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 NYDvUXBGU2mwYYPlJIF{e2G7 NUPhO5p5cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDJS2YuOVJiKFnDOVAhRSBzM37NLUBidmRidHjlJIRwf26|dILlZY0hfGG{Z3X0d{BCc3RiKFnDOVAhRSB{Mn7NLUBidmRiTVHQT{ApUUN3MDC9JFE{dk1r MoHMNVk4PzhyMkS=
IGF-Sal NWnMcpo2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIPMTJJKSzVyPUegcm0> M2ixcVE6Pzd6MEK0
CCRF-CEM (ALL) MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1nW[J42KM7:TR?= NGfSS5ZFVVOR NF\KOXVKSzVyPUGuNlM6KM7:TR?= NHuyN24yQTl7NkK3Ni=>
PC3 MoqwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGPnfVh,PSEQvF2= M2TEW2ROW09? Mmj1TWM2OD1yLkm2OUDPxE1? NHu5SG8yQTl7NkK3Ni=>
JD MoTRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\DfJ42KM7:TR?= M{fo[2ROW09? NHXGclBKSzVyPUCuN|kyKM7:TR?= M1vRS|E6QTl4Mkey
DU145 MkjiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MofiglUh|ryP M17oOGROW09? NVfLcJpSUUN3ME2xMlQ3PSEQvF2= M3vISFE6QTl4Mkey
KAG NFLnUGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEfjZ4p,PSEQvF2= NE\MXIZFVVOR MlLvTWM2OD1zLk[2OUDPxE1? M{[0cFE6QTl4Mkey
K-562 (CML) M4n1S2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYP+OUDPxE1? MmW3SG1UVw>? Mlz1TWM2OD1{LkOwNkDPxE1? MmLsNVk6QTZ{N{K=
B6-P210 (Murine ALL) Mn;IS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2r4Tp42KM7:TR?= NIGyOVJFVVOR M3nBcmlEPTB;MT6yPVMh|ryP MmH6NVk6QTZ{N{K=
LN CAP-FGC NVO2OYFnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGTmS5N,PSEQvF2= M4L1PWROW09? M{SyOmlEPTB;MT60N|Qh|ryP NU\BfmJFOTl7OU[yO|I>
VW NGTmT|RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVLC[nJThjVizszN NGK5Z3VFVVOR NXT3PJduUUN3ME2wMlAyQSEQvF2= MojpNVk6QTZ{N{K=
MV411 (B Myelomonocytic) NIXZb2JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVvjb4ZGhjVizszN M2XSTmROW09? M{\PZ2lEPTB;MD6zN{DPxE1? NV\y[lRCOTl7OU[yO|I>
MDA-PCa-2b M2S1[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnXEglUh|ryP M2PjW2ROW09? M36xR2lEPTB;MD6wPVgh|ryP M1;HOVE6QTl4Mkey
LG NIWzbW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYnJOGlYhjVizszN M4jL[2ROW09? NHvK[FRKSzVyPUCuNFM5KM7:TR?= NEHkTVkyQTl7NkK3Ni=>
RS411 (B cell precursor-ALL) NE\PSpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1\RcJ42KM7:TR?= MXLEUXNQ M3yw[GlEPTB;MD6xNFIh|ryP NHrHNXMyQTl7NkK3Ni=>
22-r-1 NYH6OXRRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFH6eol,PSEQvF2= MkiySG1UVw>? M4DEVWlEPTB;MD6xO|Uh|ryP M2[2b|E6QTl4Mkey
5838 NXvEc|A3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUjYUodrhjVizszN NWT1PIF6TE2VTx?= NV3UXpN5UUN3ME2wMlA{PCEQvF2= MXixPVk6PjJ5Mh?=
P388 (Murine) NYnkXmxXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVT+OUDPxE1? MlnvSG1UVw>? NGrYdJNKSzVyPUSuNlch|ryP NYLsWYdDOTl7OU[yO|I>
A2780/S MnPLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXn+OUDPxE1? MVvEUXNQ NFzWR4pKSzVyPUCuNVIzKM7:TR?= NX;3WopkOTl7OU[yO|I>
RDES NUOxWmNxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M33PWp42KM7:TR?= MWjEUXNQ MkPxTWM2OD1yLkCxNkDPxE1? NISzfIUyQTl7NkK3Ni=>
B6-T315I (Murine B-ALL) NXHBZnNJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH63fmR,PSEQvF2= MlP2SG1UVw>? NYfEZ3dnUUN3ME2yMlg{KM7:TR?= M3T0bFE6QTl4Mkey
TOV 112D MnzwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M13nXJ42KM7:TR?= NEe1U|NFVVOR NWLYXFUzUUN3ME2yMlE1PiEQvF2= MnmyNVk6QTZ{N{K=
TC32 NUKz[HlPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXz+OUDPxE1? NELXcWZFVVOR NFizZ5NKSzVyPUCuNFA5KM7:TR?= NYfic4FtOTl7OU[yO|I>
HL60 (acute myelocytic) MkPBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoD2glUh|ryP MVfEUXNQ MmGyTWM2OD1yLkGyJO69VQ>? NHfTbnYyQTl7NkK3Ni=>
TOV 21G NVe0eGFsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkLxglUh|ryP NWL2bHpnTE2VTx?= Mn7iTWM2OD12LkK3PUDPxE1? MWexPVk6PjJ5Mh?=
TC71 NYHv[ZpsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkPiglUh|ryP NEjJb45FVVOR MoTsTWM2OD1yLkCxOEDPxE1? M4TqXFE6QTl4Mkey
HPN-ALL (T-cell) MlvFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUP+OUDPxE1? M{e2eGROW09? NHHKdFRKSzVyPUCuOVIh|ryP MWKxPVk6PjJ5Mh?=
A2780R M4TWdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVH+OUDPxE1? NXSzVlYzTE2VTx?= MWfJR|UxRTFwNU[0JO69VQ>? NIPIPZcyQTl7NkK3Ni=>
Rh1 NV3wTYVNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWiwWYxthjVizszN NIjqcIxFVVOR NVmxcWt{UUN3ME2wMlAzPyEQvF2= NX7pW41TOTl7OU[yO|I>
Kasumi-1 (acute myeloid) NF2zXI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFvZc41,PSEQvF2= M2Pt[mROW09? MXzJR|UxRTBwMU[g{txO MWexPVk6PjJ5Mh?=
sk-ov-3 NUfobGh3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoDTglUh|ryP MV3EUXNQ NUXnSYJ3UUN3ME21MlEh|ryP MmLGNVk6QTZ{N{K=
ME M3nW[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIC0W3l,PSEQvF2= NX;2ZnNzTE2VTx?= MlrCTWM2OD1yLkCxOUDPxE1? NGr0ZZoyQTl7NkK3Ni=>
L1210 (Murine lymphocytic) Mmj1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYr+OUDPxE1? M3PMSmROW09? MlHyTWM2OD1{LkO5JO69VQ>? NWf2RXI3OTl7OU[yO|I>
sw-626 M{XsVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVT+OUDPxE1? M2XBRmROW09? MoLTTWM2OD1{LkOwOkDPxE1? M2HUd|E6QTl4Mkey
CTR M3fEOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF30enR,PSEQvF2= NHizT2hFVVOR MW\JR|UxRTBwMkWzJO69VQ>? NHfRWYIyQTl7NkK3Ni=>
ML2 (Myelomonocytic) MljRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWL+OUDPxE1? MUXEUXNQ NGHoe3JKSzVyPUCuNFkh|ryP NVnabI9iOTl7OU[yO|I>
ovcar-3 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV3+OUDPxE1? MoHISG1UVw>? NHvOT3pKSzVyPUWg{txO NX;sUHpLOTl7OU[yO|I>
Rh36 NILVfoZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkXyglUh|ryP Mnj2SG1UVw>? NV;INY5yUUN3ME2xMlQ{OiEQvF2= MVqxPVk6PjJ5Mh?=
MOLM-13 (acute myeloid) NEnRNHFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MonzglUh|ryP MnTlSG1UVw>? M4G5[2lEPTB;MD60NkDPxE1? NIPLPWYyQTl7NkK3Ni=>
ovcar-4 NHnvfG1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1[xVZ42KM7:TR?= Mnq1SG1UVw>? NHLT[nVKSzVyPUGg{txO MnXsNVk6QTZ{N{K=
Rh41 NVnXS2FuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXj+OUDPxE1? MnflSG1UVw>? M{C1TGlEPTB;MD6wNFUh|ryP M4r4OVE6QTl4Mkey
Mutz 2 (acute myeloid) NX\MdlVwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M124Z542KM7:TR?= MWHEUXNQ Ml\1TWM2OD1zLkG1JO69VQ>? NYDlNWJTOTl7OU[yO|I>
ovcar-5 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4mx[542KM7:TR?= M3\H[mROW09? MlzFTWM2OD1yLkC1JO69VQ>? Mo\VNVk6QTZ{N{K=
RD1 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGHWUZd,PSEQvF2= MYfEUXNQ M{TMfmlEPTB;MD6wOlgh|ryP NUi0ZXNSOTl7OU[yO|I>
OCI-AML 2 (acute myeloid) NF7sUYJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlrVglUh|ryP NVjMTFBSTE2VTx?= MWTJR|UxRTNwM{Og{txO M3ywZVE6QTl4Mkey
786-O M4rZSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHvpVIF,PSEQvF2= MWXEUXNQ NVzqcpNUUUN3ME2xMlY1PyEQvF2= NYTwSXM2OTl7OU[yO|I>
A673 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEnLSpl,PSEQvF2= NGi4XGZFVVOR MoPHTWM2OD1yLkSwPEDPxE1? M4XjcFE6QTl4Mkey
TALL-1 (T-cell) Mni4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXz+OUDPxE1? Mk\USG1UVw>? M37nTGlEPTB;MT6yPEDPxE1? Ml\KNVk6QTZ{N{K=
151-B NIDYOopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3fkXZ42KM7:TR?= M{jGW2ROW09? MmXxTWM2OD1{Lk[3JO69VQ>? NXnHNm1DOTl7OU[yO|I>
PFSK-1 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFfBcXh,PSEQvF2= MlHsSG1UVw>? NUPHbI9pUUN3ME2wMlE{OiEQvF2= M{njZVE6QTl4Mkey
THP-1 NWX5RZlLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXz+OUDPxE1? M2XxVWROW09? NITtdIlKSzVyPU[uOVgh|ryP MWGxPVk6PjJ5Mh?=
HEK293 M{PqZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3nZcJ42KM7:TR?= MoD0SG1UVw>? NWXiZ5Z{UUN3ME2wMlkyPSEQvF2= NVzMXoVOOTl7OU[yO|I>
DAOY Ml\TS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX7+OUDPxE1? MXnEUXNQ NFHuW3dKSzVyPUGuPVc6KM7:TR?= MkXJNVk6QTZ{N{K=
SET2 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{jIbp42KM7:TR?= MUDEUXNQ NXXpeY9HUUN3ME2wMlI6QCEQvF2= NXG2dpBROTl7OU[yO|I>
HTB-46 NX2wRpg4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUXoe2FThjVizszN NGjwbGFFVVOR M{PkfmlEPTB;NT6yOUDPxE1? NVHDPVExOTl7OU[yO|I>
SK-NAS M1XjUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NE\GSHh,PSEQvF2= MY\EUXNQ M{XLfmlEPTB;MD60PVch|ryP NGjsT4kyQTl7NkK3Ni=>
CTLL2 NX\Hd3h1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4DUWp42KM7:TR?= NW\4VHdQTE2VTx?= NYfwc3RpUUN3ME6xMlAxKM7:TR?= NWrISo9iOTl7OU[yO|I>
HTB-47 MoPRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mn7ZglUh|ryP NI\yU2hFVVOR NHm1eHpKSzVyPUKuNFU3KM7:TR?= NHXOUGYyQTl7NkK3Ni=>
LAN-1 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4r6Zp42KM7:TR?= MX\EUXNQ M37UOmlEPTB;MD6wOEDPxE1? MWWxPVk6PjJ5Mh?=
ST486 NGDGUJlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGfheJB,PSEQvF2= M1mxSGROW09? MX3JR|UxRTFwMUmg{txO NFXVeIMyQTl7NkK3Ni=>
HS766T NHO5R|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnfuglUh|ryP NXvxTGVsTE2VTx?= M37lSWlEPTB;Mj6wNFEh|ryP NXKyfmtGOTl7OU[yO|I>
IMR-32 NELjeo9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYf+OUDPxE1? Ml\5SG1UVw>? NWf4[FNXUUN3ME2wMlI3OSEQvF2= MmjFNVk6QTZ{N{K=
Daudi (Burkitt's) MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXjJendyhjVizszN M3ThTGROW09? MXHJR|UxRTJwNkO3JO69VQ>? MYOxPVk6PjJ5Mh?=
Aspc-1 M3voXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIe2fGR,PSEQvF2= MkHkSG1UVw>? NH7ybWdKSzVyPUCuN|c6KM7:TR?= M3jvclE6QTl4Mkey
SK-NSH NEf5U3hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUXWbVN3hjVizszN MojlSG1UVw>? Mk\0TWM2OD1yLkGzPUDPxE1? NHzXR2wyQTl7NkK3Ni=>
MEC-1 (Chronic B cell) M1f6cGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnHQglUh|ryP NY\xTnBHTE2VTx?= M3PjN2lEPTB;Mj62N|ch|ryP NFjLT3gyQTl7NkK3Ni=>
Capan-2 NInrOXVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVT4NWVEhjVizszN M{TLXWROW09? M1LifmlEPTB;MT63O|Qh|ryP M{jY[FE6QTl4Mkey
SHSY5Y NH7iPJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIjVNIF,PSEQvF2= MXHEUXNQ M2TsRmlEPTB;MD6xNFYh|ryP MXSxPVk6PjJ5Mh?=
U937 (Histioocytic) MlfWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIDZ[JJ,PSEQvF2= M4LYbWROW09? NFn3SIJKSzVyPkWuNFAh|ryP MlizNVk6QTZ{N{K=
Bxpc-1 NX[0R3FCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFXTS4l,PSEQvF2= MWTEUXNQ MnXsTWM2OD1zLkmyOEDPxE1? MmLHNVk6QTZ{N{K=
Bxpc-3 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXCglUh|ryP MnLjSG1UVw>? M1vG[2lEPTB-NT6wNEDPxE1? NG[x[msyQTl7NkK3Ni=>
HTB-92 Ml;xS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mkn2glUh|ryP MV3EUXNQ MoHVTWM2OD1zLkCyJO69VQ>? NVPxW2wyOTl7OU[yO|I>
OCI-LY10 (B-cell) NYLOS2dET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn3zglUh|ryP NVnFOnprTE2VTx?= NWLITZhKUUN3ME2wMlQ2KM7:TR?= Mn7rNVk6QTZ{N{K=
PANC-1 NV\4VZJXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2fmPZ42KM7:TR?= NVixR2pWTE2VTx?= NYD5W2R2UUN3ME61MlAxKM7:TR?= MmW0NVk6QTZ{N{K=
To184.T NGHXeY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NE\aPXd,PSEQvF2= MkXvSG1UVw>? MlzETWM2OD1yLkS2PUDPxE1? NVHCNW41OTl7OU[yO|I>
OCI-LY19 (B-cell) M3noO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF7HWZB,PSEQvF2= MWTEUXNQ NF\NdmlKSzVyPUCuOEDPxE1? NEn0RnoyQTl7NkK3Ni=>
PANC-1 BM NWTtZnN2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4jkUp42KM7:TR?= MnTDSG1UVw>? NUjQbHEzUUN3ME61MlAxKM7:TR?= M2C3TlE6QTl4Mkey
SA-4 M2Pkc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGXWbGt,PSEQvF2= MXvEUXNQ MWDJR|UxRTFwM{CxJO69VQ>? MnHQNVk6QTZ{N{K=
RPMI 8226 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGrB[XB,PSEQvF2= MYHEUXNQ MonxTWM2OD1zLkK5N{DPxE1? NHvXWoMyQTl7NkK3Ni=>
HPAF-II MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXjTVXBvhjVizszN NGfodGRFVVOR Mn;1TWM2OD1yLk[0OEDPxE1? MmLoNVk6QTZ{N{K=
SHP-77 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3zycJ42KM7:TR?= NF3L[o1FVVOR NWm1b5ZlUUN3ME2xMlg5QCEQvF2= MmHuNVk6QTZ{N{K=
U266 B1 NYXHe3FQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MU\+OUDPxE1? M3TLZmROW09? NHrlRXNKSzVyPUGuOlY6KM7:TR?= MVKxPVk6PjJ5Mh?=
Hs700t NF74O21Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4rCWp42KM7:TR?= MoHISG1UVw>? NFK5e5JKSzVyPUCuNlMyKM7:TR?= M4LxWlE6QTl4Mkey
NCI-446 Mkm1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3O1O542KM7:TR?= NULCfJVCTE2VTx?= MnnBTWM2OD1zLkG1OEDPxE1? MoLrNVk6QTZ{N{K=
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Rh30 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVvJXVBPhjFy4pEK{txO NYnQZ2I2UUN3ME2wMlE6KML3TR?= NWHpeYZ1OjF{OUi3OFU>
BT-12 NWSzRXdjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1fCSp4yOOLCit88US=> MX;JR|UxRTBwN{igxtVO M1PZcFIyOjl6N{S1
CHLA-266 M4joNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3rPWJ4yOOLCit88US=> NXPWO4NvUUN3ME2wMlg6KML3TR?= M3naSFIyOjl6N{S1
TC-71 M1nwSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUnaS2NPhjFy4pEK{txO MVvJR|UxRTBwMUGgxtVO NIrSbHYzOTJ7OEe0OS=>
CHLA-9 NWTVRYtjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NE[4fJp,OTEkgJtOwG0> M1zUVWlEPTB;MD6xNkDDvU1? MkL6NlEzQTh5NEW=
CHLA-10 M3r2emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWPMR4pNhjFy4pEK{txO NGjRbHlKSzVyPUCuOlIhyrWP MonpNlEzQTh5NEW=
CHLA-258 MnK2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4\LfZ4yOOLCit88US=> M3i1PWlEPTB;MD6yO{DDvU1? NYDYPJc5OjF{OUi3OFU>
GBM2 Mlm3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M13CWZ4yOOLCit88US=> NVvF[XJjUUN3ME2xMlQ4KML3TR?= MUOyNVI6QDd2NR?=
NB-1643 NHnub2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnW2glEx6oDMzszN NYnPXJJmUUN3ME2wMlEzKML3TR?= NI\HUWIzOTJ7OEe0OS=>
NB-EBc1 NV3pfnMxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUj+NVDjiIsQvF2= MVHJR|UxRTBwM{WgxtVO MnrsNlEzQTh5NEW=
CHLA-90 NEXtfnZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1;2U54yOOLCit88US=> MULJR|UxRTBwN{egxtVO MYqyNVI6QDd2NR?=
CHLA-136 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NG\Hd45,OTEkgJtOwG0> MULJR|UxRTBwNUKgxtVO NVzLN5hQOjF{OUi3OFU>
NALM-6 MoXYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVHVenRphjFy4pEK{txO Mn\MTWM2OD1yLkS5JOK2VQ>? MmXWNlEzQTh5NEW=
COG-LL-317 NW\SWmx4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV6xTll[hjFy4pEK{txO M1\NVWlEPTB;MT6zPEDDvU1? NVjEWmF{OjF{OUi3OFU>
RS4;11 NYP4d|V5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3zHc54yOOLCit88US=> MXXJR|UxRTBwM{igxtVO MnXQNlEzQTh5NEW=
MOLT-4 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3Ljcp4yOOLCit88US=> M{GwUWlEPTB;MD61N{DDvU1? NXG1XmR3OjF{OUi3OFU>
CCRF-CEM MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn\DglEx6oDMzszN NX7IdZVYUUN3ME2xMlE{KML3TR?= NG\ydlMzOTJ7OEe0OS=>
Kasumi-1 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX\j[YZ[hjFy4pEK{txO M3TnSmlEPTB;MT6yJOK2VQ>? NGn4WIEzOTJ7OEe0OS=>
Karpas-299 M2D2bmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkTQglEx6oDMzszN M2jHUWlEPTB;MT62OEDDvU1? MV2yNVI6QDd2NR?=
Ramos-RA1 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3LqNJ4yOOLCit88US=> MmnJTWM2OD1zLkOxJOK2VQ>? M{G1NFIyOjl6N{S1
Rh30  MYjGeY5kfGmxbjDhd5NigQ>? Mn7KbY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w NWnORlB3OjV7MkWzO|g>
Rh41 Ml25SpVv[3Srb36gZZN{[Xl? MlLGbY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w M{GyUFI2QTJ3M{e4
RD NH3xeIxHfW6ldHnvckBie3OjeR?= NVPsSHFXcW6mdXPld{BidiCrbnPy[YF{\SCxZjDTSmsheGixc4Doc5J6dGG2aX;u MoHkNlU6OjV|N{i=
A549 NIXv[pZMcW6jc3WgZZN{[Xl? NGr2U|QxNjYkgJtOwG0> NETHcXNFVVOR MofobY5pcWKrdIOgTWdHNUmUL1nSJIFkfGm4YYTpc44> MkDnNlY6Ojh3N{i=
NCI-H358 MXfLbY5ie2ViYYPzZZk> NXvKO3ExOC534pEK{txO MX3EUXNQ MUjpcohq[mm2czDJS2YuUVJxSWKgZYN1cX[jdHnvci=> M1S4eFI3QTJ6NUe4
A549 MoniSpVv[3Srb36gZZN{[Xl? MUOwMlXjiIsQvF2= MkDGSG1UVw>? MWrjZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM MYeyOlkzQDV5OB?=
NCI-H358 NGLwU|FHfW6ldHnvckBie3OjeR?= MoHGNE426oDMzszN M{XxfGROW09? NWLJemh[[2G3c3XzJIEh[2:wY4XydoVvfCCmZXPy[YF{\SCrbjDwbI9{eGixconsZZRm\CCDS2SgZY5lKEWUSx?= NF;Ec28zPjl{OEW3PC=>
A549 MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVXWV2E4hjFy4pEK{txO M1zZTmROW09? M4fa[2lEPTB;MD63OkDPxE1? M2nre|I3QTJ6NUe4
NCI-H358 NHrV[mtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVP+NVDjiIsQvF2= MoHqSG1UVw>? NWLoO2t4UUN3ME2xMlA6KM7:TR?= MVeyOlkzQDV5OB?=
A549 MnfvRZBweHSxc3nzJIF{e2G7 NF;FWGgxNjYkgJtOwG0> MYHEUXNQ M4TKWolv\HWlZYOgRZBweHSxc3nz NV;STJF7OjZ7Mki1O|g>
NCI-H358 M{HnNmFxd3C2b4Ppd{Bie3OjeR?= MXKwMlXjiIsQvF2= MV\EUXNQ NXLQOWZScW6mdXPld{BCeG:ydH;zbZM> M{X0eVI3QTJ6NUe4
A549 NEe3eHhHfW6ldHnvckBie3OjeR?= NUXj[olkOC534pEK{txO NVzpd4dmTE2VTx?= M1Pke5Jm\HWlZYOge492dmRiY3zvd5Vz\Q>? MW[yOlkzQDV5OB?=
NCI-H358 NX\xZmNpTnWwY4Tpc44h[XO|YYm= NFS3cYwxNjYkgJtOwG0> NF;FSHdFVVOR NYHYb3NvemWmdXPld{B4d3WwZDDjcI9{fXKn NIT4VHozPjl{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(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
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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IGF-1R Signaling Pathway Map

IGF-1R Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID