BMS-754807

Catalog No.S1124

BMS-754807 Chemical Structure

Molecular Weight(MW): 461.49

BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.

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Cited by 6 Publications

1 Customer Review

  • Clin Cancer Res 2013 19(11), 2984-94. BMS-754807 purchased from Selleck.

Purity & Quality Control

Choose Selective IGF-1R Inhibitors

Biological Activity

Description BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.
Features Muti-inhibitor of the IGR-1R/IR family.
Targets
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
TrkB [1]
(Cell-free assay)
Met [1]
(Cell-free assay)
TrkA [1]
(Cell-free assay)
1.7 nM 1.8 nM 4.1 nM 5.6 nM 7.4 nM
In vitro

BMS-754807 effectively inhibits the growth of a broad range of human tumor cell lines of different histologic origins including mesenchymal (Ewing's, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreatic, colon, and gastric), and hematopoietic (multiple myeloma and leukemia), the IC50 values range from 5 nM to 365 nM for the most sensitive cell lines. BMS-754807 inhibits proliferation of IGF-1R-Sal cells and RH41 cells with IC50 of 7 nM and 5 nM. BMS-754807 inhibits phosphorylation of IGF-1R in IGF-1R-Sal cells, Rh41 and Geo with IC50 of 13 nM, 6 nM and 21 nM. BMS-754807 inhibits phosphorylation of Akt in IGF-1R-Sal cells, Rh41 and Geo with IC50 of 22 nM, 13 nM and 16 nM. BMS-754807 induces greater apoptosis in Rh41 cells by 24 hours as indicated by an increased sub-G1 peak (23.1%), compared with control (2.4%). [1] BMS-754807 inhibits the phosphorylation of IGF-1R (IC50 = 13nM) and the downstream targets Akt (IC50 = 22nM) and MAPK (IC50 = 13nM) in the IGF-Sal cell line with IC50 consistent with the antiproliferative IC50 (7 nM) in this cell line. The crystal structure of BMS-754807 cocrystallized with the kinase domain of IGF-1R shows that the donor/acceptor/donor hydrogen bond triad with Met1052 and Glu1050 within the hinge region of the kinase. [2] BMS-754807 shows a median EC50 value of 0.62 μM against 23 cell lines in the pediatric preclinical testing program (PPTP). [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IGF-Sal MV;LbY5ie2ViYYPzZZk> M3S0ZYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiSVfGMVFTKCiLQ{WwJF0hOTOwTTmgZY5lKHSqZTDkc5dve3S{ZXHtJJRiemendIOgRYt1KCiLQ{WwJF0hOjKwTTmgZY5lKE2DUFugLGlEPTBiPTCxN45OMQ>? MoX1NVk4PzhyMkS=
IGF-Sal MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NW\qeIRVUUN3ME23JI5O M2[yblE6Pzd6MEK0
CCRF-CEM (ALL) MlHoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYH+OUDPxE1? MkWwSG1UVw>? M3S2eWlEPTB;MT6yN|kh|ryP Mmi0NVk6QTZ{N{K=
PC3 NULXblRrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIW4[5Z,PSEQvF2= NX[zelVZTE2VTx?= NHG2VoNKSzVyPUCuPVY2KM7:TR?= NGj0NG0yQTl7NkK3Ni=>
JD NX31Z4puT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4mwPZ42KM7:TR?= MVrEUXNQ NH34RnNKSzVyPUCuN|kyKM7:TR?= M3G1TlE6QTl4Mkey
DU145 NF3oNnVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYDiPJVqhjVizszN MVLEUXNQ Ml[xTWM2OD1zLkS2OUDPxE1? NVv6UodJOTl7OU[yO|I>
KAG NUPXUoFmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWH+OUDPxE1? Mm\USG1UVw>? M1fuXmlEPTB;MT62OlUh|ryP NH;PVWYyQTl7NkK3Ni=>
K-562 (CML) NU\EemFWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmnNglUh|ryP NYfFdXlLTE2VTx?= MlzMTWM2OD1{LkOwNkDPxE1? MUOxPVk6PjJ5Mh?=
B6-P210 (Murine ALL) NXPTe|lYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mnz2glUh|ryP NGjmdW1FVVOR Mlj3TWM2OD1zLkK5N{DPxE1? NV;qR|RUOTl7OU[yO|I>
LN CAP-FGC NYrt[XdsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYPiUJdjhjVizszN Mn7GSG1UVw>? NHnCfHdKSzVyPUGuOFM1KM7:TR?= MVqxPVk6PjJ5Mh?=
VW M1jneGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX7RPY97hjVizszN M1XmcGROW09? MVPJR|UxRTBwMEG5JO69VQ>? MmP4NVk6QTZ{N{K=
MV411 (B Myelomonocytic) MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1PZZZ42KM7:TR?= NFvCbpdFVVOR Mk\jTWM2OD1yLkOzJO69VQ>? NWToWVU3OTl7OU[yO|I>
MDA-PCa-2b MlG1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4\E[p42KM7:TR?= NX\TTY5iTE2VTx?= NY\aRnFmUUN3ME2wMlA6QCEQvF2= M1fzN|E6QTl4Mkey
LG M371Wmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1K0VJ42KM7:TR?= Ml7USG1UVw>? MnfUTWM2OD1yLkCzPEDPxE1? NVXDW5d7OTl7OU[yO|I>
RS411 (B cell precursor-ALL) M2TxdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NY\oVZdrhjVizszN MlzLSG1UVw>? Mlz4TWM2OD1yLkGwNkDPxE1? M3nzT|E6QTl4Mkey
22-r-1 NFm3XlVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUP+OUDPxE1? MnPNSG1UVw>? NIjlb5lKSzVyPUCuNVc2KM7:TR?= M1TLSVE6QTl4Mkey
5838 MorBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoDrglUh|ryP NWTINmVTTE2VTx?= M2\ISGlEPTB;MD6wN|Qh|ryP Mnm5NVk6QTZ{N{K=
P388 (Murine) MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3zTSZ42KM7:TR?= Mle0SG1UVw>? MWHJR|UxRTRwMkeg{txO MXWxPVk6PjJ5Mh?=
A2780/S NXTyeoQ3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn\SglUh|ryP NHzJd25FVVOR MVfJR|UxRTBwMUKyJO69VQ>? MUWxPVk6PjJ5Mh?=
RDES M{jrfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGWzXnN,PSEQvF2= NFfmNHBFVVOR M4rrcWlEPTB;MD6wNVIh|ryP M2HRPVE6QTl4Mkey
B6-T315I (Murine B-ALL) MmK3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4jNdJ42KM7:TR?= M{fxT2ROW09? M{TK[GlEPTB;Mj64N{DPxE1? MWexPVk6PjJ5Mh?=
TOV 112D Mo\MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3LzXJ42KM7:TR?= MW\EUXNQ NYXGbWpXUUN3ME2yMlE1PiEQvF2= NITBeIYyQTl7NkK3Ni=>
TC32 NYjaRXRmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH3KOld,PSEQvF2= NUDZWJlpTE2VTx?= NIXYSJNKSzVyPUCuNFA5KM7:TR?= M4PFc|E6QTl4Mkey
HL60 (acute myelocytic) NH3oTVRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2rVep42KM7:TR?= M4\mNWROW09? NIPLVG1KSzVyPUCuNVIh|ryP MmjDNVk6QTZ{N{K=
TOV 21G NH3jSGpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1;odZ42KM7:TR?= NFH5fYFFVVOR NW\Tb5B7UUN3ME20MlI4QSEQvF2= M1vKXlE6QTl4Mkey
TC71 M1Hxcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUDNR4lihjVizszN NHToZ3dFVVOR MofrTWM2OD1yLkCxOEDPxE1? NWHmTm1{OTl7OU[yO|I>
HPN-ALL (T-cell) NX35bXV5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnPiglUh|ryP MmnBSG1UVw>? NIjQblJKSzVyPUCuOVIh|ryP NHzIfFcyQTl7NkK3Ni=>
A2780R MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mnq1glUh|ryP M4HmcWROW09? NHG5XWZKSzVyPUGuOVY1KM7:TR?= MXuxPVk6PjJ5Mh?=
Rh1 MmWzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHHWeFN,PSEQvF2= NVL0S|hrTE2VTx?= NF[yVmhKSzVyPUCuNFI4KM7:TR?= MYOxPVk6PjJ5Mh?=
Kasumi-1 (acute myeloid) MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3[wV542KM7:TR?= MWXEUXNQ MXPJR|UxRTBwMU[g{txO NVfD[mExOTl7OU[yO|I>
sk-ov-3 NF:5NlZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUjLXFU4hjVizszN MmPNSG1UVw>? NV[3N4VtUUN3ME21MlEh|ryP MkX6NVk6QTZ{N{K=
ME M1nrS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFTHU2Z,PSEQvF2= NHrFUWVFVVOR M3\VVmlEPTB;MD6wNVUh|ryP MYmxPVk6PjJ5Mh?=
L1210 (Murine lymphocytic) M1HIO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkSxglUh|ryP M2TPVmROW09? MmXQTWM2OD1{LkO5JO69VQ>? NFT0fVEyQTl7NkK3Ni=>
sw-626 NIDEU2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1POdZ42KM7:TR?= Mkf3SG1UVw>? Mlu2TWM2OD1{LkOwOkDPxE1? M1jnWlE6QTl4Mkey
CTR MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmHFglUh|ryP MnLVSG1UVw>? Mn;pTWM2OD1yLkK1N{DPxE1? MWmxPVk6PjJ5Mh?=
ML2 (Myelomonocytic) NYLxWHl3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mkf6glUh|ryP MXjEUXNQ MkD0TWM2OD1yLkC5JO69VQ>? MmL1NVk6QTZ{N{K=
ovcar-3 M1LNcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFLUfoN,PSEQvF2= NHrtdFZFVVOR MkLFTWM2OD13IN88US=> MW[xPVk6PjJ5Mh?=
Rh36 NEPpXopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M173Np42KM7:TR?= Moi5SG1UVw>? MmjTTWM2OD1zLkSzNkDPxE1? M3ewbVE6QTl4Mkey
MOLM-13 (acute myeloid) M3jhbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NES0Rox,PSEQvF2= NYHpXIVuTE2VTx?= NIqyelRKSzVyPUCuOFIh|ryP M3v6PVE6QTl4Mkey
ovcar-4 NEiyNGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MknHglUh|ryP NI\lVJpFVVOR MYjJR|UxRTFizszN NHLhWGIyQTl7NkK3Ni=>
Rh41 NYP4[mJmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYD+OUDPxE1? MmixSG1UVw>? MnX6TWM2OD1yLkCwOUDPxE1? M{fRNVE6QTl4Mkey
Mutz 2 (acute myeloid) Mn\SS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{[3TZ42KM7:TR?= MYfEUXNQ MXTJR|UxRTFwMUWg{txO NFW5NVIyQTl7NkK3Ni=>
ovcar-5 NH3aUodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVHkbFByhjVizszN MnTvSG1UVw>? NETuU49KSzVyPUCuNFUh|ryP MUKxPVk6PjJ5Mh?=
RD1 MlH0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2rs[Z42KM7:TR?= MVTEUXNQ MUPJR|UxRTBwME[4JO69VQ>? MYSxPVk6PjJ5Mh?=
OCI-AML 2 (acute myeloid) NFrINJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV;+OUDPxE1? NFvCfY1FVVOR NYm1bGk1UUN3ME2zMlM{KM7:TR?= M4\ZTVE6QTl4Mkey
786-O NF;hRmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHXkW3F,PSEQvF2= NY\kSYpTTE2VTx?= M3r4d2lEPTB;MT62OFch|ryP NF\TPZoyQTl7NkK3Ni=>
A673 M1;lNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXyy[lNnhjVizszN NG[0cY5FVVOR M13tUGlEPTB;MD60NFgh|ryP MVixPVk6PjJ5Mh?=
TALL-1 (T-cell) M4Huemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmjFglUh|ryP NEX2fm1FVVOR NGjENoRKSzVyPUGuNlgh|ryP Mm\GNVk6QTZ{N{K=
151-B M1Xlfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4LEW542KM7:TR?= MXPEUXNQ MXXJR|UxRTJwNkeg{txO M1TtXlE6QTl4Mkey
PFSK-1 NVjldFFVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmD4glUh|ryP NUH6dXo5TE2VTx?= NYXDOGpVUUN3ME2wMlE{OiEQvF2= M{LGV|E6QTl4Mkey
THP-1 MoOxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWX1eGpDhjVizszN MorPSG1UVw>? MWDJR|UxRTZwNUig{txO Mo\rNVk6QTZ{N{K=
HEK293 MoLNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1G4TZ42KM7:TR?= NVLvc4tCTE2VTx?= NXznR3dFUUN3ME2wMlkyPSEQvF2= MWqxPVk6PjJ5Mh?=
DAOY M2XEbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4XFV542KM7:TR?= NITQUGVFVVOR M2LBdmlEPTB;MT65O|kh|ryP Mlj5NVk6QTZ{N{K=
SET2 NYTtWWt6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M13FN542KM7:TR?= NVX2bGJRTE2VTx?= NETvd3VKSzVyPUCuNlk5KM7:TR?= Mlu1NVk6QTZ{N{K=
HTB-46 NYPaUmNmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1qyXZ42KM7:TR?= M4LLXmROW09? MUTJR|UxRTVwMkWg{txO NVG0ZZpKOTl7OU[yO|I>
SK-NAS NX7E[3VYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4Pl[J42KM7:TR?= MWDEUXNQ MX7JR|UxRTBwNEm3JO69VQ>? NEXOXm8yQTl7NkK3Ni=>
CTLL2 MkHCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWLVbYt2hjVizszN NUjWU3YzTE2VTx?= NET0PHNKSzVyPkGuNFAh|ryP M{\ldlE6QTl4Mkey
HTB-47 NIPxT2ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2G0Rp42KM7:TR?= NEXXdlFFVVOR MnnyTWM2OD1{LkC1OkDPxE1? NFfz[ogyQTl7NkK3Ni=>
LAN-1 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnzvglUh|ryP NXzQeo01TE2VTx?= M{nld2lEPTB;MD6wOEDPxE1? NX3kOYpZOTl7OU[yO|I>
ST486 NIPWeGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmDlglUh|ryP NILEd|RFVVOR M1TofmlEPTB;MT6xPUDPxE1? M1rsN|E6QTl4Mkey
HS766T MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWL+OUDPxE1? M4\hWmROW09? NHm0Oo5KSzVyPUKuNFAyKM7:TR?= Mnq3NVk6QTZ{N{K=
IMR-32 MmO1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXX+OUDPxE1? Mmm1SG1UVw>? Mk\rTWM2OD1yLkK2NUDPxE1? NXjhT2M{OTl7OU[yO|I>
Daudi (Burkitt's) NYrjcoc1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{m4cZ42KM7:TR?= M1qwSWROW09? MmDzTWM2OD1{Lk[zO{DPxE1? M3uxUlE6QTl4Mkey
Aspc-1 M3P2TGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M33wV542KM7:TR?= NXK2Ro96TE2VTx?= NET2fIlKSzVyPUCuN|c6KM7:TR?= NV;hXXBmOTl7OU[yO|I>
SK-NSH M4HmN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYrmUZE5hjVizszN M1rO[mROW09? MVPJR|UxRTBwMUO5JO69VQ>? MnHINVk6QTZ{N{K=
MEC-1 (Chronic B cell) NEPUemtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVn+OUDPxE1? MoTJSG1UVw>? MoP5TWM2OD1{Lk[zO{DPxE1? M3XsdFE6QTl4Mkey
Capan-2 M1rZcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUjlTYJ7hjVizszN MUXEUXNQ NF\Z[VhKSzVyPUGuO|c1KM7:TR?= MnLLNVk6QTZ{N{K=
SHSY5Y NIfzSZpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV7+OUDPxE1? Ml\PSG1UVw>? NW\SUmVRUUN3ME2wMlExPiEQvF2= M1vvTVE6QTl4Mkey
U937 (Histioocytic) MoHLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWH+OUDPxE1? MlfrSG1UVw>? NIjRXY5KSzVyPkWuNFAh|ryP MoT5NVk6QTZ{N{K=
Bxpc-1 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4PYV542KM7:TR?= NIHIU3ZFVVOR MUXJR|UxRTFwOUK0JO69VQ>? MVmxPVk6PjJ5Mh?=
Bxpc-3 NHjmPIpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF31V2d,PSEQvF2= M134PGROW09? MXzJR|UxRjVwMECg{txO MX6xPVk6PjJ5Mh?=
HTB-92 M3\lVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTzbXpEhjVizszN NYrzNGtNTE2VTx?= NEG3Z|NKSzVyPUGuNFIh|ryP NXu2R5JEOTl7OU[yO|I>
OCI-LY10 (B-cell) MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGTze|B,PSEQvF2= MoHiSG1UVw>? MnPyTWM2OD1yLkS1JO69VQ>? NHnJXWwyQTl7NkK3Ni=>
PANC-1 NVHDTWI{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYr+OUDPxE1? NWLje2kzTE2VTx?= M{\DdWlEPTB-NT6wNEDPxE1? NI\rNVMyQTl7NkK3Ni=>
To184.T NIDnfnRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVf4bmFUhjVizszN NVjodItwTE2VTx?= M3zOOmlEPTB;MD60Olkh|ryP NFHWPJUyQTl7NkK3Ni=>
OCI-LY19 (B-cell) MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWT+OUDPxE1? NEDLdm5FVVOR Mmj1TWM2OD1yLkSg{txO NIPCS|gyQTl7NkK3Ni=>
PANC-1 BM Ml61S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWP+OUDPxE1? MmTPSG1UVw>? NVjteZpHUUN3ME61MlAxKM7:TR?= MkDGNVk6QTZ{N{K=
SA-4 NETBOI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2OyfJ42KM7:TR?= MYDEUXNQ NYLMeJBJUUN3ME2xMlMxOSEQvF2= M1\mUVE6QTl4Mkey
RPMI 8226 NFHoeHNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnH0glUh|ryP MYjEUXNQ M2TRfWlEPTB;MT6yPVMh|ryP MVKxPVk6PjJ5Mh?=
HPAF-II NGXYWlVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEfRelF,PSEQvF2= NGi4U4tFVVOR MWTJR|UxRTBwNkS0JO69VQ>? NFKwdHcyQTl7NkK3Ni=>
SHP-77 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX3+OUDPxE1? NVqzZ2tVTE2VTx?= M1zYVmlEPTB;MT64PFgh|ryP M3PjR|E6QTl4Mkey
U266 B1 M4O4fGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2DhOZ42KM7:TR?= MUHEUXNQ MWPJR|UxRTFwNk[5JO69VQ>? M{f3bVE6QTl4Mkey
Hs700t MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVz+OUDPxE1? NEXWNo5FVVOR NVPENpJIUUN3ME2wMlI{OSEQvF2= M3TWOFE6QTl4Mkey
NCI-446 NH[2RpBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHrKfmt,PSEQvF2= MkHzSG1UVw>? MkjETWM2OD1zLkG1OEDPxE1? NXHhTJhoOTl7OU[yO|I>
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HT1080/S NYLDN2hpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NID0NVR,PSEQvF2= Mn;JSG1UVw>? M{PDZmlEPTB;MD61N|Eh|ryP MV2xPVk6PjJ5Mh?=
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M109 MkDjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NES3NoF,PSEQvF2= MUDEUXNQ MkLCTWM2OD1zLkC1OUDPxE1? NHexfFQyQTl7NkK3Ni=>
BT549 NGeyPGJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH3GUWx,PSEQvF2= M3XlSWROW09? M3fybmlEPTB;MT62OFUh|ryP NGDVcHgyQTl7NkK3Ni=>
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H460 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{jQXp42KM7:TR?= Mln3SG1UVw>? NULJR2RDUUN3ME2wMlc6PSEQvF2= NXi3ZlJ7OTl7OU[yO|I>
MCF-7 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1nQO542KM7:TR?= NFLyXXlFVVOR NHTmfWlKSzVyPUCuNFE3KM7:TR?= M3nSelE6QTl4Mkey
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SW480 MoGyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2LMOp42KM7:TR?= M{fGdWROW09? MUfJR|UxRjVwMECg{txO NIDlW3MyQTl7NkK3Ni=>
L2987 M2\IU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M136WZ42KM7:TR?= NVfIdFVvTE2VTx?= M33BcGlEPTB;MD60OFIh|ryP NGXCeIcyQTl7NkK3Ni=>
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H661 0.573 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXjNNo1[hjVizszN NGq1b25FVVOR MnL5TWM2OD1yLkW3N{DPxE1? NW\Y[|hROTl7OU[yO|I>
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Rh30 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MW\+NVDjiIsQvF2= NYHadYlzUUN3ME2wMlE6KML3TR?= MknyNlEzQTh5NEW=
BT-12 NEDZe3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWX+NVDjiIsQvF2= NEHKNWNKSzVyPUCuO|ghyrWP M{jobVIyOjl6N{S1
CHLA-266 Ml7MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmHKglEx6oDMzszN M4jxR2lEPTB;MD64PUDDvU1? MmW0NlEzQTh5NEW=
TC-71 M3LyT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnPuglEx6oDMzszN M4T5eWlEPTB;MD6xNUDDvU1? MWWyNVI6QDd2NR?=
CHLA-9 M4LOcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX7+NVDjiIsQvF2= Mnm4TWM2OD1yLkGyJOK2VQ>? Mn;ZNlEzQTh5NEW=
CHLA-10 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVj+NVDjiIsQvF2= NGK4UFBKSzVyPUCuOlIhyrWP NFW2[4ozOTJ7OEe0OS=>
CHLA-258 NIS3UpBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGPndZV,OTEkgJtOwG0> NWf1UWVIUUN3ME2wMlI4KML3TR?= M{W4RVIyOjl6N{S1
GBM2 NYnad|Y5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1yzOp4yOOLCit88US=> NGSwW2tKSzVyPUGuOFchyrWP M2DMelIyOjl6N{S1
NB-1643 NEfFSFZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2q4U54yOOLCit88US=> MWLJR|UxRTBwMUKgxtVO NGXzOJEzOTJ7OEe0OS=>
NB-EBc1 MmjSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYX+NVDjiIsQvF2= Mke2TWM2OD1yLkO1JOK2VQ>? Moj4NlEzQTh5NEW=
CHLA-90 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MojWglEx6oDMzszN MYDJR|UxRTBwN{egxtVO M3\wR|IyOjl6N{S1
CHLA-136 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1PPOp4yOOLCit88US=> NHTCPGZKSzVyPUCuOVIhyrWP MYeyNVI6QDd2NR?=
NALM-6 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1rvT54yOOLCit88US=> NVrwNG5EUUN3ME2wMlQ6KML3TR?= MYGyNVI6QDd2NR?=
COG-LL-317 M4jKOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEXFbJV,OTEkgJtOwG0> MkD2TWM2OD1zLkO4JOK2VQ>? Mk\hNlEzQTh5NEW=
RS4;11 NH7SNpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWf+NVDjiIsQvF2= MoG1TWM2OD1yLkO4JOK2VQ>? M2TYXFIyOjl6N{S1
MOLT-4 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVT+NVDjiIsQvF2= M{TGR2lEPTB;MD61N{DDvU1? Mof3NlEzQTh5NEW=
CCRF-CEM MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWC1fVVHhjFy4pEK{txO NV7X[mJqUUN3ME2xMlE{KML3TR?= M2HJUVIyOjl6N{S1
Kasumi-1 MojOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFfVfWJ,OTEkgJtOwG0> NH3FUnRKSzVyPUGuNkDDvU1? M37QTFIyOjl6N{S1
Karpas-299 MmjkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF7qbVV,OTEkgJtOwG0> M4fMOWlEPTB;MT62OEDDvU1? NELETo4zOTJ7OEe0OS=>
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Rh30  MlXSSpVv[3Srb36gZZN{[Xl? Mn\UbY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w NUn3SoU{OjV7MkWzO|g>
Rh41 MUjGeY5kfGmxbjDhd5NigQ>? MkG3bY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w NGDKT4QzPTl{NUO3PC=>
RD MmHYSpVv[3Srb36gZZN{[Xl? MVjpcoR2[2W|IHHuJIlv[3KnYYPlJI9nKFOISzDwbI9{eGixconsZZRqd25? MmP3NlU6OjV|N{i=
A549 NV3SWGxjU2mwYYPlJIF{e2G7 MWSwMlXjiIsQvF2= M2\ZZ2ROW09? NF76fJRqdmirYnn0d{BKT0ZvSWKvTXIh[WO2aY\heIlwdg>? Mkn2NlY6Ojh3N{i=
NCI-H358 NWnYVGdDU2mwYYPlJIF{e2G7 NFH0b|AxNjYkgJtOwG0> M{TVfmROW09? MXjpcohq[mm2czDJS2YuUVJxSWKgZYN1cX[jdHnvci=> NUPYSmwxOjZ7Mki1O|g>
A549 M1:1VGZ2dmO2aX;uJIF{e2G7 MlzyNE426oDMzszN M4\SNGROW09? NWHEcpg6[2G3c3XzJIEh[2:wY4XydoVvfCCmZXPy[YF{\SCrbjDwbI9{eGixconsZZRm\CCDS2SgZY5lKEWUSx?= NYDLVGQ5OjZ7Mki1O|g>
NCI-H358 NYTVTW8{TnWwY4Tpc44h[XO|YYm= NFy0RlMxNjYkgJtOwG0> MUnEUXNQ MX;jZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM NHLURVUzPjl{OEW3PC=>
A549 M3nEdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVi2VlZ2hjFy4pEK{txO NUW3WG5DTE2VTx?= MV\JR|UxRTBwN{[g{txO NH70UoUzPjl{OEW3PC=>
NCI-H358 MmXaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3nHT54yOOLCit88US=> Ml:3SG1UVw>? MULJR|UxRTFwMEmg{txO NHHmW2IzPjl{OEW3PC=>
A549 MYTBdI9xfG:|aYOgZZN{[Xl? MnfrNE426oDMzszN NGDXUZlFVVOR MUjpcoR2[2W|IFHwc5B1d3Orcx?= NHn0SIQzPjl{OEW3PC=>
NCI-H358 M{n3[2Fxd3C2b4Ppd{Bie3OjeR?= MnXNNE426oDMzszN M4\zfGROW09? MoXibY5lfWOnczDBdI9xfG:|aYO= NVXwN3lxOjZ7Mki1O|g>
A549 NGHJUHZHfW6ldHnvckBie3OjeR?= NEPaTFAxNjYkgJtOwG0> Mn;FSG1UVw>? MnHndoVlfWOnczD3c5Vv\CClbH;zeZJm MYKyOlkzQDV5OB?=
NCI-H358 NWnIU4FXTnWwY4Tpc44h[XO|YYm= MmLmNE426oDMzszN M3XvVGROW09? NWWzVFl2emWmdXPld{B4d3WwZDDjcI9{fXKn Mki2NlY6Ojh3N{i=

... Click to View More Cell Line Experimental Data

In vivo BMS-754807 (12.5mg/kg, orally) inhibits IGF-1R phosphorylation in tumor and serum in IGF-1R-Sal tumor–bearing nude mice. BMS-754807 inhibits tumor growth in a selected group of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3), and mesenchymal (RD1 and Rh41) xenograft tumor models with TGI ranging from 53% to 115%. [1] BMS-754807 (6.25 mg/kg) achieves complete tumor growth inhibition in the transgenic-derived IGF-Sal tumor mouse model with correlated inhibition of pIGF-1R and pAKT. The protein binding for BMS-754807 ranges from of 98.5% in mouse plasma to 95.9% in human plasma. BMS-754807 results in clearance of 113 (mL/min)/kg, 20 (mL/min)/kg, 3.5 (mL/min)/kg and 41 (mL/min)/kg. [2] BMS-754807 (25 mg/kg) significantly inhibits tumor in KT-5 (Wilms), KT-14 (rhabdoid), Rh28 (rhabdomyosarcoma), and OS-1 xenografts mice model. [3]

Protocol

Kinase Assay:[1]
+ Expand

Kinase inhibition assays:

The primary screen for BMS-754807 is an in vitro kinase assay using recombinant human IGF-1 receptor enzyme in biochemical assays using synthetic peptide KKSRGDYMTMQIG as a phosphoacceptor substrate. The selectivity profile is evaluated against multiple recombinant enzymes that are generated at BMS or purchased externally. The enzymatic assays are performed in Ubottom 384-well plates using a 30 μL reaction volume in assay buffer (100 mM Hepes pH 7.4, 10 mM MgCl2, 0.015% Brij35 and 4 mM DTT). The 60 minute reactions are initiated by combining ATP (concentration equivalent to Km ATP), 1.5 μM fluoresceinlabeled peptide substrate, enzyme and BMS-754807. The reactions are terminated with EDTA. The reaction mixtures are analyzed on the Caliper LabChip 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data are calculated by comparison to enzyme-free control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. Compounds are dissolved in dimethylsulfoxide (DMSO, 10mM stock) and evaluated at eleven concentrations. IC50 values are derived by non-linear regression analysis of the dose response curves.
Cell Research:[1]
+ Expand
  • Cell lines: IGF-1R-Sal, RH41 and Geo cell lines
  • Concentrations: 365 nM
  • Incubation Time: 72 hours
  • Method: Cells are grown at their optimal density in RPMI +GlutaMax supplemented with 10% heat-inactivated fetal bovine serum (FBS), 10 mM Hepes, penicillin, and streptomycin. Cell proliferation is evaluated by incorporation of 3H-thymidine into DNA after exposure of cells to BMS-754807 for 72 hours. Results are expressed as an IC50, which is the drug concentration required to inhibit cell proliferation by 50% compared with untreated control cells.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: IGF-1R-Sal, GEO, Colo205, JJN3, RD1 or Rh41 tumor–bearing nude mice
  • Formulation: Mixture of polyethylene glycol 400 (PEG400/water (4:1; vol/vol)
  • Dosages: 150 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (199.35 mM)
Ethanol 92 mg/mL (199.35 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
5mg/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 461.49
Formula

C23H24FN9O

CAS No. 1001350-96-4
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01525823 Completed Healthy Volunteers Bristol-Myers Squibb February 2012 Phase 1
NCT01525823 Completed Healthy Volunteers Bristol-Myers Squibb February 2012 Phase 1
NCT01225172 Completed Breast Cancer Bristol-Myers Squibb|Mayo Clinic December 2010 Phase 2
NCT01225172 Completed Breast Cancer Bristol-Myers Squibb|Mayo Clinic December 2010 Phase 2
NCT00908024 Terminated Colorectal Cancer|Head and Neck Cancer|Neoplasm Metastasis Bristol-Myers Squibb October 2009 Phase 1|Phase 2
NCT00908024 Terminated Colorectal Cancer|Head and Neck Cancer|Neoplasm Metastasis Bristol-Myers Squibb October 2009 Phase 1|Phase 2

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

If you have any other enquiries, please leave a message.

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IGF-1R Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID