BMS-754807

For research use only.

Catalog No.S1124

29 publications

BMS-754807 Chemical Structure

CAS No. 1001350-96-4

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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Selleck's BMS-754807 has been cited by 29 publications

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 NWTqdGVoU2mwYYPlJIF{e2G7 NVHCfZUycW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDJS2YuOVJiKFnDOVAhRSBzM37NLUBidmRidHjlJIRwf26|dILlZY0hfGG{Z3X0d{BCc3RiKFnDOVAhRSB{Mn7NLUBidmRiTVHQT{ApUUN3MDC9JFE{dk1r MYSxPVc4QDB{NB?=
IGF-Sal MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2HlWmlEPTB;NzDuUS=> MoH4NVk4PzhyMkS=
CCRF-CEM (ALL) NFjQWo1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NInwSpZ,PSEQvF2= MXrEUXNQ MVfJR|UxRTFwMkO5JO69VQ>? MWWxPVk6PjJ5Mh?=
PC3 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlnOglUh|ryP M2jtfWROW09? MXTJR|UxRTBwOU[1JO69VQ>? M1;wdFE6QTl4Mkey
JD MnrIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2PHWJ42KM7:TR?= NXPwfHllTE2VTx?= M{fVcmlEPTB;MD6zPVEh|ryP M1v2W|E6QTl4Mkey
DU145 M4LXOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX3xS|E6hjVizszN MkXhSG1UVw>? NFvGNW9KSzVyPUGuOFY2KM7:TR?= Mn\PNVk6QTZ{N{K=
KAG MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWTEZ2M2hjVizszN NYLxdpluTE2VTx?= MlHnTWM2OD1zLk[2OUDPxE1? NHPDfpIyQTl7NkK3Ni=>
K-562 (CML) MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWPnUo5zhjVizszN NGGwbHhFVVOR M1zuS2lEPTB;Mj6zNFIh|ryP Mo\ONVk6QTZ{N{K=
B6-P210 (Murine ALL) MnLYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXz+OUDPxE1? MUHEUXNQ Mn;zTWM2OD1zLkK5N{DPxE1? NIDRb2YyQTl7NkK3Ni=>
LN CAP-FGC MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXO4NWJmhjVizszN MlHtSG1UVw>? MoHqTWM2OD1zLkSzOEDPxE1? Ml7oNVk6QTZ{N{K=
VW NVzjS446T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIDjVpV,PSEQvF2= NIfT[2JFVVOR MWjJR|UxRTBwMEG5JO69VQ>? Ml\xNVk6QTZ{N{K=
MV411 (B Myelomonocytic) M1WzNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH\jToR,PSEQvF2= MYXEUXNQ NEjmeFVKSzVyPUCuN|Mh|ryP NVvGZW1GOTl7OU[yO|I>
MDA-PCa-2b MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1LhfZ42KM7:TR?= MW\EUXNQ NFu5OWdKSzVyPUCuNFk5KM7:TR?= NEi3UXIyQTl7NkK3Ni=>
LG MlnGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\mN542KM7:TR?= NWDSbXBRTE2VTx?= MUTJR|UxRTBwMEO4JO69VQ>? NWfkXnhsOTl7OU[yO|I>
RS411 (B cell precursor-ALL) MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUj+OUDPxE1? MU\EUXNQ M{ntWWlEPTB;MD6xNFIh|ryP M1e4NlE6QTl4Mkey
22-r-1 NWL0b4pIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MljuglUh|ryP M1SxcGROW09? NXXlOIZnUUN3ME2wMlE4PSEQvF2= M{XoRVE6QTl4Mkey
5838 NHq1TlhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MY\+OUDPxE1? MVrEUXNQ NYrueppjUUN3ME2wMlA{PCEQvF2= MV6xPVk6PjJ5Mh?=
P388 (Murine) NWPpfFRrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXixfYRyhjVizszN M4XXV2ROW09? MV\JR|UxRTRwMkeg{txO MX:xPVk6PjJ5Mh?=
A2780/S NWLF[29WT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH7oSIV,PSEQvF2= MV3EUXNQ NUjBVpdoUUN3ME2wMlEzOiEQvF2= MmOzNVk6QTZ{N{K=
RDES NUPRS2hJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUj+OUDPxE1? MWPEUXNQ Mm\xTWM2OD1yLkCxNkDPxE1? MlHnNVk6QTZ{N{K=
B6-T315I (Murine B-ALL) NH\vRopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVK2VGdqhjVizszN M3HxXGROW09? MkHUTWM2OD1{LkizJO69VQ>? NUXycpFzOTl7OU[yO|I>
TOV 112D MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEfwR2R,PSEQvF2= MVvEUXNQ NWi2U5Z6UUN3ME2yMlE1PiEQvF2= M1;yTVE6QTl4Mkey
TC32 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXHD[FJkhjVizszN M1ryZ2ROW09? NWHBWWhUUUN3ME2wMlAxQCEQvF2= NV\sS|FlOTl7OU[yO|I>
HL60 (acute myelocytic) NVTsZpliT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEPMbWx,PSEQvF2= NYHZW3A1TE2VTx?= NVfDfZBUUUN3ME2wMlEzKM7:TR?= NV;IN2pLOTl7OU[yO|I>
TOV 21G NIPsT|dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnfYglUh|ryP M2fOTmROW09? MmPFTWM2OD12LkK3PUDPxE1? NEfMcHcyQTl7NkK3Ni=>
TC71 MlzDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGnlVpd,PSEQvF2= MWfEUXNQ M1PrbWlEPTB;MD6wNVQh|ryP MWqxPVk6PjJ5Mh?=
HPN-ALL (T-cell) M3nTU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXjYdIU2hjVizszN Mlj2SG1UVw>? NXXFXVZUUUN3ME2wMlUzKM7:TR?= M4GzU|E6QTl4Mkey
A2780R NWHmfXN[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUf+OUDPxE1? MV7EUXNQ M2q3emlEPTB;MT61OlQh|ryP M4\qfVE6QTl4Mkey
Rh1 NV[4T|R1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXT+OUDPxE1? M1jtV2ROW09? MmCzTWM2OD1yLkCyO{DPxE1? MnXjNVk6QTZ{N{K=
Kasumi-1 (acute myeloid) Ml\3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXn+OUDPxE1? MXTEUXNQ M2K4emlEPTB;MD6xOkDPxE1? MlfkNVk6QTZ{N{K=
sk-ov-3 NGToTWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{O5UZ42KM7:TR?= M{nrdmROW09? M2nLUGlEPTB;NT6xJO69VQ>? MV2xPVk6PjJ5Mh?=
ME NV\4VYhDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVX+OUDPxE1? NWC5U2RMTE2VTx?= M2TvS2lEPTB;MD6wNVUh|ryP M1vKfVE6QTl4Mkey
L1210 (Murine lymphocytic) MoH1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MojHglUh|ryP MoLvSG1UVw>? MWjJR|UxRTJwM{mg{txO NXT3XpJwOTl7OU[yO|I>
sw-626 NETlfXdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmK5glUh|ryP MonPSG1UVw>? M3r5O2lEPTB;Mj6zNFYh|ryP MUCxPVk6PjJ5Mh?=
CTR MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLnOolXhjVizszN MVXEUXNQ NFXzSIVKSzVyPUCuNlU{KM7:TR?= M4DaZ|E6QTl4Mkey
ML2 (Myelomonocytic) NX;tVVB7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUH+OUDPxE1? M4r4VGROW09? Mmq0TWM2OD1yLkC5JO69VQ>? MnT4NVk6QTZ{N{K=
ovcar-3 NYnJbXNHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIDnN3J,PSEQvF2= MmfVSG1UVw>? Ml\nTWM2OD13IN88US=> NHPYZowyQTl7NkK3Ni=>
Rh36 NGnFdFJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3O0O542KM7:TR?= NUO4e4NCTE2VTx?= NXz4R3F6UUN3ME2xMlQ{OiEQvF2= NVn6UHhzOTl7OU[yO|I>
MOLM-13 (acute myeloid) NETIbpFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYP4Z5dxhjVizszN MlHvSG1UVw>? Mn75TWM2OD1yLkSyJO69VQ>? NVnnVJhMOTl7OU[yO|I>
ovcar-4 MofRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUj+OUDPxE1? NIHjZpNFVVOR NXOzSJMyUUN3ME2xJO69VQ>? M3[0UFE6QTl4Mkey
Rh41 M{DTWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVT+OUDPxE1? MULEUXNQ M1j0bWlEPTB;MD6wNFUh|ryP MnTRNVk6QTZ{N{K=
Mutz 2 (acute myeloid) MkfVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoPJglUh|ryP NFfzendFVVOR M3\CVmlEPTB;MT6xOUDPxE1? NHXJPZkyQTl7NkK3Ni=>
ovcar-5 Mkj2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIn1SXB,PSEQvF2= MmPjSG1UVw>? NUn1S5BjUUN3ME2wMlA2KM7:TR?= M2PQ[VE6QTl4Mkey
RD1 NYXr[JRST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH\IWHh,PSEQvF2= NXTmbnczTE2VTx?= Mn;STWM2OD1yLkC2PEDPxE1? MnzaNVk6QTZ{N{K=
OCI-AML 2 (acute myeloid) MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVL+OUDPxE1? Mo\WSG1UVw>? NHvvVFFKSzVyPUOuN|Mh|ryP NFPjVoEyQTl7NkK3Ni=>
786-O NEPnbHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2T1bp42KM7:TR?= MUfEUXNQ M3iwemlEPTB;MT62OFch|ryP NHjWUWIyQTl7NkK3Ni=>
A673 NEj6PIhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGTYSYZ,PSEQvF2= M1PscGROW09? MVnJR|UxRTBwNEC4JO69VQ>? MW[xPVk6PjJ5Mh?=
TALL-1 (T-cell) NU[wcnFTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NG\MWFd,PSEQvF2= M13UbWROW09? NVPnb2tXUUN3ME2xMlI5KM7:TR?= MXOxPVk6PjJ5Mh?=
151-B MkHoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX[1VJA1hjVizszN MmnZSG1UVw>? NV\kcYVIUUN3ME2yMlY4KM7:TR?= MoDxNVk6QTZ{N{K=
PFSK-1 NH3sOoxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVfKT5dYhjVizszN NEPoUHhFVVOR M3\MOmlEPTB;MD6xN|Ih|ryP Ml3rNVk6QTZ{N{K=
THP-1 NWn1NZJNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVz+OUDPxE1? NV3SNWJETE2VTx?= MkjZTWM2OD14LkW4JO69VQ>? MWCxPVk6PjJ5Mh?=
HEK293 Mme2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkHoglUh|ryP M4X2[GROW09? M3P3Z2lEPTB;MD65NVUh|ryP M2XrNFE6QTl4Mkey
DAOY NIft[mRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3;MSp42KM7:TR?= MYfEUXNQ MVfJR|UxRTFwOUe5JO69VQ>? NF\UeIgyQTl7NkK3Ni=>
SET2 M3\yWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFPqfnF,PSEQvF2= NXzKSJRFTE2VTx?= M2nFVmlEPTB;MD6yPVgh|ryP NHq4ZWsyQTl7NkK3Ni=>
HTB-46 MknpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2riNZ42KM7:TR?= NWHlfXY3TE2VTx?= MUTJR|UxRTVwMkWg{txO M1PZ[lE6QTl4Mkey
SK-NAS MnfFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV\5b3JQhjVizszN MYTEUXNQ NHq0SldKSzVyPUCuOFk4KM7:TR?= MV6xPVk6PjJ5Mh?=
CTLL2 M2n1Xmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXj+OUDPxE1? MnjOSG1UVw>? NXTSWFgxUUN3ME6xMlAxKM7:TR?= NE\T[ZkyQTl7NkK3Ni=>
HTB-47 MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYT+OUDPxE1? NFrNUlRFVVOR MmLkTWM2OD1{LkC1OkDPxE1? MXGxPVk6PjJ5Mh?=
LAN-1 NWHkTZA2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWD+OUDPxE1? NYDT[4JVTE2VTx?= NHvXcYZKSzVyPUCuNFQh|ryP M2TkO|E6QTl4Mkey
ST486 M{LPOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVz+OUDPxE1? M2S0[WROW09? MoLOTWM2OD1zLkG5JO69VQ>? M1TqTVE6QTl4Mkey
HS766T NYrHWFRQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGP5ZYJ,PSEQvF2= NXXTcJd1TE2VTx?= NG\wSW9KSzVyPUKuNFAyKM7:TR?= M3vUUFE6QTl4Mkey
IMR-32 M3rqRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHPYWm1,PSEQvF2= M3PSRmROW09? MVXJR|UxRTBwMk[xJO69VQ>? MVGxPVk6PjJ5Mh?=
Daudi (Burkitt's) M2jjSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFP2XHN,PSEQvF2= NGfkVVFFVVOR MX;JR|UxRTJwNkO3JO69VQ>? M3PrNVE6QTl4Mkey
Aspc-1 M4SzXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4TzeZ42KM7:TR?= NXjvPY1jTE2VTx?= M4\BWmlEPTB;MD6zO|kh|ryP M4jQSVE6QTl4Mkey
SK-NSH NGnZe|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2jDOp42KM7:TR?= M1j6cGROW09? NIfPWYlKSzVyPUCuNVM6KM7:TR?= MYSxPVk6PjJ5Mh?=
MEC-1 (Chronic B cell) M{HuT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVn+OUDPxE1? M3rR[WROW09? M{njfWlEPTB;Mj62N|ch|ryP NXfwUGZOOTl7OU[yO|I>
Capan-2 M4\JR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlPZglUh|ryP M1PoXWROW09? NVrD[WFFUUN3ME2xMlc4PCEQvF2= M13Mb|E6QTl4Mkey
SHSY5Y MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHO0UIl,PSEQvF2= M3ThUGROW09? Mk\hTWM2OD1yLkGwOkDPxE1? MXyxPVk6PjJ5Mh?=
U937 (Histioocytic) NWDvRnhqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFXRVHN,PSEQvF2= M4PaeWROW09? M2q4S2lEPTB-NT6wNEDPxE1? NFT4docyQTl7NkK3Ni=>
Bxpc-1 M1\iR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYH+OUDPxE1? NWLVWZFVTE2VTx?= NIi5W4lKSzVyPUGuPVI1KM7:TR?= M1zoS|E6QTl4Mkey
Bxpc-3 NHS5ZXNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYH+OUDPxE1? NFnQcmZFVVOR M{[ye2lEPTB-NT6wNEDPxE1? MmW5NVk6QTZ{N{K=
HTB-92 MnfSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnriglUh|ryP MYTEUXNQ Mne3TWM2OD1zLkCyJO69VQ>? NYCzclA4OTl7OU[yO|I>
OCI-LY10 (B-cell) MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWS5WopChjVizszN NF6w[pFFVVOR M4XRPWlEPTB;MD60OUDPxE1? MX2xPVk6PjJ5Mh?=
PANC-1 M4PvTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoX4glUh|ryP NHPjbmdFVVOR NUT3VmNFUUN3ME61MlAxKM7:TR?= MU[xPVk6PjJ5Mh?=
To184.T MkHSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2nN[p42KM7:TR?= MlnaSG1UVw>? NVHrc2hjUUN3ME2wMlQ3QSEQvF2= MUKxPVk6PjJ5Mh?=
OCI-LY19 (B-cell) M4XwOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXT+OUDPxE1? NHHHRmhFVVOR NWn6UFNvUUN3ME2wMlQh|ryP MVyxPVk6PjJ5Mh?=
PANC-1 BM MmrQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1Tqep42KM7:TR?= M3TtcmROW09? MmP2TWM2OD53LkCwJO69VQ>? M3HaUVE6QTl4Mkey
SA-4 MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXH+OUDPxE1? M{PWcmROW09? NIfoPFhKSzVyPUGuN|AyKM7:TR?= MVexPVk6PjJ5Mh?=
RPMI 8226 NFnPfZpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Moi5glUh|ryP NXjWO2N7TE2VTx?= MlLPTWM2OD1zLkK5N{DPxE1? MY[xPVk6PjJ5Mh?=
HPAF-II NUTxblFkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYrCd5I{hjVizszN M2fhOWROW09? NIDMZ3lKSzVyPUCuOlQ1KM7:TR?= MmjRNVk6QTZ{N{K=
SHP-77 NIPaR2lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1m0Rp42KM7:TR?= MWLEUXNQ NULhVHBYUUN3ME2xMlg5QCEQvF2= NYnvUVNUOTl7OU[yO|I>
U266 B1 M4TqTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{XuUp42KM7:TR?= M3XJNWROW09? NEHofmlKSzVyPUGuOlY6KM7:TR?= MXmxPVk6PjJ5Mh?=
Hs700t MkXsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUD+OUDPxE1? NIC1O5hFVVOR NGG3PGZKSzVyPUCuNlMyKM7:TR?= MUixPVk6PjJ5Mh?=
NCI-446 MlPCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGTrfG1,PSEQvF2= NF6y[HBFVVOR NXGzT4p7UUN3ME2xMlE2PCEQvF2= NY\reG9yOTl7OU[yO|I>
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M109 NGXJelZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUnEcWw6hjVizszN NVjTU3RyTE2VTx?= Mo\QTWM2OD1zLkC1OUDPxE1? NVHNSGhXOTl7OU[yO|I>
BT549 NGjrdWVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYLIUoJ4hjVizszN NF7oeZZFVVOR M17rV2lEPTB;MT62OFUh|ryP NWPsV4xtOTl7OU[yO|I>
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BT474 (S) MnnmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEnvWXV,PSEQvF2= MVzEUXNQ NIHKZnpKSzVyPUKuOFA{KM7:TR?= MlXiNVk6QTZ{N{K=
HT-29 Mn;KS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFT2fId,PSEQvF2= Mkn2SG1UVw>? M{\6R2lEPTB;Mj6xNFMh|ryP M3uycFE6QTl4Mkey
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SW480 M4LM[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVn+OUDPxE1? MUHEUXNQ MnrMTWM2OD53LkCwJO69VQ>? M3LVfFE6QTl4Mkey
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H1437 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NU\vXXh5hjVizszN MoPnSG1UVw>? MYPJR|UxRTBwNUKzJO69VQ>? NH3VUYYyQTl7NkK3Ni=>
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H2087 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFq5XZd,PSEQvF2= MoPNSG1UVw>? NW\CS|l5UUN3ME6xMlAxKM7:TR?= MXexPVk6PjJ5Mh?=
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MDA-MB-435S M3viT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYX+OUDPxE1? NVPQVWFSTE2VTx?= NUfKUHNwUUN3ME2xMlg3QSEQvF2= MXGxPVk6PjJ5Mh?=
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KM12SM MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFi1b2R,PSEQvF2= NX7rUHVpTE2VTx?= NX3VRopxUUN3ME2wMlA2QSEQvF2= NHW5Z3MyQTl7NkK3Ni=>
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Rh41 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEXmcFh,OTEkgJtOwG0> NGT2ZoRKSzVyPUCuNFchyrWP MYOyNVI6QDd2NR?=
Rh18 M17BV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEfYN3N,OTEkgJtOwG0> NGS1dlJKSzVyPUSuPVYhyrWP MWmyNVI6QDd2NR?=
Rh30 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoDCglEx6oDMzszN MYrJR|UxRTBwMUmgxtVO M2TFT|IyOjl6N{S1
BT-12 NYfjPIJ7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWq5W3RGhjFy4pEK{txO NFP3ZnJKSzVyPUCuO|ghyrWP MVmyNVI6QDd2NR?=
CHLA-266 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWfEOGtDhjFy4pEK{txO Mo\1TWM2OD1yLki5JOK2VQ>? MkDhNlEzQTh5NEW=
TC-71 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGfZNGZ,OTEkgJtOwG0> NWPQW5J{UUN3ME2wMlEyKML3TR?= M3u2O|IyOjl6N{S1
CHLA-9 Mmf3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1X6NZ4yOOLCit88US=> NX\WXmVFUUN3ME2wMlEzKML3TR?= NESy[4ozOTJ7OEe0OS=>
CHLA-10 M2L3[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmP3glEx6oDMzszN MmjtTWM2OD1yLk[yJOK2VQ>? MkPqNlEzQTh5NEW=
CHLA-258 NXjndVh5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2naVp4yOOLCit88US=> NGPuTmdKSzVyPUCuNlchyrWP NGi5UIozOTJ7OEe0OS=>
GBM2 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYm3XIxEhjFy4pEK{txO M3Xx[WlEPTB;MT60O{DDvU1? MnHiNlEzQTh5NEW=
NB-1643 MnTsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mo\pglEx6oDMzszN M4X3RWlEPTB;MD6xNkDDvU1? NU\WVll4OjF{OUi3OFU>
NB-EBc1 NHnscZJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEn4OWt,OTEkgJtOwG0> NFHWb4tKSzVyPUCuN|UhyrWP NF72SI4zOTJ7OEe0OS=>
CHLA-90 NH61T|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnuzglEx6oDMzszN NUfoUJdSUUN3ME2wMlc4KML3TR?= NUDDZ5VWOjF{OUi3OFU>
CHLA-136 NXyyOIlmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVHhNJJuhjFy4pEK{txO M3XHOmlEPTB;MD61NkDDvU1? M3rkT|IyOjl6N{S1
NALM-6 M1fiUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NG\iUYJ,OTEkgJtOwG0> M1XHOGlEPTB;MD60PUDDvU1? M3\5NVIyOjl6N{S1
COG-LL-317 M3jqcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoPGglEx6oDMzszN M13XOWlEPTB;MT6zPEDDvU1? MoDHNlEzQTh5NEW=
RS4;11 M2rQfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoPlglEx6oDMzszN NUH2PWx5UUN3ME2wMlM5KML3TR?= M2fyOlIyOjl6N{S1
MOLT-4 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH7WVJF,OTEkgJtOwG0> MoXyTWM2OD1yLkWzJOK2VQ>? M1rGSVIyOjl6N{S1
CCRF-CEM NEOyemhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnfSglEx6oDMzszN NXTVT2ZsUUN3ME2xMlE{KML3TR?= MkTnNlEzQTh5NEW=
Kasumi-1 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX\rb5JVhjFy4pEK{txO MWTJR|UxRTFwMjFCuW0> MUeyNVI6QDd2NR?=
Karpas-299 M4LZfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkfxglEx6oDMzszN NIi3[VlKSzVyPUGuOlQhyrWP Ml\ENlEzQTh5NEW=
Ramos-RA1 MnHOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF;CRlN,OTEkgJtOwG0> NU\SNmZ5UUN3ME2xMlMyKML3TR?= NYXQXppLOjF{OUi3OFU>
Rh30  NEnt[ldHfW6ldHnvckBie3OjeR?= NF\pZlZqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:|cHjvdplt[XSrb36= MUSyOVkzPTN5OB?=
Rh41 NIPPbIRHfW6ldHnvckBie3OjeR?= MnWxbY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w NIDrSY0zPTl{NUO3PC=>
