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 M1f0[mtqdmG|ZTDhd5NigQ>? MXf+NVDjiIsQvF2= M3vNXmROW09? M2\rcolvcGmkaYTzJGlITi2LUjD3bZRpKEmFNUCgc4YhOC5yOE[gxtEhOC5yMkig{txO NEC1WooyPTB3MEmxOS=>
A14 NIfyW2xMcW6jc3WgZZN{[Xl? NITXTIV,OTEkgJtOwG0> NYKxU4d6TE2VTx?= MWPpcohq[mm2czDJcpNTKHerdHigTWM2OCCxZjCyMlMhyrFiMD6xOlMh|ryP NYnKRmFpOTVyNUC5NVU>
A431  NWX1coJkU2mwYYPlJIF{e2G7 MmToglEx6oDMzszN NEDHXotFVVOR Mk\QbY5pcWKrdIOgTGVTOSC5aYToJGlEPTBib3[gQlExKM7:TR?= M2TOWVE2ODVyOUG1
A31  MWLLbY5ie2ViYYPzZZk> NYXvPJAzhjFy4pEK{txO NYPiWWlHTE2VTx?= MUXpcohq[mm2czDQSGdHWiC5aYToJGlEPTBib3[gQlExKM7:TR?= NHHEWmUyPTB3MEmxOS=>
GIST882 MYfLbY5ie2ViYYPzZZk> NGjHW41,OTEkgJtOwG0> NFfMR2xFVVOR MnL2bY5pcWKrdIOgZ{1McXRid3n0bEBKSzVyIH;mJF42KM7:TR?= NHe0PJMyPTB3MEmxOS=>
32D-Bcr-Abl NYm1SGNmU2mwYYPlJIF{e2G7 MVr+NVDjiIsQvF2= MoXRSG1UVw>? NVf3R2wycW6qaXLpeJMhSmO{LVHicEBxOjFyIIfpeIghUUN3MDDv[kA,OTBizszN MWexOVA2ODlzNR?=
MCF-7  NXr3c|FZS3m2b4jpZ4l1gSCjc4PhfS=> NH7HNGJFVVOR Mk\6TWM2OD1zLk[0JO69VQ>? MYGxOVA2ODlzNR?=
NWT-21 M2DyOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIn3fm5FVVOR NFLHXW1KSzVyPUCuNVY{KM7:TR?= MX6xOVA2ODlzNR?=
TC-71 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{Sw[J4yKM7:TR?= NWjTfW9jTE2VTx?= Ml2zbY5pcWKrdIOgbY5{fWyrbj3sbYtmKGe{b4f0bEBn[WO2b4KtTgKBm22nZHnheIVlKGe{b4f0bC=> NF3jWXcyPTh4N{O4Oi=>
TC-71 NXS2ZmZPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnH6glfjiIsQvF2= M2TGd2ROW09? NF\iWYlKSzVyPECuOUDPxE1? MYexOVg3PzN6Nh?=
Saos-2 NHzid4FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXT+O-KBks7:TR?= NVjwZY1oTE2VTx?= MUPJR|UxRDNizszN NIe5fYkyPTh4N{O4Oi=>
U-2OS NX3E[WpvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4Hqbp446oDMzszN NHSwUnlFVVOR NGTiZWNKSzVyPECuOUDPxE1? NE\XZVQyPTh4N{O4Oi=>
SK-ES-1 NFTOV5VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3Pjep446oDMzszN Mn\BSG1UVw>? MUfJR|UxRDBwNTFOwG0> M3:3eFE2QDZ5M{i2
SK-N-MC Ml;wS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV\5W5ZVhjgkgJtOwG0> NWj5e4hqTE2VTx?= MnLxTWM2ODxyLkWg{txO NGDoU3MyPTh4N{O4Oi=>
RD-ES M1PvRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlW5glfjiIsQvF2= NVHpWG5KTE2VTx?= NYLVTotmUUN3MEywMlUh|ryP MYexOVg3PzN6Nh?=
SJ-Rh 30 NGD2b4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX;BSo45hjgkgJtOwG0> M{XKW2ROW09? NF[3cnlKSzVyPECuOUDPxE1? MXGxOVg3PzN6Nh?=
SJ-Rh 4 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYT+O-KBks7:TR?= MojpSG1UVw>? M4XFTGlEPTB:MD61JO69VQ>? NH7XdpQyPTh4N{O4Oi=>
6647 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFPENVh,P+LCit88US=> MknYSG1UVw>? NYfkVmQyUUN3MEywMlUh|ryP M{\0W|E2QDZ5M{i2
SARG Mm\LS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3;yXp446oDMzszN NGnsWnpFVVOR Mm\FTWM2ODx|IN88US=> M1SzZVE2QDZ5M{i2
MOS M4nHOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NW\kVmpmhjgkgJtOwG0> MWjEUXNQ M1TC[mlEPTB:NDFOwG0> M4rlVFE2QDZ5M{i2
IOR/OS7 NXHHO4xOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NITyWFF,P+LCit88US=> MX\EUXNQ Ml3MTWM2ODxzIN88US=> M2HMNVE2QDZ5M{i2
IOR/OS9 NIjq[ZZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4juRZ446oDMzszN NXPiZml6TE2VTx?= M1rESGlEPTB:NjFOwG0> NIrlcnYyPTh4N{O4Oi=>
IOR/OS10 NWrTcI9ST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3vmdp446oDMzszN MmHhSG1UVw>? MYfJR|UxRDVizszN M4rlPVE2QDZ5M{i2
IOR/OS14 NXPmbYd3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF3Qb5p,P+LCit88US=> MmLoSG1UVw>? MkH3TWM2ODx2IN88US=> NFzsdGEyPTh4N{O4Oi=>
LAP35 MnG2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWjQfmJHhjgkgJtOwG0> M2HQemROW09? MV3JR|UxRDBwNTFOwG0> M4jRXFE2QDZ5M{i2
IOR/BRZ M1XPXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV\+O-KBks7:TR?= Mn;vSG1UVw>? NITVNYVKSzVyPECuOUDPxE1? MYSxOVg3PzN6Nh?=
IOR/CAR NWCxRoxmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{\ZOZ446oDMzszN NF32PYFFVVOR NHXjPYRKSzVyPEGg{txO MkPLNVU5Pjd|OE[=
IOR/NGR MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGTLTIZ,P+LCit88US=> M3LCZ2ROW09? MY\JR|UxRDBwNTFOwG0> MlHuNVU5Pjd|OE[=
IOR/RCH Mm[3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWXaRod[hjgkgJtOwG0> NF\6V45FVVOR MWjJR|UxRDBwNTFOwG0> NILQc|kyPTh4N{O4Oi=>
RMZ-RC2 M1zye2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoTFglfjiIsQvF2= M1;0RmROW09? NGG0SVRKSzVyPECuOUDPxE1? MlPyNVU5Pjd|OE[=
CCA MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2O1dZ446oDMzszN MlXJSG1UVw>? MmL5TWM2ODx{IN88US=> MUGxOVg3PzN6Nh?=
RD/18 NXvyfGc1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUXq[|M4hjgkgJtOwG0> NIXVbI5FVVOR MVXJR|UxRDRizszN NHfreJcyPTh4N{O4Oi=>
OVCAR-3 MmraS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUDWTYRzhjF34pEK{txO MoTUSG1UVw>? NY\6c5NScW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NFzNcZQyPjNyMEiyNC=>
OVCAR-4 M2nmNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXLQcYoxhjF34pEK{txO M{W4R2ROW09? Ml\EbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MVOxOlMxODh{MB?=
OVCAR-3 M17WfGFxd3C2b4Ppd{Bie3OjeR?= MX;+NVXjiIsQvF2= MnHoSG1UVw>? MlLKbY5lfWOnczDhdI9xfG:|aYO= MY[xOlMxODh{MB?=
OVCAR-4 MnzDRZBweHSxc3nzJIF{e2G7 M2PVO54yPeLCit88US=> M3f5fGROW09? NV\0RldmcW6mdXPld{BieG:ydH;zbZM> Mn3lNVY{ODB6MkC=
OVCAR-3 MUfGeY5kfGmxbjDhd5NigQ>? NHP0R4x,OTYkgJtOwG0> NW\VPZgxTE2VTx?= MmrTSIVkemWjc3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? NHPUOYMyPjNyMEiyNC=>
Huh-7 MoPtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn74glEx6oDMzszN NXzxfYE4TE2VTx?= NUDOT5l4UUN3ME2xMlQh|ryP MniwNVY2OzB5M{S=
Hep-G2 MoXZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHfTZ5d,OTEkgJtOwG0> NEiw[4lFVVOR MkL2TWM2OD1zLkig{txO Mmq5NVY2OzB5M{S=
Hep-3B NHL6RmtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1XSVp4yOOLCit88US=> MkD4SG1UVw>? MXrJR|UxRTFwOTFOwG0> NVXvRXpiOTZ3M{C3N|Q>
SK-Hep-1 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGP6WY1,OTEkgJtOwG0> NY\ycZBHTE2VTx?= NXjhdlhbUUN3ME22Mlkh|ryP M1HON|E3PTNyN{O0
Huh-7 MX3GeY5kfGmxbjDhd5NigQ>? MXr+NVDjiIsQvF2= NYXhPW9qTE2VTx?= NEPF[ZBKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NXLuPZlmOTZ3M{C3N|Q>
Hep-G2 MkDHSpVv[3Srb36gZZN{[Xl? NImyNoF,OTEkgJtOwG0> MYDEUXNQ NV3IW21UUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MXWxOlU{ODd|NB?=
SK-Hep-1 MmDXSpVv[3Srb36gZZN{[Xl? NI\vTXB,OTEkgJtOwG0> Mk\1SG1UVw>? Ml3UTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NIiyTlIyPjV|MEezOC=>
BON NUXpbFVsU2mwYYPlJIF{e2G7 MVL+OkDPxE1? NWSzTFJuTE2VTx?= MWPpcoR2[2W|IHTldIhwe3Cqb4L5cIF1cW:wIH;mJGlITi1zUh?= NIf5doUyPjZyMUK4OC=>
BON MoD4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1P3Sp4yOOLCit88US=> NWiweWI6TE2VTx?= MVTJR|UxRTZwNjFOwG0> M{XIc|E3PjBzMki0
CM NI\0No1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYX+OgKBks7:TR?= MXrEUXNQ M3jybmlEPTB;Mz6zJO69VQ>? Mn7GNVY3ODF{OES=
BON MXXGeY5kfGmxbjDhd5NigQ>? M4fJV544NjYkgJtOwG0> NYT4S|ExTE2VTx?= Mnr6bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MXuxOlYxOTJ6NB?=
CM NHrqVpdHfW6ldHnvckBie3OjeR?= M2r5NJ426oDMzszN NFvYW|lFVVOR MkPGbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= Mn\UNVY3ODF{OES=
BON NWPreYl{SXCxcITvd4l{KGG|c3H5 NGi4WpN,Py534pEK{txO NILsXmpFVVOR MonhbY5lfWOnczDBdI9xfG:|aYO= MoXmNVY3ODF{OES=
CM NEDkNG9CeG:ydH;zbZMh[XO|YYm= MUD+OgKBks7:TR?= M3:2WWROW09? NIPHdXpqdmS3Y3XzJGFxd3C2b4Ppdy=> MXGxOlYxOTJ6NB?=
HT-29 NG\XcJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlXZglEx6oDMzszN NUC4NlFjTE2VTx?= MnjWTWM2OD1zLkeg{txO MX2xO|AxPzBzNR?=
HCT-116 NGfLNHVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVi4PGtxhjFy4pEK{txO M{G2XGROW09? MkXSTWM2OD1{LkWg{txO NEnLV2UyPzByN{CxOS=>
primary colorectal cancer cells MUHGeY5kfGmxbjDhd5NigQ>? M4PUcp426oDMzszN MnPUSG1UVw>? M2ThcoFtfGW{czD0bIUhdW:{cHjvcI9ogSCxZjD0bIUhemWvYXnubY5oKGOnbHzz NV7SZ2JPOTdyMEewNVU>
HTLA-230 MnrFSpVv[3Srb36gZZN{[Xl? Mmjoglgh|ryP MnvwSG1UVw>? NFLGNVNqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> MVSxO|EzOTh7OB?=
KCNR MonpSpVv[3Srb36gZZN{[Xl? NFPGNXF,QCEQvF2= NIDoW2JFVVOR M17w[olvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NX3DS5BSOTdzMkG4PVg>
SK-N-BE2c NVnTeFVLTnWwY4Tpc44h[XO|YYm= NY\UU|AzhjhizszN Ml3mSG1UVw>? Ml35bY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 M1TlPVE4OTJzOEm4
SK-N-BE NH;ISmhHfW6ldHnvckBie3OjeR?= NFq4RZp,QCEQvF2= MUTEUXNQ NHjTNIdqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M4\wcVE4OTJzOEm4
LAN-5 Ml7uSpVv[3Srb36gZZN{[Xl? MYL+PEDPxE1? MmHKSG1UVw>? Mn\ubY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NVi0PGlVOTdzMkG4PVg>
GI-CA-N NFHWcnNHfW6ldHnvckBie3OjeR?= M2O3c545KM7:TR?= MnrNSG1UVw>? Mmi2bY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 Ml3QNVcyOjF6OUi=
SH-EP M2LQWmZ2dmO2aX;uJIF{e2G7 MX3+PEDPxE1? NGD0TINFVVOR MXjpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NVLmVId3OTdzMkG4PVg>
SK-N-AS NVi4dIxbTnWwY4Tpc44h[XO|YYm= NV7HOpZvhjhizszN MVnEUXNQ NXvzUIdTcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MniyNVcyOjF6OUi=
RN-GA NXW1VIM{TnWwY4Tpc44h[XO|YYm= MWn+PEDPxE1? NFnYW|ZFVVOR MV\pcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= Mn\xNVcyOjF6OUi=
SY-5Y(N) MUnGeY5kfGmxbjDhd5NigQ>? MU\+PEDPxE1? NH7RO2xFVVOR M{PwXYlvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NVryOGdVOTdzMkG4PVg>
GI-CA-N NFfqWW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUnEeo5jhjhizszN MX7EUXNQ NWHUUpFoUUN3ME2gOk45KM7:TR?= MX2xO|EzOTh7OB?=
SH-EP NHPub4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPlco5,QCEQvF2= Mo\BSG1UVw>? MkDITWM2OD1iMzFOwG0> MVqxO|EzOTh7OB?=
HTLA-230 MmixS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV3+PEDPxE1? MWnEUXNQ M1fSV2lEPTB;IECuOUDPxE1? NXXwenVQOTdzMkG4PVg>
SK-N-BE2c MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlzBglgh|ryP NVXqVFZzTE2VTx?= NYTj[G5PUUN3ME2gNU4yKM7:TR?= M1;WXFE4OTJzOEm4
SK-N-BE2 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4\4ep45KM7:TR?= NWjyeIdlTE2VTx?= NHvwUIJKSzVyPTCzJO69VQ>? NWr0c3dHOTdzMkG4PVg>
SY-5Y (N) MkjCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYP+PEDPxE1? NHXzUW9FVVOR NF34e5NKSzVyPTCyMlQh|ryP NEHkU4IyPzF{MUi5PC=>
LAN-5 Mn3XS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYSweYhohjhizszN NXPEcYFrTE2VTx?= MoXDTWM2OD1iMD60JO69VQ>? M3rHO|E4OTJzOEm4
KCNR MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1XVS545KM7:TR?= M3rDTGROW09? MlHUTWM2OD1iMD60JO69VQ>? MV2xO|EzOTh7OB?=
RN-GA M4XH[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml3Eglgh|ryP MU\EUXNQ NYX1S5g2UUN3ME2gNU4{KM7:TR?= Mo\WNVcyOjF6OUi=
SK-N-AS NGS3Sm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWD+PEDPxE1? NUfXT21WTE2VTx?= NYrWZ25bcW6mdXPld{BieG:ydH;zbZM> MUSxO|EzOTh7OB?=
KCNR NY\FWoV1SXCxcITvd4l{KGG|c3H5 M1i5Np45KM7:TR?= MkexSG1UVw>? NWq0VVBUcW6mdXPld{BieG:ydH;zbZM> MX[xO|EzOTh7OB?=
GI-CA-N M2rqPWFxd3C2b4Ppd{Bie3OjeR?= MofFglgh|ryP M{PYVWROW09? NGTaOmJqdmS3Y3XzJIFxd3C2b4Ppdy=> MnHHNVcyOjF6OUi=
HTLA-230 MoHERZBweHSxc3nzJIF{e2G7 NUXifZI1hjhizszN Mk\hSG1UVw>? M2jmSolv\HWlZYOgZZBweHSxc3nz NFjSW2kyPzF{MUi5PC=>
SK-N-BE2c MXTBdI9xfG:|aYOgZZN{[Xl? Ml;oglgh|ryP NXfqS|ViTE2VTx?= MoHzbY5lfWOnczDhdI9xfG:|aYO= NWHhN4JsOTdzMkG4PVg>
SY-5Y (N) NHfIOJBCeG:ydH;zbZMh[XO|YYm= NEXBVY9,QCEQvF2= NITXO|NFVVOR NFLoRVhqdmS3Y3XzJIFxd3C2b4Ppdy=> MU[xO|EzOTh7OB?=
HL60AR MnziSpVv[3Srb36gZZN{[Xl? MmTZNVYxKG6P NWj4eo1x\W6qYX7j[ZMhfGinIHzleoVteyCxZjDwNldMcXBz NX;u[|Z3OTd|NkGyNlU>
HL60AR M1PGZmFxd3C2b4Ppd{Bie3OjeR?= NUTkZ4o6hjJyMDDuUS=> M1f4NYlv\HWlZYOgZZBweHSxc3nz NWHofYRYOTd|NkGyNlU>
HPAF-II NH76RmNMcW6jc3WgZZN{[Xl? MYT+NUDPxE1? NHrvZYVFVVOR NUTwW3ZUcW6qaXLpeJMhUUeILVmtcYVlcWG2ZXSgd4lodmGubHnu[y=> NIHwe2kyQDR2NUWyNC=>
HPAF-II MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVXjZ2pGhjJizszN MYTEUXNQ MljWbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M1vzXlE5PDR3NUKw
HPAF-II MmDBSpVv[3Srb36gZZN{[Xl? MV\+NkDPxE1? Mn\rSG1UVw>? MWrpcohq[mm2czDiZZNidCCjbnSgTWdHNUlvbXXkbYF1\WRicHHuZ5Jm[XSrYzDjZY5k\XJiY3XscEBucWe{YYTpc44> M4nJT|E5PDR3NUKw
TFK-1 NF3BcnJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFHyWpp,OjVyIH7N NWXxdXBNTE2VTx?= MUXJR|UxRTBwMk[g{txO NY\ubZZROjByNk[3N|Q>
EGI-1 NGGzRWRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml7wglI2OCCwTR?= NYD6[JRTTE2VTx?= MVjJR|UxRTBwMkig{txO MmHRNlAxPjZ5M{S=
CC-LP-1 NUTIclZ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnLlglI2OCCwTR?= MnfFSG1UVw>? NEPpWGZKSzVyPUCuNVUh|ryP MoXPNlAxPjZ5M{S=
CC-SW-1 NYDWVpp5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEmycVh,OjVyIH7N MWDEUXNQ Mke3TWM2OD1yLkW0JO69VQ>? M1HiXVIxODZ4N{O0
Sk-ChA-1 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFW2O5N,OjVyIH7N MYjEUXNQ MXjJR|UxRTBwMjFOwG0> MojHNlAxPjZ5M{S=
Mz-ChA-1 MojXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlfJglI2OCCwTR?= MUjEUXNQ MYjJR|UxRTFwM{mg{txO NV\ubIRKOjByNk[3N|Q>
Mz-ChA-2 MlrsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHvybG1,OjVyIH7N NGnJeHdFVVOR MUTJR|UxRTBwN{Og{txO Ml3xNlAxPjZ5M{S=
ECC-1 MVTLbY5ie2ViYYPzZZk> NHHGTVN,OTBizszN NH35SoZFVVOR NInLOJpqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSB7ODW= NHzYTnMzOTJ7NUOzOS=>
Ishikawa NGXoWmNMcW6jc3WgZZN{[Xl? MmrhglExKM7:TR?= MYLEUXNQ MkmxbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQTNn NHfkTogzOTJ7NUOzOS=>
USPC-1 M{PXWGtqdmG|ZTDhd5NigQ>? NEjN[ph,OTBizszN NFXXbG1FVVOR NXz5PYR6cW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliMUCwKS=> MljjNlEzQTV|M{W=
USPC-2 MUnLbY5ie2ViYYPzZZk> MnPuglExKM7:TR?= NHnxZlVFVVOR M1vrd4lvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl4JR?= Mn7GNlEzQTV|M{W=
ECC-1 MnO4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHLncWN,OTBizszN NHzZTYJFVVOR MmnL[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> MoHRNlEzQTV|M{W=
Ishikawa NXu4bIhoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mk\VglExKM7:TR?= NIG2[HhFVVOR M{HHdoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> Moe1NlEzQTV|M{W=
USPC-1 MmC1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYTzd3RIhjFyIN88US=> NEnZ[5JFVVOR NFrUbphl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v M2HOUFIyOjl3M{O1
USPC-2 NVfr[lNKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVf+NVAh|ryP MVnEUXNQ MoXW[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NIj6b4ozOTJ7NUOzOS=>

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 20 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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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