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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7 Customer Reviews

  • (A) KRAS mutant (SW837 and LoVo) or KRAS/PIK3CA mutant (HCT-116) colorectal cancers were treated with the indicated compounds for 6 hours (gef, gefitinib 1 μM; NVP, NVP-AEW541 1 μM; PHA, PHA-665752 1 μM), and the resulting protein lysates were immunoprecipitated with an anti-p85 antibody. The precipitated proteins were analyzed by Western blots with the indicated antibodies. Whole cell extracts were probed with the indicated antibodies. Asterisks indicate the IRS proteins for SW837 and HCT-116 cells, and ERBB3 for LoVo cells. (B) SW837 cells were grown in either normal serum (5% FBS) or low serum (0.5% FBS) and treated with vehicle, R1507 anti–IGF-IR antibody (25 μg/ml), or NVP-AEW541 (1 μM) for 6 hours. The cells were lysed and probed with the indicated antibodies.

    J Clin Invest 2011 121, 4311-21. NVP-AEW541 purchased from Selleck.

    A, cell viability reduction. TC1889 cells were treated with pharmacological inhibitors against IGF-1R (NVP and BMS), as well as a neutralizing IGF-1R antibody (aIR3) and cell viability was assessed using MTT-assays. Mouse IgG1 antibody was employed as a reference control for the effects of aIR3 at respective concentrations. Assays were performed in sextuple. Data are expressed as the mean SD (n 3). B, induction of cell death. TC1889 cells were treated with pharmacological inhibitors against IGF-1R as well as a neutralizing IGF-1R antibody and cell death was evaluated by FACS-analyses following PI-staining. Data are expressed as the mean SD (n ?3).

    Clin Cancer Res 2011 17, 2237-2249. NVP-AEW541 purchased from Selleck.

  • C, TC1889 cells were serum-starved for 16 hours, treated with vehicle or the IGF-1R inhibitor PPP, NVP, BMS, or the neutralizing IGF1R antibody aIR3 for 2 hours, and then stimulated with IGF-I (100 ng/mL) for 15 min. The activity of PI3K/Akt- and MAPK/Erk-signaling was investigated by an analysis of the expression of phosphorylated Akt, GSK3b, MEK1/2, and Erk using Western immunoblotting. Representative results are shown (n ?3). Actin served as a loading control. D, TC1889 cells were treated with vehicle or PPP, NVP, BMS, or aIR3. The activity of PI3K/Akt- and MAPK/Erk-signaling was investigated as mentioned earlier. Representative results are shown (n ?3). Actin served as a loading control.

    Clin Cancer Res 2011 17, 2237-2249. NVP-AEW541 purchased from Selleck.

    A, cell viability assay for mouse rhabdomyosarcoma cultures treated with various doses of NVP-AEW541 and immunoblot showing expression levels of Igf1r in mouse rhabdomyosarcoma primary cell cultures (U20325 and U21089) compared with the mouse myoblast cell line C2C12. B, anchorage-dependent colony formation assay showing increased inhibition of colony formation by mouse rhabdomyosarcoma cultures compared to mouse myoblast cell line C2C12 on treatment with increasing doses of NVPAEW541. C, anchorageindependent colony formation by mouse rhabdomyosarcoma cultures (U20325) is inhibited on treatment with NVP-AEW541, indicated by a decrease in colony size. The scale bar represents 50mm. The number of colonies formed in soft agar also is reduced on treatment with NVP-AEW541. D, Western blot showing decrease in the phosphorylation of Igf1r, P70 S6 kinase, IRS1, Akt, Mapk, and Shc on treatment of the mouse rhabdomyosarcoma primary cell cultures (U20325) with increasing amounts of NVPAEW541.

    Mol Cancer Ther 2011 10:697-707. NVP-AEW541 purchased from Selleck.

  • A, treating the mouse rhabdomyosarcoma primary cell cultures (U20325) with increasing amount of NVP-AEW541 induces cell cycle arrest in the G1 phase. B, at moderately high concentrations of NVP-AEW541, the mouse rhabdomyosarcoma cells (U20325) show increased apoptosis as evident by the presence of cleaved caspase-3 at 5 mmol/L (but not at 2 mmol/L, unpublished data). C, representative (median) images of luminescence emitted by rhabdomyosarcoma primary cell cultures grown on quail CAM and being treated with DMSO, imatinib, and NVP-AEW541. The images are displayed with a minimum–maximum scale of 2 106 to 2 107 photons/s/cm2/steradian. D, graphical representation of the intensity of bioluminescence signal emitted by rhabdomyosarcoma primary cell cultures grown on quail CAM that were being treated with DMSO, imatinib (100 mmol/L), or NVPAEW541(10 mmol/L).

    Mol Cancer Ther 2011 10:697-707. NVP-AEW541 purchased from Selleck.

    Combination of NVP-AEW541 and lapatinib cooperatively inhibits the growth of NVP-AEW541 resistant murine rhabdomyosarcoma primary cell cultures with Igf1r/Her2 complexes. Cell viability assay for Naïve, untreated (U20325; A) and NVP-AEW541 innately resistant mouse rhabdomyosarcoma primary culture (U44676; B) treated with varying concentrations of NVP-AEW541, lapatinib, or a combination of both. Naïve cells (U20325) were sensitive to NVP-AEW541, but lapatinib had no cooperativity. In contrast, NVP-AEW541 at moderate doses increased cell growth in resistant cell cultures (U44676). However, this paradoxical effect was reduced by the addition of lapatinib, although lapatinib treatment alone had very little effect. C, the NVP-AEW541 resistant primary tumor cell line (U44676) was treated with DMSO, 5mmol/L lapatinib, 5 mmol/L NVP-AEW541, and a combination of 5 mmol/L NVP-AEW541 t lapatinib for 25 minutes and Western blot analysis was done on lysates for p-Igf1r and p-Her2.

    Mol Cancer Ther 2011 10, 697-707. NVP-AEW541 purchased from Selleck.

  • Inhibition of IGF-IR/InsR or PI3K abrogates AKT membrane localization and phosphorylation. MCF-7/LTED cells were transfected with an AKT PH-GFP plasmid. On day four, cells were treated with 100 ng/ml IGF-I in serum-free medium for 15 minutes, or pre-incubated with 10% DCC-FBS ?1 uM AEW541 or 1 uM BKM120 for 30 minutes followed by treatment with 2 uM AZD5363 for four hours. Cells were viewed in a LSM 510Meta confocal microscope at 40x magnification.

    Breast Cancer Res 2013 15, R55. NVP-AEW541 purchased from Selleck.

