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.
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
A14 NWLEc2VlU2mwYYPlJIF{e2G7 M4TEWJ4yOOLCit88US=> NHf0eFFFVVOR MVfpcohq[mm2czDJcpNTKHerdHigTWM2OCCxZjCyMlMhyrFiMD6xOlMh|ryP MoC5NVUxPTB7MUW=
NWT-21 NUjVWlRST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkTxSG1UVw>? Ml7QTWM2OD1yLkG2N{DPxE1? NVXi[Y1vOTVyNUC5NVU>
TC-71 M4fWVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1;5Xp4yKM7:TR?= M1HxOWROW09? NVKwdlA1cW6qaXLpeJMhcW6|dXzpck1tcWunIHfyc5d1cCCoYXP0c5IuUeLCk33l[IlifGWmIHfyc5d1cA>? NI\iXmwyPTh4N{O4Oi=>
TC-71 MlnrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2TOOp446oDMzszN NYrDTYRNTE2VTx?= MoS1TWM2ODxyLkWg{txO M2HXbVE2QDZ5M{i2
Saos-2 NXfic5JGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX3seGZbhjgkgJtOwG0> NF3te3BFVVOR NIi4O3ZKSzVyPEOg{txO M3zaZ|E2QDZ5M{i2
U-2OS MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1LhUZ446oDMzszN M3XFbWROW09? MmjGTWM2ODxyLkWg{txO MVixOVg3PzN6Nh?=
SK-ES-1 MkXWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYnON3FHhjgkgJtOwG0> NGjqfmRFVVOR MV3JR|UxRDBwNTFOwG0> MkG0NVU5Pjd|OE[=
SK-N-MC NGjwUplIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPkNph,P+LCit88US=> MlLJSG1UVw>? MXLJR|UxRDBwNTFOwG0> MonyNVU5Pjd|OE[=
RD-ES M1LmUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGXWWIV,P+LCit88US=> NGTDc2dFVVOR MVfJR|UxRDBwNTFOwG0> MnrFNVU5Pjd|OE[=
SJ-Rh 30 NEHvWGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWjCbWV7hjgkgJtOwG0> NV\QSoZVTE2VTx?= M1HteGlEPTB:MD61JO69VQ>? NYXJZnM4OTV6NkezPFY>
SJ-Rh 4 Mnu0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmPLglfjiIsQvF2= M{\sc2ROW09? M1OxPWlEPTB:MD61JO69VQ>? NFzCWVAyPTh4N{O4Oi=>
6647 NF7kfIZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGTlW5Z,P+LCit88US=> NHP1fYNFVVOR MYLJR|UxRDBwNTFOwG0> NFqxcHoyPTh4N{O4Oi=>
SARG MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnrVglfjiIsQvF2= M2fmdmROW09? NHnrc3VKSzVyPEOg{txO MYSxOVg3PzN6Nh?=
MOS MmrDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHTZe5N,P+LCit88US=> NInLV4pFVVOR NWnVSnlxUUN3MEy0JO69VQ>? MVmxOVg3PzN6Nh?=
IOR/OS7 MmjNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3j1PZ446oDMzszN MVXEUXNQ NV;wXIx5UUN3MEyxJO69VQ>? M4HsO|E2QDZ5M{i2
IOR/OS9 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4HQWZ446oDMzszN NGfPW5FFVVOR Mni0TWM2ODx4IN88US=> NIHaVWoyPTh4N{O4Oi=>
IOR/OS10 NFS1bmtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{\h[Z446oDMzszN NHXmUYtFVVOR NUnxd2RtUUN3MEy1JO69VQ>? NHjXWHgyPTh4N{O4Oi=>
IOR/OS14 M3;ENGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYj+O-KBks7:TR?= NWTJbm9iTE2VTx?= Mor5TWM2ODx2IN88US=> M2jaWVE2QDZ5M{i2
IOR/CAR NGHuOZJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYj+O-KBks7:TR?= MVfEUXNQ NHiwSoZKSzVyPEGg{txO M37SWFE2QDZ5M{i2
IOR/RCH NGHzUGpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFnnbGV,P+LCit88US=> Mne3SG1UVw>? NE[zfmpKSzVyPECuOUDPxE1? MWSxOVg3PzN6Nh?=
RMZ-RC2 MmrBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF\LeHR,P+LCit88US=> M{DlcWROW09? M2LiNGlEPTB:MD61JO69VQ>? M3;UdVE2QDZ5M{i2
CCA MlHiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmL4glfjiIsQvF2= MoOwSG1UVw>? M1jCcWlEPTB:MjFOwG0> NYfB[Xp[OTV6NkezPFY>
RD/18 NUDGfpIxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXTKZYJihjgkgJtOwG0> M3u5W2ROW09? NHu1NpdKSzVyPESg{txO MkfINVU5Pjd|OE[=
OVCAR-3 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkPjglE26oDMzszN NXvrc|BlTE2VTx?= M2rod4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MWmxOlMxODh{MB?=
OVCAR-4 M2XEV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M33EXp4yPeLCit88US=> M3PhOGROW09? NHTCPHZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MWSxOlMxODh{MB?=
OVCAR-3 M1jSSWFxd3C2b4Ppd{Bie3OjeR?= NFjUOY5,OTYkgJtOwG0> M1jT[mROW09? NI\NNXRqdmS3Y3XzJIFxd3C2b4Ppdy=> NEn6WXAyPjNyMEiyNC=>
OVCAR-4 NIHrXHBCeG:ydH;zbZMh[XO|YYm= MWL+NVXjiIsQvF2= M1jZbWROW09? NVTY[pltcW6mdXPld{BieG:ydH;zbZM> MUSxOlMxODh{MB?=
OVCAR-3 MoHJSpVv[3Srb36gZZN{[Xl? NV3LU3VohjF34pEK{txO M4XydGROW09? M{nnfmRm[3KnYYPld{BxcG:|cHjvdplt[XSrb36gc4YhSUuW M3rY[|E3OzByOEKw
Huh-7 MnnwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MorLglEx6oDMzszN M1HmXGROW09? NEXUd4FKSzVyPUGuOEDPxE1? NG\pflgyPjV|MEezOC=>
Hep-G2 MljmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4i1bJ4yOOLCit88US=> NXv3OINHTE2VTx?= M17WXGlEPTB;MT64JO69VQ>? NV7XUHNJOTZ3M{C3N|Q>
Hep-3B NX[w[lAzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmX3glEx6oDMzszN NF7VS3ZFVVOR MlLxTWM2OD1zLkmg{txO MWGxOlU{ODd|NB?=
SK-Hep-1 NE\UV|ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn3QglEx6oDMzszN MXTEUXNQ NUTFXJEyUUN3ME22Mlkh|ryP M1LwZ|E3PTNyN{O0
Huh-7 M{CxWGZ2dmO2aX;uJIF{e2G7 NXG3XXBWhjFy4pEK{txO MnLNSG1UVw>? NXnYRZJWUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MXyxOlU{ODd|NB?=
Hep-G2 M{jGOWZ2dmO2aX;uJIF{e2G7 MYn+NVDjiIsQvF2= NH3ze4VFVVOR NET0R45KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MknNNVY2OzB5M{S=
SK-Hep-1 M4jkPGZ2dmO2aX;uJIF{e2G7 NELmOFB,OTEkgJtOwG0> NGL3SWlFVVOR MnrSTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NVnk[VVXOTZ3M{C3N|Q>
BON MWHLbY5ie2ViYYPzZZk> NGrWSWd,PiEQvF2= MnLkSG1UVw>? NUTkeVdncW6mdXPld{Bl\XCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXI> MnLyNVY3ODF{OES=
BON M{\mO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXjMT252hjFy4pEK{txO NI\tVoJFVVOR NXi1fohVUUN3ME22MlYh|ryP NWDsZolGOTZ4MEGyPFQ>
CM MorCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnHoglXjiIsQvF2= MYPEUXNQ NXTSb|djUUN3ME2zMlMh|ryP Mnz0NVY3ODF{OES=
BON NI\oSYhHfW6ldHnvckBie3OjeR?= NYjHVHRVhjdwNfMAju69VQ>? NFfIe5RFVVOR NIDINZFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M4K4dVE3PjBzMki0
CM MXjGeY5kfGmxbjDhd5NigQ>? M{nJU5426oDMzszN NEn3PIhFVVOR M4TuOYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M13pXlE3PjBzMki0
BON Mni4RZBweHSxc3nzJIF{e2G7 M4rxOJ44NjYkgJtOwG0> MmrOSG1UVw>? MmjkbY5lfWOnczDBdI9xfG:|aYO= M3jYeFE3PjBzMki0
CM Mm\2RZBweHSxc3nzJIF{e2G7 NYT2U2M5hjYkgJtOwG0> MXXEUXNQ NVjuTINlcW6mdXPld{BCeG:ydH;zbZM> MXKxOlYxOTJ6NB?=
HT-29 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1y4d54yOOLCit88US=> M3X5fGROW09? NF;kUnVKSzVyPUGuO{DPxE1? NH;jNIwyPzByN{CxOS=>
HCT-116 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV3t[GY4hjFy4pEK{txO M{fqe2ROW09? NYq3V3E{UUN3ME2yMlUh|ryP MkfhNVcxODdyMUW=
primary colorectal cancer cells Ml\ESpVv[3Srb36gZZN{[Xl? MVz+OgKBks7:TR?= MlvCSG1UVw>? NUTsOGZG[Wy2ZYLzJJRp\SCvb4LwbI9td2e7IH;mJJRp\SC{ZX3hbY5qdmdiY3XscJM> MnPoNVcxODdyMUW=
HTLA-230 MmXCSpVv[3Srb36gZZN{[Xl? NYriPGtVhjhizszN NIe1O|ZFVVOR MXzpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MUmxO|EzOTh7OB?=
KCNR NFvtRZJHfW6ldHnvckBie3OjeR?= Mn\vglgh|ryP MnzBSG1UVw>? MVLpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NFXMRlEyPzF{MUi5PC=>
SK-N-BE2c NHXFXI1HfW6ldHnvckBie3OjeR?= NGLocI1,QCEQvF2= MlzrSG1UVw>? MlvibY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MnHuNVcyOjF6OUi=
SK-N-BE M4fkUmZ2dmO2aX;uJIF{e2G7 MUD+PEDPxE1? NEnXWGVFVVOR MUPpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= M4DsbFE4OTJzOEm4
GI-CA-N MlnjSpVv[3Srb36gZZN{[Xl? Mo\iglgh|ryP NVvCdHd6TE2VTx?= NXe2cmF1cW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 NUDUOnIxOTdzMkG4PVg>
SH-EP M4js[mZ2dmO2aX;uJIF{e2G7 MUX+PEDPxE1? M1jw[mROW09? MWfpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= Ml;tNVcyOjF6OUi=
SK-N-AS MULGeY5kfGmxbjDhd5NigQ>? NXLBcmZUhjhizszN MnvTSG1UVw>? Ml;ZbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MmTPNVcyOjF6OUi=
RN-GA MoDqSpVv[3Srb36gZZN{[Xl? M3PEZ545KM7:TR?= M{PvSmROW09? NV;3dno1cW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 NXH0NZg1OTdzMkG4PVg>
SY-5Y(N) M2XofGZ2dmO2aX;uJIF{e2G7 NIrtUpF,QCEQvF2= M37FcmROW09? M1q5WolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MV2xO|EzOTh7OB?=
GI-CA-N NH60c4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M33KWp45KM7:TR?= NVv2epd7TE2VTx?= MkTETWM2OD1iNj64JO69VQ>? MoPlNVcyOjF6OUi=
SH-EP MkDXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlTZglgh|ryP NGjXdZJFVVOR MmT4TWM2OD1iMzFOwG0> MYKxO|EzOTh7OB?=
HTLA-230 MkjVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlPmglgh|ryP NXHlZ2l4TE2VTx?= NHjCTplKSzVyPTCwMlUh|ryP MXOxO|EzOTh7OB?=
SK-N-BE2c MkCxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX\OUFJbhjhizszN MXXEUXNQ NF7Pc4RKSzVyPTCxMlEh|ryP MV6xO|EzOTh7OB?=
SK-N-BE2 NH\6eJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkSwglgh|ryP NFLLXVRFVVOR NYW1UGZqUUN3ME2gN{DPxE1? NYnj[|VsOTdzMkG4PVg>
SY-5Y (N) MlK2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFfuRmh,QCEQvF2= MnzaSG1UVw>? MXHJR|UxRSB{LkSg{txO M3TUfVE4OTJzOEm4
LAN-5 M1zVbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml7wglgh|ryP M4PYTmROW09? MkTMTWM2OD1iMD60JO69VQ>? NX;aUoJ[OTdzMkG4PVg>
KCNR MnLvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NU\wNXVNhjhizszN MYXEUXNQ Mn;yTWM2OD1iMD60JO69VQ>? MUexO|EzOTh7OB?=
KCNR M3;3cmFxd3C2b4Ppd{Bie3OjeR?= NHTaZmd,QCEQvF2= M4m1T2ROW09? M1;JdYlv\HWlZYOgZZBweHSxc3nz M{nEd|E4OTJzOEm4
GI-CA-N M2fISGFxd3C2b4Ppd{Bie3OjeR?= NFnVXFB,QCEQvF2= M4HXfGROW09? MlzCbY5lfWOnczDhdI9xfG:|aYO= NXS3WHM3OTdzMkG4PVg>
HTLA-230 NH3zOphCeG:ydH;zbZMh[XO|YYm= M1HMZp45KM7:TR?= NF7JVoNFVVOR MlXvbY5lfWOnczDhdI9xfG:|aYO= MVqxO|EzOTh7OB?=
SK-N-BE2c NGXsUVBCeG:ydH;zbZMh[XO|YYm= MYj+PEDPxE1? MnriSG1UVw>? NXf6ZZl7cW6mdXPld{BieG:ydH;zbZM> MonKNVcyOjF6OUi=
SY-5Y (N) M1H6OWFxd3C2b4Ppd{Bie3OjeR?= Ml3zglgh|ryP NHe4eWJFVVOR NEDI[FVqdmS3Y3XzJIFxd3C2b4Ppdy=> MXGxO|EzOTh7OB?=
HL60AR MX\GeY5kfGmxbjDhd5NigQ>? MXuxOlAhdk1? NH\ROW9mdmijbnPld{B1cGVibHX2[Yx{KG:oIICyO2tqeDF? MnPyNVc{PjF{MkW=
HL60AR MXXBdI9xfG:|aYOgZZN{[Xl? NYDKS3RChjJyMDDuUS=> NHzjV3BqdmS3Y3XzJIFxd3C2b4Ppdy=> M3HtPVE4OzZzMkK1
HPAF-II MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF3iU21,OiEQvF2= NUKyUmdtTE2VTx?= MljKbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NYm4OlRvOTh2NEW1NlA>
HPAF-II M1LGTGZ2dmO2aX;uJIF{e2G7 Mm[0glIh|ryP MV7EUXNQ NU\lNWtLcW6qaXLpeJMh[mG|YXygZY5lKEmJRj3JMY1m\GmjdHXkJJBidmO{ZXH0bYMh[2GwY3XyJINmdGxibXnndoF1cW:w MmOwNVg1PDV3MkC=
TFK-1 M1HJbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEP6ZZp,OjVyIH7N MWnEUXNQ NFfIOlNKSzVyPUCuNlYh|ryP MmPYNlAxPjZ5M{S=
EGI-1 MnLsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4nZPJ4zPTBibl2= NILGOW9FVVOR MXTJR|UxRTBwMkig{txO MnzhNlAxPjZ5M{S=
CC-LP-1 M3rNPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{\tZ54zPTBibl2= NVjhfIRWTE2VTx?= MUHJR|UxRTBwMUWg{txO MkOwNlAxPjZ5M{S=
CC-SW-1 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXj+NlUxKG6P MYnEUXNQ MomzTWM2OD1yLkW0JO69VQ>? NHjTdZEzODB4NkezOC=>
Sk-ChA-1 MmLoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlnrglI2OCCwTR?= MYLEUXNQ M{WyfmlEPTB;MD6yJO69VQ>? NULkfoxFOjByNk[3N|Q>
Mz-ChA-1 NFnYVGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3\kd54zPTBibl2= NVHH[3J4TE2VTx?= MlzwTWM2OD1zLkO5JO69VQ>? MYeyNFA3Pjd|NB?=
Mz-ChA-2 MoDOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYj+NlUxKG6P NGTtbGVFVVOR NIfLfWtKSzVyPUCuO|Mh|ryP MVeyNFA3Pjd|NB?=
ECC-1 MY\LbY5ie2ViYYPzZZk> NFLPd2l,OTBizszN MknqSG1UVw>? NXvPcI5IcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOUil M2HET|IyOjl3M{O1
Ishikawa MlXQT4lv[XOnIHHzd4F6 MUP+NVAh|ryP MUjEUXNQ MoTmbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQTNn MlzqNlEzQTV|M{W=
USPC-1 NFTaUI5McW6jc3WgZZN{[Xl? Mk\lglExKM7:TR?= NVHPfYJsTE2VTx?= MXnpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUAyODBn MUGyNVI6PTN|NR?=
USPC-2 M2roVmtqdmG|ZTDhd5NigQ>? NUHJOWN2hjFyIN88US=> MkXSSG1UVw>? NF[yflFqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSB7NjW= M1G1W|IyOjl3M{O1
ECC-1 NGnyT4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYf+NVAh|ryP NF[4c2tFVVOR Mmno[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NGLLZ3IzOTJ7NUOzOS=>
Ishikawa NYToZ4RrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX7GU2tYhjFyIN88US=> M1HDbWROW09? MUTk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u NUfHVolOOjF{OUWzN|U>
USPC-1 NWDyN5A1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVv0NVhOhjFyIN88US=> NULCellpTE2VTx?= MVLk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MmP1NlEzQTV|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]


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]
+ 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 to the product individually and in order:
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


CAS No. 475489-16-8
Storage powder
Synonyms AEW541

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID