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 NInNNmNMcW6jc3WgZZN{[Xl? NHTHUnp,OTEkgJtOwG0> MYnEUXNQ NEPpeWpqdmirYnn0d{BKT0ZvSWKge4l1cCCLQ{WwJI9nKDBwMEi2JOKyKDBwMEK4JO69VQ>? NWTlelB5OTVyNUC5NVU>
A14 MmX0T4lv[XOnIHHzd4F6 MVL+NVDjiIsQvF2= MVfEUXNQ M4jDfYlvcGmkaYTzJGlve1Jid3n0bEBKSzVyIH;mJFIvOyEEsTCwMlE3OyEQvF2= NWDRNIhXOTVyNUC5NVU>
A431  M{C3dWtqdmG|ZTDhd5NigQ>? MlS2glEx6oDMzszN MlW4SG1UVw>? MkPSbY5pcWKrdIOgTGVTOSC5aYToJGlEPTBib3[gQlExKM7:TR?= Ml73NVUxPTB7MUW=
A31  NHG3[mxMcW6jc3WgZZN{[Xl? MnTWglEx6oDMzszN MnW5SG1UVw>? M17zV4lvcGmkaYTzJHBFT0[UIIfpeIghUUN3MDDv[kA,OTBizszN NGftfnUyPTB3MEmxOS=>
GIST882 M4L2XmtqdmG|ZTDhd5NigQ>? NHvJ[5J,OTEkgJtOwG0> MULEUXNQ MWnpcohq[mm2czDjMWtqfCC5aYToJGlEPTBib3[gQlUh|ryP M3HqSFE2ODVyOUG1
32D-Bcr-Abl NUfYSINbU2mwYYPlJIF{e2G7 NXnLOY4xhjFy4pEK{txO M1fBR2ROW09? NVrRTllGcW6qaXLpeJMhSmO{LVHicEBxOjFyIIfpeIghUUN3MDDv[kA,OTBizszN NF7aVVIyPTB3MEmxOS=>
MCF-7  M1H1NGN6fG:6aXPpeJkh[XO|YYm= NG\ZTodFVVOR M2OxN2lEPTB;MT62OEDPxE1? Ml;aNVUxPTB7MUW=
NWT-21 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoOwSG1UVw>? MUXJR|UxRTBwMU[zJO69VQ>? NU\MUolEOTVyNUC5NVU>
TC-71 NIXE[XZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4\T[Z4yKM7:TR?= MkjqSG1UVw>? MkDtbY5pcWKrdIOgbY5{fWyrbj3sbYtmKGe{b4f0bEBn[WO2b4KtTgKBm22nZHnheIVlKGe{b4f0bC=> NELCbooyPTh4N{O4Oi=>
TC-71 Mki2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4rYe5446oDMzszN MV\EUXNQ MoC0TWM2ODxyLkWg{txO MXOxOVg3PzN6Nh?=
Saos-2 M1rKZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWL+O-KBks7:TR?= NEHCR4hFVVOR NGrnTZlKSzVyPEOg{txO MXKxOVg3PzN6Nh?=
U-2OS NWXk[GhvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIHxell,P+LCit88US=> MVfEUXNQ NEX6PWtKSzVyPECuOUDPxE1? NHnwOlYyPTh4N{O4Oi=>
SK-ES-1 M37Pb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYL+O-KBks7:TR?= NGfaRoNFVVOR NVzqZm5wUUN3MEywMlUh|ryP MkDKNVU5Pjd|OE[=
SK-N-MC NYi3ZnN{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2jaU5446oDMzszN MWfEUXNQ NWTSRYt[UUN3MEywMlUh|ryP MUKxOVg3PzN6Nh?=
RD-ES M2rLPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1zzOp446oDMzszN MVLEUXNQ NEi1coZKSzVyPECuOUDPxE1? MX[xOVg3PzN6Nh?=
SJ-Rh 30 MmDUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVnVPHVJhjgkgJtOwG0> M3PES2ROW09? MoCxTWM2ODxyLkWg{txO NHjqcYMyPTh4N{O4Oi=>
SJ-Rh 4 NX\KZWF{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1O5[J446oDMzszN NIrFOJlFVVOR NHu2TFNKSzVyPECuOUDPxE1? NVXKXok2OTV6NkezPFY>
6647 NVjUOWh6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX;a[ldJhjgkgJtOwG0> M3nJeWROW09? M2jWTmlEPTB:MD61JO69VQ>? NULCc217OTV6NkezPFY>
SARG NVfvTmwzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGmzXnF,P+LCit88US=> MULEUXNQ MnnCTWM2ODx|IN88US=> M3HWVlE2QDZ5M{i2
MOS MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnPUglfjiIsQvF2= MUDEUXNQ NHj0co5KSzVyPESg{txO MoC2NVU5Pjd|OE[=
IOR/OS7 NIC5cnJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXj+O-KBks7:TR?= MlPDSG1UVw>? NUPpUYh4UUN3MEyxJO69VQ>? MYexOVg3PzN6Nh?=
IOR/OS9 NUnkSmM{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NG\Zc5B,P+LCit88US=> M4K2Z2ROW09? M{PreWlEPTB:NjFOwG0> NUjDT|RLOTV6NkezPFY>
IOR/OS10 NYTGXZFjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXT+O-KBks7:TR?= MWjEUXNQ MVTJR|UxRDVizszN NHrRSY0yPTh4N{O4Oi=>
IOR/OS14 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX;+O-KBks7:TR?= NGXNZoNFVVOR M3W5fGlEPTB:NDFOwG0> NV:5[pZ1OTV6NkezPFY>
LAP35 NVq1WFJpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlvBglfjiIsQvF2= NIXkOWpFVVOR MnHkTWM2ODxyLkWg{txO NEC0U24yPTh4N{O4Oi=>
IOR/BRZ MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVv+O-KBks7:TR?= NISwd45FVVOR M1nvWGlEPTB:MD61JO69VQ>? NUfEZYNzOTV6NkezPFY>
IOR/CAR NXewbI5{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEW1NJR,P+LCit88US=> NYrmSVY3TE2VTx?= M1zDR2lEPTB:MTFOwG0> MUexOVg3PzN6Nh?=
IOR/NGR NUX4SpVpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWfkVWg3hjgkgJtOwG0> NYOzdHZ[TE2VTx?= MmDMTWM2ODxyLkWg{txO MoTRNVU5Pjd|OE[=
IOR/RCH NWrHOFAyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVf+O-KBks7:TR?= M1PGOWROW09? NHrxNphKSzVyPECuOUDPxE1? MVKxOVg3PzN6Nh?=
RMZ-RC2 MnXJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU\+O-KBks7:TR?= NFPIO29FVVOR MWHJR|UxRDBwNTFOwG0> MWGxOVg3PzN6Nh?=
CCA M2e4W2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{HnPJ446oDMzszN MmjJSG1UVw>? MU\JR|UxRDJizszN MoXpNVU5Pjd|OE[=
RD/18 NYLkXId1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWj+O-KBks7:TR?= MnLhSG1UVw>? Mn3XTWM2ODx2IN88US=> NITifVAyPTh4N{O4Oi=>
OVCAR-3 M4[yUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmK4glE26oDMzszN MWLEUXNQ NIn5Oo9qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NIHLWmgyPjNyMEiyNC=>
OVCAR-4 NHrVRlFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmLiglE26oDMzszN Ml7DSG1UVw>? MWfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NEHINZgyPjNyMEiyNC=>
OVCAR-3 MUjBdI9xfG:|aYOgZZN{[Xl? MVP+NVXjiIsQvF2= M1TwRmROW09? NXPuT4RtcW6mdXPld{BieG:ydH;zbZM> NWO3XG41OTZ|MEC4NlA>
OVCAR-4 MVPBdI9xfG:|aYOgZZN{[Xl? MXT+NVXjiIsQvF2= NHXqPY1FVVOR NVvYe3o5cW6mdXPld{BieG:ydH;zbZM> M13EeVE3OzByOEKw
OVCAR-3 Mm\6SpVv[3Srb36gZZN{[Xl? NFLJb2l,OTYkgJtOwG0> M2PVPGROW09? MWHE[YNz\WG|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? M4fmdFE3OzByOEKw
Huh-7 M370V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXvjeWl1hjFy4pEK{txO MVjEUXNQ MnL1TWM2OD1zLkSg{txO NHHXPIUyPjV|MEezOC=>
Hep-G2 M3rESGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEHuXYd,OTEkgJtOwG0> NIPYVI9FVVOR NXXqeYpWUUN3ME2xMlgh|ryP Mkm1NVY2OzB5M{S=
Hep-3B MoDSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVPT[GpMhjFy4pEK{txO M37DUGROW09? M3PoS2lEPTB;MT65JO69VQ>? NWr4[IdzOTZ3M{C3N|Q>
SK-Hep-1 M4rSR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWXwZ2VFhjFy4pEK{txO NGLiWJZFVVOR MnP0TWM2OD14Lkmg{txO NXLQOpNYOTZ3M{C3N|Q>
Huh-7 MVXGeY5kfGmxbjDhd5NigQ>? MUn+NVDjiIsQvF2= NYnjTGZWTE2VTx?= MnTFTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M4ToRVE3PTNyN{O0
Hep-G2 M1\sN2Z2dmO2aX;uJIF{e2G7 NILKNm1,OTEkgJtOwG0> M3T3SGROW09? M1LhVmlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MoLoNVY2OzB5M{S=
SK-Hep-1 M1HOeWZ2dmO2aX;uJIF{e2G7 MV;+NVDjiIsQvF2= MnPZSG1UVw>? MXLJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 Mne3NVY2OzB5M{S=
BON NID0PHVMcW6jc3WgZZN{[Xl? MXr+OkDPxE1? MXLEUXNQ NXHkW|c6cW6mdXPld{Bl\XCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXI> NHn3N3UyPjZyMUK4OC=>
BON NYfPN3VST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlnkglEx6oDMzszN MVnEUXNQ MV;JR|UxRTZwNjFOwG0> MVixOlYxOTJ6NB?=
CM MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4Tkd5426oDMzszN M1LMNmROW09? MljuTWM2OD1|LkOg{txO M4XOXFE3PjBzMki0
BON M3S0e2Z2dmO2aX;uJIF{e2G7 M{O5Xp44NjYkgJtOwG0> NWDUOY8yTE2VTx?= M36xT4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MlraNVY3ODF{OES=
CM MU\GeY5kfGmxbjDhd5NigQ>? NUDGT|k4hjYkgJtOwG0> NF\6b3dFVVOR NHz5RVRqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NInhUpoyPjZyMUK4OC=>
BON NIH5WWRCeG:ydH;zbZMh[XO|YYm= NFTw[2t,Py534pEK{txO NEX1XpVFVVOR MUHpcoR2[2W|IFHwc5B1d3Orcx?= NIrGbpIyPjZyMUK4OC=>
CM NXPMfZpvSXCxcITvd4l{KGG|c3H5 NGHhSoV,PeLCit88US=> MonWSG1UVw>? NED3S4xqdmS3Y3XzJGFxd3C2b4Ppdy=> NHjYfnYyPjZyMUK4OC=>
HT-29 MoDSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVXtW5p6hjFy4pEK{txO MYfEUXNQ Ml3DTWM2OD1zLkeg{txO NHTDfoUyPzByN{CxOS=>
HCT-116 NUDzN3ZST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGDZSZp,OTEkgJtOwG0> NUi1PHZpTE2VTx?= MmfjTWM2OD1{LkWg{txO NV6xW4tqOTdyMEewNVU>
primary colorectal cancer cells M4XJSWZ2dmO2aX;uJIF{e2G7 MWr+OgKBks7:TR?= NHuwT3BFVVOR NWDtNHo2[Wy2ZYLzJJRp\SCvb4LwbI9td2e7IH;mJJRp\SC{ZX3hbY5qdmdiY3XscJM> M2SyNVE4ODB5MEG1
HTLA-230 M3XhNWZ2dmO2aX;uJIF{e2G7 NUjneWN{hjhizszN MmHWSG1UVw>? NUW2VJllcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 NYLUUoprOTdzMkG4PVg>
KCNR M4jlTGZ2dmO2aX;uJIF{e2G7 MV3+PEDPxE1? NXv2TIoyTE2VTx?= MVvpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MXKxO|EzOTh7OB?=
SK-N-BE2c Ml7aSpVv[3Srb36gZZN{[Xl? M{LpWp45KM7:TR?= NHvFfVJFVVOR MUfpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MlvQNVcyOjF6OUi=
SK-N-BE NFjVU49HfW6ldHnvckBie3OjeR?= NYH0bmdGhjhizszN NFX2RVJFVVOR NHHzWYtqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M1rXVFE4OTJzOEm4
LAN-5 MonTSpVv[3Srb36gZZN{[Xl? M2jnXJ45KM7:TR?= MWrEUXNQ NF3KT3hqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> MmrYNVcyOjF6OUi=
GI-CA-N NE[1c4VHfW6ldHnvckBie3OjeR?= MkDZglgh|ryP MnnxSG1UVw>? NGj6dmpqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M{jT[lE4OTJzOEm4
SH-EP NIC3d5NHfW6ldHnvckBie3OjeR?= NFPjWJB,QCEQvF2= NYD2SWZqTE2VTx?= MWfpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NWPDfVJ[OTdzMkG4PVg>
SK-N-AS M33heWZ2dmO2aX;uJIF{e2G7 M1T4R545KM7:TR?= Ml\JSG1UVw>? MluwbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 M1fNblE4OTJzOEm4
RN-GA NFPTeWFHfW6ldHnvckBie3OjeR?= NFzsTm5,QCEQvF2= MljPSG1UVw>? M2HndYlvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> Mn;jNVcyOjF6OUi=
SY-5Y(N) MUnGeY5kfGmxbjDhd5NigQ>? M1nqN545KM7:TR?= Moj6SG1UVw>? NGDYXJlqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NH[4VIwyPzF{MUi5PC=>
GI-CA-N NUWybpFiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnThglgh|ryP MmDhSG1UVw>? MlHMTWM2OD1iNj64JO69VQ>? M2GzS|E4OTJzOEm4
SH-EP MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFG4dnl,QCEQvF2= M4[3RWROW09? NHvSVmRKSzVyPTCzJO69VQ>? NIX3dZEyPzF{MUi5PC=>
HTLA-230 MmLES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIHTN3Z,QCEQvF2= MkT3SG1UVw>? MVnJR|UxRSByLkWg{txO MVexO|EzOTh7OB?=
SK-N-BE2c MnvqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4PDb545KM7:TR?= NX7TVYV2TE2VTx?= NH:xV5JKSzVyPTCxMlEh|ryP NX3ET2tJOTdzMkG4PVg>
SK-N-BE2 NFjaSlJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mnvvglgh|ryP MlnISG1UVw>? NHXLSWFKSzVyPTCzJO69VQ>? M1HaU|E4OTJzOEm4
SY-5Y (N) NHj3[|FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXz+PEDPxE1? M3nD[WROW09? NGD5XIdKSzVyPTCyMlQh|ryP MlzrNVcyOjF6OUi=
LAN-5 MmXxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFf4VoV,QCEQvF2= Mk\OSG1UVw>? M1\GPGlEPTB;IECuOEDPxE1? MnPpNVcyOjF6OUi=
KCNR NH24eFNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHTYdWJ,QCEQvF2= MlG4SG1UVw>? NIPZbJZKSzVyPTCwMlQh|ryP NFjiS5YyPzF{MUi5PC=>
RN-GA NHz4bIdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWH+PEDPxE1? NFfvcYpFVVOR NGC0cJdKSzVyPTCxMlMh|ryP NULVNnlLOTdzMkG4PVg>
SK-N-AS M3zad2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3W1Z545KM7:TR?= NF\U[mxFVVOR NETHd4RqdmS3Y3XzJIFxd3C2b4Ppdy=> NEjkSFYyPzF{MUi5PC=>
KCNR NW\2NoR7SXCxcITvd4l{KGG|c3H5 MmfEglgh|ryP NXP3T2Z1TE2VTx?= NXTiWYhvcW6mdXPld{BieG:ydH;zbZM> NH72docyPzF{MUi5PC=>
GI-CA-N M17oVmFxd3C2b4Ppd{Bie3OjeR?= NGHXSmZ,QCEQvF2= MYrEUXNQ MmDjbY5lfWOnczDhdI9xfG:|aYO= NXvNTZU6OTdzMkG4PVg>
HTLA-230 NXnIWJllSXCxcITvd4l{KGG|c3H5 M1\QR545KM7:TR?= MknaSG1UVw>? NWrI[5NTcW6mdXPld{BieG:ydH;zbZM> NI\aXmUyPzF{MUi5PC=>
SK-N-BE2c M37MOGFxd3C2b4Ppd{Bie3OjeR?= NInXZW9,QCEQvF2= M2LvNmROW09? MYnpcoR2[2W|IHHwc5B1d3Orcx?= MVOxO|EzOTh7OB?=
SY-5Y (N) M2jHeGFxd3C2b4Ppd{Bie3OjeR?= NHvtTmF,QCEQvF2= MnHjSG1UVw>? NWeybmkxcW6mdXPld{BieG:ydH;zbZM> Mn;uNVcyOjF6OUi=
HL60AR NGHoVXVHfW6ldHnvckBie3OjeR?= MonWNVYxKG6P NHHIenZmdmijbnPld{B1cGVibHX2[Yx{KG:oIICyO2tqeDF? M1OzVVE4OzZzMkK1
HL60AR M3mwOWFxd3C2b4Ppd{Bie3OjeR?= M1zYTJ4zODBibl2= MVPpcoR2[2W|IHHwc5B1d3Orcx?= MVmxO|M3OTJ{NR?=
HPAF-II NVL1cXl2U2mwYYPlJIF{e2G7 NYT1c5dMhjFizszN MmfwSG1UVw>? MYrpcohq[mm2czDJS2YuUS2vZXTpZZRm\CC|aXfuZYxtcW6p NIfWfGkyQDR2NUWyNC=>
HPAF-II Mn;MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHLYO|d,OiEQvF2= MU\EUXNQ NFHxWWpqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NYLKTmZQOTh2NEW1NlA>
HPAF-II MVvGeY5kfGmxbjDhd5NigQ>? NG\S[3R,OiEQvF2= MlnmSG1UVw>? MUHpcohq[mm2czDiZZNidCCjbnSgTWdHNUlvbXXkbYF1\WRicHHuZ5Jm[XSrYzDjZY5k\XJiY3XscEBucWe{YYTpc44> NW\5XXRmOTh2NEW1NlA>
TFK-1 NX\XOGlPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHLZdXd,OjVyIH7N M4Tj[mROW09? NXPpUoRNUUN3ME2wMlI3KM7:TR?= Mkm3NlAxPjZ5M{S=
EGI-1 NUHWUYlkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmDyglI2OCCwTR?= NFTL[21FVVOR MkWxTWM2OD1yLkK4JO69VQ>? MUiyNFA3Pjd|NB?=
CC-LP-1 NUXDTmtpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXTNOG5uhjJ3MDDuUS=> MoLaSG1UVw>? M37aOWlEPTB;MD6xOUDPxE1? MmjoNlAxPjZ5M{S=
CC-SW-1 M{O0UWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXfXdW93hjJ3MDDuUS=> M3XaNWROW09? NVHUZoZoUUN3ME2wMlU1KM7:TR?= MmjZNlAxPjZ5M{S=
Sk-ChA-1 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4PDWJ4zPTBibl2= NXHNcJVNTE2VTx?= NGi1SZNKSzVyPUCuNkDPxE1? MorCNlAxPjZ5M{S=
Mz-ChA-1 M3rNWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmrUglI2OCCwTR?= MlfWSG1UVw>? NXLzXWM1UUN3ME2xMlM6KM7:TR?= NWfGSZV2OjByNk[3N|Q>
Mz-ChA-2 M1nXOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1LWd54zPTBibl2= M3PVd2ROW09? MXzJR|UxRTBwN{Og{txO NVSyc5liOjByNk[3N|Q>
ECC-1 MVnLbY5ie2ViYYPzZZk> MWT+NVAh|ryP MULEUXNQ M4\SW4lvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl6JR?= M4DxXFIyOjl3M{O1
Ishikawa MXnLbY5ie2ViYYPzZZk> NWXjOVQ3hjFyIN88US=> MUTEUXNQ MUXpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6OyV? M{LCXFIyOjl3M{O1
USPC-1 MXnLbY5ie2ViYYPzZZk> NVq1SYlQhjFyIN88US=> Mn3pSG1UVw>? M{nNd4lvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDFyMDW= NHS2W24zOTJ7NUOzOS=>
USPC-2 NFHQdJhMcW6jc3WgZZN{[Xl? M3foNJ4yOCEQvF2= NVzZVItvTE2VTx?= MnzrbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQTZn NEKwXXAzOTJ7NUOzOS=>
ECC-1 MmjOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFvQTnZ,OTBizszN MoPHSG1UVw>? NVnabXMy\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NX\lV4ExOjF{OUWzN|U>
Ishikawa M4fXXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoX1glExKM7:TR?= NYi0c3NETE2VTx?= NIDW[Fdl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MXGyNVI6PTN|NR?=
USPC-1 NWG2OGFuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVn+NVAh|ryP NIXBW3BFVVOR NEGy[ZRl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v Mke0NlEzQTV|M{W=
USPC-2 NVHhfWtET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVXsRpc2hjFyIN88US=> M1[3[WROW09? MY\k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MmWzNlEzQTV|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 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
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