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 MoPiT4lv[XOnIHHzd4F6 NFnUNnB,OTEkgJtOwG0> NWf4cYc4TE2VTx?= M33rbolvcGmkaYTzJGlITi2LUjD3bZRpKEmFNUCgc4YhOC5yOE[gxtEhOC5yMkig{txO MVexOVA2ODlzNR?=
A14 NGmxU41McW6jc3WgZZN{[Xl? MVn+NVDjiIsQvF2= M2q5RWROW09? NY\sfGtbcW6qaXLpeJMhUW6|UjD3bZRpKEmFNUCgc4YhOi5|INMxJFAvOTZ|IN88US=> MlfoNVUxPTB7MUW=
A431  NHzLelBMcW6jc3WgZZN{[Xl? MnXrglEx6oDMzszN NIXLU5pFVVOR NV\lRoFWcW6qaXLpeJMhUEWUMTD3bZRpKEmFNUCgc4YhRjFyIN88US=> MVKxOVA2ODlzNR?=
A31  MkPWT4lv[XOnIHHzd4F6 NXrTN49VhjFy4pEK{txO NVjoSXlETE2VTx?= NEL6bmtqdmirYnn0d{BRTEeIUjD3bZRpKEmFNUCgc4YhRjFyIN88US=> NF3CfW4yPTB3MEmxOS=>
GIST882 M2jETmtqdmG|ZTDhd5NigQ>? M3X0PZ4yOOLCit88US=> NF;PeoRFVVOR M1qzNIlvcGmkaYTzJIMuU2m2IIfpeIghUUN3MDDv[kA,PSEQvF2= Ml7aNVUxPTB7MUW=
32D-Bcr-Abl NUXDbGlyU2mwYYPlJIF{e2G7 M4\PbJ4yOOLCit88US=> NVywOHFETE2VTx?= NEDqSFJqdmirYnn0d{BD[3JvQXLsJJAzOTBid3n0bEBKSzVyIH;mJF4yOCEQvF2= M{LPc|E2ODVyOUG1
MCF-7  NVXyeGpmS3m2b4jpZ4l1gSCjc4PhfS=> MXHEUXNQ MoDJTWM2OD1zLk[0JO69VQ>? NVHMV2dLOTVyNUC5NVU>
NWT-21 NX7xbWtjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mli3SG1UVw>? MmPPTWM2OD1yLkG2N{DPxE1? MUOxOVA2ODlzNR?=
TC-71 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGHSc3F,OSEQvF2= MkDNSG1UVw>? MlrLbY5pcWKrdIOgbY5{fWyrbj3sbYtmKGe{b4f0bEBn[WO2b4KtTgKBm22nZHnheIVlKGe{b4f0bC=> MX6xOVg3PzN6Nh?=
TC-71 MlvaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHXqNHF,P+LCit88US=> NV30clgzTE2VTx?= NFTLNHBKSzVyPECuOUDPxE1? M4\icVE2QDZ5M{i2
Saos-2 NV3USlZsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3jzTJ446oDMzszN MV7EUXNQ NHTIWFhKSzVyPEOg{txO NEjmd5QyPTh4N{O4Oi=>
U-2OS MojsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{L1TJ446oDMzszN NXr3T3JlTE2VTx?= NGPvZ4tKSzVyPECuOUDPxE1? Mn30NVU5Pjd|OE[=
SK-ES-1 M4PUUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXHT[WYzhjgkgJtOwG0> MXXEUXNQ MVfJR|UxRDBwNTFOwG0> MlnhNVU5Pjd|OE[=
SK-N-MC NGHNcI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4n1Xp446oDMzszN NH\kS4tFVVOR NIjjUJlKSzVyPECuOUDPxE1? NH2wTmQyPTh4N{O4Oi=>
RD-ES Mm\VS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUizV|ZqhjgkgJtOwG0> M3vL[mROW09? MXTJR|UxRDBwNTFOwG0> M3jpNlE2QDZ5M{i2
SJ-Rh 30 M1zJSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3\MZZ446oDMzszN M1\tRWROW09? MYrJR|UxRDBwNTFOwG0> NVjudINCOTV6NkezPFY>
SJ-Rh 4 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX[5XVZYhjgkgJtOwG0> NXHXd|dWTE2VTx?= MmGzTWM2ODxyLkWg{txO M2e5dFE2QDZ5M{i2
6647 NHXGS4JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3\CXZ446oDMzszN NUPiVm1tTE2VTx?= M4jyeWlEPTB:MD61JO69VQ>? MnnyNVU5Pjd|OE[=
SARG MkW1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn\yglfjiIsQvF2= MnnaSG1UVw>? Mk\2TWM2ODx|IN88US=> MWWxOVg3PzN6Nh?=
MOS NIi3VJhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVTUbIE3hjgkgJtOwG0> M2HmXGROW09? NITOdYlKSzVyPESg{txO MljyNVU5Pjd|OE[=
IOR/OS7 Mkn1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUL+O-KBks7:TR?= NFXu[2lFVVOR NIj0R|ZKSzVyPEGg{txO MlL6NVU5Pjd|OE[=
IOR/OS9 NGq3NZZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{DvNJ446oDMzszN NEHCV5RFVVOR NYjifIhEUUN3MEy2JO69VQ>? M3vzRVE2QDZ5M{i2
IOR/OS10 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUj+O-KBks7:TR?= NUfHXYN4TE2VTx?= M2DkS2lEPTB:NTFOwG0> MYOxOVg3PzN6Nh?=
IOR/OS14 MnrlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlLhglfjiIsQvF2= MoW3SG1UVw>? NH;iZphKSzVyPESg{txO M3HJNlE2QDZ5M{i2
LAP35 NVPVVodUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH\MTpJ,P+LCit88US=> MYXEUXNQ MlGyTWM2ODxyLkWg{txO MWSxOVg3PzN6Nh?=
IOR/BRZ MnruS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWj+O-KBks7:TR?= NYfDTnZUTE2VTx?= NGLIWJhKSzVyPECuOUDPxE1? Mki5NVU5Pjd|OE[=
IOR/CAR MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWDKNmxGhjgkgJtOwG0> NXfNNpFyTE2VTx?= NUPEOItGUUN3MEyxJO69VQ>? M2LNN|E2QDZ5M{i2
IOR/NGR M3eyb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF3nV2p,P+LCit88US=> MVvEUXNQ M3fzNmlEPTB:MD61JO69VQ>? NHXsdXUyPTh4N{O4Oi=>
IOR/RCH NIXCZndIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVr+O-KBks7:TR?= MYTEUXNQ MVvJR|UxRDBwNTFOwG0> NX6xRlR7OTV6NkezPFY>
RMZ-RC2 MnXUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlnlglfjiIsQvF2= NES2c|hFVVOR M3naXmlEPTB:MD61JO69VQ>? MYqxOVg3PzN6Nh?=
CCA M1v0Vmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTNeolVhjgkgJtOwG0> M2HOeGROW09? M2TsbWlEPTB:MjFOwG0> MW[xOVg3PzN6Nh?=
RD/18 Ml70S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFTIO2d,P+LCit88US=> NFLyfI1FVVOR NV7zVYVTUUN3MEy0JO69VQ>? NWjoT|dCOTV6NkezPFY>
OVCAR-3 NYrOSJY6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIDTNId,OTYkgJtOwG0> MmrlSG1UVw>? NX6zRYI5cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MYCxOlMxODh{MB?=
OVCAR-4 NUfwTWlQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3\tdJ4yPeLCit88US=> NUn4b3JDTE2VTx?= MYnpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NFrTfoMyPjNyMEiyNC=>
OVCAR-3 MWnBdI9xfG:|aYOgZZN{[Xl? MYP+NVXjiIsQvF2= Mln6SG1UVw>? NUTRSWJJcW6mdXPld{BieG:ydH;zbZM> MmCxNVY{ODB6MkC=
OVCAR-4 MnPaRZBweHSxc3nzJIF{e2G7 M3XHXZ4yPeLCit88US=> MUjEUXNQ NUHmTng6cW6mdXPld{BieG:ydH;zbZM> MoD0NVY{ODB6MkC=
OVCAR-3 NWrVTFB5TnWwY4Tpc44h[XO|YYm= NIjVU|Z,OTYkgJtOwG0> MWXEUXNQ M3SwTmRm[3KnYYPld{BxcG:|cHjvdplt[XSrb36gc4YhSUuW Mlj4NVY{ODB6MkC=
Huh-7 NVvLcIo5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVP+NVDjiIsQvF2= MWLEUXNQ NF\vNpBKSzVyPUGuOEDPxE1? M1zzOlE3PTNyN{O0
Hep-G2 NX7wc|BjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MofLglEx6oDMzszN NWHvOGVDTE2VTx?= M4rUfmlEPTB;MT64JO69VQ>? MojyNVY2OzB5M{S=
Hep-3B NInnbFhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVn+NVDjiIsQvF2= M1zqPGROW09? NGraOmdKSzVyPUGuPUDPxE1? NVH6bYZpOTZ3M{C3N|Q>
SK-Hep-1 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2C2TJ4yOOLCit88US=> NX7Wc2w6TE2VTx?= MlHnTWM2OD14Lkmg{txO NX\sR5A2OTZ3M{C3N|Q>
Huh-7 M2DOcGZ2dmO2aX;uJIF{e2G7 MWn+NVDjiIsQvF2= MnfVSG1UVw>? Mm[0TY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NUjscIN2OTZ3M{C3N|Q>
Hep-G2 NIGxVIlHfW6ldHnvckBie3OjeR?= MUf+NVDjiIsQvF2= M4e0XmROW09? NGTuW4JKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NV3Nd45tOTZ3M{C3N|Q>
SK-Hep-1 NVO1eWl2TnWwY4Tpc44h[XO|YYm= MV;+NVDjiIsQvF2= MVrEUXNQ Ml3yTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MlLJNVY2OzB5M{S=
BON NFu3SHpMcW6jc3WgZZN{[Xl? MV\+OkDPxE1? NFu2U4VFVVOR MnfRbY5lfWOnczDk[ZBpd3OyaH;yfYxifGmxbjDv[kBKT0ZvMWK= NUDuO4JnOTZ4MEGyPFQ>
BON NUTC[FZHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MknhglEx6oDMzszN NVGyeodnTE2VTx?= MVXJR|UxRTZwNjFOwG0> M3j6e|E3PjBzMki0
CM NVrkTlBYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3PneJ426oDMzszN MXnEUXNQ MlS2TWM2OD1|LkOg{txO NVTnWJRpOTZ4MEGyPFQ>
BON MonQSpVv[3Srb36gZZN{[Xl? NHH2[Wt,Py534pEK{txO NHHKSIdFVVOR Ml[2bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NGXiSWYyPjZyMUK4OC=>
CM M2[5RmZ2dmO2aX;uJIF{e2G7 Mo\6glXjiIsQvF2= MnvCSG1UVw>? NVfYUmsycW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NFTHcHgyPjZyMUK4OC=>
BON MYjBdI9xfG:|aYOgZZN{[Xl? MX\+O{426oDMzszN NWfGUGxsTE2VTx?= MV7pcoR2[2W|IFHwc5B1d3Orcx?= NXjH[Wg5OTZ4MEGyPFQ>
CM MYfBdI9xfG:|aYOgZZN{[Xl? MYP+OgKBks7:TR?= NESzfWRFVVOR NF\CSXFqdmS3Y3XzJGFxd3C2b4Ppdy=> M{[4XVE3PjBzMki0
HT-29 NWTvXWdQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnHvglEx6oDMzszN NFvBOXRFVVOR M4XZPWlEPTB;MT63JO69VQ>? NUDTWGpKOTdyMEewNVU>
HCT-116 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXTrZnkxhjFy4pEK{txO MlGzSG1UVw>? NWr1eZdCUUN3ME2yMlUh|ryP MVGxO|AxPzBzNR?=
primary colorectal cancer cells M2PTXmZ2dmO2aX;uJIF{e2G7 NHjqO2h,PeLCit88US=> NHrjc2dFVVOR NVG0U|Zb[Wy2ZYLzJJRp\SCvb4LwbI9td2e7IH;mJJRp\SC{ZX3hbY5qdmdiY3XscJM> NGfNU5cyPzByN{CxOS=>
HTLA-230 M2X3S2Z2dmO2aX;uJIF{e2G7 MU\+PEDPxE1? MoDVSG1UVw>? M1rqdolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NUTKW4FvOTdzMkG4PVg>
KCNR MkX5SpVv[3Srb36gZZN{[Xl? MnT2glgh|ryP NUSxS2RbTE2VTx?= MkXibY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MV6xO|EzOTh7OB?=
SK-N-BE2c NX\NdXJZTnWwY4Tpc44h[XO|YYm= MnPsglgh|ryP MnzXSG1UVw>? NEL5[mFqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> MUmxO|EzOTh7OB?=
SK-N-BE MmW1SpVv[3Srb36gZZN{[Xl? NX\BbHhPhjhizszN NVG5Zo9qTE2VTx?= MV3pcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NVzUbGx7OTdzMkG4PVg>
LAN-5 M323SGZ2dmO2aX;uJIF{e2G7 NVKzTXZohjhizszN MmPrSG1UVw>? MYjpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NH\QXogyPzF{MUi5PC=>
GI-CA-N NUW5[GFMTnWwY4Tpc44h[XO|YYm= Mmqyglgh|ryP NUHtUIhMTE2VTx?= NVjFWoU4cW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 M4PNbVE4OTJzOEm4
