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 NXH0O5dLU2mwYYPlJIF{e2G7 MYL+NVDjiIsQvF2= MkTFSG1UVw>? NGOzcphqdmirYnn0d{BKT0ZvSWKge4l1cCCLQ{WwJI9nKDBwMEi2JOKyKDBwMEK4JO69VQ>? M3PSO|E2ODVyOUG1
A14 Mlv1T4lv[XOnIHHzd4F6 MoiwglEx6oDMzszN Ml:5SG1UVw>? NHvETlZqdmirYnn0d{BKdnOUIIfpeIghUUN3MDDv[kAzNjNiwsGgNE4yPjNizszN MVqxOVA2ODlzNR?=
A431  NYDrPIF2U2mwYYPlJIF{e2G7 MYn+NVDjiIsQvF2= MlfHSG1UVw>? Mn7HbY5pcWKrdIOgTGVTOSC5aYToJGlEPTBib3[gQlExKM7:TR?= NYHSRXR{OTVyNUC5NVU>
A31  M4\LcmtqdmG|ZTDhd5NigQ>? MV3+NVDjiIsQvF2= M3\0TWROW09? NVr4fXo1cW6qaXLpeJMhWESJRmKge4l1cCCLQ{WwJI9nKD5zMDFOwG0> MXyxOVA2ODlzNR?=
GIST882 MWXLbY5ie2ViYYPzZZk> MnG3glEx6oDMzszN MUPEUXNQ NEPRbG1qdmirYnn0d{BkNUurdDD3bZRpKEmFNUCgc4YhRjVizszN NYHnNpRUOTVyNUC5NVU>
32D-Bcr-Abl NYjBUY1vU2mwYYPlJIF{e2G7 NIPKVGV,OTEkgJtOwG0> M2LP[2ROW09? M3vaVYlvcGmkaYTzJGJkei2DYnygdFIyOCC5aYToJGlEPTBib3[gQlExKM7:TR?= NHXvc3AyPTB3MEmxOS=>
MCF-7  MlPuR5l1d3irY3n0fUBie3OjeR?= NE\TfmdFVVOR Ml;vTWM2OD1zLk[0JO69VQ>? NV;6V5M5OTVyNUC5NVU>
NWT-21 NUfmdINHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXXyRnp2TE2VTx?= M3jBUWlEPTB;MD6xOlMh|ryP M2rsT|E2ODVyOUG1
TC-71 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFfRemx,OSEQvF2= MUTEUXNQ MYPpcohq[mm2czDpcpN2dGmwLXzpb4Uh\3Kxd4ToJIZi[3Sxcj3J5qCUdWWmaXH0[YQh\3Kxd4To NHXicIEyPTh4N{O4Oi=>
TC-71 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkHjglfjiIsQvF2= MlHSSG1UVw>? MlnDTWM2ODxyLkWg{txO NHT0N|cyPTh4N{O4Oi=>
Saos-2 Mkn1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUDyV25xhjgkgJtOwG0> M{fnW2ROW09? NHfBWY9KSzVyPEOg{txO MkKyNVU5Pjd|OE[=
U-2OS MlHXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEPGOnN,P+LCit88US=> Mo\OSG1UVw>? NILIS2xKSzVyPECuOUDPxE1? NVrld3ZROTV6NkezPFY>
SK-ES-1 NW\ZXZJTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3HCXp446oDMzszN MU\EUXNQ NEHuR3RKSzVyPECuOUDPxE1? NHjGUW4yPTh4N{O4Oi=>
SK-N-MC M1P2Rmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml2zglfjiIsQvF2= NH:2UXdFVVOR MXXJR|UxRDBwNTFOwG0> MV6xOVg3PzN6Nh?=
RD-ES NXLiOWxCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWPid2RGhjgkgJtOwG0> M3fYNGROW09? M1jMV2lEPTB:MD61JO69VQ>? Mk[5NVU5Pjd|OE[=
SJ-Rh 30 NW\qT2d1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml\LglfjiIsQvF2= MYPEUXNQ NETQc5FKSzVyPECuOUDPxE1? MV2xOVg3PzN6Nh?=
SJ-Rh 4 NFWzcJNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXzaU4xshjgkgJtOwG0> MoLlSG1UVw>? MV;JR|UxRDBwNTFOwG0> MnfLNVU5Pjd|OE[=
6647 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUXCe5NthjgkgJtOwG0> NWT2R5o6TE2VTx?= NXfzfVE2UUN3MEywMlUh|ryP MYCxOVg3PzN6Nh?=
SARG MlT0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHHPZXR,P+LCit88US=> NXjGWnpyTE2VTx?= MVzJR|UxRDNizszN NELpSm4yPTh4N{O4Oi=>
MOS NF3LZ4NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlTGglfjiIsQvF2= NF\2XXVFVVOR M1W2SmlEPTB:NDFOwG0> NELSbnAyPTh4N{O4Oi=>
IOR/OS7 Mmf2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3LsWZ446oDMzszN MnnjSG1UVw>? NH:4VXNKSzVyPEGg{txO NHfnPVMyPTh4N{O4Oi=>
IOR/OS9 NEXafXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M17FXZ446oDMzszN NHHROmlFVVOR NVXaPFJZUUN3MEy2JO69VQ>? NFzITVMyPTh4N{O4Oi=>
IOR/OS10 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYO2OYVzhjgkgJtOwG0> NV7Dd2pvTE2VTx?= NVPxSnJLUUN3MEy1JO69VQ>? NHPJbogyPTh4N{O4Oi=>
IOR/OS14 MnfKS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MW\+O-KBks7:TR?= MkH3SG1UVw>? MXrJR|UxRDRizszN MnG1NVU5Pjd|OE[=
LAP35 M37nVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4LFSp446oDMzszN NEjlbmJFVVOR M4LLSGlEPTB:MD61JO69VQ>? MYWxOVg3PzN6Nh?=
IOR/BRZ Mn\ZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MofuglfjiIsQvF2= NV7ZcnpETE2VTx?= MlfoTWM2ODxyLkWg{txO MV[xOVg3PzN6Nh?=
IOR/CAR MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV\jVnBJhjgkgJtOwG0> MlnvSG1UVw>? NFL1OZVKSzVyPEGg{txO NWXiSGdYOTV6NkezPFY>
IOR/NGR MoP4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWL6V481hjgkgJtOwG0> MVrEUXNQ NXT5RXhLUUN3MEywMlUh|ryP NF3vXngyPTh4N{O4Oi=>
IOR/RCH M1zK[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml\pglfjiIsQvF2= NYjnSYk6TE2VTx?= MoTYTWM2ODxyLkWg{txO NVz1XmdqOTV6NkezPFY>
RMZ-RC2 NHnlbI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NETxU29,P+LCit88US=> NUTNc2k1TE2VTx?= NHzxZYtKSzVyPECuOUDPxE1? M{\rT|E2QDZ5M{i2
CCA M{LjV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXPYS286hjgkgJtOwG0> M4XrSWROW09? NWfIW5prUUN3MEyyJO69VQ>? M2fLZVE2QDZ5M{i2
RD/18 NGjkUIxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmfRglfjiIsQvF2= NXvqZm5wTE2VTx?= NVri[W4{UUN3MEy0JO69VQ>? NHKyfWYyPTh4N{O4Oi=>
OVCAR-3 MnzES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml\TglE26oDMzszN MYnEUXNQ NYTvPWJFcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M3XjNFE3OzByOEKw
OVCAR-4 NIK2R4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NETOenB,OTYkgJtOwG0> M3u3OWROW09? NFLMfmlqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MUmxOlMxODh{MB?=
OVCAR-3 MWPBdI9xfG:|aYOgZZN{[Xl? NFP3[lZ,OTYkgJtOwG0> NX:2VWRyTE2VTx?= NWLqcJVjcW6mdXPld{BieG:ydH;zbZM> NGfYOXUyPjNyMEiyNC=>
OVCAR-4 NHnLdJpCeG:ydH;zbZMh[XO|YYm= NWO5RmxYhjF34pEK{txO MnK1SG1UVw>? MXjpcoR2[2W|IHHwc5B1d3Orcx?= MknyNVY{ODB6MkC=
OVCAR-3 NETDdWhHfW6ldHnvckBie3OjeR?= Ml;xglE26oDMzszN MUTEUXNQ MnTGSIVkemWjc3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? NVLQZlBMOTZ|MEC4NlA>
Huh-7 NHjodWlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3XFcJ4yOOLCit88US=> M1qzZWROW09? MoDRTWM2OD1zLkSg{txO NXLCVJJxOTZ3M{C3N|Q>
Hep-G2 MoPIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUH+NVDjiIsQvF2= MkLzSG1UVw>? MoWyTWM2OD1zLkig{txO NXvPZ5pQOTZ3M{C3N|Q>
Hep-3B M4DafWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUTWRWZrhjFy4pEK{txO MUHEUXNQ M2XKNWlEPTB;MT65JO69VQ>? MUixOlU{ODd|NB?=
SK-Hep-1 MnLmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnzOglEx6oDMzszN M{PxSGROW09? MWnJR|UxRTZwOTFOwG0> MYKxOlU{ODd|NB?=
Huh-7 NVjnW4Z[TnWwY4Tpc44h[XO|YYm= MnrzglEx6oDMzszN M3XXd2ROW09? MmnRTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NXfEU2U3OTZ3M{C3N|Q>
Hep-G2 M3e1eWZ2dmO2aX;uJIF{e2G7 NViycJA3hjFy4pEK{txO NF;LR|RFVVOR NFPqcY1KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 Mof0NVY2OzB5M{S=
SK-Hep-1 NX[2[|ROTnWwY4Tpc44h[XO|YYm= NUnLRlVXhjFy4pEK{txO NILaTpZFVVOR MnLjTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NUXteo9LOTZ3M{C3N|Q>
BON M1PZUWtqdmG|ZTDhd5NigQ>? M1HhW543KM7:TR?= NWezWJduTE2VTx?= NH\3PZlqdmS3Y3XzJIRmeGixc4Doc5J6dGG2aX;uJI9nKEmJRj2xVi=> NH;ySGoyPjZyMUK4OC=>
BON NX3QVIZXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUP+NVDjiIsQvF2= NUL2UlFuTE2VTx?= NVe5V3NSUUN3ME22MlYh|ryP MmjyNVY3ODF{OES=
CM MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVyxUnFChjYkgJtOwG0> MoX1SG1UVw>? MmDqTWM2OD1|LkOg{txO NV;sVJJzOTZ4MEGyPFQ>
BON MXzGeY5kfGmxbjDhd5NigQ>? NXXGbY81hjdwNfMAju69VQ>? NHHLeYVFVVOR NGnnSXpqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NGTXUmcyPjZyMUK4OC=>
CM MUHGeY5kfGmxbjDhd5NigQ>? Ml2yglXjiIsQvF2= MlLrSG1UVw>? NEDmSodqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NUGzZXE{OTZ4MEGyPFQ>
BON NFTQeYJCeG:ydH;zbZMh[XO|YYm= MXz+O{426oDMzszN MkDLSG1UVw>? Mn7rbY5lfWOnczDBdI9xfG:|aYO= MkjQNVY3ODF{OES=
CM NWO0[2ZTSXCxcITvd4l{KGG|c3H5 M4Lmfp426oDMzszN MmOySG1UVw>? NH3ocFNqdmS3Y3XzJGFxd3C2b4Ppdy=> NGnIPGUyPjZyMUK4OC=>
HT-29 NGHTdXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEjXbmt,OTEkgJtOwG0> NF7mNGJFVVOR NXnyVFdFUUN3ME2xMlch|ryP MmX2NVcxODdyMUW=
HCT-116 NWPIVVVTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYH+NVDjiIsQvF2= M{HYe2ROW09? M1rzUWlEPTB;Mj61JO69VQ>? NITqdYgyPzByN{CxOS=>
primary colorectal cancer cells NWnvSFdvTnWwY4Tpc44h[XO|YYm= M2HDe5426oDMzszN MkjJSG1UVw>? MXvhcJRmenNidHjlJI1wenCqb3zv[5khd2ZidHjlJJJmdWGrbnnu[{Bk\Wyucx?= M2HXSFE4ODB5MEG1
HTLA-230 NGPSS|ZHfW6ldHnvckBie3OjeR?= MYP+PEDPxE1? MVfEUXNQ MWjpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NVy5eY54OTdzMkG4PVg>
KCNR MV3GeY5kfGmxbjDhd5NigQ>? NYDYenBrhjhizszN Mlz1SG1UVw>? MYfpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MYGxO|EzOTh7OB?=
SK-N-BE2c NIfJV|BHfW6ldHnvckBie3OjeR?= Mnewglgh|ryP NGfNdmRFVVOR MX\pcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= M1T2W|E4OTJzOEm4
SK-N-BE M4DxfGZ2dmO2aX;uJIF{e2G7 NF2xSmp,QCEQvF2= M1\WXmROW09? M4fWR4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NHzPOY0yPzF{MUi5PC=>
LAN-5 Mo\0SpVv[3Srb36gZZN{[Xl? MVn+PEDPxE1? NITMNplFVVOR NVXyUXFrcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 NU\5SlBHOTdzMkG4PVg>
GI-CA-N MVjGeY5kfGmxbjDhd5NigQ>? Mnu1glgh|ryP NVXFZ3NrTE2VTx?= M1vWT4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NXTabWhvOTdzMkG4PVg>
SH-EP NH3QOVRHfW6ldHnvckBie3OjeR?= NI[xbYp,QCEQvF2= NITo[G9FVVOR NVrWeGlJcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 MmX0NVcyOjF6OUi=
SK-N-AS Mk[zSpVv[3Srb36gZZN{[Xl? MV3+PEDPxE1? MVzEUXNQ NFu0XmtqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NYrLUmF5OTdzMkG4PVg>
RN-GA MkG2SpVv[3Srb36gZZN{[Xl? Mkm4glgh|ryP NWruWmJSTE2VTx?= NIPLZmhqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NF:2fpUyPzF{MUi5PC=>
SY-5Y(N) NGK0UoJHfW6ldHnvckBie3OjeR?= NIPjb21,QCEQvF2= NFXSO4ZFVVOR NYmyOGRNcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 NVGxd5JvOTdzMkG4PVg>
GI-CA-N NUXD[4NrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnLIglgh|ryP MVzEUXNQ NVTVUHZsUUN3ME2gOk45KM7:TR?= MUGxO|EzOTh7OB?=
SH-EP Mn7jS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV7+PEDPxE1? NFLQepRFVVOR MXfJR|UxRSB|IN88US=> M2LLb|E4OTJzOEm4
HTLA-230 MmKxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVPwNml[hjhizszN NXj2N|FxTE2VTx?= NYfwO2lqUUN3ME2gNE42KM7:TR?= MYSxO|EzOTh7OB?=
SK-N-BE2c Mn3GS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2fmT545KM7:TR?= MlnaSG1UVw>? NFm5TpBKSzVyPTCxMlEh|ryP MmLWNVcyOjF6OUi=
SK-N-BE2 NFLufJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEHzXoN,QCEQvF2= M4HZUmROW09? M2XDVGlEPTB;IEOg{txO M3m1[lE4OTJzOEm4
SY-5Y (N) MlPWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M33wdZ45KM7:TR?= MmD0SG1UVw>? MljOTWM2OD1iMj60JO69VQ>? MkfYNVcyOjF6OUi=
LAN-5 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEnnTWl,QCEQvF2= NVzUT2FJTE2VTx?= MV\JR|UxRSByLkSg{txO Mn[zNVcyOjF6OUi=
KCNR MmTrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYX+PEDPxE1? NX7IZWx2TE2VTx?= NIH5SmNKSzVyPTCwMlQh|ryP NIn6TVIyPzF{MUi5PC=>
RN-GA Mn\NS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYD+PEDPxE1? NWHuO3RkTE2VTx?= M4O0WGlEPTB;IEGuN{DPxE1? NVLPWFVWOTdzMkG4PVg>
SK-N-AS M2L6O2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYm3[oc6hjhizszN NXTCdHEyTE2VTx?= MV;pcoR2[2W|IHHwc5B1d3Orcx?= MYWxO|EzOTh7OB?=
KCNR NXG3XY1iSXCxcITvd4l{KGG|c3H5 M1rhbZ45KM7:TR?= M1zHU2ROW09? MUTpcoR2[2W|IHHwc5B1d3Orcx?= M{GzSlE4OTJzOEm4
GI-CA-N MnfMRZBweHSxc3nzJIF{e2G7 NH61cGN,QCEQvF2= M3n1bGROW09? NFH4VG1qdmS3Y3XzJIFxd3C2b4Ppdy=> NEPpbIMyPzF{MUi5PC=>
HTLA-230 M3PQSWFxd3C2b4Ppd{Bie3OjeR?= M1fqc545KM7:TR?= MnzISG1UVw>? MUjpcoR2[2W|IHHwc5B1d3Orcx?= M1Tl[|E4OTJzOEm4
SK-N-BE2c NV;2SGdzSXCxcITvd4l{KGG|c3H5 MoDKglgh|ryP NUfs[ng3TE2VTx?= NEDJfGVqdmS3Y3XzJIFxd3C2b4Ppdy=> NH\oVGcyPzF{MUi5PC=>
SY-5Y (N) MmnWRZBweHSxc3nzJIF{e2G7 MVr+PEDPxE1? NGnZb5BFVVOR MYjpcoR2[2W|IHHwc5B1d3Orcx?= MWKxO|EzOTh7OB?=
HL60AR NILhV4JHfW6ldHnvckBie3OjeR?= NUO3fFdmOTZyIH7N NX\r[Xlj\W6qYX7j[ZMhfGinIHzleoVteyCxZjDwNldMcXBz Ml;MNVc{PjF{MkW=
HL60AR MWfBdI9xfG:|aYOgZZN{[Xl? MmPOglIxOCCwTR?= NVrPS2ZGcW6mdXPld{BieG:ydH;zbZM> Ml;TNVc{PjF{MkW=
HPAF-II M1LvZ2tqdmG|ZTDhd5NigQ>? NEjveJp,OSEQvF2= MnzQSG1UVw>? NXeybnR7cW6qaXLpeJMhUUeILVmtcYVlcWG2ZXSgd4lodmGubHnu[y=> M{PvflE5PDR3NUKw
HPAF-II NIS2PW9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1vUeZ4zKM7:TR?= NEjmeodFVVOR NVXvb2NEcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NHTmWHEyQDR2NUWyNC=>
HPAF-II MVjGeY5kfGmxbjDhd5NigQ>? NVjWVolIhjJizszN NYGyV4FJTE2VTx?= MYDpcohq[mm2czDiZZNidCCjbnSgTWdHNUlvbXXkbYF1\WRicHHuZ5Jm[XSrYzDjZY5k\XJiY3XscEBucWe{YYTpc44> NUDqcHU6OTh2NEW1NlA>
TFK-1 Ml\mS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYL+NlUxKG6P MXzEUXNQ MVrJR|UxRTBwMk[g{txO MVWyNFA3Pjd|NB?=
EGI-1 M4HPemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4i4eJ4zPTBibl2= MmXlSG1UVw>? M{\OZmlEPTB;MD6yPEDPxE1? M1jvflIxODZ4N{O0
CC-LP-1 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUHae5BthjJ3MDDuUS=> NYPGc|M2TE2VTx?= MVLJR|UxRTBwMUWg{txO MX2yNFA3Pjd|NB?=
CC-SW-1 NI\6O|FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4XPcZ4zPTBibl2= MVXEUXNQ MmfOTWM2OD1yLkW0JO69VQ>? MlfhNlAxPjZ5M{S=
Sk-ChA-1 NHnuO|FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2DYW54zPTBibl2= NUjGPYJTTE2VTx?= Mk\kTWM2OD1yLkKg{txO NULweIxbOjByNk[3N|Q>
Mz-ChA-1 NYm4OFFrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVPIPFI3hjJ3MDDuUS=> MnnRSG1UVw>? NYKzWWU2UUN3ME2xMlM6KM7:TR?= Mm\vNlAxPjZ5M{S=
Mz-ChA-2 NYPqfXRmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUH+NlUxKG6P MlvXSG1UVw>? NV3GcXlkUUN3ME2wMlc{KM7:TR?= M1n2WVIxODZ4N{O0
ECC-1 MWTLbY5ie2ViYYPzZZk> MoXuglExKM7:TR?= M3fpRmROW09? M33MNIlvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl6JR?= NFzhOogzOTJ7NUOzOS=>
Ishikawa Mmi1T4lv[XOnIHHzd4F6 M121O54yOCEQvF2= Ml\WSG1UVw>? MUPpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6OyV? MmfsNlEzQTV|M{W=
USPC-1 M1rB[GtqdmG|ZTDhd5NigQ>? MV;+NVAh|ryP Mn;1SG1UVw>? M4HtfolvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDFyMDW= MVWyNVI6PTN|NR?=
USPC-2 M2LBRWtqdmG|ZTDhd5NigQ>? M4q2NZ4yOCEQvF2= MlG4SG1UVw>? MnLDbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQTZn M1n4OVIyOjl3M{O1
ECC-1 NWrGUHNCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1PWN54yOCEQvF2= MWPEUXNQ NYXwWXFK\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NFHiOIMzOTJ7NUOzOS=>
Ishikawa MlSzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnfKglExKM7:TR?= M{LCdmROW09? NF[4NlVl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MVGyNVI6PTN|NR?=
USPC-1 NWjNVZd7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{PK[Z4yOCEQvF2= NUHkcVZsTE2VTx?= NHjFRpFl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v NFrF[4kzOTJ7NUOzOS=>
USPC-2 NIPD[3BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mo\CglExKM7:TR?= MkXkSG1UVw>? MV7k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MmHKNlEzQTV|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]
+ 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 to the product 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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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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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