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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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 MUjLbY5ie2ViYYPzZZk> MnHGbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXIhMEmFNUCgQUAyO26PKTDhcoQhfGinIHTve45{fHKnYX2geIFz\2W2czDBb5QhMEmFNUCgQUAzOm6PKTDhcoQhVUGSSzCoTWM2OCB;IEGzcm0q M2Tl[FE6Pzd6MEK0
IGF-Sal NWHQSZF7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHrFWYlKSzVyPUegcm0> MoS0NVk4PzhyMkS=
CCRF-CEM (ALL) NFHnNmlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2\QNp42KM7:TR?= NVjsVXF5TE2VTx?= NILHcIVKSzVyPUGuNlM6KM7:TR?= M1HyWlE6QTl4Mkey
PC3 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NI\BcnR,PSEQvF2= NG\rWXFFVVOR MkS1TWM2OD1yLkm2OUDPxE1? NVPGV4RlOTl7OU[yO|I>
JD MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MonMglUh|ryP M{\rSGROW09? NHvUSGtKSzVyPUCuN|kyKM7:TR?= NHLPN4UyQTl7NkK3Ni=>
DU145 M3K5T2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M17Ibp42KM7:TR?= NUf0TY5jTE2VTx?= M3\iO2lEPTB;MT60OlUh|ryP NFfIVY0yQTl7NkK3Ni=>
KAG M1r1TWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWPyV4pihjVizszN NHntUmxFVVOR NWDENIJ2UUN3ME2xMlY3PSEQvF2= MYKxPVk6PjJ5Mh?=
K-562 (CML) MoDOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWT+OUDPxE1? NVy4fHp3TE2VTx?= NIPYb2pKSzVyPUKuN|AzKM7:TR?= MnnoNVk6QTZ{N{K=
B6-P210 (Murine ALL) MonnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIDoco9,PSEQvF2= M2PDRWROW09? MlOxTWM2OD1zLkK5N{DPxE1? NWj1cJdwOTl7OU[yO|I>
LN CAP-FGC MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYXaXXJXhjVizszN MVLEUXNQ MkjJTWM2OD1zLkSzOEDPxE1? MnLxNVk6QTZ{N{K=
VW MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnvVglUh|ryP MX7EUXNQ NXuzU5ZJUUN3ME2wMlAyQSEQvF2= MnfsNVk6QTZ{N{K=
MV411 (B Myelomonocytic) MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkSxglUh|ryP Mk\VSG1UVw>? M2jzNGlEPTB;MD6zN{DPxE1? M2DvSVE6QTl4Mkey
MDA-PCa-2b M{HZ[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmfaglUh|ryP MnvOSG1UVw>? MYjJR|UxRTBwMEm4JO69VQ>? NUHXeXZ2OTl7OU[yO|I>
LG NHLFclVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4mzep42KM7:TR?= NYHwT286TE2VTx?= NXPFdlQ4UUN3ME2wMlA{QCEQvF2= NVyydIx5OTl7OU[yO|I>
RS411 (B cell precursor-ALL) MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV\PcJRphjVizszN NFfHZ21FVVOR MYXJR|UxRTBwMUCyJO69VQ>? MYGxPVk6PjJ5Mh?=
22-r-1 M2H4V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXv+OUDPxE1? MlfPSG1UVw>? MmLUTWM2OD1yLkG3OUDPxE1? MoK0NVk6QTZ{N{K=
5838 MlnqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX3+OUDPxE1? MmSySG1UVw>? MXjJR|UxRTBwMEO0JO69VQ>? NYHKO3FSOTl7OU[yO|I>
P388 (Murine) M4Prc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWnPNFR5hjVizszN NXLGPJhETE2VTx?= NHXQUnRKSzVyPUSuNlch|ryP M3HySVE6QTl4Mkey
A2780/S NED0W|RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVTUbJJrhjVizszN NWXpVHhETE2VTx?= NX;VVGpQUUN3ME2wMlEzOiEQvF2= MmPGNVk6QTZ{N{K=
RDES MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUD6OHhohjVizszN MYTEUXNQ MYDJR|UxRTBwMEGyJO69VQ>? M3v3VlE6QTl4Mkey
B6-T315I (Murine B-ALL) NV[5OVZPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MW\+OUDPxE1? MW\EUXNQ M37NbWlEPTB;Mj64N{DPxE1? MX:xPVk6PjJ5Mh?=
TOV 112D M1vENmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3n3eZ42KM7:TR?= NG\nUXRFVVOR NI\sNZRKSzVyPUKuNVQ3KM7:TR?= MY[xPVk6PjJ5Mh?=
TC32 MkTWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NInuOnZ,PSEQvF2= MV7EUXNQ MWfJR|UxRTBwMEC4JO69VQ>? NYrKUpRXOTl7OU[yO|I>
HL60 (acute myelocytic) NXjTPWlVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn\OglUh|ryP NEjadnBFVVOR MX3JR|UxRTBwMUKg{txO NFj3S5YyQTl7NkK3Ni=>
TOV 21G MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mli1glUh|ryP NXLNOoNtTE2VTx?= NXnUdZZOUUN3ME20MlI4QSEQvF2= NF\1TWEyQTl7NkK3Ni=>
TC71 NVnkd|c{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3z3UJ42KM7:TR?= NXLGRWJETE2VTx?= NVXSS41LUUN3ME2wMlAyPCEQvF2= MojHNVk6QTZ{N{K=
HPN-ALL (T-cell) M4[wXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXS1XFNFhjVizszN MonOSG1UVw>? NITySGRKSzVyPUCuOVIh|ryP MXGxPVk6PjJ5Mh?=
A2780R MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFPtXJd,PSEQvF2= MXzEUXNQ NY\qe4dLUUN3ME2xMlU3PCEQvF2= MUOxPVk6PjJ5Mh?=
Rh1 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUTDfZh3hjVizszN M4TkV2ROW09? MnmyTWM2OD1yLkCyO{DPxE1? MlPDNVk6QTZ{N{K=
Kasumi-1 (acute myeloid) NHu5b|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3nHVZ42KM7:TR?= NXy0dpViTE2VTx?= NE[2WIFKSzVyPUCuNVYh|ryP MUOxPVk6PjJ5Mh?=
sk-ov-3 NX3mT4pxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2nhcp42KM7:TR?= NF;seYxFVVOR NHLTdGNKSzVyPUWuNUDPxE1? NFO2O3gyQTl7NkK3Ni=>
ME MknuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlPzglUh|ryP M{D0S2ROW09? M1vRW2lEPTB;MD6wNVUh|ryP M3XuT|E6QTl4Mkey
L1210 (Murine lymphocytic) MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEnJS|V,PSEQvF2= M{DOZ2ROW09? NGe5S3VKSzVyPUKuN|kh|ryP M3nmb|E6QTl4Mkey
sw-626 M2PpXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml\HglUh|ryP MYDEUXNQ MULJR|UxRTJwM{C2JO69VQ>? NUDrSYM2OTl7OU[yO|I>
CTR NEXnNI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M37sW542KM7:TR?= NF;wd4xFVVOR M1XUbGlEPTB;MD6yOVMh|ryP MX6xPVk6PjJ5Mh?=
ML2 (Myelomonocytic) NX3VVmc5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV;+OUDPxE1? Ml7rSG1UVw>? NV7yeWo6UUN3ME2wMlA6KM7:TR?= M{nEXVE6QTl4Mkey
ovcar-3 NELob2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXqyXYM{hjVizszN Mm[5SG1UVw>? NWe2b2ZyUUN3ME21JO69VQ>? MmXKNVk6QTZ{N{K=
Rh36 MmLnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV:5RphqhjVizszN NGjmR2hFVVOR NH7ZVJFKSzVyPUGuOFMzKM7:TR?= M3HK[VE6QTl4Mkey
MOLM-13 (acute myeloid) MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoTKglUh|ryP NXXGWXcyTE2VTx?= NXvEW4xuUUN3ME2wMlQzKM7:TR?= NIfPUngyQTl7NkK3Ni=>
ovcar-4 NWrS[nN5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYXDR3RzhjVizszN M1rFVGROW09? NHHZfWxKSzVyPUGg{txO NFLSSHEyQTl7NkK3Ni=>
Rh41 M{D2bGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;xbnJ3hjVizszN MU\EUXNQ NWDmTYx6UUN3ME2wMlAxPSEQvF2= MV[xPVk6PjJ5Mh?=
Mutz 2 (acute myeloid) NUSzbJk2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYXiSphThjVizszN MVHEUXNQ MlfETWM2OD1zLkG1JO69VQ>? MX:xPVk6PjJ5Mh?=
ovcar-5 M4ruWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2LTOp42KM7:TR?= NH;ZOm5FVVOR MXPJR|UxRTBwMEWg{txO MYSxPVk6PjJ5Mh?=
RD1 NYnnOZFvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXLTVHA5hjVizszN MnvlSG1UVw>? MWDJR|UxRTBwME[4JO69VQ>? MWSxPVk6PjJ5Mh?=
OCI-AML 2 (acute myeloid) MnPOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2jzOp42KM7:TR?= M2jpR2ROW09? NEH2PFJKSzVyPUOuN|Mh|ryP MnzHNVk6QTZ{N{K=
786-O NXPYclBoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M37u[Z42KM7:TR?= NF\3bpRFVVOR M{i5TWlEPTB;MT62OFch|ryP NYHzXJpOOTl7OU[yO|I>
A673 NWrLPXNOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoHJglUh|ryP NEHTUGpFVVOR NX7wcVBoUUN3ME2wMlQxQCEQvF2= M4Tt[lE6QTl4Mkey
TALL-1 (T-cell) NX6xXJdlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV3+OUDPxE1? NUXt[5AxTE2VTx?= MnLYTWM2OD1zLkK4JO69VQ>? MoT3NVk6QTZ{N{K=
151-B MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFzXNod,PSEQvF2= NXTxeHFLTE2VTx?= NH;3OWVKSzVyPUKuOlch|ryP MmHLNVk6QTZ{N{K=
PFSK-1 Mn;CS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVLCOJFshjVizszN M1nqcGROW09? Mn7hTWM2OD1yLkGzNkDPxE1? NXrVPWFWOTl7OU[yO|I>
THP-1 NI\0TXNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGja[ph,PSEQvF2= MUXEUXNQ M3XLXGlEPTB;Nj61PEDPxE1? NVqwcGxxOTl7OU[yO|I>
HEK293 NGOzV5hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYX5Z3RFhjVizszN MmXMSG1UVw>? M{nkXmlEPTB;MD65NVUh|ryP NF73WGgyQTl7NkK3Ni=>
DAOY Moi0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFzyfJJ,PSEQvF2= Mmm2SG1UVw>? MmjETWM2OD1zLkm3PUDPxE1? M13uTlE6QTl4Mkey
SET2 M2jJbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXrxdmh3hjVizszN NXPKOZduTE2VTx?= NVf3S|ZWUUN3ME2wMlI6QCEQvF2= M4f3NlE6QTl4Mkey
HTB-46 M3TCU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEXQRVl,PSEQvF2= MVzEUXNQ M3\RW2lEPTB;NT6yOUDPxE1? M4jCclE6QTl4Mkey
SK-NAS MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWDYenFxhjVizszN MUfEUXNQ MVTJR|UxRTBwNEm3JO69VQ>? NUG5bIpOOTl7OU[yO|I>
CTLL2 MnraS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFPXeIt,PSEQvF2= NFH3dWtFVVOR Mli5TWM2OD5zLkCwJO69VQ>? NULx[2VXOTl7OU[yO|I>
HTB-47 MkfvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV\+OUDPxE1? NHnCXpdFVVOR NGPR[|hKSzVyPUKuNFU3KM7:TR?= MWSxPVk6PjJ5Mh?=
LAN-1 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mlq4glUh|ryP MorkSG1UVw>? MVHJR|UxRTBwMESg{txO MVWxPVk6PjJ5Mh?=
ST486 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYe5fIRqhjVizszN NHrnWJBFVVOR M1H5V2lEPTB;MT6xPUDPxE1? NVjKOWFHOTl7OU[yO|I>
HS766T MomzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX3GZ3lshjVizszN MlvaSG1UVw>? MYHJR|UxRTJwMECxJO69VQ>? MYWxPVk6PjJ5Mh?=
IMR-32 NYLmdIlFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHSzcJl,PSEQvF2= M3XuTWROW09? M2\iWWlEPTB;MD6yOlEh|ryP M2D6XFE6QTl4Mkey
Daudi (Burkitt's) MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHXBV2p,PSEQvF2= Ml\6SG1UVw>? NGTIbnFKSzVyPUKuOlM4KM7:TR?= Mnz2NVk6QTZ{N{K=
Aspc-1 MnHrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYPMe2RthjVizszN MkDRSG1UVw>? MkTVTWM2OD1yLkO3PUDPxE1? NW\Db|BlOTl7OU[yO|I>
SK-NSH MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NED2NXV,PSEQvF2= MlzxSG1UVw>? MnvrTWM2OD1yLkGzPUDPxE1? NYHqRY97OTl7OU[yO|I>
MEC-1 (Chronic B cell) NV\ONpoxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEPWbId,PSEQvF2= M3mw[mROW09? MVzJR|UxRTJwNkO3JO69VQ>? NIraTGYyQTl7NkK3Ni=>
Capan-2 NF7sWI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVfWNHlbhjVizszN NVTDeY9LTE2VTx?= NFm2cVhKSzVyPUGuO|c1KM7:TR?= NVPiUZN2OTl7OU[yO|I>
SHSY5Y M2LTZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4\EOJ42KM7:TR?= MWDEUXNQ M2jj[2lEPTB;MD6xNFYh|ryP MXixPVk6PjJ5Mh?=
U937 (Histioocytic) MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlX0glUh|ryP MnvJSG1UVw>? M3XtdmlEPTB-NT6wNEDPxE1? MVGxPVk6PjJ5Mh?=
Bxpc-1 MnjNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX7vc5M{hjVizszN MUPEUXNQ NIDadWRKSzVyPUGuPVI1KM7:TR?= NX\YWItuOTl7OU[yO|I>
Bxpc-3 M3jRSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV:4N4pUhjVizszN NVz4cldkTE2VTx?= NYfJWIs5UUN3ME61MlAxKM7:TR?= NInxOG4yQTl7NkK3Ni=>
HTB-92 Mn22S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M134bZ42KM7:TR?= MX7EUXNQ M4j0UmlEPTB;MT6wNkDPxE1? M1TDb|E6QTl4Mkey
OCI-LY10 (B-cell) MkHYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIXh[VV,PSEQvF2= NVq2b5ZsTE2VTx?= M2LaSGlEPTB;MD60OUDPxE1? MkHhNVk6QTZ{N{K=
PANC-1 M2q1TWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{nLfJ42KM7:TR?= M13mWWROW09? NWrueJp2UUN3ME61MlAxKM7:TR?= Mn3lNVk6QTZ{N{K=
To184.T NWj4ZXFtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFeyd5h,PSEQvF2= M1XOemROW09? Mkn4TWM2OD1yLkS2PUDPxE1? M4TZclE6QTl4Mkey
OCI-LY19 (B-cell) M3LrVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV3VeHhGhjVizszN NHP4PYZFVVOR NULRS2hxUUN3ME2wMlQh|ryP MV[xPVk6PjJ5Mh?=
PANC-1 BM M{\LSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGfSNGl,PSEQvF2= MlPaSG1UVw>? NXH2cHRDUUN3ME61MlAxKM7:TR?= M3v2c|E6QTl4Mkey
SA-4 NH32ZY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M33ydZ42KM7:TR?= M4PmbmROW09? NELrS2RKSzVyPUGuN|AyKM7:TR?= MWexPVk6PjJ5Mh?=
RPMI 8226 MkXvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{jvUJ42KM7:TR?= NGf0TWlFVVOR MVHJR|UxRTFwMkmzJO69VQ>? MoGzNVk6QTZ{N{K=
HPAF-II NGT6OIFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHPFXmd,PSEQvF2= NULWSWF3TE2VTx?= M4fiXmlEPTB;MD62OFQh|ryP MUmxPVk6PjJ5Mh?=
SHP-77 NVXiUJY2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2jJcJ42KM7:TR?= NV\afoRvTE2VTx?= MXjJR|UxRTFwOEi4JO69VQ>? Ml;qNVk6QTZ{N{K=
U266 B1 M2jpSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYn+OUDPxE1? NXrSSVZ{TE2VTx?= NYLWUZpMUUN3ME2xMlY3QSEQvF2= NYPXWXJLOTl7OU[yO|I>
Hs700t NVO4NHNsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4j2W542KM7:TR?= NH;OTGxFVVOR M3fNNGlEPTB;MD6yN|Eh|ryP NGPad4UyQTl7NkK3Ni=>
NCI-446 NV\3dJptT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXzY[XF7hjVizszN NUK3SGVJTE2VTx?= MVXJR|UxRTFwMUW0JO69VQ>? NXPOS2V3OTl7OU[yO|I>
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BT474 (S) NXeyRlA1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4jhW542KM7:TR?= MX3EUXNQ NGDYO5dKSzVyPUKuOFA{KM7:TR?= NHPEUnoyQTl7NkK3Ni=>
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Rh18 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWTXPGlZhjFy4pEK{txO MX3JR|UxRTRwOU[gxtVO NFjJSIQzOTJ7OEe0OS=>
Rh30 NH7J[ZRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2jFPZ4yOOLCit88US=> NGqxSmRKSzVyPUCuNVkhyrWP NV3MUIN2OjF{OUi3OFU>
BT-12 M2LucGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEjZb25,OTEkgJtOwG0> NYrQTlZpUUN3ME2wMlc5KML3TR?= MlrpNlEzQTh5NEW=
CHLA-266 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1jwWp4yOOLCit88US=> MYTJR|UxRTBwOEmgxtVO NWPyZVVDOjF{OUi3OFU>
TC-71 NVnLbm1MT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmXSglEx6oDMzszN M2rLfGlEPTB;MD6xNUDDvU1? MmTuNlEzQTh5NEW=
CHLA-9 NFu1T4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{jndJ4yOOLCit88US=> MYfJR|UxRTBwMUKgxtVO NVTMOWxLOjF{OUi3OFU>
CHLA-10 NWTzR2ZkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUD+NVDjiIsQvF2= MVXJR|UxRTBwNkKgxtVO MVeyNVI6QDd2NR?=
CHLA-258 NIqySndIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NETYS|Z,OTEkgJtOwG0> MljDTWM2OD1yLkK3JOK2VQ>? NFHmc4wzOTJ7OEe0OS=>
GBM2 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2DYeJ4yOOLCit88US=> NG\mNVNKSzVyPUGuOFchyrWP MmrlNlEzQTh5NEW=
NB-1643 MojCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVHSTVBmhjFy4pEK{txO MV3JR|UxRTBwMUKgxtVO MXOyNVI6QDd2NR?=
NB-EBc1 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHf6cGN,OTEkgJtOwG0> MWHJR|UxRTBwM{WgxtVO MVuyNVI6QDd2NR?=
CHLA-90 M2Pw[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkTuglEx6oDMzszN MlnYTWM2OD1yLke3JOK2VQ>? NFjpVVgzOTJ7OEe0OS=>
CHLA-136 MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4\jUZ4yOOLCit88US=> NGr3Z49KSzVyPUCuOVIhyrWP NV61bWxTOjF{OUi3OFU>
NALM-6 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmnWglEx6oDMzszN M{XnNWlEPTB;MD60PUDDvU1? M{f0ZlIyOjl6N{S1
COG-LL-317 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MljRglEx6oDMzszN M1\CRWlEPTB;MT6zPEDDvU1? M4rH[|IyOjl6N{S1
RS4;11 NHfCOWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NG\IUpl,OTEkgJtOwG0> NV3VVHFFUUN3ME2wMlM5KML3TR?= NIOweGEzOTJ7OEe0OS=>
MOLT-4 M3TrO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYX+NVDjiIsQvF2= MX\JR|UxRTBwNUOgxtVO NYfrSY06OjF{OUi3OFU>
CCRF-CEM NITzRpZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{PIb54yOOLCit88US=> MnrJTWM2OD1zLkGzJOK2VQ>? NEHCfoYzOTJ7OEe0OS=>
Kasumi-1 NIrIWYVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYX+NVDjiIsQvF2= NGrCeVJKSzVyPUGuNkDDvU1? NX;vfVJsOjF{OUi3OFU>
Karpas-299 NV3HN4Q2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlHVglEx6oDMzszN M2jxbmlEPTB;MT62OEDDvU1? NUXZVVBbOjF{OUi3OFU>
Ramos-RA1 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFvC[Hd,OTEkgJtOwG0> NVPoNHBYUUN3ME2xMlMyKML3TR?= NWfZNodGOjF{OUi3OFU>
Rh30  M4ezTWZ2dmO2aX;uJIF{e2G7 M1PROIlv\HWlZYOgZY4hcW6lcnXhd4Uhd2ZiU1\LJJBpd3OyaH;yfYxifGmxbh?= M{O0PFI2QTJ3M{e4
Rh41 MUDGeY5kfGmxbjDhd5NigQ>? NX7iPYZEcW6mdXPld{BidiCrbnPy[YF{\SCxZjDTSmsheGixc4Doc5J6dGG2aX;u MV2yOVkzPTN5OB?=
RD M1\3[GZ2dmO2aX;uJIF{e2G7 MmXRbY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w NIS3RXYzPTl{NUO3PC=>
A549 M37ZSGtqdmG|ZTDhd5NigQ>? MX[wMlXjiIsQvF2= MYDEUXNQ NHLtd5ZqdmirYnn0d{BKT0ZvSWKvTXIh[WO2aY\heIlwdg>? MlLlNlY6Ojh3N{i=
NCI-H358 MnzTT4lv[XOnIHHzd4F6 MXmwMlXjiIsQvF2= NIixfVFFVVOR NViweVMxcW6qaXLpeJMhUUeILVnSM2lTKGGldHn2ZZRqd25? MoG1NlY6Ojh3N{i=
A549 MUTGeY5kfGmxbjDhd5NigQ>? MkjPNE426oDMzszN MXHEUXNQ MmW0Z4F2e2W|IHGgZ49v[3W{cnXueEBl\WO{ZXHz[UBqdiCyaH;zdIhwenmuYYTl[EBCU1RiYX7kJGVTUw>? NHHyblkzPjl{OEW3PC=>
NCI-H358 NWPTNXh1TnWwY4Tpc44h[XO|YYm= NXvXO4dNOC534pEK{txO MV3EUXNQ NH:xPFhk[XW|ZYOgZUBkd26ldYLy[Y51KGSnY4LlZZNmKGmwIIDoc5NxcG:{eXzheIVlKEGNVDDhcoQhTVKN M{nocFI3QTJ6NUe4
A549 NGDwUI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH7IWY5,OTEkgJtOwG0> M1vmXWROW09? NUTvOIJEUUN3ME2wMlc3KM7:TR?= MUCyOlkzQDV5OB?=
NCI-H358 NWPaTGN4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVP+NVDjiIsQvF2= MmXvSG1UVw>? M37mcGlEPTB;MT6wPUDPxE1? NITPUYozPjl{OEW3PC=>
A549 MonvRZBweHSxc3nzJIF{e2G7 NVLiTY85OC534pEK{txO NFjrcnZFVVOR NHHwdFlqdmS3Y3XzJGFxd3C2b4Ppdy=> NVyzTYoyOjZ7Mki1O|g>
NCI-H358 MV7BdI9xfG:|aYOgZZN{[Xl? MkPjNE426oDMzszN NFHDfo1FVVOR M3rkZ4lv\HWlZYOgRZBweHSxc3nz MoH6NlY6Ojh3N{i=
A549 MmjOSpVv[3Srb36gZZN{[Xl? NGD5XXAxNjYkgJtOwG0> M2T2e2ROW09? M{j3UZJm\HWlZYOge492dmRiY3zvd5Vz\Q>? MYOyOlkzQDV5OB?=
NCI-H358 M4rjdmZ2dmO2aX;uJIF{e2G7 NHTCZZExNjYkgJtOwG0> MWLEUXNQ M{\nVJJm\HWlZYOge492dmRiY3zvd5Vz\Q>? NGjUZYozPjl{OEW3PC=>

... 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:
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
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
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
NCT00898716 Completed Neoplasms Bristol-Myers Squibb September 2009 Phase 1
NCT00788333 Completed Breast Cancer Bristol-Myers Squibb July 2009 Phase 1|Phase 2
NCT00793897 Completed Advanced Solid Tumors|Metastatic Solid Tumors Bristol-Myers Squibb April 2009 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID