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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In DMSO USD 414 In stock
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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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MmLiT4lv[XOnIHHzd4F6 M4DWNp4yOOLCit88US=> M{nGZmROW09? MkL6bY5pcWKrdIOgTWdHNUmUIIfpeIghUUN3MDDv[kAxNjB6NjFCtUAxNjB{ODFOwG0> NID3b2YyPTB3MEmxOS=>
A14 NIfueGpMcW6jc3WgZZN{[Xl? NW\lWIx1hjFy4pEK{txO MVjEUXNQ MULpcohq[mm2czDJcpNTKHerdHigTWM2OCCxZjCyMlMhyrFiMD6xOlMh|ryP MX6xOVA2ODlzNR?=
A431  NF3KOW5McW6jc3WgZZN{[Xl? M3LJUJ4yOOLCit88US=> MoHYSG1UVw>? NIPKZ4tqdmirYnn0d{BJTVJzIIfpeIghUUN3MDDv[kA,OTBizszN MljwNVUxPTB7MUW=
A31  MYHLbY5ie2ViYYPzZZk> NV3VbIZKhjFy4pEK{txO MoP1SG1UVw>? NH3tbZJqdmirYnn0d{BRTEeIUjD3bZRpKEmFNUCgc4YhRjFyIN88US=> MXKxOVA2ODlzNR?=
GIST882 NHmwZ2tMcW6jc3WgZZN{[Xl? M{Hq[J4yOOLCit88US=> NX\xdHNZTE2VTx?= Mmj0bY5pcWKrdIOgZ{1McXRid3n0bEBKSzVyIH;mJF42KM7:TR?= NEjNdYoyPTB3MEmxOS=>
32D-Bcr-Abl M4nzfGtqdmG|ZTDhd5NigQ>? NV7rXZRFhjFy4pEK{txO MoDOSG1UVw>? M3LPSYlvcGmkaYTzJGJkei2DYnygdFIyOCC5aYToJGlEPTBib3[gQlExKM7:TR?= Mn3oNVUxPTB7MUW=
MCF-7  NX7rSWRjS3m2b4jpZ4l1gSCjc4PhfS=> M{LjN2ROW09? MV;JR|UxRTFwNkSg{txO Mn7MNVUxPTB7MUW=
NWT-21 M1n3fWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmCzSG1UVw>? MlL3TWM2OD1yLkG2N{DPxE1? NV7sOGdSOTVyNUC5NVU>
TC-71 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHjwNGZ,OSEQvF2= Mn3WSG1UVw>? NIPKRpVqdmirYnn0d{BqdnO3bHnuMYxqc2ViZ4Lve5RpKG[jY4Tvdk1K6oDVbXXkbYF1\WRiZ4Lve5Rp NGrDXIwyPTh4N{O4Oi=>
TC-71 NXTGZmRVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXz5TXRWhjgkgJtOwG0> MUDEUXNQ NEn4eoNKSzVyPECuOUDPxE1? NUL0dIcxOTV6NkezPFY>
Saos-2 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1\jZp446oDMzszN M4LqbGROW09? NW[xeHNnUUN3MEyzJO69VQ>? NEnVeG8yPTh4N{O4Oi=>
U-2OS NUDJXXk4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NID3UpJ,P+LCit88US=> M4\2dmROW09? MVTJR|UxRDBwNTFOwG0> NFXyVHUyPTh4N{O4Oi=>
SK-ES-1 M3PsTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnvqglfjiIsQvF2= MnHPSG1UVw>? MUfJR|UxRDBwNTFOwG0> NEDxNIoyPTh4N{O4Oi=>
SK-N-MC M{\TPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX;+O-KBks7:TR?= M1:0XmROW09? MVTJR|UxRDBwNTFOwG0> NYmwUYdLOTV6NkezPFY>
RD-ES M1HucWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlrUglfjiIsQvF2= M1K1ZmROW09? NXjNcoIxUUN3MEywMlUh|ryP NEDyTmsyPTh4N{O4Oi=>
SJ-Rh 30 NGTFOWtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MY\+O-KBks7:TR?= MojRSG1UVw>? NVrEeGExUUN3MEywMlUh|ryP M17GXVE2QDZ5M{i2
SJ-Rh 4 M1XpUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXH+O-KBks7:TR?= NU\MNXVsTE2VTx?= NELGVY9KSzVyPECuOUDPxE1? NYi0SIVHOTV6NkezPFY>
6647 NIXrbo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEC1clF,P+LCit88US=> MXrEUXNQ M2ezeWlEPTB:MD61JO69VQ>? MnfQNVU5Pjd|OE[=
SARG NXPLR2UyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mo[xglfjiIsQvF2= M1iyTWROW09? NGnFWGVKSzVyPEOg{txO M{jGUlE2QDZ5M{i2
MOS MkXvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEnINnV,P+LCit88US=> MUHEUXNQ M33SRWlEPTB:NDFOwG0> Mn3jNVU5Pjd|OE[=
IOR/OS7 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXy3XGVYhjgkgJtOwG0> NUXz[o4yTE2VTx?= MVjJR|UxRDFizszN NYPiXXFXOTV6NkezPFY>
IOR/OS9 Mn;iS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUGxUIRnhjgkgJtOwG0> NXnpSFhHTE2VTx?= NV\VdnZCUUN3MEy2JO69VQ>? M4DaUVE2QDZ5M{i2
IOR/OS10 MmDzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYi1cZgyhjgkgJtOwG0> NHfPT4VFVVOR Mm\2TWM2ODx3IN88US=> M{XrWVE2QDZ5M{i2
IOR/OS14 NGjjc4dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWH+O-KBks7:TR?= MoLqSG1UVw>? NXLtfZJbUUN3MEy0JO69VQ>? MnHxNVU5Pjd|OE[=
LAP35 M3f0WWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYixN5hIhjgkgJtOwG0> NFftNYRFVVOR MWrJR|UxRDBwNTFOwG0> M{\afFE2QDZ5M{i2
IOR/BRZ NF\jZW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPQb5B,P+LCit88US=> NF35Z4tFVVOR NX31R2syUUN3MEywMlUh|ryP M4O1d|E2QDZ5M{i2
IOR/CAR M4P0b2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVX+O-KBks7:TR?= Ml\JSG1UVw>? NHnaVmpKSzVyPEGg{txO NF3UfpAyPTh4N{O4Oi=>
IOR/NGR M{T1Zmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIf4fJJ,P+LCit88US=> M{nqeGROW09? NVfjdXBJUUN3MEywMlUh|ryP NVPVUWlkOTV6NkezPFY>
IOR/RCH NWrjXoVoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVr0[JVyhjgkgJtOwG0> NH30bWtFVVOR M{XIbWlEPTB:MD61JO69VQ>? M3\QRVE2QDZ5M{i2
RMZ-RC2 NFP0[FlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV7+O-KBks7:TR?= NV3PNlNnTE2VTx?= NVvBfpIyUUN3MEywMlUh|ryP NHKzbm0yPTh4N{O4Oi=>
CCA MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3X2UZ446oDMzszN NWPJOpF6TE2VTx?= NFruSlRKSzVyPEKg{txO M1fFTVE2QDZ5M{i2
RD/18 NHHoS5FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFzlenR,P+LCit88US=> MVXEUXNQ NYD5U445UUN3MEy0JO69VQ>? MVmxOVg3PzN6Nh?=
OVCAR-3 MlXnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVHrbo5IhjF34pEK{txO M4PDd2ROW09? NV;TS4pncW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v Mmm5NVY{ODB6MkC=
OVCAR-4 NXzibno6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVLaXXdshjF34pEK{txO NFHrbmhFVVOR MWfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MUGxOlMxODh{MB?=
OVCAR-3 Mo\aRZBweHSxc3nzJIF{e2G7 MWP+NVXjiIsQvF2= MWLEUXNQ NWiyWIRHcW6mdXPld{BieG:ydH;zbZM> MX:xOlMxODh{MB?=
OVCAR-4 NFK4V4hCeG:ydH;zbZMh[XO|YYm= M{j0Xp4yPeLCit88US=> NF\4VoJFVVOR MonpbY5lfWOnczDhdI9xfG:|aYO= NX36RlVoOTZ|MEC4NlA>
OVCAR-3 NU\GclV7TnWwY4Tpc44h[XO|YYm= M1K2[J4yPeLCit88US=> MlvoSG1UVw>? NWfXXGhXTGWlcnXhd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= MmLUNVY{ODB6MkC=
Huh-7 NY\ONlR5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGruSVh,OTEkgJtOwG0> NUfuZYxWTE2VTx?= NXnOTolRUUN3ME2xMlQh|ryP NX3QSYc3OTZ3M{C3N|Q>
Hep-G2 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIOwVm9,OTEkgJtOwG0> MXjEUXNQ NVj1VoM2UUN3ME2xMlgh|ryP NEe4bWoyPjV|MEezOC=>
Hep-3B NIn5NHNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXEOHRIhjFy4pEK{txO MVnEUXNQ MlHCTWM2OD1zLkmg{txO NUjGdnZIOTZ3M{C3N|Q>
SK-Hep-1 NUXlbYNsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGrzR2d,OTEkgJtOwG0> MoXWSG1UVw>? NGfUPGNKSzVyPU[uPUDPxE1? NWHXVlJTOTZ3M{C3N|Q>
Huh-7 MXXGeY5kfGmxbjDhd5NigQ>? MX7+NVDjiIsQvF2= M{C2NmROW09? M4G3XWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NUfiVJptOTZ3M{C3N|Q>
Hep-G2 M3TFZ2Z2dmO2aX;uJIF{e2G7 MUf+NVDjiIsQvF2= NVfwV3NHTE2VTx?= MoKyTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MomxNVY2OzB5M{S=
SK-Hep-1 M3fGOGZ2dmO2aX;uJIF{e2G7 NVLsbmhZhjFy4pEK{txO MW\EUXNQ NV7ZUYxCUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NXPQOJc5OTZ3M{C3N|Q>
BON NWDuUXAxU2mwYYPlJIF{e2G7 M1fEO543KM7:TR?= MlHsSG1UVw>? M3rIXYlv\HWlZYOg[IVxcG:|cHjvdplt[XSrb36gc4YhUUeILUHS NYTQTXFYOTZ4MEGyPFQ>
BON NF3sZ4tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnvWglEx6oDMzszN M2HXPGROW09? M{X2[mlEPTB;Nj62JO69VQ>? M3LXd|E3PjBzMki0
CM M1nJXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mm\yglXjiIsQvF2= NH;nVJlFVVOR MVLJR|UxRTNwMzFOwG0> NInWfnoyPjZyMUK4OC=>
BON MXfGeY5kfGmxbjDhd5NigQ>? MUP+O{426oDMzszN MYjEUXNQ M1;qRYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NHexblkyPjZyMUK4OC=>
CM M4qzUmZ2dmO2aX;uJIF{e2G7 M2j2fp426oDMzszN MoCySG1UVw>? M4\Sdolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= Mm\HNVY3ODF{OES=
BON MlnpRZBweHSxc3nzJIF{e2G7 NWezOZhphjdwNfMAju69VQ>? NYr4SnlQTE2VTx?= MXXpcoR2[2W|IFHwc5B1d3Orcx?= Mn73NVY3ODF{OES=
CM MofpRZBweHSxc3nzJIF{e2G7 MUT+OgKBks7:TR?= M4G1UWROW09? NXfEVJJWcW6mdXPld{BCeG:ydH;zbZM> MVyxOlYxOTJ6NB?=
HT-29 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoDoglEx6oDMzszN M3WzRmROW09? M2\MZmlEPTB;MT63JO69VQ>? MmPnNVcxODdyMUW=
HCT-116 NH;iWG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NI[yS4J,OTEkgJtOwG0> NWrid2Q6TE2VTx?= NEniS|lKSzVyPUKuOUDPxE1? MVqxO|AxPzBzNR?=
primary colorectal cancer cells MX;GeY5kfGmxbjDhd5NigQ>? M{jTe5426oDMzszN NV:2[YhNTE2VTx?= NVHrV|RI[Wy2ZYLzJJRp\SCvb4LwbI9td2e7IH;mJJRp\SC{ZX3hbY5qdmdiY3XscJM> MXqxO|AxPzBzNR?=
HTLA-230 MWXGeY5kfGmxbjDhd5NigQ>? NYn3cpVYhjhizszN M2jmVGROW09? MVHpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MknmNVcyOjF6OUi=
KCNR NGLXVHpHfW6ldHnvckBie3OjeR?= NVz3V4R7hjhizszN M4rDUmROW09? MlHhbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 MVixO|EzOTh7OB?=
SK-N-BE2c MX\GeY5kfGmxbjDhd5NigQ>? NWH3TopbhjhizszN NFvHTXNFVVOR NH\pZlZqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> M4PIdFE4OTJzOEm4
SK-N-BE MnnvSpVv[3Srb36gZZN{[Xl? MkW0glgh|ryP M4rSdmROW09? MVnpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= MnTENVcyOjF6OUi=
LAN-5 MlfNSpVv[3Srb36gZZN{[Xl? MVj+PEDPxE1? MlfwSG1UVw>? NH;MTppqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NVzxS|h7OTdzMkG4PVg>
GI-CA-N MWDGeY5kfGmxbjDhd5NigQ>? MVT+PEDPxE1? NG\r[25FVVOR NFLobHFqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> NH3HUlgyPzF{MUi5PC=>
SH-EP MWfGeY5kfGmxbjDhd5NigQ>? NYDQWY5xhjhizszN MUDEUXNQ M3HibolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MkPZNVcyOjF6OUi=
SK-N-AS Ml2zSpVv[3Srb36gZZN{[Xl? NXXHWJBThjhizszN MXPEUXNQ MknabY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NH\tZnAyPzF{MUi5PC=>
RN-GA Mnq4SpVv[3Srb36gZZN{[Xl? MX;+PEDPxE1? NY\Tbo9qTE2VTx?= MmP1bY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NVPYXHhpOTdzMkG4PVg>
SY-5Y(N) MlnMSpVv[3Srb36gZZN{[Xl? MX\+PEDPxE1? NVLlPXFnTE2VTx?= NX3wXWlEcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 M{DOV|E4OTJzOEm4
GI-CA-N NXTmSXFGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV;zTphNhjhizszN NWKzclhHTE2VTx?= M{jUOWlEPTB;IE[uPEDPxE1? NU\EXFdnOTdzMkG4PVg>
SH-EP MmjTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUT+PEDPxE1? M{XJTmROW09? NU\2XGxtUUN3ME2gN{DPxE1? M4juPFE4OTJzOEm4
HTLA-230 NGWxXHJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MofXglgh|ryP M3jMcmROW09? NXK4NVBCUUN3ME2gNE42KM7:TR?= NIe0fYMyPzF{MUi5PC=>
SK-N-BE2c MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVj+PEDPxE1? MWjEUXNQ Mlr6TWM2OD1iMT6xJO69VQ>? Mo\GNVcyOjF6OUi=
SK-N-BE2 NUW5O|JYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHr1fFl,QCEQvF2= NXvFTZBNTE2VTx?= NXmxOWpjUUN3ME2gN{DPxE1? NUj4XZRyOTdzMkG4PVg>
SY-5Y (N) MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NE\yWmd,QCEQvF2= M1XWVGROW09? NEDOTVZKSzVyPTCyMlQh|ryP M4LzR|E4OTJzOEm4
LAN-5 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYq2XFdHhjhizszN NWjkbYhVTE2VTx?= MWfJR|UxRSByLkSg{txO MoLGNVcyOjF6OUi=
KCNR MljjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXizS49FhjhizszN MXfEUXNQ MXjJR|UxRSByLkSg{txO M37zW|E4OTJzOEm4
RN-GA MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFfGdWx,QCEQvF2= NIjOVGtFVVOR M4n4T2lEPTB;IEGuN{DPxE1? MYGxO|EzOTh7OB?=
SK-N-AS M33HeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlrXglgh|ryP NXX5cnFuTE2VTx?= MUjpcoR2[2W|IHHwc5B1d3Orcx?= Mn\YNVcyOjF6OUi=
KCNR M374TmFxd3C2b4Ppd{Bie3OjeR?= MYL+PEDPxE1? M{e2eGROW09? MoP3bY5lfWOnczDhdI9xfG:|aYO= M1PJc|E4OTJzOEm4
GI-CA-N MYDBdI9xfG:|aYOgZZN{[Xl? Mnfoglgh|ryP MVnEUXNQ MVzpcoR2[2W|IHHwc5B1d3Orcx?= NV:yV|lxOTdzMkG4PVg>
HTLA-230 NHLQdZJCeG:ydH;zbZMh[XO|YYm= MX7+PEDPxE1? NHOyVWlFVVOR NFLRSW1qdmS3Y3XzJIFxd3C2b4Ppdy=> M165fVE4OTJzOEm4
SK-N-BE2c MVPBdI9xfG:|aYOgZZN{[Xl? Ml3nglgh|ryP NWDvboJDTE2VTx?= NGTDUHdqdmS3Y3XzJIFxd3C2b4Ppdy=> MlLONVcyOjF6OUi=
SY-5Y (N) NV\hTGNVSXCxcITvd4l{KGG|c3H5 NGfB[Vh,QCEQvF2= M2jTeWROW09? NFnXUJJqdmS3Y3XzJIFxd3C2b4Ppdy=> M4TsPFE4OTJzOEm4
HL60AR NIfrT4dHfW6ldHnvckBie3OjeR?= MmDzNVYxKG6P MVzlcohidmOnczD0bIUhdGW4ZXzzJI9nKHB{N1vpdFE> NFPY[IgyPzN4MUKyOS=>
HL60AR MoLtRZBweHSxc3nzJIF{e2G7 MWP+NlAxKG6P Mo\JbY5lfWOnczDhdI9xfG:|aYO= MoHINVc{PjF{MkW=
HPAF-II MUTLbY5ie2ViYYPzZZk> MljIglEh|ryP Mlj4SG1UVw>? MoTFbY5pcWKrdIOgTWdHNUlvbXXkbYF1\WRic3nncoFtdGmwZx?= NH7kU3cyQDR2NUWyNC=>
HPAF-II M{TaWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXj+NkDPxE1? NHfPdo9FVVOR MVPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M4\DdFE5PDR3NUKw
HPAF-II NI[1SYRHfW6ldHnvckBie3OjeR?= MYn+NkDPxE1? NHnYdnNFVVOR M2rzUYlvcGmkaYTzJIJie2GuIHHu[EBKT0ZvST3t[YRq[XSnZDDwZY5kemWjdHnjJINidmOncjDj[YxtKG2rZ4LheIlwdg>? NEfOPFYyQDR2NUWyNC=>
TFK-1 MneyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mly5glI2OCCwTR?= MkfCSG1UVw>? Mmi3TWM2OD1yLkK2JO69VQ>? MYeyNFA3Pjd|NB?=
EGI-1 M{jk[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX3QU|dvhjJ3MDDuUS=> M3jLWGROW09? M{jUcWlEPTB;MD6yPEDPxE1? Mmm4NlAxPjZ5M{S=
CC-LP-1 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWL0NI9uhjJ3MDDuUS=> NV;sUmpOTE2VTx?= MVvJR|UxRTBwMUWg{txO NEDGSpkzODB4NkezOC=>
CC-SW-1 MkHyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3jrc54zPTBibl2= Mn7nSG1UVw>? NWLqPI1[UUN3ME2wMlU1KM7:TR?= NX\DXIpbOjByNk[3N|Q>
Sk-ChA-1 NVHGTlczT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWX+NlUxKG6P MnG4SG1UVw>? NFLZbFJKSzVyPUCuNkDPxE1? M2jJe|IxODZ4N{O0
Mz-ChA-1 M4fuWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1rJd54zPTBibl2= M1HlRWROW09? MX;JR|UxRTFwM{mg{txO MkDHNlAxPjZ5M{S=
Mz-ChA-2 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkTIglI2OCCwTR?= NGHtOXVFVVOR NWXUe2NLUUN3ME2wMlc{KM7:TR?= MmDiNlAxPjZ5M{S=
ECC-1 NEj1bJNMcW6jc3WgZZN{[Xl? M4rJdp4yOCEQvF2= MkPmSG1UVw>? MVLpcohq[mm2czDJS2YuUVJiYXP0bZZifGmxbjDifUA6QCV? NVr4dGZUOjF{OUWzN|U>
Ishikawa Ml[zT4lv[XOnIHHzd4F6 NWnoOFJshjFyIN88US=> MV;EUXNQ MnLubY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQTNn NEPSWo0zOTJ7NUOzOS=>
USPC-1 Ml7aT4lv[XOnIHHzd4F6 MWL+NVAh|ryP NIHYfoxFVVOR NHnyN3RqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSBzMECl MUKyNVI6PTN|NR?=
USPC-2 NInhTmpMcW6jc3WgZZN{[Xl? MnLkglExKM7:TR?= MWjEUXNQ NWnSSoNqcW6qaXLpeJMhUUeILVnSJIFkfGm4YYTpc44h[nliOU[l NXXjcWJ3OjF{OUWzN|U>
ECC-1 NV;wNnZET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NG\qVHd,OTBizszN NGfBZZFFVVOR MWjk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u NGfMZnAzOTJ7NUOzOS=>
Ishikawa NIn0U3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4DpRZ4yOCEQvF2= MYLEUXNQ NFTYVnll\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v M4\ocFIyOjl3M{O1
USPC-1 MkTmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mm\JglExKM7:TR?= NVLycHRoTE2VTx?= NIC5[nRl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MVGyNVI6PTN|NR?=
USPC-2 M333SWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHewXml,OTBizszN M3rIb2ROW09? M3roRoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NXPxd2pFOjF{OUWzN|U>

... 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