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 NUPrNohMU2mwYYPlJIF{e2G7 NW\sVIo1cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDJS2YuOVJiKFnDOVAhRSBzM37NLUBidmRidHjlJIRwf26|dILlZY0hfGG{Z3X0d{BCc3RiKFnDOVAhRSB{Mn7NLUBidmRiTVHQT{ApUUN3MDC9JFE{dk1r MXKxPVc4QDB{NB?=
IGF-Sal MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVrJR|UxRTdibl2= M{HNZ|E6Pzd6MEK0
CCRF-CEM (ALL) MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHnjZox,PSEQvF2= NX7aXWJNTE2VTx?= NFz2bIhKSzVyPUGuNlM6KM7:TR?= M1;rOVE6QTl4Mkey
PC3 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUf+OUDPxE1? MXTEUXNQ NUXiflVPUUN3ME2wMlk3PSEQvF2= NUe5NGxqOTl7OU[yO|I>
JD NYPpNmQ2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2GwN542KM7:TR?= MVrEUXNQ NGezNHVKSzVyPUCuN|kyKM7:TR?= M{eyNVE6QTl4Mkey
DU145 NVTrTY5OT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmL4glUh|ryP NEKxRm1FVVOR NFT5dJZKSzVyPUGuOFY2KM7:TR?= M4nGUFE6QTl4Mkey
KAG NH\WNHVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWX+OUDPxE1? M{DZSmROW09? MVTJR|UxRTFwNk[1JO69VQ>? MWmxPVk6PjJ5Mh?=
K-562 (CML) NUjuXoRvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFr6SYx,PSEQvF2= NV24XGJTTE2VTx?= MXjJR|UxRTJwM{CyJO69VQ>? NHfoSVAyQTl7NkK3Ni=>
B6-P210 (Murine ALL) NFjRXVNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFP1Wlh,PSEQvF2= MlvhSG1UVw>? Mn;FTWM2OD1zLkK5N{DPxE1? NIjlPYcyQTl7NkK3Ni=>
LN CAP-FGC M3TlfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGPmRYR,PSEQvF2= NHXIfWdFVVOR NIDMNY1KSzVyPUGuOFM1KM7:TR?= M3LPfVE6QTl4Mkey
VW MmHrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVn+OUDPxE1? MUjEUXNQ MknkTWM2OD1yLkCxPUDPxE1? NUPISWJJOTl7OU[yO|I>
MV411 (B Myelomonocytic) NXvzb2ViT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYPU[FhrhjVizszN NGfheW1FVVOR MnPhTWM2OD1yLkOzJO69VQ>? NETRWooyQTl7NkK3Ni=>
MDA-PCa-2b NGDhZVJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlW3glUh|ryP MlzESG1UVw>? M2q4b2lEPTB;MD6wPVgh|ryP Mm\rNVk6QTZ{N{K=
LG NULjNHB2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYH+OUDPxE1? NH7KZmJFVVOR Mn[yTWM2OD1yLkCzPEDPxE1? MUixPVk6PjJ5Mh?=
RS411 (B cell precursor-ALL) NIHPVZJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHG3fZN,PSEQvF2= MUfEUXNQ NF\t[nlKSzVyPUCuNVAzKM7:TR?= M2nQb|E6QTl4Mkey
22-r-1 NIHqOJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVTxbWVQhjVizszN NX\JNo9FTE2VTx?= M4PRW2lEPTB;MD6xO|Uh|ryP MYexPVk6PjJ5Mh?=
5838 M1L2bGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M37WdZ42KM7:TR?= MmTkSG1UVw>? NELaS3lKSzVyPUCuNFM1KM7:TR?= MnryNVk6QTZ{N{K=
P388 (Murine) NUX1VHdMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVW5PIE2hjVizszN NX7scYVTTE2VTx?= MkflTWM2OD12LkK3JO69VQ>? NF71d24yQTl7NkK3Ni=>
A2780/S NVfxZ4Z6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{T1Tp42KM7:TR?= NHPHPHJFVVOR MnLiTWM2OD1yLkGyNkDPxE1? NXTQTFBtOTl7OU[yO|I>
RDES NXrY[WtUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2rGWJ42KM7:TR?= MoTlSG1UVw>? MnX5TWM2OD1yLkCxNkDPxE1? MojrNVk6QTZ{N{K=
B6-T315I (Murine B-ALL) MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV61Xo1IhjVizszN M13XW2ROW09? Mn25TWM2OD1{LkizJO69VQ>? MUCxPVk6PjJ5Mh?=
TOV 112D MlfNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXjO[YFRhjVizszN Mnu1SG1UVw>? MXvJR|UxRTJwMUS2JO69VQ>? Ml\VNVk6QTZ{N{K=
TC32 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{XCcJ42KM7:TR?= MmriSG1UVw>? M1nscGlEPTB;MD6wNFgh|ryP M{LOOVE6QTl4Mkey
HL60 (acute myelocytic) M{O1d2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUT+OUDPxE1? MlvOSG1UVw>? NGTnUnZKSzVyPUCuNVIh|ryP NGXCUZEyQTl7NkK3Ni=>
TOV 21G MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYH+OUDPxE1? NYnhRY9lTE2VTx?= Mn\zTWM2OD12LkK3PUDPxE1? MnfGNVk6QTZ{N{K=
TC71 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYX+OUDPxE1? NUjNNmw{TE2VTx?= NFPxVXVKSzVyPUCuNFE1KM7:TR?= NFTlSFUyQTl7NkK3Ni=>
HPN-ALL (T-cell) NF61NmRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVr+OUDPxE1? MlroSG1UVw>? MYPJR|UxRTBwNUKg{txO M4XKVVE6QTl4Mkey
A2780R NHTVfmpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWn+OUDPxE1? MV;EUXNQ M{nlOWlEPTB;MT61OlQh|ryP M3\jWlE6QTl4Mkey
Rh1 M2fyS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M37l[J42KM7:TR?= MYjEUXNQ NEXocnNKSzVyPUCuNFI4KM7:TR?= Mki2NVk6QTZ{N{K=
Kasumi-1 (acute myeloid) NIW1UpFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mlz3glUh|ryP M1vCd2ROW09? NGOwWmlKSzVyPUCuNVYh|ryP MUCxPVk6PjJ5Mh?=
sk-ov-3 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MW\+OUDPxE1? NEjO[WhFVVOR NGG0R5NKSzVyPUWuNUDPxE1? M1\BflE6QTl4Mkey
ME NEHXV2xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHjlPJN,PSEQvF2= MlH5SG1UVw>? M3vzWWlEPTB;MD6wNVUh|ryP NEnhe|IyQTl7NkK3Ni=>
L1210 (Murine lymphocytic) NYXiWo5iT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnvaglUh|ryP NVPLT3NETE2VTx?= MkjWTWM2OD1{LkO5JO69VQ>? NYTHNVJGOTl7OU[yO|I>
sw-626 NYHOT2lCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEHhWFZ,PSEQvF2= NGr4XnNFVVOR NWHBUFVtUUN3ME2yMlMxPiEQvF2= MUCxPVk6PjJ5Mh?=
CTR M2fCd2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXXt[Wo{hjVizszN M{XreWROW09? NVvzZnhGUUN3ME2wMlI2OyEQvF2= NV;n[nRQOTl7OU[yO|I>
ML2 (Myelomonocytic) NXToVmdUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYr+OUDPxE1? MmDVSG1UVw>? MX;JR|UxRTBwMEmg{txO NEj4d40yQTl7NkK3Ni=>
ovcar-3 M2C1Vmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYX+OUDPxE1? NHjtV3FFVVOR M1nOeGlEPTB;NTFOwG0> NV\rW4x5OTl7OU[yO|I>
Rh36 NWfvUFRkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2nYOp42KM7:TR?= Mk[5SG1UVw>? NXXSNJFOUUN3ME2xMlQ{OiEQvF2= M2fyPFE6QTl4Mkey
MOLM-13 (acute myeloid) MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWT+OUDPxE1? MWfEUXNQ MojMTWM2OD1yLkSyJO69VQ>? NGey[4UyQTl7NkK3Ni=>
ovcar-4 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYroPXo4hjVizszN MnLTSG1UVw>? NG\rcGJKSzVyPUGg{txO M{T4N|E6QTl4Mkey
Rh41 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXuglUh|ryP NGq2Vm9FVVOR M1XVTWlEPTB;MD6wNFUh|ryP NVHnVnJ5OTl7OU[yO|I>
Mutz 2 (acute myeloid) MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGXpVXB,PSEQvF2= M3fnZ2ROW09? MX\JR|UxRTFwMUWg{txO MXSxPVk6PjJ5Mh?=
ovcar-5 NUfTTVZlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUf+OUDPxE1? NXjucIJWTE2VTx?= MVjJR|UxRTBwMEWg{txO Mk[xNVk6QTZ{N{K=
RD1 NVnKXos5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGPEPZV,PSEQvF2= MnfCSG1UVw>? MkS5TWM2OD1yLkC2PEDPxE1? NXzRZ5M3OTl7OU[yO|I>
OCI-AML 2 (acute myeloid) NVPZOGV4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mo\6glUh|ryP NUTrTVlRTE2VTx?= M3fKdmlEPTB;Mz6zN{DPxE1? NITRWm0yQTl7NkK3Ni=>
786-O NYi0[|lXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX\zd2VUhjVizszN NHXVcJFFVVOR NWrZWnlQUUN3ME2xMlY1PyEQvF2= NGe1XHIyQTl7NkK3Ni=>
A673 M3qyTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUT+OUDPxE1? M1vmNWROW09? NH3lRnNKSzVyPUCuOFA5KM7:TR?= NWHV[YZSOTl7OU[yO|I>
TALL-1 (T-cell) NX7EdWNOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVize3dQhjVizszN MU\EUXNQ NHS0VmNKSzVyPUGuNlgh|ryP MnjVNVk6QTZ{N{K=
151-B MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkmzglUh|ryP M4O0[2ROW09? MoK3TWM2OD1{Lk[3JO69VQ>? MWWxPVk6PjJ5Mh?=
PFSK-1 MoLxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkfZglUh|ryP M1Ti[2ROW09? NGK5V45KSzVyPUCuNVMzKM7:TR?= Mn35NVk6QTZ{N{K=
THP-1 NUj6Z2RDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MW\+OUDPxE1? NVz4N4RqTE2VTx?= M{S0dmlEPTB;Nj61PEDPxE1? MX:xPVk6PjJ5Mh?=
HEK293 Mly4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGrlOFl,PSEQvF2= NEPvXIhFVVOR NHHSeGxKSzVyPUCuPVE2KM7:TR?= NXHrdolkOTl7OU[yO|I>
DAOY MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYGxfVdUhjVizszN MkDxSG1UVw>? MlflTWM2OD1zLkm3PUDPxE1? NFzSdXYyQTl7NkK3Ni=>
SET2 Ml;aS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmj4glUh|ryP M1q4SmROW09? NUHYWYJbUUN3ME2wMlI6QCEQvF2= NEL4[IgyQTl7NkK3Ni=>
HTB-46 MlqwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1P2R542KM7:TR?= M{jZfmROW09? MlPnTWM2OD13LkK1JO69VQ>? NHrvOmIyQTl7NkK3Ni=>
SK-NAS NXXadIlnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXT+OUDPxE1? NVPVOlg6TE2VTx?= NVTHPHRGUUN3ME2wMlQ6PyEQvF2= MVuxPVk6PjJ5Mh?=
CTLL2 MlXiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWrle28zhjVizszN M{DxfGROW09? MmDNTWM2OD5zLkCwJO69VQ>? MkDwNVk6QTZ{N{K=
HTB-47 NEDvOJRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVThN|J1hjVizszN NV\yeJZjTE2VTx?= NHnVO|lKSzVyPUKuNFU3KM7:TR?= MVKxPVk6PjJ5Mh?=
LAN-1 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEfZb|F,PSEQvF2= NEnCTZBFVVOR MWXJR|UxRTBwMESg{txO Mn3QNVk6QTZ{N{K=
ST486 NEXtdXBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFiweJF,PSEQvF2= MVXEUXNQ NYXmS4FuUUN3ME2xMlE6KM7:TR?= MnX5NVk6QTZ{N{K=
HS766T M1zKPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVHyXHE2hjVizszN MYnEUXNQ M3O2RmlEPTB;Mj6wNFEh|ryP NVHSV25sOTl7OU[yO|I>
IMR-32 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUTmR49[hjVizszN NYXXeHhHTE2VTx?= NGTyeo1KSzVyPUCuNlYyKM7:TR?= NVfibWRVOTl7OU[yO|I>
Daudi (Burkitt's) NYjRTHdLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4r0PZ42KM7:TR?= NWjzb|ZKTE2VTx?= NVS0T2s6UUN3ME2yMlY{PyEQvF2= NVf2VJN6OTl7OU[yO|I>
Aspc-1 MkfVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml3lglUh|ryP NFzpNJJFVVOR NFPSTXlKSzVyPUCuN|c6KM7:TR?= NVvT[o1YOTl7OU[yO|I>
SK-NSH M1\aPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3P5SZ42KM7:TR?= M{DsOGROW09? MWnJR|UxRTBwMUO5JO69VQ>? NEjTZ44yQTl7NkK3Ni=>
MEC-1 (Chronic B cell) NV3FflJFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NETDO2x,PSEQvF2= MYPEUXNQ NY\XR|dPUUN3ME2yMlY{PyEQvF2= MoTPNVk6QTZ{N{K=
Capan-2 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFHoeo1,PSEQvF2= NH:1fmdFVVOR M4DDUmlEPTB;MT63O|Qh|ryP MXKxPVk6PjJ5Mh?=
SHSY5Y NY[3OoJVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{P6UZ42KM7:TR?= M3m4fWROW09? MmLGTWM2OD1yLkGwOkDPxE1? M1HXZVE6QTl4Mkey
U937 (Histioocytic) M3LleGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYDKZ2FvhjVizszN NYm5WG5yTE2VTx?= NVXoe4pNUUN3ME61MlAxKM7:TR?= MoO2NVk6QTZ{N{K=
Bxpc-1 Moj2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEm1cFV,PSEQvF2= MXHEUXNQ NVPZUplNUUN3ME2xMlkzPCEQvF2= M2LMblE6QTl4Mkey
Bxpc-3 NVewUGt1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGLFPXB,PSEQvF2= NGHNbGJFVVOR MXTJR|UxRjVwMECg{txO Ml\yNVk6QTZ{N{K=
HTB-92 Ml\ZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXP+OUDPxE1? NFzi[21FVVOR M1H4NmlEPTB;MT6wNkDPxE1? MWqxPVk6PjJ5Mh?=
OCI-LY10 (B-cell) NFnIZ|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mor0glUh|ryP NYK4cZF7TE2VTx?= NWjYd25HUUN3ME2wMlQ2KM7:TR?= MoLGNVk6QTZ{N{K=
PANC-1 M4Hac2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2jkO542KM7:TR?= M3T4NmROW09? MmPBTWM2OD53LkCwJO69VQ>? M2n6dFE6QTl4Mkey
To184.T NG\3ZYZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVfEcYtxhjVizszN NGfLeIVFVVOR M3XEc2lEPTB;MD60Olkh|ryP MUCxPVk6PjJ5Mh?=
OCI-LY19 (B-cell) MnzMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MW\+OUDPxE1? NWnwOYNTTE2VTx?= M4\afWlEPTB;MD60JO69VQ>? NGS4Xo8yQTl7NkK3Ni=>
PANC-1 BM MkSzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXn+OUDPxE1? NWrQZXBwTE2VTx?= NXzUTFF{UUN3ME61MlAxKM7:TR?= NIDRcYEyQTl7NkK3Ni=>
SA-4 M1PSXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUXPdXc6hjVizszN MnjuSG1UVw>? MUDJR|UxRTFwM{CxJO69VQ>? MlKwNVk6QTZ{N{K=
RPMI 8226 M13LVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXn+OUDPxE1? Mn;uSG1UVw>? M{PsfmlEPTB;MT6yPVMh|ryP MknBNVk6QTZ{N{K=
HPAF-II MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2D4O542KM7:TR?= MULEUXNQ MY\JR|UxRTBwNkS0JO69VQ>? NGfNXnkyQTl7NkK3Ni=>
SHP-77 M4jnOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mm\YglUh|ryP NWDWSWpxTE2VTx?= MoDFTWM2OD1zLki4PEDPxE1? NV35RZNEOTl7OU[yO|I>
U266 B1 MmL2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWLWRldKhjVizszN NH7nOYFFVVOR MYHJR|UxRTFwNk[5JO69VQ>? NFPFeXUyQTl7NkK3Ni=>
Hs700t M1ewNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3vQeZ42KM7:TR?= MWfEUXNQ M2PsZWlEPTB;MD6yN|Eh|ryP NXSxXnl1OTl7OU[yO|I>
NCI-446 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NILNeJh,PSEQvF2= MojqSG1UVw>? MmjYTWM2OD1zLkG1OEDPxE1? M{DjR|E6QTl4Mkey
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Rh18 M{P6XWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmrhglEx6oDMzszN MXLJR|UxRTRwOU[gxtVO NFz3RmEzOTJ7OEe0OS=>
Rh30 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUX+NVDjiIsQvF2= NE\EPXZKSzVyPUCuNVkhyrWP NUXp[npROjF{OUi3OFU>
BT-12 NHfRbYhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnTpglEx6oDMzszN M1TWPWlEPTB;MD63PEDDvU1? MkT0NlEzQTh5NEW=
CHLA-266 NUHp[pdXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3fyTZ4yOOLCit88US=> NFnyNHBKSzVyPUCuPFkhyrWP NUnHdldJOjF{OUi3OFU>
TC-71 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NILWRo5,OTEkgJtOwG0> MUHJR|UxRTBwMUGgxtVO MkS4NlEzQTh5NEW=
CHLA-9 M1OzV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MknYglEx6oDMzszN NWrl[owzUUN3ME2wMlEzKML3TR?= M2\ORVIyOjl6N{S1
CHLA-10 M4DXbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{[3fJ4yOOLCit88US=> NGCyTIhKSzVyPUCuOlIhyrWP MonXNlEzQTh5NEW=
CHLA-258 NHTCPVNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1rHU54yOOLCit88US=> MnuwTWM2OD1yLkK3JOK2VQ>? MmT0NlEzQTh5NEW=
GBM2 NFzHS3lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MljUglEx6oDMzszN NWfm[HBsUUN3ME2xMlQ4KML3TR?= NHz1R2EzOTJ7OEe0OS=>
NB-1643 NVvoWoJDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml\MglEx6oDMzszN M3zPW2lEPTB;MD6xNkDDvU1? NIToOpUzOTJ7OEe0OS=>
NB-EBc1 M2PxT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVvqU|Z5hjFy4pEK{txO NHzKOI5KSzVyPUCuN|UhyrWP NXXQW2d3OjF{OUi3OFU>
CHLA-90 NYTxe3ByT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{i2Vp4yOOLCit88US=> MnH5TWM2OD1yLke3JOK2VQ>? MnXkNlEzQTh5NEW=
CHLA-136 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEHqV25,OTEkgJtOwG0> M335SWlEPTB;MD61NkDDvU1? NXvZPIJMOjF{OUi3OFU>
NALM-6 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWjnOmtMhjFy4pEK{txO NYDI[5Z1UUN3ME2wMlQ6KML3TR?= M4HhRVIyOjl6N{S1
COG-LL-317 NV3tRVdOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVz5XZpNhjFy4pEK{txO NFvoPJJKSzVyPUGuN|ghyrWP MX:yNVI6QDd2NR?=
RS4;11 NXvQfFJ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mo\ZglEx6oDMzszN MoT1TWM2OD1yLkO4JOK2VQ>? M3X5fVIyOjl6N{S1
MOLT-4 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkW4glEx6oDMzszN NUHKVng5UUN3ME2wMlU{KML3TR?= M16yWFIyOjl6N{S1
CCRF-CEM NHXxbWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2qwfZ4yOOLCit88US=> MYTJR|UxRTFwMUOgxtVO NWXJflRSOjF{OUi3OFU>
Kasumi-1 NGLNS4pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYf+NVDjiIsQvF2= MVvJR|UxRTFwMjFCuW0> M1TqWVIyOjl6N{S1
Karpas-299 NGjZO2NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIXZT3R,OTEkgJtOwG0> NV7sdIRqUUN3ME2xMlY1KML3TR?= M4izfFIyOjl6N{S1
Ramos-RA1 M2fTVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUf+NVDjiIsQvF2= NH3lbWJKSzVyPUGuN|EhyrWP MUSyNVI6QDd2NR?=
Rh30  MYfGeY5kfGmxbjDhd5NigQ>? M2jueIlv\HWlZYOgZY4hcW6lcnXhd4Uhd2ZiU1\LJJBpd3OyaH;yfYxifGmxbh?= NIP1[oczPTl{NUO3PC=>
Rh41 MnrJSpVv[3Srb36gZZN{[Xl? M3nqUIlv\HWlZYOgZY4hcW6lcnXhd4Uhd2ZiU1\LJJBpd3OyaH;yfYxifGmxbh?= NGeyPYIzPTl{NUO3PC=>
RD NIH6OnhHfW6ldHnvckBie3OjeR?= NWS3OIh[cW6mdXPld{BidiCrbnPy[YF{\SCxZjDTSmsheGixc4Doc5J6dGG2aX;u MU[yOVkzPTN5OB?=
A549 MYnLbY5ie2ViYYPzZZk> MnLINE426oDMzszN MWDEUXNQ MnHHbY5pcWKrdIOgTWdHNUmUL1nSJIFkfGm4YYTpc44> NVn2RYtbOjZ7Mki1O|g>
NCI-H358 NXXnWnhwU2mwYYPlJIF{e2G7 NEm1OYExNjYkgJtOwG0> NHP6V|RFVVOR MlrabY5pcWKrdIOgTWdHNUmUL1nSJIFkfGm4YYTpc44> NIDxXZEzPjl{OEW3PC=>
A549 MmnDSpVv[3Srb36gZZN{[Xl? MnPjNE426oDMzszN MYDEUXNQ NXz3TZV4[2G3c3XzJIEh[2:wY4XydoVvfCCmZXPy[YF{\SCrbjDwbI9{eGixconsZZRm\CCDS2SgZY5lKEWUSx?= NV3oephVOjZ7Mki1O|g>
NCI-H358 NX3jVIY{TnWwY4Tpc44h[XO|YYm= MV6wMlXjiIsQvF2= MoPGSG1UVw>? M{jWS4NifXOnczDhJINwdmO3coLlcpQh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSUuWIHHu[EBGWkt? NWfxfJdiOjZ7Mki1O|g>
A549 NH72fnVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXj+NVDjiIsQvF2= NUjFV5NmTE2VTx?= MWnJR|UxRTBwN{[g{txO M{fxXFI3QTJ6NUe4
NCI-H358 NILsc29Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1HJfJ4yOOLCit88US=> MW\EUXNQ M{PmSmlEPTB;MT6wPUDPxE1? NYXrXWE4OjZ7Mki1O|g>
A549 NUnPVHV6SXCxcITvd4l{KGG|c3H5 M1W1eVAvPeLCit88US=> NVnSSYFLTE2VTx?= MorxbY5lfWOnczDBdI9xfG:|aYO= NXLReIV6OjZ7Mki1O|g>
NCI-H358 NF7me2hCeG:ydH;zbZMh[XO|YYm= MXWwMlXjiIsQvF2= M3rISGROW09? MlnCbY5lfWOnczDBdI9xfG:|aYO= NFXwd4kzPjl{OEW3PC=>
A549 MYTGeY5kfGmxbjDhd5NigQ>? NWS3UGxiOC534pEK{txO NWPCTHBZTE2VTx?= NGD6cFZz\WS3Y3XzJJdwfW6mIHPsc5N2emV? NWizRmhiOjZ7Mki1O|g>
NCI-H358 MnnMSpVv[3Srb36gZZN{[Xl? NG\vXGQxNjYkgJtOwG0> MnToSG1UVw>? NIrLZppz\WS3Y3XzJJdwfW6mIHPsc5N2emV? NILjVI0zPjl{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
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
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