdplt[XSrb36gc4YhUUeILUHS MXuxOlYxOTJ6NB?=
BON NYHyeGlGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{POW54yOOLCit88US=> M3fDemROW09? NHjYVnlKSzVyPU[uOkDPxE1? M4rFS|E3PjBzMki0
CM MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHftcY9,PeLCit88US=> MW\EUXNQ NF;ISIdKSzVyPUOuN{DPxE1? MmjjNVY3ODF{OES=
BON MoqySpVv[3Srb36gZZN{[Xl? NUTxfIYyhjdwNfMAju69VQ>? NXS3TVM1TE2VTx?= M4frbIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= Ml60NVY3ODF{OES=
CM MV3GeY5kfGmxbjDhd5NigQ>? NVf3NmRZhjYkgJtOwG0> NH;WTGVFVVOR MV7pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NWLPW4dkOTZ4MEGyPFQ>
BON NV3wS4dUSXCxcITvd4l{KGG|c3H5 MmTjglcvPeLCit88US=> MYDEUXNQ NUP1fHdWcW6mdXPld{BCeG:ydH;zbZM> NGS0N3EyPjZyMUK4OC=>
CM NWHiVohMSXCxcITvd4l{KGG|c3H5 NILRclZ,PeLCit88US=> MWHEUXNQ Mm[2bY5lfWOnczDBdI9xfG:|aYO= MYixOlYxOTJ6NB?=
HT-29 MlK3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV[ye|Z7hjFy4pEK{txO MV\EUXNQ MYnJR|UxRTFwNzFOwG0> MV2xO|AxPzBzNR?=
HCT-116 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV7+NVDjiIsQvF2= MmrZSG1UVw>? Mn3ZTWM2OD1{LkWg{txO MUOxO|AxPzBzNR?=
primary colorectal cancer cells MlfHSpVv[3Srb36gZZN{[Xl? NX7qWoNVhjYkgJtOwG0> NH7XU2NFVVOR Mn\oZYx1\XK|IITo[UBud3KyaH;sc4d6KG:oIITo[UBz\W2jaX7pcoch[2WubIO= MV:xO|AxPzBzNR?=
HTLA-230 MWjGeY5kfGmxbjDhd5NigQ>? NILNZWp,QCEQvF2= M4HnPGROW09? NUTtNJZycW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MkTnNVcyOjF6OUi=
KCNR MUXGeY5kfGmxbjDhd5NigQ>? NWnSSVF5hjhizszN NELCc|BFVVOR NEHsd|NqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NHH0Z4syPzF{MUi5PC=>
SK-N-BE2c NHnPcFZHfW6ldHnvckBie3OjeR?= NF3aeZd,QCEQvF2= MlW0SG1UVw>? MoXTbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NWiwWZdbOTdzMkG4PVg>
SK-N-BE NInrTohHfW6ldHnvckBie3OjeR?= MWn+PEDPxE1? MmjpSG1UVw>? M2DmT4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> M2XTZVE4OTJzOEm4
LAN-5 MljwSpVv[3Srb36gZZN{[Xl? NF[1N5R,QCEQvF2= MVvEUXNQ M4PKUolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MoXiNVcyOjF6OUi=
GI-CA-N MnTZSpVv[3Srb36gZZN{[Xl? NXz5clk6hjhizszN MY\EUXNQ NHLzR2xqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> Mn;zNVcyOjF6OUi=
SH-EP M3LZW2Z2dmO2aX;uJIF{e2G7 NGrCfIN,QCEQvF2= MmSwSG1UVw>? MlHObY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 M3uzSVE4OTJzOEm4
SK-N-AS NVrL[G1qTnWwY4Tpc44h[XO|YYm= MW\+PEDPxE1? MXjEUXNQ MknMbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NHL4VXAyPzF{MUi5PC=>
RN-GA M3faRmZ2dmO2aX;uJIF{e2G7 M4q1W545KM7:TR?= MoXTSG1UVw>? NGPKWmpqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NFzSWVkyPzF{MUi5PC=>
SY-5Y(N) NFzmVXJHfW6ldHnvckBie3OjeR?= MkTFglgh|ryP M2noXWROW09? MmP1bY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 Mon0NVcyOjF6OUi=
GI-CA-N NIXscHRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXnvbpBIhjhizszN MYTEUXNQ M2G1SmlEPTB;IE[uPEDPxE1? NILte|IyPzF{MUi5PC=>
SH-EP NH\PNIZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYnGcVBKhjhizszN NHL4RYRFVVOR MnrQTWM2OD1iMzFOwG0> NIX2NXQyPzF{MUi5PC=>
HTLA-230 NUDOWIZ3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1nDXZ45KM7:TR?= MmLiSG1UVw>? MVjJR|UxRSByLkWg{txO MYGxO|EzOTh7OB?=
SK-N-BE2c MkXDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmSxglgh|ryP NWDQcZRlTE2VTx?= MmPOTWM2OD1iMT6xJO69VQ>? MonoNVcyOjF6OUi=
SK-N-BE2 NGWyUGlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NELHcJd,QCEQvF2= NIfkb|RFVVOR MXTJR|UxRSB|IN88US=> NEj3bHIyPzF{MUi5PC=>
SY-5Y (N) MnjnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEP1U3J,QCEQvF2= NFrYcG9FVVOR M4DEe2lEPTB;IEKuOEDPxE1? NGXQXZoyPzF{MUi5PC=>
LAN-5 NUPObGhJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1vwS545KM7:TR?= MVLEUXNQ M3;KcmlEPTB;IECuOEDPxE1? NITrPI0yPzF{MUi5PC=>
KCNR NVTYe4ZbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mm\Sglgh|ryP MWfEUXNQ M{HhTWlEPTB;IECuOEDPxE1? M33UU|E4OTJzOEm4
RN-GA NV7IfGRHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHTXXXJ,QCEQvF2= MmHrSG1UVw>? MnXZTWM2OD1iMT6zJO69VQ>? NFLiVY8yPzF{MUi5PC=>
SK-N-AS MnPCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYn+PEDPxE1? NIDIS25FVVOR NXnmU|ExcW6mdXPld{BieG:ydH;zbZM> NEf2cJYyPzF{MUi5PC=>
KCNR NVXlXXBzSXCxcITvd4l{KGG|c3H5 MYD+PEDPxE1? NVzsRotHTE2VTx?= MWnpcoR2[2W|IHHwc5B1d3Orcx?= NFWxdYgyPzF{MUi5PC=>
GI-CA-N MXLBdI9xfG:|aYOgZZN{[Xl? MVT+PEDPxE1? MWTEUXNQ MmDRbY5lfWOnczDhdI9xfG:|aYO= NFGwdnIyPzF{MUi5PC=>
HTLA-230 MUjBdI9xfG:|aYOgZZN{[Xl? NW\jXZNuhjhizszN M3i4e2ROW09? MkLJbY5lfWOnczDhdI9xfG:|aYO= NYLzb5UzOTdzMkG4PVg>
SK-N-BE2c NGr5eGlCeG:ydH;zbZMh[XO|YYm= Mmf2glgh|ryP MULEUXNQ MmW1bY5lfWOnczDhdI9xfG:|aYO= M{HhbFE4OTJzOEm4
SY-5Y (N) MmfxRZBweHSxc3nzJIF{e2G7 MkDCglgh|ryP MVnEUXNQ NUe2T4hWcW6mdXPld{BieG:ydH;zbZM> NHvmWW0yPzF{MUi5PC=>
HL60AR MkLLSpVv[3Srb36gZZN{[Xl? Mm\HNVYxKG6P MXLlcohidmOnczD0bIUhdGW4ZXzzJI9nKHB{N1vpdFE> M{LyT|E4OzZzMkK1
HL60AR NWrXcHUzSXCxcITvd4l{KGG|c3H5 MlT1glIxOCCwTR?= NFLjOFBqdmS3Y3XzJIFxd3C2b4Ppdy=> MnXKNVc{PjF{MkW=
HPAF-II NIPGXJZMcW6jc3WgZZN{[Xl? Mkm2glEh|ryP MoLVSG1UVw>? M{TKOIlvcGmkaYTzJGlITi2LLX3l[IlifGWmIIPp[45idGyrbne= NIXYVlgyQDR2NUWyNC=>
HPAF-II NI\JVJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmLGglIh|ryP M4\aW2ROW09? NFy1UWZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NHzMV5IyQDR2NUWyNC=>
HPAF-II M4jtUGZ2dmO2aX;uJIF{e2G7 MXv+NkDPxE1? NGHrVZZFVVOR NVj4TY8{cW6qaXLpeJMh[mG|YXygZY5lKEmJRj3JMY1m\GmjdHXkJJBidmO{ZXH0bYMh[2GwY3XyJINmdGxibXnndoF1cW:w NYLEeY1sOTh2NEW1NlA>
TFK-1 MoW4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4HmNJ4zPTBibl2= MXnEUXNQ NYfvW|JGUUN3ME2wMlI3KM7:TR?= MWOyNFA3Pjd|NB?=
EGI-1 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2HnRZ4zPTBibl2= M2jyNWROW09? MkP0TWM2OD1yLkK4JO69VQ>? M2DlNFIxODZ4N{O0
CC-LP-1 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXj+NlUxKG6P NW\QZpB2TE2VTx?= MnzoTWM2OD1yLkG1JO69VQ>? NYe0[mZtOjByNk[3N|Q>
CC-SW-1 NH:4SVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIrYSHB,OjVyIH7N NH7rUnpFVVOR MVLJR|UxRTBwNUSg{txO NYXDXIdYOjByNk[3N|Q>
Sk-ChA-1 MljoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX\zVnhwhjJ3MDDuUS=> NX\JZZdKTE2VTx?= NVnUWJlYUUN3ME2wMlIh|ryP NHrsb|AzODB4NkezOC=>
Mz-ChA-1 NYPmUlE1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MljEglI2OCCwTR?= MYnEUXNQ M4niZ2lEPTB;MT6zPUDPxE1? M37DdlIxODZ4N{O0
Mz-ChA-2 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoG3glI2OCCwTR?= NIfEV4hFVVOR MVfJR|UxRTBwN{Og{txO MV[yNFA3Pjd|NB?=
ECC-1 NIS2fWhMcW6jc3WgZZN{[Xl? MnnvglExKM7:TR?= MU\EUXNQ NWC1WYJPcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOUil NYnCVnlNOjF{OUWzN|U>
Ishikawa NWrQUWQ{U2mwYYPlJIF{e2G7 NYDLe2JohjFyIN88US=> M4PtfWROW09? NY\1e5NucW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOUOl M4DTV|IyOjl3M{O1
USPC-1 NYHXXXc1U2mwYYPlJIF{e2G7 MUX+NVAh|ryP NIrlbHNFVVOR NHjtZ3BqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSBzMECl NYPJclBPOjF{OUWzN|U>
USPC-2 NVzzcFNMU2mwYYPlJIF{e2G7 NWro[414hjFyIN88US=> NY\sdmo4TE2VTx?= NEn1R3BqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSB7NjW= NV25TIJ7OjF{OUWzN|U>
ECC-1 MoDaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVH+NVAh|ryP MkHSSG1UVw>? NF3QXIVl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MojNNlEzQTV|M{W=
Ishikawa NX;OZmRoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4nOeJ4yOCEQvF2= MWTEUXNQ MVjk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MoezNlEzQTV|M{W=
USPC-1 NEHFXXVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4r6[54yOCEQvF2= M4HkcmROW09? MWfk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u NFvrNWEzOTJ7NUOzOS=>
USPC-2 MoTRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkO2glExKM7:TR?= MV\EUXNQ MVrk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MVeyNVI6PTN|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
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
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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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