SH-EP NYXhTI84TnWwY4Tpc44h[XO|YYm= MYj+PEDPxE1? MnnjSG1UVw>? M2K4XYlvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MmLDNVcyOjF6OUi=
SK-N-AS MlHTSpVv[3Srb36gZZN{[Xl? M1yzSZ45KM7:TR?= MYnEUXNQ MkLCbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NIm2RogyPzF{MUi5PC=>
RN-GA MVXGeY5kfGmxbjDhd5NigQ>? MYf+PEDPxE1? NHj3NohFVVOR MV7pcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NGHpXGMyPzF{MUi5PC=>
SY-5Y(N) MUTGeY5kfGmxbjDhd5NigQ>? NEDPRZV,QCEQvF2= MmjhSG1UVw>? Mn\XbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NEjOb4IyPzF{MUi5PC=>
GI-CA-N MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlLzglgh|ryP MUjEUXNQ NYrMe2lsUUN3ME2gOk45KM7:TR?= NUC3Z|Q2OTdzMkG4PVg>
SH-EP NEDJS4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWH+PEDPxE1? NXTGUmx5TE2VTx?= NVS2UnZ6UUN3ME2gN{DPxE1? M374XFE4OTJzOEm4
HTLA-230 Ml;5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmS0glgh|ryP MV\EUXNQ M2n2WmlEPTB;IECuOUDPxE1? MX2xO|EzOTh7OB?=
SK-N-BE2c NW\pUI9MT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEXTPGl,QCEQvF2= NWLydmN2TE2VTx?= NGnHOXVKSzVyPTCxMlEh|ryP MnLmNVcyOjF6OUi=
SK-N-BE2 M2f0[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NInBNmR,QCEQvF2= MoruSG1UVw>? MYDJR|UxRSB|IN88US=> MlHjNVcyOjF6OUi=
SY-5Y (N) NYTJXI51T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2ewZp45KM7:TR?= NHTiUYRFVVOR NF3tN|dKSzVyPTCyMlQh|ryP NVHFRZpLOTdzMkG4PVg>
LAN-5 MknxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1K4NJ45KM7:TR?= NFHyWmtFVVOR M2KwV2lEPTB;IECuOEDPxE1? MkW3NVcyOjF6OUi=
KCNR NUe1Wo5jT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWXaVpZwhjhizszN M2XmTGROW09? NEPDZopKSzVyPTCwMlQh|ryP M4\2OVE4OTJzOEm4
RN-GA MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlXYglgh|ryP M4TyOWROW09? MYjJR|UxRSBzLkOg{txO Mkf2NVcyOjF6OUi=
SK-N-AS NETRSnpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYT+PEDPxE1? NHr2T4pFVVOR NV3HPIY1cW6mdXPld{BieG:ydH;zbZM> NIjBbWIyPzF{MUi5PC=>
KCNR NHjBWWRCeG:ydH;zbZMh[XO|YYm= NXLOPIE6hjhizszN MUfEUXNQ MUfpcoR2[2W|IHHwc5B1d3Orcx?= MYKxO|EzOTh7OB?=
GI-CA-N MUfBdI9xfG:|aYOgZZN{[Xl? NYe3TmYzhjhizszN Moi0SG1UVw>? M{HSTIlv\HWlZYOgZZBweHSxc3nz NUjJfndxOTdzMkG4PVg>
HTLA-230 NXXHTI15SXCxcITvd4l{KGG|c3H5 NXnzeodGhjhizszN NWj0eHlwTE2VTx?= MYTpcoR2[2W|IHHwc5B1d3Orcx?= MWOxO|EzOTh7OB?=
SK-N-BE2c Mn75RZBweHSxc3nzJIF{e2G7 NFP3WHd,QCEQvF2= M1m2SGROW09? M4\lOolv\HWlZYOgZZBweHSxc3nz NHPQRpcyPzF{MUi5PC=>
SY-5Y (N) M{HDW2Fxd3C2b4Ppd{Bie3OjeR?= MV\+PEDPxE1? NVPCfGNGTE2VTx?= M1vC[4lv\HWlZYOgZZBweHSxc3nz MmrmNVcyOjF6OUi=
HL60AR NFPy[2tHfW6ldHnvckBie3OjeR?= NUjKSldlOTZyIH7N M37LbYVvcGGwY3XzJJRp\SCuZY\lcJMhd2ZicEK3T4lxOQ>? Mkn3NVc{PjF{MkW=
HL60AR MULBdI9xfG:|aYOgZZN{[Xl? MWH+NlAxKG6P M4\UeYlv\HWlZYOgZZBweHSxc3nz MVGxO|M3OTJ{NR?=
HPAF-II M2i0[GtqdmG|ZTDhd5NigQ>? M3LiV54yKM7:TR?= MlnOSG1UVw>? M4\GXolvcGmkaYTzJGlITi2LLX3l[IlifGWmIIPp[45idGyrbne= MYqxPFQ1PTV{MB?=
HPAF-II MmXmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV7tfVZFhjJizszN NFfJOnNFVVOR M1fSRolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NX7PXlB2OTh2NEW1NlA>
HPAF-II MnvNSpVv[3Srb36gZZN{[Xl? MWD+NkDPxE1? M4P2bGROW09? Ml;YbY5pcWKrdIOgZoF{[WxiYX7kJGlITi2LLX3l[IlifGWmIIDhcoNz\WG2aXOgZ4Fv[2W{IHPlcIwhdWmpcnH0bY9v NXvnWFE1OTh2NEW1NlA>
TFK-1 Ml7mS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUT1OnM4hjJ3MDDuUS=> NGPUTINFVVOR NUfje5BYUUN3ME2wMlI3KM7:TR?= M4nQflIxODZ4N{O0
EGI-1 NHLVZVJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mny3glI2OCCwTR?= MoXrSG1UVw>? NY\LOFJ[UUN3ME2wMlI5KM7:TR?= MmXJNlAxPjZ5M{S=
CC-LP-1 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Moi2glI2OCCwTR?= NHSzOHRFVVOR NYXrTYp2UUN3ME2wMlE2KM7:TR?= NFXOeIYzODB4NkezOC=>
CC-SW-1 NVHQZ29FT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVz+NlUxKG6P M{LkZ2ROW09? NIK2XnRKSzVyPUCuOVQh|ryP NUHabHVVOjByNk[3N|Q>
Sk-ChA-1 NX;N[lNVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUf+NlUxKG6P MnzPSG1UVw>? M2jsdmlEPTB;MD6yJO69VQ>? MlTsNlAxPjZ5M{S=
Mz-ChA-1 NWHpb3pQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUn+NlUxKG6P MUHEUXNQ M3HQd2lEPTB;MT6zPUDPxE1? MmfRNlAxPjZ5M{S=
Mz-ChA-2 NFjRRWRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF\tRop,OjVyIH7N M2PCbmROW09? M3L1fGlEPTB;MD63N{DPxE1? MljYNlAxPjZ5M{S=
ECC-1 NYXDbpV3U2mwYYPlJIF{e2G7 NYq0WlE5hjFyIN88US=> MljvSG1UVw>? MmmxbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQThn MYWyNVI6PTN|NR?=
Ishikawa MWTLbY5ie2ViYYPzZZk> NFfFVYp,OTBizszN M{PXPWROW09? M{m3NIlvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl|JR?= Mln4NlEzQTV|M{W=
USPC-1 NEXOR5NMcW6jc3WgZZN{[Xl? NFraR2F,OTBizszN MUHEUXNQ NEfxZ5FqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSBzMECl NILxfXczOTJ7NUOzOS=>
USPC-2 NUPpeWhYU2mwYYPlJIF{e2G7 NUX0ZZh5hjFyIN88US=> NUj3dVZHTE2VTx?= NUjHXIZxcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOU[l NWXTUYhtOjF{OUWzN|U>
ECC-1 MkjFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoDiglExKM7:TR?= Mn3FSG1UVw>? M3fubYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> M3y0bVIyOjl3M{O1
Ishikawa NU\VfphYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnPWglExKM7:TR?= NELnfXJFVVOR MlW3[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NF7ifmEzOTJ7NUOzOS=>
USPC-1 NWLNbIt6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mnm1glExKM7:TR?= MorrSG1UVw>? M1LFT4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NXvseXNlOjF{OUWzN|U>
USPC-2 MljMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmq0glExKM7:TR?= MXTEUXNQ MVTk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u NHfqVZYzOTJ7NUOzOS=>

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
Synonyms AEW541

Bio Calculators

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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