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 Mof5T4lv[XOnIHHzd4F6 MnnwbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXIhMEmFNUCgQUAyO26PKTDhcoQhfGinIHTve45{fHKnYX2geIFz\2W2czDBb5QhMEmFNUCgQUAzOm6PKTDhcoQhVUGSSzCoTWM2OCB;IEGzcm0q MWOxPVc4QDB{NB?=
IGF-Sal MoeyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVroR25IUUN3ME23JI5O NIHERlcyQTd5OECyOC=>
CCRF-CEM (ALL) MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWP2b5RWhjVizszN NG\CTFlFVVOR NG\6O2hKSzVyPUGuNlM6KM7:TR?= MXixPVk6PjJ5Mh?=
PC3 NHPtbWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXf+OUDPxE1? NVnuc2hzTE2VTx?= NYj5e4l5UUN3ME2wMlk3PSEQvF2= MoizNVk6QTZ{N{K=
JD MkOyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXfiSmhDhjVizszN NGLze2ZFVVOR NVLSTYF6UUN3ME2wMlM6OSEQvF2= MmW0NVk6QTZ{N{K=
DU145 NHzuNXFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mlv5glUh|ryP Mnq2SG1UVw>? M1PUTGlEPTB;MT60OlUh|ryP M1uxcVE6QTl4Mkey
KAG NYjB[2tGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml21glUh|ryP NEj3XIVFVVOR NVixOlczUUN3ME2xMlY3PSEQvF2= NWf1XoNmOTl7OU[yO|I>
K-562 (CML) NFf2eodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYP+OUDPxE1? NWn6eWRbTE2VTx?= MX3JR|UxRTJwM{CyJO69VQ>? MWexPVk6PjJ5Mh?=
B6-P210 (Murine ALL) M1fVN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkG1glUh|ryP M17lfmROW09? NELJUFNKSzVyPUGuNlk{KM7:TR?= NXjvdpZxOTl7OU[yO|I>
LN CAP-FGC M3\lNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3jHbJ42KM7:TR?= NUHKZVBWTE2VTx?= MW\JR|UxRTFwNEO0JO69VQ>? NV\LRWpSOTl7OU[yO|I>
VW NYnxTpptT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWmxWIM6hjVizszN M2fLdWROW09? NVT6bG5FUUN3ME2wMlAyQSEQvF2= MnHONVk6QTZ{N{K=
MV411 (B Myelomonocytic) NIDNOFBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2izWZ42KM7:TR?= M3[4VGROW09? M3XEV2lEPTB;MD6zN{DPxE1? MVGxPVk6PjJ5Mh?=
MDA-PCa-2b M2n1emdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2jaOp42KM7:TR?= NYPmNpVpTE2VTx?= MXTJR|UxRTBwMEm4JO69VQ>? NHXDZZYyQTl7NkK3Ni=>
LG MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkXDglUh|ryP NFzQOnVFVVOR M3vRcGlEPTB;MD6wN|gh|ryP M3rqR|E6QTl4Mkey
RS411 (B cell precursor-ALL) NYi2VnU4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnPJglUh|ryP MnOxSG1UVw>? NW\LUFRNUUN3ME2wMlExOiEQvF2= MnKwNVk6QTZ{N{K=
22-r-1 M3O1RWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnOwglUh|ryP NEHrOGxFVVOR M17rSmlEPTB;MD6xO|Uh|ryP NFLPZlgyQTl7NkK3Ni=>
5838 Mo\wS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXH+OUDPxE1? NXfJSI9uTE2VTx?= NXnBVVdPUUN3ME2wMlA{PCEQvF2= MWqxPVk6PjJ5Mh?=
P388 (Murine) NHu3TFdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NG[5Snd,PSEQvF2= NHvISXZFVVOR NFXlVpZKSzVyPUSuNlch|ryP MV6xPVk6PjJ5Mh?=
A2780/S MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXmxbVVJhjVizszN NF;vZ3BFVVOR MVvJR|UxRTBwMUKyJO69VQ>? NILWSmcyQTl7NkK3Ni=>
RDES MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYqzW3dKhjVizszN Mn7BSG1UVw>? M3PxfmlEPTB;MD6wNVIh|ryP MUGxPVk6PjJ5Mh?=
B6-T315I (Murine B-ALL) NHT3eXFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV3+OUDPxE1? NHqwSVdFVVOR NX3SV5pkUUN3ME2yMlg{KM7:TR?= MWSxPVk6PjJ5Mh?=
TOV 112D Mn;sS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYLncW5thjVizszN NWnIcItuTE2VTx?= NI\JXXFKSzVyPUKuNVQ3KM7:TR?= M4S3[VE6QTl4Mkey
TC32 MmHYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\vZp42KM7:TR?= NXHWemJnTE2VTx?= NIfLeVhKSzVyPUCuNFA5KM7:TR?= NGf3W5oyQTl7NkK3Ni=>
HL60 (acute myelocytic) MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXf+OUDPxE1? MnLDSG1UVw>? MnrJTWM2OD1yLkGyJO69VQ>? MWOxPVk6PjJ5Mh?=
TOV 21G M{fQXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXnoUVZIhjVizszN MkTVSG1UVw>? M2nZOWlEPTB;ND6yO|kh|ryP MorjNVk6QTZ{N{K=
TC71 M37tRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFr3[JZ,PSEQvF2= NWDyeJp3TE2VTx?= NWXRfJNrUUN3ME2wMlAyPCEQvF2= NFXLOYsyQTl7NkK3Ni=>
HPN-ALL (T-cell) M2\ZVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVPu[4hqhjVizszN NGLoe4JFVVOR NFu1[mVKSzVyPUCuOVIh|ryP M33wSVE6QTl4Mkey
A2780R MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2jQfJ42KM7:TR?= NHPPc4xFVVOR MYLJR|UxRTFwNU[0JO69VQ>? NGfXXmEyQTl7NkK3Ni=>
Rh1 NEj4fnBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml3LglUh|ryP NH:xOJZFVVOR NGjUNYJKSzVyPUCuNFI4KM7:TR?= M{P2fVE6QTl4Mkey
Kasumi-1 (acute myeloid) Ml36S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlfKglUh|ryP NWX2SXpzTE2VTx?= MUDJR|UxRTBwMU[g{txO NFzrRWoyQTl7NkK3Ni=>
sk-ov-3 NUGyPWdbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXrCN4h5hjVizszN Ml;ISG1UVw>? NGDSZ5dKSzVyPUWuNUDPxE1? MXixPVk6PjJ5Mh?=
ME MnLLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIe4e|J,PSEQvF2= NUK5NGVWTE2VTx?= MleyTWM2OD1yLkCxOUDPxE1? MkG3NVk6QTZ{N{K=
L1210 (Murine lymphocytic) NUfmbW5nT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mkf4glUh|ryP MlLsSG1UVw>? MUjJR|UxRTJwM{mg{txO NEPHPGsyQTl7NkK3Ni=>
sw-626 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoGyglUh|ryP NF\TcYZFVVOR M3vxSGlEPTB;Mj6zNFYh|ryP NFPodYQyQTl7NkK3Ni=>
CTR MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGHEXFd,PSEQvF2= NGLUcGdFVVOR NFrpUG1KSzVyPUCuNlU{KM7:TR?= MlnINVk6QTZ{N{K=
ML2 (Myelomonocytic) MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHPufHJ,PSEQvF2= NGLs[ppFVVOR NWe0SnRXUUN3ME2wMlA6KM7:TR?= MWOxPVk6PjJ5Mh?=
ovcar-3 MnS2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYL1UXZChjVizszN M4fuOmROW09? NU\0fI57UUN3ME21JO69VQ>? NVPUW4ZlOTl7OU[yO|I>
Rh36 MoHRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVjHT3dUhjVizszN M{Dvc2ROW09? M3HDZWlEPTB;MT60N|Ih|ryP Mn6yNVk6QTZ{N{K=
MOLM-13 (acute myeloid) NY\rVoFXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MojYglUh|ryP MUfEUXNQ NWjxclZmUUN3ME2wMlQzKM7:TR?= M2\UO|E6QTl4Mkey
ovcar-4 Mne0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnTnglUh|ryP NGHhemhFVVOR M{ju[WlEPTB;MTFOwG0> NXvZU2k4OTl7OU[yO|I>
Rh41 NHjEbXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWP+OUDPxE1? NEjKb|FFVVOR NG\McFZKSzVyPUCuNFA2KM7:TR?= MVexPVk6PjJ5Mh?=
Mutz 2 (acute myeloid) NF7RfVFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHjXXWV,PSEQvF2= NUD1bWZsTE2VTx?= Mk\UTWM2OD1zLkG1JO69VQ>? Mlq3NVk6QTZ{N{K=
ovcar-5 MnPiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUDyUZo4hjVizszN M{\1OGROW09? NG[1SXlKSzVyPUCuNFUh|ryP M1jqbVE6QTl4Mkey
RD1 NEHSR2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX\xcnhphjVizszN NXr1NoNGTE2VTx?= MVnJR|UxRTBwME[4JO69VQ>? M2TQSFE6QTl4Mkey
OCI-AML 2 (acute myeloid) M4\kS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4\HTZ42KM7:TR?= MoHsSG1UVw>? MWjJR|UxRTNwM{Og{txO NUnq[5lmOTl7OU[yO|I>
786-O M1nkXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mof1glUh|ryP NEfyTFVFVVOR MmX2TWM2OD1zLk[0O{DPxE1? M1P5RVE6QTl4Mkey
A673 M3TXUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUf4bGNXhjVizszN M1PWZ2ROW09? NWP2TIhPUUN3ME2wMlQxQCEQvF2= NWjOS2M2OTl7OU[yO|I>
TALL-1 (T-cell) NGezWVhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWX+OUDPxE1? NYXmWo5MTE2VTx?= NHfBOnlKSzVyPUGuNlgh|ryP MUKxPVk6PjJ5Mh?=
151-B NFT0d5RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIjjUHh,PSEQvF2= MlzTSG1UVw>? MXjJR|UxRTJwNkeg{txO NGrnfXIyQTl7NkK3Ni=>
PFSK-1 M2DxWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlzMglUh|ryP M32xUmROW09? NF73WI1KSzVyPUCuNVMzKM7:TR?= MlrJNVk6QTZ{N{K=
THP-1 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXP+OUDPxE1? NXrpWGxPTE2VTx?= MWPJR|UxRTZwNUig{txO MXSxPVk6PjJ5Mh?=
HEK293 MnjMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYGzd4RohjVizszN M{DWemROW09? NH\L[YdKSzVyPUCuPVE2KM7:TR?= M{LJcVE6QTl4Mkey
DAOY Mmj0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmXsglUh|ryP NFzj[GRFVVOR MWrJR|UxRTFwOUe5JO69VQ>? NV7IOGJZOTl7OU[yO|I>
SET2 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3;nOJ42KM7:TR?= MXvEUXNQ Mn3qTWM2OD1yLkK5PEDPxE1? NUnld5VqOTl7OU[yO|I>
HTB-46 NWr1eI9vT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoroglUh|ryP MWnEUXNQ NV;mVHNPUUN3ME21MlI2KM7:TR?= M1XCW|E6QTl4Mkey
SK-NAS MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHLUO2Z,PSEQvF2= NHrlS4JFVVOR MUjJR|UxRTBwNEm3JO69VQ>? MU[xPVk6PjJ5Mh?=
CTLL2 NVPrT2ozT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV3Hb5h7hjVizszN M{jaUGROW09? MWTJR|UxRjFwMECg{txO M1nsRlE6QTl4Mkey
HTB-47 NV\s[JhJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3vCZ542KM7:TR?= MmPnSG1UVw>? MkLJTWM2OD1{LkC1OkDPxE1? NXvPV4w1OTl7OU[yO|I>
LAN-1 NWjUd3ZjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{Dmep42KM7:TR?= Mmm2SG1UVw>? NEHyWndKSzVyPUCuNFQh|ryP M{H2cFE6QTl4Mkey
ST486 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3mxO542KM7:TR?= NUTNSWN6TE2VTx?= MYnJR|UxRTFwMUmg{txO MX[xPVk6PjJ5Mh?=
HS766T NWSzeIJlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVj3eGw4hjVizszN Mm\wSG1UVw>? MVzJR|UxRTJwMECxJO69VQ>? MXyxPVk6PjJ5Mh?=
IMR-32 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2rJV542KM7:TR?= MV\EUXNQ M2jpSWlEPTB;MD6yOlEh|ryP NVnw[Y11OTl7OU[yO|I>
Daudi (Burkitt's) M2ewVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVr+OUDPxE1? MnnzSG1UVw>? M4i2TGlEPTB;Mj62N|ch|ryP MXyxPVk6PjJ5Mh?=
Aspc-1 NGT3[GtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEfwb|V,PSEQvF2= NWLnTG15TE2VTx?= MVjJR|UxRTBwM{e5JO69VQ>? MVqxPVk6PjJ5Mh?=
SK-NSH Mn7KS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M13Obp42KM7:TR?= MXLEUXNQ NGnDRVlKSzVyPUCuNVM6KM7:TR?= NULK[HlrOTl7OU[yO|I>
MEC-1 (Chronic B cell) M{O5Rmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUL+OUDPxE1? M1XLUWROW09? NInOdYVKSzVyPUKuOlM4KM7:TR?= NH3EVlcyQTl7NkK3Ni=>
Capan-2 NFPWd4FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUn+OUDPxE1? MV;EUXNQ NWfl[nZGUUN3ME2xMlc4PCEQvF2= NUnEepZlOTl7OU[yO|I>
SHSY5Y NXXHS4xlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnPoglUh|ryP M1T4ZWROW09? MmDPTWM2OD1yLkGwOkDPxE1? MoLPNVk6QTZ{N{K=
U937 (Histioocytic) NIe3eJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1q2fJ42KM7:TR?= MoK0SG1UVw>? M4DibmlEPTB-NT6wNEDPxE1? MXuxPVk6PjJ5Mh?=
Bxpc-1 M{\YUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH3nWI5,PSEQvF2= MX7EUXNQ MX7JR|UxRTFwOUK0JO69VQ>? MoL5NVk6QTZ{N{K=
Bxpc-3 MlTRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3PKOp42KM7:TR?= M3\MO2ROW09? MnPXTWM2OD53LkCwJO69VQ>? NI\u[|kyQTl7NkK3Ni=>
HTB-92 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWjOeJFXhjVizszN NWX2eYNrTE2VTx?= NYS3SGM3UUN3ME2xMlAzKM7:TR?= MUSxPVk6PjJ5Mh?=
OCI-LY10 (B-cell) M4CzXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUL+OUDPxE1? MnHESG1UVw>? M1LCU2lEPTB;MD60OUDPxE1? NHz2bHkyQTl7NkK3Ni=>
PANC-1 NEfnPGdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1\nTZ42KM7:TR?= Mk\HSG1UVw>? Mlr5TWM2OD53LkCwJO69VQ>? NFHOZVcyQTl7NkK3Ni=>
To184.T NVTOXWxwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{fxcp42KM7:TR?= MoXmSG1UVw>? NHTpcohKSzVyPUCuOFY6KM7:TR?= NF\2[osyQTl7NkK3Ni=>
OCI-LY19 (B-cell) MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWD+OUDPxE1? M{[3PWROW09? M2PYe2lEPTB;MD60JO69VQ>? MX6xPVk6PjJ5Mh?=
PANC-1 BM Mn\US5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWnYTIRHhjVizszN MmTJSG1UVw>? NXjHcFVvUUN3ME61MlAxKM7:TR?= NVz1cmVFOTl7OU[yO|I>
SA-4 MmntS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEnoUWh,PSEQvF2= M{Gyc2ROW09? MmrSTWM2OD1zLkOwNUDPxE1? MWCxPVk6PjJ5Mh?=
RPMI 8226 M3PtRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2TZNZ42KM7:TR?= MmfOSG1UVw>? NUTDWFduUUN3ME2xMlI6OyEQvF2= NG[zWGMyQTl7NkK3Ni=>
HPAF-II M4npZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1TWOZ42KM7:TR?= NITEe2pFVVOR NEfzSIFKSzVyPUCuOlQ1KM7:TR?= NYTHeIpIOTl7OU[yO|I>
SHP-77 M{nqfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWS5NFE{hjVizszN M{DkemROW09? NVjZNotLUUN3ME2xMlg5QCEQvF2= M2\jfVE6QTl4Mkey
U266 B1 NVXZPWZTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGnte|l,PSEQvF2= MVXEUXNQ M17GUmlEPTB;MT62Olkh|ryP NYfm[mJzOTl7OU[yO|I>
Hs700t NVLidXRLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4HjNJ42KM7:TR?= NFz4eIZFVVOR NX;zNFBsUUN3ME2wMlI{OSEQvF2= MYSxPVk6PjJ5Mh?=
NCI-446 NF7Qb4FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV\+OUDPxE1? NXnhUolkTE2VTx?= NXTQVYtGUUN3ME2xMlE2PCEQvF2= NWH4cI5COTl7OU[yO|I>
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Rh30 NX;xT3R6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4Dpcp4yOOLCit88US=> MmHGTWM2OD1yLkG5JOK2VQ>? MUSyNVI6QDd2NR?=
BT-12 NILyc5BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXHjdHQ5hjFy4pEK{txO MofpTWM2OD1yLke4JOK2VQ>? NVrTeIw{OjF{OUi3OFU>
CHLA-266 NIXXXYNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1XLcp4yOOLCit88US=> M3;EVGlEPTB;MD64PUDDvU1? MYOyNVI6QDd2NR?=
TC-71 M{[4SGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWL+NVDjiIsQvF2= MUfJR|UxRTBwMUGgxtVO NVHEPXBvOjF{OUi3OFU>
CHLA-9 M{POcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MW\+NVDjiIsQvF2= NH7SWZhKSzVyPUCuNVIhyrWP M{PUOFIyOjl6N{S1
CHLA-10 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWj+NVDjiIsQvF2= MoPOTWM2OD1yLk[yJOK2VQ>? M2DBPFIyOjl6N{S1
CHLA-258 M2nwRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVT+NVDjiIsQvF2= NHX1NHBKSzVyPUCuNlchyrWP M2rrO|IyOjl6N{S1
GBM2 M37nZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYDkNo54hjFy4pEK{txO MYLJR|UxRTFwNEegxtVO M2\MRlIyOjl6N{S1
NB-1643 MnPuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{fUdZ4yOOLCit88US=> NULoPHc1UUN3ME2wMlEzKML3TR?= MmLRNlEzQTh5NEW=
NB-EBc1 NHyySGJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFv5dY9,OTEkgJtOwG0> MU\JR|UxRTBwM{WgxtVO M{n6dlIyOjl6N{S1
CHLA-90 NXnTd4VPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUD+NVDjiIsQvF2= MWjJR|UxRTBwN{egxtVO M1nBelIyOjl6N{S1
CHLA-136 NGLvZpZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MU\+NVDjiIsQvF2= MULJR|UxRTBwNUKgxtVO NGOxOHEzOTJ7OEe0OS=>
NALM-6 NFXL[ppIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NILKd4Z,OTEkgJtOwG0> NE[4SoxKSzVyPUCuOFkhyrWP M4fLcVIyOjl6N{S1
COG-LL-317 MomxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWPvNHl1hjFy4pEK{txO Ml6zTWM2OD1zLkO4JOK2VQ>? NX\MVldJOjF{OUi3OFU>
RS4;11 Mm\lS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3rhZp4yOOLCit88US=> MUfJR|UxRTBwM{igxtVO NIjMXnAzOTJ7OEe0OS=>
MOLT-4 NFLmblVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYDuWoZyhjFy4pEK{txO NYO3[283UUN3ME2wMlU{KML3TR?= NFP3ZpIzOTJ7OEe0OS=>
CCRF-CEM MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXf4S4ZQhjFy4pEK{txO MXHJR|UxRTFwMUOgxtVO NV;m[G54OjF{OUi3OFU>
Kasumi-1 MlPMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYr+NVDjiIsQvF2= M3;XUWlEPTB;MT6yJOK2VQ>? M2XDSlIyOjl6N{S1
Karpas-299 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX\vcGx{hjFy4pEK{txO NIrDdnpKSzVyPUGuOlQhyrWP NXTne5I2OjF{OUi3OFU>
Ramos-RA1 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX;1[YtUhjFy4pEK{txO M3nQO2lEPTB;MT6zNUDDvU1? M3XObVIyOjl6N{S1
Rh30  NF62dHZHfW6ldHnvckBie3OjeR?= Mki0bY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w NELJSXczPTl{NUO3PC=>
Rh41 MoC3SpVv[3Srb36gZZN{[Xl? MkPObY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w MX2yOVkzPTN5OB?=
RD NI[4V3RHfW6ldHnvckBie3OjeR?= M2rMdolv\HWlZYOgZY4hcW6lcnXhd4Uhd2ZiU1\LJJBpd3OyaH;yfYxifGmxbh?= M2rSblI2QTJ3M{e4
A549 MXnLbY5ie2ViYYPzZZk> NXvBO4ZrOC534pEK{txO NV30PIJFTE2VTx?= M33VUYlvcGmkaYTzJGlITi2LUj;JVkBi[3SrdnH0bY9v M{[2WFI3QTJ6NUe4
NCI-H358 NY\jenJ[U2mwYYPlJIF{e2G7 NIjTOZExNjYkgJtOwG0> M2L4c2ROW09? Ml3UbY5pcWKrdIOgTWdHNUmUL1nSJIFkfGm4YYTpc44> NGDmSZgzPjl{OEW3PC=>
A549 NYflNWtVTnWwY4Tpc44h[XO|YYm= M1nSNlAvPeLCit88US=> MXHEUXNQ NUfoO|BE[2G3c3XzJIEh[2:wY4XydoVvfCCmZXPy[YF{\SCrbjDwbI9{eGixconsZZRm\CCDS2SgZY5lKEWUSx?= M1S5ZlI3QTJ6NUe4
NCI-H358 NITMPFJHfW6ldHnvckBie3OjeR?= NVuyRm5GOC534pEK{txO NFjTdW9FVVOR MVzjZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM M3Pp[VI3QTJ6NUe4
A549 M1XwXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVLxV415hjFy4pEK{txO MX\EUXNQ NXjIZ2pGUUN3ME2wMlc3KM7:TR?= NYPHTlZROjZ7Mki1O|g>
NCI-H358 Mm[1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFfBNYp,OTEkgJtOwG0> MYLEUXNQ M3LPZmlEPTB;MT6wPUDPxE1? MWmyOlkzQDV5OB?=
A549 NUHXXFV6SXCxcITvd4l{KGG|c3H5 MU[wMlXjiIsQvF2= NV3DUYpCTE2VTx?= M2q1Z4lv\HWlZYOgRZBweHSxc3nz M{\nbVI3QTJ6NUe4
NCI-H358 NFHi[JJCeG:ydH;zbZMh[XO|YYm= M2fYO|AvPeLCit88US=> MorkSG1UVw>? NELX[3lqdmS3Y3XzJGFxd3C2b4Ppdy=> M3LYOlI3QTJ6NUe4
A549 NUPhZYJGTnWwY4Tpc44h[XO|YYm= NFXmPXQxNjYkgJtOwG0> Mn21SG1UVw>? MljKdoVlfWOnczD3c5Vv\CClbH;zeZJm NFfNPHMzPjl{OEW3PC=>
NCI-H358 M3P5[GZ2dmO2aX;uJIF{e2G7 MkHqNE426oDMzszN M1vIbWROW09? NHzoXGVz\WS3Y3XzJJdwfW6mIHPsc5N2emV? NWrBVWZoOjZ7Mki1O|g>

... 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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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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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