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 NVPDcHdkU2mwYYPlJIF{e2G7 MXjpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEmJRj2xVkApUUN3MDC9JFE{dk1rIHHu[EB1cGViZH;3cpN1emWjbTD0ZZJo\XS|IFHreEApUUN3MDC9JFIzdk1rIHHu[EBOSVCNIDjJR|UxKD1iMUPuUUk> NEn6WlYyQTd5OECyOC=>
IGF-Sal M4HLOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{nBSmlEPTB;NzDuUS=> MWWxPVc4QDB{NB?=
CCRF-CEM (ALL) MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3\JXp42KM7:TR?= M4Pud2ROW09? NX24emg{UUN3ME2xMlI{QSEQvF2= MXKxPVk6PjJ5Mh?=
PC3 M1rSXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHnjN4h,PSEQvF2= MUXEUXNQ MWLJR|UxRTBwOU[1JO69VQ>? M{LTe|E6QTl4Mkey
JD Mlu3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEXCNI9,PSEQvF2= NUDORW1[TE2VTx?= MWDJR|UxRTBwM{mxJO69VQ>? Mnu3NVk6QTZ{N{K=
DU145 NEfkVoZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYf+OUDPxE1? M1uz[2ROW09? MV;JR|UxRTFwNE[1JO69VQ>? MXyxPVk6PjJ5Mh?=
KAG MmPkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFjjd4d,PSEQvF2= MljzSG1UVw>? NGDVU3BKSzVyPUGuOlY2KM7:TR?= Mn\PNVk6QTZ{N{K=
K-562 (CML) MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3jpSp42KM7:TR?= NYPxNpFUTE2VTx?= NX\5NlhMUUN3ME2yMlMxOiEQvF2= NGGzcFkyQTl7NkK3Ni=>
B6-P210 (Murine ALL) Ml;tS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MofCglUh|ryP MVfEUXNQ NVzPWph2UUN3ME2xMlI6OyEQvF2= NHHzVXIyQTl7NkK3Ni=>
LN CAP-FGC NFmzc|FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPFPYZ,PSEQvF2= MVnEUXNQ M2jnT2lEPTB;MT60N|Qh|ryP NEnBZWwyQTl7NkK3Ni=>
VW MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{ezZZ42KM7:TR?= NGfqTHlFVVOR NGnvUVFKSzVyPUCuNFE6KM7:TR?= MVuxPVk6PjJ5Mh?=
MV411 (B Myelomonocytic) NUjDZYh7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF7EeJp,PSEQvF2= NVTacWVoTE2VTx?= MkXkTWM2OD1yLkOzJO69VQ>? MlPINVk6QTZ{N{K=
MDA-PCa-2b M3KyVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmrQglUh|ryP NVLWc41kTE2VTx?= NGHKW2lKSzVyPUCuNFk5KM7:TR?= M4\DS|E6QTl4Mkey
LG NVXIOFdpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV7tbGw1hjVizszN NWTvSVhpTE2VTx?= NGO3[IlKSzVyPUCuNFM5KM7:TR?= MoT0NVk6QTZ{N{K=
RS411 (B cell precursor-ALL) NXv0cmxlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3:3d542KM7:TR?= NGXFNI1FVVOR MX;JR|UxRTBwMUCyJO69VQ>? NH\EW4gyQTl7NkK3Ni=>
22-r-1 M1nIOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2T4Zp42KM7:TR?= NX3VPZYzTE2VTx?= MlPITWM2OD1yLkG3OUDPxE1? NXrNU|l2OTl7OU[yO|I>
5838 M4fCWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUn+OUDPxE1? MXfEUXNQ M2S4N2lEPTB;MD6wN|Qh|ryP NVrnT4tlOTl7OU[yO|I>
P388 (Murine) NETURo9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{DRTp42KM7:TR?= NX7SVm42TE2VTx?= NYr1V5BkUUN3ME20MlI4KM7:TR?= M2HyXFE6QTl4Mkey
A2780/S M33CPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2frcJ42KM7:TR?= NEW3W2ZFVVOR MlfxTWM2OD1yLkGyNkDPxE1? NWf1ZVVLOTl7OU[yO|I>
RDES Mnr0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mlr1glUh|ryP M{m0T2ROW09? M4PpbWlEPTB;MD6wNVIh|ryP MnTxNVk6QTZ{N{K=
B6-T315I (Murine B-ALL) MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml;kglUh|ryP MoDVSG1UVw>? M{\aXWlEPTB;Mj64N{DPxE1? NGXJXY0yQTl7NkK3Ni=>
TOV 112D MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWD+OUDPxE1? Mlf5SG1UVw>? M2LP[2lEPTB;Mj6xOFYh|ryP NXe3cnVwOTl7OU[yO|I>
TC32 MojqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlPnglUh|ryP MWrEUXNQ M1fiTmlEPTB;MD6wNFgh|ryP M{CxXFE6QTl4Mkey
HL60 (acute myelocytic) NHvTdVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYr+OUDPxE1? MVzEUXNQ NWiyZpRCUUN3ME2wMlEzKM7:TR?= NI\aT2syQTl7NkK3Ni=>
TOV 21G MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWf+OUDPxE1? Ml;ESG1UVw>? MlPtTWM2OD12LkK3PUDPxE1? NWrLRnVvOTl7OU[yO|I>
TC71 NVfzeYJ3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGjWRnl,PSEQvF2= MYrEUXNQ MWLJR|UxRTBwMEG0JO69VQ>? M{DmZlE6QTl4Mkey
HPN-ALL (T-cell) MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEDNcIR,PSEQvF2= MVXEUXNQ NETI[W1KSzVyPUCuOVIh|ryP M1PINlE6QTl4Mkey
A2780R NFTIXpdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFHkSlJ,PSEQvF2= NHq5SGJFVVOR M1n4SGlEPTB;MT61OlQh|ryP NFXJU28yQTl7NkK3Ni=>
Rh1 MnLhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUH+OUDPxE1? M3vvUGROW09? NXX0Zph3UUN3ME2wMlAzPyEQvF2= Ml65NVk6QTZ{N{K=
Kasumi-1 (acute myeloid) MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mo\nglUh|ryP NIrHVGpFVVOR NYezbnh5UUN3ME2wMlE3KM7:TR?= Mn6yNVk6QTZ{N{K=
sk-ov-3 NGn4[m9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M13UeJ42KM7:TR?= NF;BOI5FVVOR MknQTWM2OD13LkGg{txO MlPNNVk6QTZ{N{K=
ME MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVX+OUDPxE1? NFrvS|VFVVOR M33xWWlEPTB;MD6wNVUh|ryP M2LTdFE6QTl4Mkey
L1210 (Murine lymphocytic) M4q3OWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX;2SINHhjVizszN MVvEUXNQ M4LBXWlEPTB;Mj6zPUDPxE1? MV:xPVk6PjJ5Mh?=
sw-626 MlHNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2fsS542KM7:TR?= Mnv5SG1UVw>? MnnGTWM2OD1{LkOwOkDPxE1? MnexNVk6QTZ{N{K=
CTR MnTxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX;+OUDPxE1? NFPIUXlFVVOR M2TOWWlEPTB;MD6yOVMh|ryP MkfGNVk6QTZ{N{K=
ML2 (Myelomonocytic) NHPmVlVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXvM[m01hjVizszN MYrEUXNQ MkTGTWM2OD1yLkC5JO69VQ>? MlXaNVk6QTZ{N{K=
ovcar-3 NXG5PJFrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3\MOJ42KM7:TR?= MX;EUXNQ M1zOWmlEPTB;NTFOwG0> MUexPVk6PjJ5Mh?=
Rh36 NIrrfHBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1ziOJ42KM7:TR?= MlLySG1UVw>? MkLETWM2OD1zLkSzNkDPxE1? MYSxPVk6PjJ5Mh?=
MOLM-13 (acute myeloid) NUfKZm9GT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnPkglUh|ryP NX\ZbJQyTE2VTx?= M3\ofGlEPTB;MD60NkDPxE1? MXixPVk6PjJ5Mh?=
ovcar-4 NHLmUGZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFXER3V,PSEQvF2= NXTIcFl{TE2VTx?= M{\l[mlEPTB;MTFOwG0> MkDoNVk6QTZ{N{K=
Rh41 MlvjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV7hV|UxhjVizszN MVvEUXNQ NELXbpBKSzVyPUCuNFA2KM7:TR?= NHPRe|QyQTl7NkK3Ni=>
Mutz 2 (acute myeloid) NXHzOWtxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUn+OUDPxE1? MnqzSG1UVw>? MUTJR|UxRTFwMUWg{txO NEOxR5cyQTl7NkK3Ni=>
ovcar-5 M1LIfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIe1bYR,PSEQvF2= MnvoSG1UVw>? M134[WlEPTB;MD6wOUDPxE1? M1zDU|E6QTl4Mkey
RD1 NEHQOIdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NI\mWIF,PSEQvF2= MnLwSG1UVw>? MmP2TWM2OD1yLkC2PEDPxE1? Mk\tNVk6QTZ{N{K=
OCI-AML 2 (acute myeloid) MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3nWcp42KM7:TR?= M3nTNGROW09? MUTJR|UxRTNwM{Og{txO NGe4WHgyQTl7NkK3Ni=>
786-O MoHyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4O2WJ42KM7:TR?= NIX2cFhFVVOR NH[wXnRKSzVyPUGuOlQ4KM7:TR?= M17DOFE6QTl4Mkey
A673 MonvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnHxglUh|ryP MlXMSG1UVw>? MUPJR|UxRTBwNEC4JO69VQ>? NF3BVHMyQTl7NkK3Ni=>
TALL-1 (T-cell) M2OyUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1L0Xp42KM7:TR?= MVPEUXNQ M4TkeGlEPTB;MT6yPEDPxE1? MkfkNVk6QTZ{N{K=
151-B MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnHUglUh|ryP MYnEUXNQ NX7RT5o3UUN3ME2yMlY4KM7:TR?= MWCxPVk6PjJ5Mh?=
PFSK-1 M1jFWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUP+OUDPxE1? NWHxSYVKTE2VTx?= MWPJR|UxRTBwMUOyJO69VQ>? NF3sb5UyQTl7NkK3Ni=>
THP-1 Mmj2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M33CNZ42KM7:TR?= NFLIUopFVVOR NUn0XnI{UUN3ME22MlU5KM7:TR?= MV:xPVk6PjJ5Mh?=
HEK293 Ml7iS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkLzglUh|ryP NWHNVXU1TE2VTx?= MXXJR|UxRTBwOUG1JO69VQ>? NHfzcoUyQTl7NkK3Ni=>
DAOY NYDsdXJCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnO1glUh|ryP NWHUWXZqTE2VTx?= MknuTWM2OD1zLkm3PUDPxE1? M4i0blE6QTl4Mkey
SET2 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWW5UXB5hjVizszN MYjEUXNQ MWPJR|UxRTBwMkm4JO69VQ>? NYPTUHh{OTl7OU[yO|I>
HTB-46 NXTCeXdLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFi1eJh,PSEQvF2= NHvweHVFVVOR NXfCTW15UUN3ME21MlI2KM7:TR?= NF;ER|AyQTl7NkK3Ni=>
SK-NAS M4nUUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV7+OUDPxE1? NUTGUlNCTE2VTx?= M2qzfmlEPTB;MD60PVch|ryP NVO5T4tQOTl7OU[yO|I>
CTLL2 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX7RR243hjVizszN MWHEUXNQ NVey[lJkUUN3ME6xMlAxKM7:TR?= NYP0SIF4OTl7OU[yO|I>
HTB-47 NXzwUY93T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4nHWJ42KM7:TR?= M{LIfWROW09? NULUcItkUUN3ME2yMlA2PiEQvF2= NGXDTlUyQTl7NkK3Ni=>
LAN-1 NGn1WGdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEHGXVR,PSEQvF2= MVLEUXNQ MljOTWM2OD1yLkC0JO69VQ>? MmnkNVk6QTZ{N{K=
ST486 NW\PWI81T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIe2PY1,PSEQvF2= NFja[3JFVVOR MlPGTWM2OD1zLkG5JO69VQ>? NH3SS3EyQTl7NkK3Ni=>
HS766T M3Lo[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1vYVZ42KM7:TR?= MYnEUXNQ NEfsVYZKSzVyPUKuNFAyKM7:TR?= MVqxPVk6PjJ5Mh?=
IMR-32 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWPVdYtuhjVizszN Mn[3SG1UVw>? MlrrTWM2OD1yLkK2NUDPxE1? M{X0fVE6QTl4Mkey
Daudi (Burkitt's) MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEnQbHR,PSEQvF2= MXvEUXNQ NWnGfoRiUUN3ME2yMlY{PyEQvF2= NI[yVlAyQTl7NkK3Ni=>
Aspc-1 M{n4ZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVvpPFJZhjVizszN MmT3SG1UVw>? M{X0bmlEPTB;MD6zO|kh|ryP MmDZNVk6QTZ{N{K=
SK-NSH M{joXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkLxglUh|ryP MWXEUXNQ MYTJR|UxRTBwMUO5JO69VQ>? MVWxPVk6PjJ5Mh?=
MEC-1 (Chronic B cell) NVq5VJp2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUjDZ5BjhjVizszN NIS0SIlFVVOR NYr0eIhbUUN3ME2yMlY{PyEQvF2= MWmxPVk6PjJ5Mh?=
Capan-2 M1\C[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUj1SnY5hjVizszN MkjYSG1UVw>? M{PXUmlEPTB;MT63O|Qh|ryP NHm5[pEyQTl7NkK3Ni=>
SHSY5Y NGTKbWpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4HYXZ42KM7:TR?= MmnZSG1UVw>? Mny3TWM2OD1yLkGwOkDPxE1? MnX4NVk6QTZ{N{K=
U937 (Histioocytic) MoTVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX7+OUDPxE1? MkjTSG1UVw>? MV;JR|UxRjVwMECg{txO MX:xPVk6PjJ5Mh?=
Bxpc-1 NXjnVFZCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV;+OUDPxE1? MkXySG1UVw>? MXfJR|UxRTFwOUK0JO69VQ>? M{C2RVE6QTl4Mkey
Bxpc-3 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnO5glUh|ryP NGnnbplFVVOR NEnUNYRKSzVyPkWuNFAh|ryP MXOxPVk6PjJ5Mh?=
HTB-92 M1;vN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFjHeHl,PSEQvF2= NYPjd|J6TE2VTx?= NUDT[ll5UUN3ME2xMlAzKM7:TR?= M3f4WVE6QTl4Mkey
OCI-LY10 (B-cell) MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4XjSZ42KM7:TR?= M2G4T2ROW09? M2L2PWlEPTB;MD60OUDPxE1? M3ezT|E6QTl4Mkey
PANC-1 MkjTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2DrcJ42KM7:TR?= MU\EUXNQ MkXKTWM2OD53LkCwJO69VQ>? NUnJ[XU4OTl7OU[yO|I>
To184.T NUDZ[HZ4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUT+OUDPxE1? MVrEUXNQ MWfJR|UxRTBwNE[5JO69VQ>? NFzDSZYyQTl7NkK3Ni=>
OCI-LY19 (B-cell) M2T3NGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXrYcZlmhjVizszN NF;jeIVFVVOR NF3j[ZBKSzVyPUCuOEDPxE1? MVqxPVk6PjJ5Mh?=
PANC-1 BM NGH2TVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVT+OUDPxE1? NH;zWmpFVVOR NILhVW9KSzVyPkWuNFAh|ryP MYSxPVk6PjJ5Mh?=
SA-4 MoHXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXr+OUDPxE1? MVrEUXNQ MVrJR|UxRTFwM{CxJO69VQ>? MWOxPVk6PjJ5Mh?=
RPMI 8226 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2C5Xp42KM7:TR?= NFLJXoFFVVOR Mkf3TWM2OD1zLkK5N{DPxE1? MVGxPVk6PjJ5Mh?=
HPAF-II NGDCXpZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2TRUp42KM7:TR?= MV\EUXNQ M3q0UmlEPTB;MD62OFQh|ryP NGS5Z2EyQTl7NkK3Ni=>
SHP-77 NYHleYRxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmLYglUh|ryP MlP2SG1UVw>? MU\JR|UxRTFwOEi4JO69VQ>? NInifW8yQTl7NkK3Ni=>
U266 B1 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHK5ZWh,PSEQvF2= NELKO5BFVVOR MWnJR|UxRTFwNk[5JO69VQ>? MnK4NVk6QTZ{N{K=
Hs700t MoSxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{HQe542KM7:TR?= NH71b2FFVVOR M2S0[mlEPTB;MD6yN|Eh|ryP NYnVWVRZOTl7OU[yO|I>
NCI-446 NXjTWlB7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUXCdZNLhjVizszN NVPPTnJMTE2VTx?= MYLJR|UxRTFwMUW0JO69VQ>? M1PmWlE6QTl4Mkey
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Rh18 NYHBd4xKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVm0cnNShjFy4pEK{txO NGDzO4lKSzVyPUSuPVYhyrWP M122SlIyOjl6N{S1
Rh30 M1XRUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVv+NVDjiIsQvF2= NUK1Spg2UUN3ME2wMlE6KML3TR?= Mn64NlEzQTh5NEW=
BT-12 M1W4dWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NE\Id2x,OTEkgJtOwG0> MoPxTWM2OD1yLke4JOK2VQ>? NXvKbVBEOjF{OUi3OFU>
CHLA-266 M1zkdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1u5OJ4yOOLCit88US=> MYfJR|UxRTBwOEmgxtVO NGq1cY8zOTJ7OEe0OS=>
TC-71 M3z1c2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1f5eJ4yOOLCit88US=> NGD0Z3RKSzVyPUCuNVEhyrWP MWiyNVI6QDd2NR?=
CHLA-9 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWXtTYc3hjFy4pEK{txO MnHkTWM2OD1yLkGyJOK2VQ>? M1KxZ|IyOjl6N{S1
CHLA-10 NVPvXHd3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWr+NVDjiIsQvF2= M{LS[mlEPTB;MD62NkDDvU1? MUWyNVI6QDd2NR?=
CHLA-258 NEi5PG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXHLZmkzhjFy4pEK{txO MnrRTWM2OD1yLkK3JOK2VQ>? MYWyNVI6QDd2NR?=
GBM2 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlXDglEx6oDMzszN NYnxR4ExUUN3ME2xMlQ4KML3TR?= M1vxTVIyOjl6N{S1
NB-1643 M4H2dWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGTPS2p,OTEkgJtOwG0> MV7JR|UxRTBwMUKgxtVO MWqyNVI6QDd2NR?=
NB-EBc1 NW\uc|NsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnjLglEx6oDMzszN NYTIbnZuUUN3ME2wMlM2KML3TR?= MYmyNVI6QDd2NR?=
CHLA-90 MkLiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3jndJ4yOOLCit88US=> NF3iWo5KSzVyPUCuO|chyrWP MYeyNVI6QDd2NR?=
CHLA-136 M{TNN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3ToTZ4yOOLCit88US=> M{PBRWlEPTB;MD61NkDDvU1? M{PsSFIyOjl6N{S1
NALM-6 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MW\+NVDjiIsQvF2= Mn7QTWM2OD1yLkS5JOK2VQ>? M3vNWFIyOjl6N{S1
COG-LL-317 M{P4WWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoXkglEx6oDMzszN M3zNbGlEPTB;MT6zPEDDvU1? MYSyNVI6QDd2NR?=
RS4;11 M1z5c2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH;kUnN,OTEkgJtOwG0> NHmwNlBKSzVyPUCuN|ghyrWP NVf5b5I3OjF{OUi3OFU>
MOLT-4 Ml7yS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWq0NmFUhjFy4pEK{txO MlH6TWM2OD1yLkWzJOK2VQ>? M2XyOlIyOjl6N{S1
CCRF-CEM MmHxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3i1cJ4yOOLCit88US=> MnnrTWM2OD1zLkGzJOK2VQ>? MnzhNlEzQTh5NEW=
Kasumi-1 Mnm3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn;XglEx6oDMzszN NXfuR|duUUN3ME2xMlIhyrWP MXyyNVI6QDd2NR?=
Karpas-299 NHGyeZlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml:0glEx6oDMzszN MmXoTWM2OD1zLk[0JOK2VQ>? M17zVlIyOjl6N{S1
Ramos-RA1 NIq1N3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFy1[WF,OTEkgJtOwG0> NFXLSo5KSzVyPUGuN|EhyrWP MkLENlEzQTh5NEW=
Rh30  NETaVXRHfW6ldHnvckBie3OjeR?= NHfV[nhqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:|cHjvdplt[XSrb36= MXmyOVkzPTN5OB?=
Rh41 NELySG9HfW6ldHnvckBie3OjeR?= NX75RZY5cW6mdXPld{BidiCrbnPy[YF{\SCxZjDTSmsheGixc4Doc5J6dGG2aX;u NXPJO3FNOjV7MkWzO|g>
RD M{D3NGZ2dmO2aX;uJIF{e2G7 M3e0OYlv\HWlZYOgZY4hcW6lcnXhd4Uhd2ZiU1\LJJBpd3OyaH;yfYxifGmxbh?= Mn\xNlU6OjV|N{i=
A549 MnPhT4lv[XOnIHHzd4F6 MWmwMlXjiIsQvF2= MYXEUXNQ M4ftPYlvcGmkaYTzJGlITi2LUj;JVkBi[3SrdnH0bY9v M2jNV|I3QTJ6NUe4
NCI-H358 NIfjUGdMcW6jc3WgZZN{[Xl? NFvXbJQxNjYkgJtOwG0> NInT[HpFVVOR M1\uPYlvcGmkaYTzJGlITi2LUj;JVkBi[3SrdnH0bY9v NGOwNHYzPjl{OEW3PC=>
A549 MkfpSpVv[3Srb36gZZN{[Xl? M3vkcFAvPeLCit88US=> MorFSG1UVw>? MYTjZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM MYSyOlkzQDV5OB?=
NCI-H358 NWHLXI1lTnWwY4Tpc44h[XO|YYm= MnvaNE426oDMzszN NUfubYh1TE2VTx?= MVzjZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM MV2yOlkzQDV5OB?=
A549 NFW1fVFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVP0fpAzhjFy4pEK{txO MVnEUXNQ MmfMTWM2OD1yLke2JO69VQ>? M3\qO|I3QTJ6NUe4
NCI-H358 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFSxdZR,OTEkgJtOwG0> NXOycXJNTE2VTx?= MVXJR|UxRTFwMEmg{txO M2DPPVI3QTJ6NUe4
A549 NVO0OGpHSXCxcITvd4l{KGG|c3H5 MVewMlXjiIsQvF2= M3Xsd2ROW09? Mnj4bY5lfWOnczDBdI9xfG:|aYO= NFyzXoszPjl{OEW3PC=>
NCI-H358 NEHpU|hCeG:ydH;zbZMh[XO|YYm= MoHnNE426oDMzszN M3;xOGROW09? NEm4XpBqdmS3Y3XzJGFxd3C2b4Ppdy=> NILSWIgzPjl{OEW3PC=>
A549 NXXNW|d[TnWwY4Tpc44h[XO|YYm= MYCwMlXjiIsQvF2= NIj2SZlFVVOR NXr3Z5hnemWmdXPld{B4d3WwZDDjcI9{fXKn NEn4T2UzPjl{OEW3PC=>
NCI-H358 M{fKfWZ2dmO2aX;uJIF{e2G7 MYKwMlXjiIsQvF2= NGr3fohFVVOR MVLy[YR2[2W|IIfveY5lKGOub4P1doU> M4fvNFI3QTJ6NUe4

... 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

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IGF-1R Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID