NVP-AEW541

For research use only.

Catalog No.S1034 Synonyms: AEW541

43 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 43 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 MV3LbY5ie2ViYYPzZZk> MkX5glEx6oDMzszN M17OR2ROW09? NGG4c|ZqdmirYnn0d{BKT0ZvSWKge4l1cCCLQ{WwJI9nKDBwMEi2JOKyKDBwMEK4JO69VQ>? NIe0XnIyPTB3MEmxOS=>
A14 NEPFTGFMcW6jc3WgZZN{[Xl? M3ToS54yOOLCit88US=> MojrSG1UVw>? MVXpcohq[mm2czDJcpNTKHerdHigTWM2OCCxZjCyMlMhyrFiMD6xOlMh|ryP M3;W[VE2ODVyOUG1
A431  MlnrT4lv[XOnIHHzd4F6 MlH6glEx6oDMzszN NF7R[llFVVOR M1nLNIlvcGmkaYTzJGhGWjFid3n0bEBKSzVyIH;mJF4yOCEQvF2= NIDZfFIyPTB3MEmxOS=>
A31  M2rZdWtqdmG|ZTDhd5NigQ>? NEjXOFR,OTEkgJtOwG0> NWrqTmFITE2VTx?= NI\lb3ZqdmirYnn0d{BRTEeIUjD3bZRpKEmFNUCgc4YhRjFyIN88US=> MYWxOVA2ODlzNR?=
GIST882 NXfveJBEU2mwYYPlJIF{e2G7 NYOzRXNOhjFy4pEK{txO NXXjXmFTTE2VTx?= NE\KeJJqdmirYnn0d{BkNUurdDD3bZRpKEmFNUCgc4YhRjVizszN M2nvZVE2ODVyOUG1
32D-Bcr-Abl M4DKOGtqdmG|ZTDhd5NigQ>? NX7aVXN5hjFy4pEK{txO MVHEUXNQ NUS2ZotbcW6qaXLpeJMhSmO{LVHicEBxOjFyIIfpeIghUUN3MDDv[kA,OTBizszN M4XyeFE2ODVyOUG1
MCF-7  M4D6d2N6fG:6aXPpeJkh[XO|YYm= NV7RNIZUTE2VTx?= NYHLSVlqUUN3ME2xMlY1KM7:TR?= NEm1cpcyPTB3MEmxOS=>
NWT-21 Mk[yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2XtUmROW09? MnW5TWM2OD1yLkG2N{DPxE1? NHHyOmEyPTB3MEmxOS=>
TC-71 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1PySp4yKM7:TR?= MXnEUXNQ M3;KfIlvcGmkaYTzJIlve3WuaX6tcIls\SCpcn;3eIgh\mGldH;yMWnjiJOvZXTpZZRm\CCpcn;3eIg> Ml7xNVU5Pjd|OE[=
TC-71 NIPuc4RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVX+O-KBks7:TR?= MV\EUXNQ MXfJR|UxRDBwNTFOwG0> MlnvNVU5Pjd|OE[=
Saos-2 M4PCOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWjPN5RjhjgkgJtOwG0> NV3UfWI4TE2VTx?= NFr4dVRKSzVyPEOg{txO NG\xRXUyPTh4N{O4Oi=>
U-2OS NXLySI9DT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFvre|V,P+LCit88US=> NVXp[mJJTE2VTx?= Mnm3TWM2ODxyLkWg{txO NHjWNosyPTh4N{O4Oi=>
SK-ES-1 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M37tfp446oDMzszN MVXEUXNQ M{fIeGlEPTB:MD61JO69VQ>? NH7FT2IyPTh4N{O4Oi=>
SK-N-MC MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFixe|N,P+LCit88US=> M{fpTmROW09? NVLzS5JJUUN3MEywMlUh|ryP Mn;aNVU5Pjd|OE[=
RD-ES NEPrSoxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXr0fZFkhjgkgJtOwG0> NYjRcVZTTE2VTx?= MnG3TWM2ODxyLkWg{txO MV2xOVg3PzN6Nh?=
SJ-Rh 30 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1jONZ446oDMzszN NFnjWHhFVVOR NVTkVZhPUUN3MEywMlUh|ryP NUH4Vlg5OTV6NkezPFY>
SJ-Rh 4 MlPmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVPQNpJMhjgkgJtOwG0> Mn\iSG1UVw>? Mmn6TWM2ODxyLkWg{txO MVixOVg3PzN6Nh?=
6647 M3vvT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV;WVFdjhjgkgJtOwG0> MljySG1UVw>? MnTlTWM2ODxyLkWg{txO MY[xOVg3PzN6Nh?=
SARG NUe1O3Z1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlnqglfjiIsQvF2= MXzEUXNQ NFq1enRKSzVyPEOg{txO MnKwNVU5Pjd|OE[=
MOS M2nRUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MofkglfjiIsQvF2= NETRNHBFVVOR NWfT[4puUUN3MEy0JO69VQ>? MmjNNVU5Pjd|OE[=
IOR/OS7 M{XPbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIWxblF,P+LCit88US=> NX31T4xoTE2VTx?= MY\JR|UxRDFizszN MonsNVU5Pjd|OE[=
IOR/OS9 M3r6Umdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUL0V4FrhjgkgJtOwG0> NIPwTYVFVVOR MWTJR|UxRDZizszN NH;ER24yPTh4N{O4Oi=>
IOR/OS10 M3rjRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHP1O|Z,P+LCit88US=> M2\uPGROW09? M{nvNWlEPTB:NTFOwG0> NH7YbJMyPTh4N{O4Oi=>
IOR/OS14 NGjFWXRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEC5eVV,P+LCit88US=> NUnNT5prTE2VTx?= MnfYTWM2ODx2IN88US=> MlzFNVU5Pjd|OE[=
LAP35 NWD1XndYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXLJe2s3hjgkgJtOwG0> NF;oPIxFVVOR NXj1T5p5UUN3MEywMlUh|ryP MoXmNVU5Pjd|OE[=
IOR/BRZ MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWL+O-KBks7:TR?= NEHV[3dFVVOR M3PsOGlEPTB:MD61JO69VQ>? M1;O[FE2QDZ5M{i2
IOR/CAR MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWrSbZA2hjgkgJtOwG0> NGT3bFhFVVOR MkPBTWM2ODxzIN88US=> NGfkbWwyPTh4N{O4Oi=>
IOR/NGR MnK1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M13IWp446oDMzszN MlnsSG1UVw>? NXW2c3Q4UUN3MEywMlUh|ryP NFX4cHQyPTh4N{O4Oi=>
IOR/RCH NGi3V21Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWf3N4VzhjgkgJtOwG0> MYPEUXNQ NUmyT|l2UUN3MEywMlUh|ryP NVHI[lBJOTV6NkezPFY>
RMZ-RC2 MkXMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF;qSIx,P+LCit88US=> M2jjb2ROW09? M2rqb2lEPTB:MD61JO69VQ>? M2HCT|E2QDZ5M{i2
CCA MnfwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkT3glfjiIsQvF2= NEfkeXlFVVOR MWTJR|UxRDJizszN MoP1NVU5Pjd|OE[=
RD/18 Mn;CS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\nZp446oDMzszN M4nqVWROW09? MlGxTWM2ODx2IN88US=> NFHW[mIyPTh4N{O4Oi=>
OVCAR-3 NWns[5UzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1rMXJ4yPeLCit88US=> M1juS2ROW09? NUfX[4M3cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MXGxOlMxODh{MB?=
OVCAR-4 NIj2[ohIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYOy[WZVhjF34pEK{txO MWXEUXNQ NEfWcI1qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M4XyPFE3OzByOEKw
OVCAR-3 NWXJ[|ZvSXCxcITvd4l{KGG|c3H5 Mn7lglE26oDMzszN M1\ndmROW09? MULpcoR2[2W|IHHwc5B1d3Orcx?= NX;heI9nOTZ|MEC4NlA>
OVCAR-4 NH3nZ49CeG:ydH;zbZMh[XO|YYm= M4D6Up4yPeLCit88US=> NFPOXWtFVVOR Mn\NbY5lfWOnczDhdI9xfG:|aYO= NY\xV45lOTZ|MEC4NlA>
OVCAR-3 Ml\DSpVv[3Srb36gZZN{[Xl? NWXC[o55hjF34pEK{txO M1u4emROW09? M{[3OmRm[3KnYYPld{BxcG:|cHjvdplt[XSrb36gc4YhSUuW MoriNVY{ODB6MkC=
Huh-7 NEG5ZWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NInjUox,OTEkgJtOwG0> NH3kWXpFVVOR NWfGUW9UUUN3ME2xMlQh|ryP NY\tR3ZFOTZ3M{C3N|Q>
Hep-G2 NUPtfGlJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFPvZ4R,OTEkgJtOwG0> NUPoRYptTE2VTx?= M{PrT2lEPTB;MT64JO69VQ>? MYOxOlU{ODd|NB?=
Hep-3B NGfOR4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml3SglEx6oDMzszN MYrEUXNQ NXe0d3B[UUN3ME2xMlkh|ryP NY\PeoxmOTZ3M{C3N|Q>
SK-Hep-1 MnP4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1:wep4yOOLCit88US=> MXjEUXNQ NGXiTopKSzVyPU[uPUDPxE1? NUXST4J4OTZ3M{C3N|Q>
Huh-7 M4nTNGZ2dmO2aX;uJIF{e2G7 M3TwcZ4yOOLCit88US=> M1;4[2ROW09? M2XYNWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= Mn7vNVY2OzB5M{S=
Hep-G2 NUHrPGwxTnWwY4Tpc44h[XO|YYm= NVfPc5VyhjFy4pEK{txO NITaTGlFVVOR MkTQTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NGLaVXQyPjV|MEezOC=>
SK-Hep-1 MX7GeY5kfGmxbjDhd5NigQ>? MU\+NVDjiIsQvF2= NVXSd4RuTE2VTx?= MlTzTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MmW3NVY2OzB5M{S=
BON NHq2dJlMcW6jc3WgZZN{[Xl? M2LuT543KM7:TR?= M2fJ[2ROW09? M3\GT4lv\HWlZYOg[IVxcG:|cHjvdplt[XSrb36gc4YhUUeILUHS MkLTNVY3ODF{OES=
BON MlvHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXf+NVDjiIsQvF2= NVrVZ5pDTE2VTx?= M1\Db2lEPTB;Nj62JO69VQ>? MnjPNVY3ODF{OES=
CM NVLGeJNnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVTFOlBnhjYkgJtOwG0> MnXQSG1UVw>? NF;tcWhKSzVyPUOuN{DPxE1? NGfpPFEyPjZyMUK4OC=>
BON MWTGeY5kfGmxbjDhd5NigQ>? MlvvglcvPeLCit88US=> NF\ET2NFVVOR MY\pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NIPydmEyPjZyMUK4OC=>
CM MmfzSpVv[3Srb36gZZN{[Xl? M1;3N5426oDMzszN NH\GfpRFVVOR NHLSWYxqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NHLIfI4yPjZyMUK4OC=>
BON NUi1PWU5SXCxcITvd4l{KGG|c3H5 Mn;YglcvPeLCit88US=> MWnEUXNQ Mn[xbY5lfWOnczDBdI9xfG:|aYO= Ml\WNVY3ODF{OES=
CM MYfBdI9xfG:|aYOgZZN{[Xl? MU\+OgKBks7:TR?= Ml7PSG1UVw>? M2fmO4lv\HWlZYOgRZBweHSxc3nz MUSxOlYxOTJ6NB?=
HT-29 NIHBNoRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkfYglEx6oDMzszN NYjYOoQ3TE2VTx?= MWjJR|UxRTFwNzFOwG0> NHjzeGQyPzByN{CxOS=>
HCT-116 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVX+NVDjiIsQvF2= NFriZ3dFVVOR NYX1N2U3UUN3ME2yMlUh|ryP MoPpNVcxODdyMUW=
primary colorectal cancer cells NESzO5FHfW6ldHnvckBie3OjeR?= NVnwc3prhjYkgJtOwG0> NVPNbVJ6TE2VTx?= M37jU4FtfGW{czD0bIUhdW:{cHjvcI9ogSCxZjD0bIUhemWvYXnubY5oKGOnbHzz MW[xO|AxPzBzNR?=
HTLA-230 NXrrO25rTnWwY4Tpc44h[XO|YYm= M1m1OJ45KM7:TR?= MkfNSG1UVw>? M1Lhb4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NGrBS3cyPzF{MUi5PC=>
KCNR M1HESWZ2dmO2aX;uJIF{e2G7 NH\j[Yh,QCEQvF2= Ml;wSG1UVw>? Mlu3bY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NWXoZo5xOTdzMkG4PVg>
SK-N-BE2c MYLGeY5kfGmxbjDhd5NigQ>? Mn[zglgh|ryP M1vnSmROW09? M4HWOolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> M{LkfFE4OTJzOEm4
SK-N-BE NUnCemdFTnWwY4Tpc44h[XO|YYm= NWjvOYc4hjhizszN Ml;5SG1UVw>? MX;pcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NFLSdokyPzF{MUi5PC=>
LAN-5 MkH6SpVv[3Srb36gZZN{[Xl? NV;QNFVlhjhizszN NXO4PFBTTE2VTx?= M2\uZolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MUKxO|EzOTh7OB?=
GI-CA-N M4DWVWZ2dmO2aX;uJIF{e2G7 MVT+PEDPxE1? MkS2SG1UVw>? M2n1OolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> M4PZe|E4OTJzOEm4
SH-EP NH;4NWlHfW6ldHnvckBie3OjeR?= NVrxbXozhjhizszN M3Pp[mROW09? MkTTbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MnzxNVcyOjF6OUi=
SK-N-AS NIDZdVRHfW6ldHnvckBie3OjeR?= MoDuglgh|ryP MUXEUXNQ NUfMRm1JcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MYKxO|EzOTh7OB?=
RN-GA NUWxUWJmTnWwY4Tpc44h[XO|YYm= NWK3dZNShjhizszN NGHtbYVFVVOR NEG0S2lqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M1nlSVE4OTJzOEm4
SY-5Y(N) NF\OW3lHfW6ldHnvckBie3OjeR?= NUS1U3VVhjhizszN MUXEUXNQ NGXCTVdqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> Moe1NVcyOjF6OUi=
GI-CA-N Mn7tS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGrhdIZ,QCEQvF2= NUnV[2dCTE2VTx?= NFHtOmtKSzVyPTC2Mlgh|ryP M3r6PFE4OTJzOEm4
SH-EP NFPlcZhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF3ucZF,QCEQvF2= MmTGSG1UVw>? NXWwNGwzUUN3ME2gN{DPxE1? MUSxO|EzOTh7OB?=
HTLA-230 Mn;xS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXn+PEDPxE1? M2fPdGROW09? MoG5TWM2OD1iMD61JO69VQ>? MYixO|EzOTh7OB?=
SK-N-BE2c NYfvXXRTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkLBglgh|ryP MYjEUXNQ NGfkO3lKSzVyPTCxMlEh|ryP MXuxO|EzOTh7OB?=
SK-N-BE2 NUfUXYxUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVn+PEDPxE1? MmH2SG1UVw>? NH;1WJNKSzVyPTCzJO69VQ>? MlHENVcyOjF6OUi=
SY-5Y (N) NI[x[4VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUH+PEDPxE1? MmPaSG1UVw>? NU\nOIN[UUN3ME2gNk41KM7:TR?= M2SxRVE4OTJzOEm4
LAN-5 NUPzTXp1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYD+PEDPxE1? NHTjNFZFVVOR Ml60TWM2OD1iMD60JO69VQ>? NEK4bIQyPzF{MUi5PC=>
KCNR NHTEXHlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NW\2W2hxhjhizszN MkLySG1UVw>? MXfJR|UxRSByLkSg{txO NYPQSpV[OTdzMkG4PVg>
RN-GA NUnFRm91T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mnf6glgh|ryP M1zUcWROW09? M3PFR2lEPTB;IEGuN{DPxE1? NULQUm9jOTdzMkG4PVg>
SK-N-AS NHzBdmdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{jGRZ45KM7:TR?= MXvEUXNQ NGHjfmdqdmS3Y3XzJIFxd3C2b4Ppdy=> MnHmNVcyOjF6OUi=
KCNR MlvlRZBweHSxc3nzJIF{e2G7 NH3SNnl,QCEQvF2= NFXBR3ZFVVOR M37N[olv\HWlZYOgZZBweHSxc3nz M3PIT|E4OTJzOEm4
GI-CA-N NV3GSFRySXCxcITvd4l{KGG|c3H5 MoXmglgh|ryP NHXS[llFVVOR M1fWc4lv\HWlZYOgZZBweHSxc3nz NUP4TVg3OTdzMkG4PVg>
HTLA-230 MoTiRZBweHSxc3nzJIF{e2G7 NGP0doZ,QCEQvF2= NEDs[5ZFVVOR MmDWbY5lfWOnczDhdI9xfG:|aYO= MmP5NVcyOjF6OUi=
SK-N-BE2c NGi3VXpCeG:ydH;zbZMh[XO|YYm= NILieJR,QCEQvF2= NX\WR2N[TE2VTx?= MXjpcoR2[2W|IHHwc5B1d3Orcx?= MVixO|EzOTh7OB?=
SY-5Y (N) NYTwOHl6SXCxcITvd4l{KGG|c3H5 M1f3bZ45KM7:TR?= MkewSG1UVw>? MV7pcoR2[2W|IHHwc5B1d3Orcx?= MkDTNVcyOjF6OUi=
HL60AR MmOySpVv[3Srb36gZZN{[Xl? NVXpZXExOTZyIH7N NFzRXpJmdmijbnPld{B1cGVibHX2[Yx{KG:oIICyO2tqeDF? NFXmeFcyPzN4MUKyOS=>
HL60AR MojIRZBweHSxc3nzJIF{e2G7 NILnSmN,OjByIH7N NUnnZ2lPcW6mdXPld{BieG:ydH;zbZM> M4Dyb|E4OzZzMkK1
HPAF-II NUjMdGNUU2mwYYPlJIF{e2G7 NY\mUG0yhjFizszN M3fwUGROW09? NEK3[YNqdmirYnn0d{BKT0ZvST3t[YRq[XSnZDDzbYdv[WyuaX7n NWT6eIdiOTh2NEW1NlA>
HPAF-II NGD2ZWpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIHEOWF,OiEQvF2= M2fWVGROW09? M4LWZYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MkPjNVg1PDV3MkC=
HPAF-II M{jXcmZ2dmO2aX;uJIF{e2G7 Mn25glIh|ryP NFe5XmZFVVOR M3vB[IlvcGmkaYTzJIJie2GuIHHu[EBKT0ZvST3t[YRq[XSnZDDwZY5kemWjdHnjJINidmOncjDj[YxtKG2rZ4LheIlwdg>? NYrGTop5OTh2NEW1NlA>
TFK-1 M2H3[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoXtglI2OCCwTR?= Ml\HSG1UVw>? Mnr0TWM2OD1yLkK2JO69VQ>? MWqyNFA3Pjd|NB?=
EGI-1 NEXIbnZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIDBeIt,OjVyIH7N NIjoS|lFVVOR MnGzTWM2OD1yLkK4JO69VQ>? M3PlTFIxODZ4N{O0
CC-LP-1 M37Jfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEjoW4J,OjVyIH7N M3TzfmROW09? MkO3TWM2OD1yLkG1JO69VQ>? MlO0NlAxPjZ5M{S=
CC-SW-1 M1;jWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYL+NlUxKG6P NHqxOZlFVVOR M{\jcWlEPTB;MD61OEDPxE1? NFS2UIszODB4NkezOC=>
Sk-ChA-1 NXXKPXhrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnzxglI2OCCwTR?= NHL2dYNFVVOR NEnSeVlKSzVyPUCuNkDPxE1? NH72WGUzODB4NkezOC=>
Mz-ChA-1 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVG1PXhNhjJ3MDDuUS=> NUnZOGxITE2VTx?= NFfVZXlKSzVyPUGuN|kh|ryP Mkj2NlAxPjZ5M{S=
Mz-ChA-2 M2LRbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUX+NlUxKG6P MlzCSG1UVw>? NHf6XoVKSzVyPUCuO|Mh|ryP NFzNOpozODB4NkezOC=>
ECC-1 NWjiSYRNU2mwYYPlJIF{e2G7 M4HLcp4yOCEQvF2= M1n4UGROW09? MVPpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6QCV? MoH5NlEzQTV|M{W=
Ishikawa NWS0W3BKU2mwYYPlJIF{e2G7 MmDFglExKM7:TR?= NFP1Z45FVVOR Ml\ybY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQTNn MkW2NlEzQTV|M{W=
USPC-1 NGHvUHdMcW6jc3WgZZN{[Xl? MXP+NVAh|ryP NVzZfJd{TE2VTx?= MoHNbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhOTByJR?= MkDYNlEzQTV|M{W=
USPC-2 NIX1fYJMcW6jc3WgZZN{[Xl? M1z3Op4yOCEQvF2= NVi2cXZFTE2VTx?= M1T4O4lvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl4JR?= MnmwNlEzQTV|M{W=
ECC-1 NGX4c|dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmrmglExKM7:TR?= MkTXSG1UVw>? MmK5[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NHmwPZQzOTJ7NUOzOS=>
Ishikawa MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYHTeGZxhjFyIN88US=> M2DYfWROW09? NEHJR3Bl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v M1u4elIyOjl3M{O1
USPC-1 MnzYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFvmPVR,OTBizszN NHzESoxFVVOR NYHvRVNG\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NEH0[nQzOTJ7NUOzOS=>
USPC-2 MkLoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1;Ffp4yOCEQvF2= Mn;wSG1UVw>? NXjqZ5JL\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? Mo\BNlEzQTV|M{W=

... 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