RD MnzCSpVv[3Srb36gZZN{[Xl? NUjRNGRCcW6mdXPld{BidiCrbnPy[YF{\SCxZjDTSmsheGixc4Doc5J6dGG2aX;u Ml\VNlU6OjV|N{i=
A549 MnLvT4lv[XOnIHHzd4F6 NUPkRmZ5OC534pEK{txO M{L0e2ROW09? NYW5RWoxcW6qaXLpeJMhUUeILVnSM2lTKGGldHn2ZZRqd25? MofFNlY6Ojh3N{i=
NCI-H358 MYLLbY5ie2ViYYPzZZk> NXX6Zog1OC534pEK{txO MoTrSG1UVw>? NGO1Z25qdmirYnn0d{BKT0ZvSWKvTXIh[WO2aY\heIlwdg>? M1vEflI3QTJ6NUe4
A549 NXzCc29MTnWwY4Tpc44h[XO|YYm= NUP4NWNyOC534pEK{txO NGLJW2pFVVOR NWTKcmJl[2G3c3XzJIEh[2:wY4XydoVvfCCmZXPy[YF{\SCrbjDwbI9{eGixconsZZRm\CCDS2SgZY5lKEWUSx?= M1;sfVI3QTJ6NUe4
NCI-H358 M1f1dWZ2dmO2aX;uJIF{e2G7 NIW2RmQxNjYkgJtOwG0> MUjEUXNQ M4\xXoNifXOnczDhJINwdmO3coLlcpQh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSUuWIHHu[EBGWkt? NFS1d3ozPjl{OEW3PC=>
A549 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYHxW|JyhjFy4pEK{txO NYO5SXN4TE2VTx?= MoTuTWM2OD1yLke2JO69VQ>? Mn3yNlY6Ojh3N{i=
NCI-H358 M2Dzemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYr+NVDjiIsQvF2= NVz1c3lUTE2VTx?= MlnCTWM2OD1zLkC5JO69VQ>? Mk\INlY6Ojh3N{i=
A549 MY\BdI9xfG:|aYOgZZN{[Xl? M{nVRlAvPeLCit88US=> M4\oR2ROW09? MWHpcoR2[2W|IFHwc5B1d3Orcx?= NUHZTZhwOjZ7Mki1O|g>
NCI-H358 NUHrcJljSXCxcITvd4l{KGG|c3H5 NEjwVWExNjYkgJtOwG0> M2HnOmROW09? MkjlbY5lfWOnczDBdI9xfG:|aYO= NH\0WokzPjl{OEW3PC=>
A549 M4f5OmZ2dmO2aX;uJIF{e2G7 NVrwO4Q1OC534pEK{txO NH\FcXdFVVOR MUfy[YR2[2W|IIfveY5lKGOub4P1doU> NYr2WIlEOjZ7Mki1O|g>
NCI-H358 MnrySpVv[3Srb36gZZN{[Xl? NVTXc21oOC534pEK{txO NInKeJZFVVOR NEXHT|hz\WS3Y3XzJJdwfW6mIHPsc5N2emV? NVvn[WFlOjZ7Mki1O|g>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-IGFIRRβ/InsRβ / IGFIRβ / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 26136493     


(C) T4105 cells were treated with OSI-906 or BMS-754807 at indicated concentrations for 24 hours, lysed, and subjected to immunoblotting.

26136493
Growth inhibition assay
Cell viability; 

PubMed: 30754629     


Response of SK-CO-1 to various drugs and drug combinations.

30754629
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]
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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]
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  • 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]
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  • Animal Models: IGF-1R-Sal, GEO, Colo205, JJN3, RD1 or Rh41 tumor–bearing nude mice
  • 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
Smiles CC1(CCCN1C2=NN3C=CC=C3C(=N2)NC4=NNC(=C4)C5CC5)C(=O)NC6=CN=C(C=C6)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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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).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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

The Serial Dilution Calculator Equation

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID