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 M17YUmtqdmG|ZTDhd5NigQ>? NFLTXpR,OTEkgJtOwG0> NF3UeYZFVVOR NYjNN29IcW6qaXLpeJMhUUeILVnSJJdqfGhiSVO1NEBw\iByLkC4OkDDuSByLkCyPEDPxE1? M4LRXFE2ODVyOUG1
A14 MUnLbY5ie2ViYYPzZZk> MlG2glEx6oDMzszN MkL1SG1UVw>? MnjCbY5pcWKrdIOgTY5{WiC5aYToJGlEPTBib3[gNk4{KMLzIECuNVY{KM7:TR?= Ml\WNVUxPTB7MUW=
A431  NWHmS4VvU2mwYYPlJIF{e2G7 MX\+NVDjiIsQvF2= MofKSG1UVw>? NUHIeGJscW6qaXLpeJMhUEWUMTD3bZRpKEmFNUCgc4YhRjFyIN88US=> NGC2SWcyPTB3MEmxOS=>
A31  MlLYT4lv[XOnIHHzd4F6 M3z3dp4yOOLCit88US=> MofUSG1UVw>? M2XXdIlvcGmkaYTzJHBFT0[UIIfpeIghUUN3MDDv[kA,OTBizszN MkW3NVUxPTB7MUW=
GIST882 M2rjWWtqdmG|ZTDhd5NigQ>? NYHxXmw{hjFy4pEK{txO NFrEWHBFVVOR MWrpcohq[mm2czDjMWtqfCC5aYToJGlEPTBib3[gQlUh|ryP M2jxNlE2ODVyOUG1
32D-Bcr-Abl MoLGT4lv[XOnIHHzd4F6 NXrpd3oxhjFy4pEK{txO Mn7sSG1UVw>? M2n3XolvcGmkaYTzJGJkei2DYnygdFIyOCC5aYToJGlEPTBib3[gQlExKM7:TR?= M1P3VlE2ODVyOUG1
MCF-7  NXH4fm93S3m2b4jpZ4l1gSCjc4PhfS=> NETNTlVFVVOR NF3ZcJhKSzVyPUGuOlQh|ryP NUW3Z4dUOTVyNUC5NVU>
NWT-21 NXnkUVFQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3TvVGROW09? NYSxb5l3UUN3ME2wMlE3OyEQvF2= Mo\qNVUxPTB7MUW=
TC-71 NXjidXkyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnuyglEh|ryP M4rRN2ROW09? MXvpcohq[mm2czDpcpN2dGmwLXzpb4Uh\3Kxd4ToJIZi[3Sxcj3J5qCUdWWmaXH0[YQh\3Kxd4To M{PHSVE2QDZ5M{i2
TC-71 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXX+O-KBks7:TR?= MmDvSG1UVw>? NYTM[pRZUUN3MEywMlUh|ryP M4jGWVE2QDZ5M{i2
Saos-2 NV:4ZZdsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX2xdJEyhjgkgJtOwG0> M2\oNWROW09? MYrJR|UxRDNizszN MXOxOVg3PzN6Nh?=
U-2OS MkPlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVL+O-KBks7:TR?= NHvJdW9FVVOR MlzMTWM2ODxyLkWg{txO MUWxOVg3PzN6Nh?=
SK-ES-1 NYfpfmlZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUX+O-KBks7:TR?= M1rZbWROW09? MmrvTWM2ODxyLkWg{txO NUnMR5lZOTV6NkezPFY>
SK-N-MC M13DVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVn+O-KBks7:TR?= M3i2UGROW09? M2X5emlEPTB:MD61JO69VQ>? NV\xV2ZROTV6NkezPFY>
RD-ES MlS2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIqzNWF,P+LCit88US=> NVzze|N7TE2VTx?= MkXqTWM2ODxyLkWg{txO M{TrRVE2QDZ5M{i2
SJ-Rh 30 NEThRodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEXPU2x,P+LCit88US=> MoLLSG1UVw>? M2jP[WlEPTB:MD61JO69VQ>? MmHVNVU5Pjd|OE[=
SJ-Rh 4 NIjr[YFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFv0TWl,P+LCit88US=> NV\aZlNlTE2VTx?= NVn3O4Y{UUN3MEywMlUh|ryP M2i3VFE2QDZ5M{i2
6647 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4XaSp446oDMzszN NXz1foRETE2VTx?= M13ZdWlEPTB:MD61JO69VQ>? M1O0PVE2QDZ5M{i2
SARG MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlfFglfjiIsQvF2= NXzBZm05TE2VTx?= NX:2[2M6UUN3MEyzJO69VQ>? MUexOVg3PzN6Nh?=
MOS MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYT+O-KBks7:TR?= NYq1XHUzTE2VTx?= MWDJR|UxRDRizszN MljaNVU5Pjd|OE[=
IOR/OS7 NU\xNFk5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXrBV41mhjgkgJtOwG0> NX\jZo9ETE2VTx?= NHnVXmpKSzVyPEGg{txO NUKwOYR1OTV6NkezPFY>
IOR/OS9 NEe2VYZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mk\IglfjiIsQvF2= NF\2ZYtFVVOR NEDmcZVKSzVyPE[g{txO Mnj2NVU5Pjd|OE[=
IOR/OS10 M4LWVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUL+O-KBks7:TR?= MomzSG1UVw>? NFezSIpKSzVyPEWg{txO NYezbldrOTV6NkezPFY>
IOR/OS14 NX7ReYV3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX;We3duhjgkgJtOwG0> MYnEUXNQ NGnTUllKSzVyPESg{txO MoXnNVU5Pjd|OE[=
LAP35 NX7Q[pZ7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWGwUIpRhjgkgJtOwG0> NGq2OXhFVVOR NFXFUWVKSzVyPECuOUDPxE1? Mm[0NVU5Pjd|OE[=
IOR/BRZ Moe2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkThglfjiIsQvF2= NXLPfnI2TE2VTx?= Ml3ZTWM2ODxyLkWg{txO MWSxOVg3PzN6Nh?=
IOR/CAR MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlzVglfjiIsQvF2= M4j3[mROW09? NEHjcWlKSzVyPEGg{txO NV7FRVlNOTV6NkezPFY>
IOR/NGR M2ny[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{TSWZ446oDMzszN M13MSmROW09? MormTWM2ODxyLkWg{txO NUi4cIxDOTV6NkezPFY>
IOR/RCH NGTGW3hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnPEglfjiIsQvF2= M4T1OmROW09? NVvJe|V4UUN3MEywMlUh|ryP NWLyZphROTV6NkezPFY>
RMZ-RC2 M3;QbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mnq1glfjiIsQvF2= NWTX[3ZITE2VTx?= NH;CcGpKSzVyPECuOUDPxE1? NIjFcnQyPTh4N{O4Oi=>
CCA MlPsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV3+O-KBks7:TR?= NHzqNYpFVVOR M2rNZmlEPTB:MjFOwG0> NGPHPHUyPTh4N{O4Oi=>
RD/18 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIDZT|Z,P+LCit88US=> MlGwSG1UVw>? NV70[VJOUUN3MEy0JO69VQ>? MoXpNVU5Pjd|OE[=
OVCAR-3 NEfCb4lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MY\+NVXjiIsQvF2= MVzEUXNQ MVrpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M4e0WFE3OzByOEKw
OVCAR-4 NYf5fGhST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFewbGd,OTYkgJtOwG0> Mk\KSG1UVw>? MmTRbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NH\z[3QyPjNyMEiyNC=>
OVCAR-3 M13jdWFxd3C2b4Ppd{Bie3OjeR?= MmexglE26oDMzszN NWTJNXdlTE2VTx?= MXnpcoR2[2W|IHHwc5B1d3Orcx?= NFHNZWkyPjNyMEiyNC=>
OVCAR-4 NVno[JNpSXCxcITvd4l{KGG|c3H5 NHvFUm1,OTYkgJtOwG0> NXT3b4RXTE2VTx?= MXTpcoR2[2W|IHHwc5B1d3Orcx?= MVKxOlMxODh{MB?=
OVCAR-3 MlLsSpVv[3Srb36gZZN{[Xl? MVH+NVXjiIsQvF2= MX3EUXNQ MlnaSIVkemWjc3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? NVH4XY5NOTZ|MEC4NlA>
Huh-7 MmjSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVq1bYhmhjFy4pEK{txO M3fWOmROW09? NVXoWm97UUN3ME2xMlQh|ryP M2LvUFE3PTNyN{O0
Hep-G2 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1LH[J4yOOLCit88US=> NEPHWIFFVVOR MlTjTWM2OD1zLkig{txO M4HmPVE3PTNyN{O0
Hep-3B MlOzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHfyZpZ,OTEkgJtOwG0> MXnEUXNQ NX7US4ZbUUN3ME2xMlkh|ryP NIjVSlQyPjV|MEezOC=>
SK-Hep-1 NYPWU4lCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWX1NpV5hjFy4pEK{txO MkLoSG1UVw>? MUnJR|UxRTZwOTFOwG0> M{fzb|E3PTNyN{O0
Huh-7 NYTZdlZYTnWwY4Tpc44h[XO|YYm= M33xcp4yOOLCit88US=> NUC4dJNWTE2VTx?= NEC0dFFKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MmD5NVY2OzB5M{S=
Hep-G2 M1TUc2Z2dmO2aX;uJIF{e2G7 MX\+NVDjiIsQvF2= M{e4[mROW09? MXjJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MU[xOlU{ODd|NB?=
SK-Hep-1 NYfu[osyTnWwY4Tpc44h[XO|YYm= NEW5Xnd,OTEkgJtOwG0> M{TyeGROW09? MYLJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NIfaN2oyPjV|MEezOC=>
BON NELHUHNMcW6jc3WgZZN{[Xl? NEO0VHJ,PiEQvF2= NYfTW2MzTE2VTx?= NWP1NmpGcW6mdXPld{Bl\XCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXI> NXHyOod2OTZ4MEGyPFQ>
BON MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NInF[Ih,OTEkgJtOwG0> Ml[4SG1UVw>? NF7FNIFKSzVyPU[uOkDPxE1? M1P3U|E3PjBzMki0
CM NYHuNlVxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3TWbZ426oDMzszN MnfSSG1UVw>? MlHPTWM2OD1|LkOg{txO NVXHVmhiOTZ4MEGyPFQ>
BON MXnGeY5kfGmxbjDhd5NigQ>? NXLub2o1hjdwNfMAju69VQ>? MX\EUXNQ M1TjTIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M1fNZ|E3PjBzMki0
CM NUHQRlBHTnWwY4Tpc44h[XO|YYm= Ml;1glXjiIsQvF2= M3y0XmROW09? NH3a[GRqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M4ry[lE3PjBzMki0
BON NXu5U3F5SXCxcITvd4l{KGG|c3H5 MnH4glcvPeLCit88US=> NHLNXopFVVOR MWPpcoR2[2W|IFHwc5B1d3Orcx?= NIX0VooyPjZyMUK4OC=>
CM NV6wSpFrSXCxcITvd4l{KGG|c3H5 NFXwPGx,PeLCit88US=> M1jmOWROW09? MofWbY5lfWOnczDBdI9xfG:|aYO= NFzhVogyPjZyMUK4OC=>
HT-29 M2Gx[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mln0glEx6oDMzszN NXG2UYlOTE2VTx?= MXrJR|UxRTFwNzFOwG0> MX:xO|AxPzBzNR?=
HCT-116 NIT3PHFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkPHglEx6oDMzszN NWfxSpdmTE2VTx?= MnfYTWM2OD1{LkWg{txO MnqyNVcxODdyMUW=
primary colorectal cancer cells M3niWmZ2dmO2aX;uJIF{e2G7 M2Tu[5426oDMzszN NXjn[W5iTE2VTx?= M{DDOIFtfGW{czD0bIUhdW:{cHjvcI9ogSCxZjD0bIUhemWvYXnubY5oKGOnbHzz M1z3elE4ODB5MEG1
HTLA-230 MlLYSpVv[3Srb36gZZN{[Xl? M3uyNZ45KM7:TR?= NFj4d5VFVVOR NI\pOoxqdmirYnn0d{BKT0ZvSVmtcYVlcWG2ZXSgd5RqdXWuYYTpc44hd2ZiSVfGMWlTKGGwZDDBb5Q> MXSxO|EzOTh7OB?=
KCNR MnT0SpVv[3Srb36gZZN{[Xl? NGOxdpJ,QCEQvF2= MorySG1UVw>? MX3pcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= M4ezV|E4OTJzOEm4
SK-N-BE2c M4DNXmZ2dmO2aX;uJIF{e2G7 NEXOdYR,QCEQvF2= MWPEUXNQ MXXpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NGn0UGsyPzF{MUi5PC=>
SK-N-BE NX33cG5wTnWwY4Tpc44h[XO|YYm= MV7+PEDPxE1? Mly1SG1UVw>? M33wfIlvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> MmP0NVcyOjF6OUi=
LAN-5 M4P0UWZ2dmO2aX;uJIF{e2G7 M3;VWJ45KM7:TR?= NXiyfWFOTE2VTx?= MlWzbY5pcWKrdIOgTWdHNUmLLX3l[IlifGWmIIP0bY12dGG2aX;uJI9nKEmJRj3JVkBidmRiQXv0 NIXBNVQyPzF{MUi5PC=>
GI-CA-N NXKwZXp{TnWwY4Tpc44h[XO|YYm= NIPy[Ih,QCEQvF2= M4DFS2ROW09? NWDBdI1tcW6qaXLpeJMhUUeILVnJMY1m\GmjdHXkJJN1cW23bHH0bY9vKG:oIFnHSk1KWiCjbnSgRYt1 M3vLOlE4OTJzOEm4
SH-EP NFXWZ4VHfW6ldHnvckBie3OjeR?= NVv4fmYyhjhizszN MXTEUXNQ MYjpcohq[mm2czDJS2YuUUlvbXXkbYF1\WRic4TpcZVt[XSrb36gc4YhUUeILVnSJIFv\CCDa4S= NX3wR|g1OTdzMkG4PVg>
SK-N-AS MUjGeY5kfGmxbjDhd5NigQ>? MWH+PEDPxE1? NY\GRVYzTE2VTx?= M2TCb4lvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NV7sW|RUOTdzMkG4PVg>
RN-GA NUfHdGJKTnWwY4Tpc44h[XO|YYm= NGPCS2x,QCEQvF2= MULEUXNQ M2HIcIlvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> NF3zZVgyPzF{MUi5PC=>
SY-5Y(N) M{LKN2Z2dmO2aX;uJIF{e2G7 MnLLglgh|ryP NYLjTHUxTE2VTx?= M2XPUolvcGmkaYTzJGlITi2LST3t[YRq[XSnZDDzeIlufWyjdHnvckBw\iCLR1[tTXIh[W6mIFHreC=> M4j0R|E4OTJzOEm4
GI-CA-N M1nIcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlO3glgh|ryP NYPRcItwTE2VTx?= M3HQbGlEPTB;IE[uPEDPxE1? MXmxO|EzOTh7OB?=
SH-EP MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml3pglgh|ryP NYHEbGk6TE2VTx?= M4[5WGlEPTB;IEOg{txO NYHJR5NIOTdzMkG4PVg>
HTLA-230 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUT+PEDPxE1? MULEUXNQ MYjJR|UxRSByLkWg{txO M3HVblE4OTJzOEm4
SK-N-BE2c MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mk\Rglgh|ryP NILCdY5FVVOR MWXJR|UxRSBzLkGg{txO MnPuNVcyOjF6OUi=
SK-N-BE2 NIm3UoJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXn6OYZLhjhizszN NX3sbIhHTE2VTx?= Mnm3TWM2OD1iMzFOwG0> NUjod|Y4OTdzMkG4PVg>
SY-5Y (N) MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkHJglgh|ryP NF\YUIZFVVOR M1LHeWlEPTB;IEKuOEDPxE1? MmrYNVcyOjF6OUi=
LAN-5 NFnMb5BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnTJglgh|ryP NWPucXFwTE2VTx?= MmPGTWM2OD1iMD60JO69VQ>? MYWxO|EzOTh7OB?=
KCNR MlTpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{LQVp45KM7:TR?= MVnEUXNQ MmfLTWM2OD1iMD60JO69VQ>? MWixO|EzOTh7OB?=
RN-GA Mk\JS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2r2e545KM7:TR?= NXLCXnBrTE2VTx?= M3nUNGlEPTB;IEGuN{DPxE1? MVuxO|EzOTh7OB?=
SK-N-AS NH;BepZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGTVSY5,QCEQvF2= Mn\vSG1UVw>? NEHORXZqdmS3Y3XzJIFxd3C2b4Ppdy=> MlWwNVcyOjF6OUi=
KCNR MX7BdI9xfG:|aYOgZZN{[Xl? NIP3[mt,QCEQvF2= MlzZSG1UVw>? NIjtdXJqdmS3Y3XzJIFxd3C2b4Ppdy=> M1rzPFE4OTJzOEm4
GI-CA-N NVLMT45NSXCxcITvd4l{KGG|c3H5 M{DWNJ45KM7:TR?= M2jzNGROW09? M1\xbIlv\HWlZYOgZZBweHSxc3nz NFjKZZkyPzF{MUi5PC=>
HTLA-230 NXPXTXk2SXCxcITvd4l{KGG|c3H5 MnH0glgh|ryP NUWzO4NtTE2VTx?= NWD6cJdxcW6mdXPld{BieG:ydH;zbZM> MVuxO|EzOTh7OB?=
SK-N-BE2c MnHoRZBweHSxc3nzJIF{e2G7 MmLQglgh|ryP NXLvSmJJTE2VTx?= NXPabop7cW6mdXPld{BieG:ydH;zbZM> NFfXR3YyPzF{MUi5PC=>
SY-5Y (N) MYHBdI9xfG:|aYOgZZN{[Xl? NYn5[ZNvhjhizszN NVvYS3JPTE2VTx?= Mmf5bY5lfWOnczDhdI9xfG:|aYO= MV2xO|EzOTh7OB?=
HL60AR NULmT4tbTnWwY4Tpc44h[XO|YYm= Mn3LNVYxKG6P NIfoXmdmdmijbnPld{B1cGVibHX2[Yx{KG:oIICyO2tqeDF? NYnrWW1NOTd|NkGyNlU>
HL60AR M3TmN2Fxd3C2b4Ppd{Bie3OjeR?= MmC5glIxOCCwTR?= M1e1VYlv\HWlZYOgZZBweHSxc3nz NWDOclBXOTd|NkGyNlU>
HPAF-II M13jTWtqdmG|ZTDhd5NigQ>? NHfPcpB,OSEQvF2= M2LyNWROW09? MX;pcohq[mm2czDJS2YuUS2vZXTpZZRm\CC|aXfuZYxtcW6p NHqyUocyQDR2NUWyNC=>
HPAF-II MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUT+NkDPxE1? MXXEUXNQ M{Xqe4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NXXBWWRQOTh2NEW1NlA>
HPAF-II MUnGeY5kfGmxbjDhd5NigQ>? MV7+NkDPxE1? MmrFSG1UVw>? MVvpcohq[mm2czDiZZNidCCjbnSgTWdHNUlvbXXkbYF1\WRicHHuZ5Jm[XSrYzDjZY5k\XJiY3XscEBucWe{YYTpc44> NYrVPXdCOTh2NEW1NlA>
TFK-1 NILJNXZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVP+NlUxKG6P MnvvSG1UVw>? MmCyTWM2OD1yLkK2JO69VQ>? NHfMR2MzODB4NkezOC=>
EGI-1 NFLsVo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkTTglI2OCCwTR?= M2qxVmROW09? MYTJR|UxRTBwMkig{txO NHXTNoIzODB4NkezOC=>
CC-LP-1 NXXCVmlrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mni2glI2OCCwTR?= MmHwSG1UVw>? M1jUPWlEPTB;MD6xOUDPxE1? M1vxWlIxODZ4N{O0
CC-SW-1 NX3OdJN6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXjxdWY3hjJ3MDDuUS=> M3LiOmROW09? MWrJR|UxRTBwNUSg{txO NYfiS2N7OjByNk[3N|Q>
Sk-ChA-1 M4XIOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXvaeHFShjJ3MDDuUS=> MlrhSG1UVw>? NX;TXZVbUUN3ME2wMlIh|ryP NHjEWI0zODB4NkezOC=>
Mz-ChA-1 MlzzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXj+NlUxKG6P NVuwb45NTE2VTx?= NISzb2dKSzVyPUGuN|kh|ryP MXiyNFA3Pjd|NB?=
Mz-ChA-2 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV3mNVhThjJ3MDDuUS=> MUjEUXNQ NWX4eZhlUUN3ME2wMlc{KM7:TR?= MViyNFA3Pjd|NB?=
ECC-1 MnjoT4lv[XOnIHHzd4F6 NHLUOJR,OTBizszN Mm\2SG1UVw>? MknVbY5pcWKrdIOgTWdHNUmUIHHjeIl3[XSrb36gZpkhQThn M4nSPVIyOjl3M{O1
Ishikawa M3yxeWtqdmG|ZTDhd5NigQ>? NV\Yd3JJhjFyIN88US=> M4nlcGROW09? M1jPN4lvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDl|JR?= M2\EUVIyOjl3M{O1
USPC-1 NWO1NWJnU2mwYYPlJIF{e2G7 MUf+NVAh|ryP NXfHPY84TE2VTx?= M{D1VIlvcGmkaYTzJGlITi2LUjDhZ5RqfmG2aX;uJIJ6KDFyMDW= NVryUpVDOjF{OUWzN|U>
USPC-2 NVnnSW8yU2mwYYPlJIF{e2G7 MVv+NVAh|ryP M2HRcmROW09? NGXwNmhqdmirYnn0d{BKT0ZvSWKgZYN1cX[jdHnvckBjgSB7NjW= MUeyNVI6PTN|NR?=
ECC-1 M33iS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1zpTJ4yOCEQvF2= NV6yZZo3TE2VTx?= NXXuUmNq\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NILRWHozOTJ7NUOzOS=>
Ishikawa NIXyZ4lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MomyglExKM7:TR?= NILseY9FVVOR M{fDUoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NV;RNVUyOjF{OUWzN|U>
USPC-1 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmTSglExKM7:TR?= NHHrW2xFVVOR MoPF[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> MmnoNlEzQTV|M{W=
USPC-2 M1;oUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXT+NVAh|ryP M3HKb2ROW09? MXjk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u NF[4OmMzOTJ7NUOzOS=>

... 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
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
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