BMS-754807

For research use only.

Catalog No.S1124

23 publications

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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Selleck's BMS-754807 has been cited by 23 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 MUPLbY5ie2ViYYPzZZk> MXrpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEmJRj2xVkApUUN3MDC9JFE{dk1rIHHu[EB1cGViZH;3cpN1emWjbTD0ZZJo\XS|IFHreEApUUN3MDC9JFIzdk1rIHHu[EBOSVCNIDjJR|UxKD1iMUPuUUk> NGfITGMyQTd5OECyOC=>
IGF-Sal M{jDV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4S1OWlEPTB;NzDuUS=> NVPTO4ZoOTl5N{iwNlQ>
CCRF-CEM (ALL) NVqzUVdkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmfNglUh|ryP NGqze|BFVVOR MkDNTWM2OD1zLkKzPUDPxE1? MkixNVk6QTZ{N{K=
PC3 NXvKeplUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVLDTIpPhjVizszN NWT0NpMyTE2VTx?= NYLNNHdFUUN3ME2wMlk3PSEQvF2= MXmxPVk6PjJ5Mh?=
JD MknkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXH+OUDPxE1? NEnmVplFVVOR MkWwTWM2OD1yLkO5NUDPxE1? NYLG[4xMOTl7OU[yO|I>
DU145 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVSyeI1IhjVizszN NUHwdZBSTE2VTx?= MXXJR|UxRTFwNE[1JO69VQ>? NUX6ZYJWOTl7OU[yO|I>
KAG NWTuWlR5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVT+OUDPxE1? NVLZOWJPTE2VTx?= MXzJR|UxRTFwNk[1JO69VQ>? M3nVU|E6QTl4Mkey
K-562 (CML) NYLIZpVpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHzKRY5,PSEQvF2= M3jXemROW09? MoCyTWM2OD1{LkOwNkDPxE1? NW\EdnB5OTl7OU[yO|I>
B6-P210 (Murine ALL) MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1SzXp42KM7:TR?= MWPEUXNQ NW\ud45xUUN3ME2xMlI6OyEQvF2= MUixPVk6PjJ5Mh?=
LN CAP-FGC NIPiUVRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV;kTVBFhjVizszN M{XlVWROW09? M2D0eWlEPTB;MT60N|Qh|ryP MkfmNVk6QTZ{N{K=
VW MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHXhZXd,PSEQvF2= NIrPdGtFVVOR NUDXPI0yUUN3ME2wMlAyQSEQvF2= MoHuNVk6QTZ{N{K=
MV411 (B Myelomonocytic) NIqySGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYXtfJpPhjVizszN MlzWSG1UVw>? NF7jXnBKSzVyPUCuN|Mh|ryP NWmz[pVROTl7OU[yO|I>
MDA-PCa-2b MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIW4fmV,PSEQvF2= MlXESG1UVw>? NVzMWppsUUN3ME2wMlA6QCEQvF2= Mn76NVk6QTZ{N{K=
LG NY\DZndPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MniwglUh|ryP NVe3V3pHTE2VTx?= MYDJR|UxRTBwMEO4JO69VQ>? MWGxPVk6PjJ5Mh?=
RS411 (B cell precursor-ALL) MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWDqXmtwhjVizszN MlzWSG1UVw>? NH7qPItKSzVyPUCuNVAzKM7:TR?= MlvzNVk6QTZ{N{K=
22-r-1 NGTxPVJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVTqR5U5hjVizszN MVXEUXNQ NGDURnlKSzVyPUCuNVc2KM7:TR?= NEnZNXYyQTl7NkK3Ni=>
5838 MkS2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{PPPZ42KM7:TR?= M4LOWWROW09? NWfQWZFIUUN3ME2wMlA{PCEQvF2= MojmNVk6QTZ{N{K=
P388 (Murine) Mm\qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4f6fZ42KM7:TR?= NELHdlhFVVOR MWPJR|UxRTRwMkeg{txO Mn3UNVk6QTZ{N{K=
A2780/S M4\Ufmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF\aOXN,PSEQvF2= MYTEUXNQ NVfIbY55UUN3ME2wMlEzOiEQvF2= NH7LSmIyQTl7NkK3Ni=>
RDES MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYjZbJh7hjVizszN M1fKRWROW09? NI\Md|JKSzVyPUCuNFEzKM7:TR?= NVfSUFhIOTl7OU[yO|I>
B6-T315I (Murine B-ALL) NXLXe|dNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHvle4p,PSEQvF2= MnTOSG1UVw>? MVXJR|UxRTJwOEOg{txO MkThNVk6QTZ{N{K=
TOV 112D M{G0Z2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXrzdVRqhjVizszN M3;iZmROW09? MWfJR|UxRTJwMUS2JO69VQ>? MonNNVk6QTZ{N{K=
TC32 M3fON2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYL+OUDPxE1? MX7EUXNQ MoHETWM2OD1yLkCwPEDPxE1? M2L2OFE6QTl4Mkey
HL60 (acute myelocytic) MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYHlXXhWhjVizszN NXWweI1DTE2VTx?= NFL2b4dKSzVyPUCuNVIh|ryP MmrPNVk6QTZ{N{K=
TOV 21G MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUT+OUDPxE1? MoXLSG1UVw>? MkTsTWM2OD12LkK3PUDPxE1? MYWxPVk6PjJ5Mh?=
TC71 NGLs[VNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFLZUXV,PSEQvF2= MoXLSG1UVw>? M1rM[GlEPTB;MD6wNVQh|ryP NFfoNFIyQTl7NkK3Ni=>
HPN-ALL (T-cell) NV\5U4RGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEfFPFB,PSEQvF2= MV7EUXNQ NHzJZnZKSzVyPUCuOVIh|ryP NYOyZXpROTl7OU[yO|I>
A2780R MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4n1bp42KM7:TR?= NV3kOokzTE2VTx?= MofCTWM2OD1zLkW2OEDPxE1? NVrUR2lEOTl7OU[yO|I>
Rh1 NFKwUpdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoWwglUh|ryP NUGwcmtETE2VTx?= MXPJR|UxRTBwMEK3JO69VQ>? NFfQOYIyQTl7NkK3Ni=>
Kasumi-1 (acute myeloid) M4PWPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX3aVGNwhjVizszN M1;lTGROW09? MVvJR|UxRTBwMU[g{txO NHHsd4EyQTl7NkK3Ni=>
sk-ov-3 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH\kVWV,PSEQvF2= NX3Ze|JWTE2VTx?= NVjm[VBZUUN3ME21MlEh|ryP NGTjdVQyQTl7NkK3Ni=>
ME M1zxc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mo[xglUh|ryP MUPEUXNQ Mm\jTWM2OD1yLkCxOUDPxE1? NIHhS5UyQTl7NkK3Ni=>
L1210 (Murine lymphocytic) M3TDN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3PTV542KM7:TR?= NX63T3JvTE2VTx?= NWnKb|dNUUN3ME2yMlM6KM7:TR?= MV:xPVk6PjJ5Mh?=
sw-626 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVXHNWlohjVizszN MYPEUXNQ MUTJR|UxRTJwM{C2JO69VQ>? M3y5OFE6QTl4Mkey
CTR NYDwd4pJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkfSglUh|ryP MV\EUXNQ M3;SPWlEPTB;MD6yOVMh|ryP MUOxPVk6PjJ5Mh?=
ML2 (Myelomonocytic) NF\pN3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUDiSHpihjVizszN NGjneVdFVVOR NU\1b4VFUUN3ME2wMlA6KM7:TR?= MYmxPVk6PjJ5Mh?=
ovcar-3 M{HQZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFj0b|N,PSEQvF2= NIfPNIdFVVOR NEjJbo1KSzVyPUWg{txO NXrJUFYzOTl7OU[yO|I>
Rh36 NUSydopJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnPFglUh|ryP NFjvR4dFVVOR M1jINWlEPTB;MT60N|Ih|ryP NXHDbm54OTl7OU[yO|I>
MOLM-13 (acute myeloid) M3;DN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml[wglUh|ryP Mk\0SG1UVw>? M{fKOGlEPTB;MD60NkDPxE1? MXqxPVk6PjJ5Mh?=
ovcar-4 M2LhOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkntglUh|ryP Mkf2SG1UVw>? NX\3em8xUUN3ME2xJO69VQ>? NFe3Z3kyQTl7NkK3Ni=>
Rh41 NYqxNpg5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUjaVZFVhjVizszN MUXEUXNQ M4nhSGlEPTB;MD6wNFUh|ryP MkjXNVk6QTZ{N{K=
Mutz 2 (acute myeloid) MmCwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVX+OUDPxE1? NIjvdI9FVVOR NUD2WJVzUUN3ME2xMlE2KM7:TR?= NYHHNZJFOTl7OU[yO|I>
ovcar-5 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NInJZ2R,PSEQvF2= MoK3SG1UVw>? NH7LO5lKSzVyPUCuNFUh|ryP NVzzS3RWOTl7OU[yO|I>
RD1 NEnEflJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIWxR4R,PSEQvF2= M13HZ2ROW09? MkWxTWM2OD1yLkC2PEDPxE1? NXnZPIpIOTl7OU[yO|I>
OCI-AML 2 (acute myeloid) MnjjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYf+OUDPxE1? M4HQTGROW09? MnzITWM2OD1|LkOzJO69VQ>? Mn7QNVk6QTZ{N{K=
786-O NX3Fb25ET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4PhVp42KM7:TR?= M3PibWROW09? NH;xbHdKSzVyPUGuOlQ4KM7:TR?= MmrSNVk6QTZ{N{K=
A673 NVW4cHpTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFTaRZB,PSEQvF2= NXy4PHhXTE2VTx?= MVrJR|UxRTBwNEC4JO69VQ>? NVu2e3UyOTl7OU[yO|I>
TALL-1 (T-cell) MmD1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mo[0glUh|ryP M13vc2ROW09? M{C2bmlEPTB;MT6yPEDPxE1? MWexPVk6PjJ5Mh?=
151-B MnjuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXu4NoZ2hjVizszN NILuNHBFVVOR Mm\YTWM2OD1{Lk[3JO69VQ>? NEXycnoyQTl7NkK3Ni=>
PFSK-1 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1:wOp42KM7:TR?= M3nxOGROW09? NX7IUYJTUUN3ME2wMlE{OiEQvF2= MVmxPVk6PjJ5Mh?=
THP-1 NFj6PG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnrxglUh|ryP NVztfmw1TE2VTx?= M1izdGlEPTB;Nj61PEDPxE1? NFjMPZUyQTl7NkK3Ni=>
HEK293 NXfHWmQ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2naUZ42KM7:TR?= MlfSSG1UVw>? M4T3fGlEPTB;MD65NVUh|ryP MYqxPVk6PjJ5Mh?=
DAOY NX3qcGM6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUH+OUDPxE1? M3PQbmROW09? NWW2[YlkUUN3ME2xMlk4QSEQvF2= NX35SYZOOTl7OU[yO|I>
SET2 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEHnTlh,PSEQvF2= Mnv0SG1UVw>? NUfvbmZuUUN3ME2wMlI6QCEQvF2= M{HMU|E6QTl4Mkey
HTB-46 M13Re2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmTCglUh|ryP NXm2N3JDTE2VTx?= M3X0OGlEPTB;NT6yOUDPxE1? NUXTNnVxOTl7OU[yO|I>
SK-NAS NWnuc5Z1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmfRglUh|ryP MYDEUXNQ NXHtSIppUUN3ME2wMlQ6PyEQvF2= NEL5epUyQTl7NkK3Ni=>
CTLL2 M1ntOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX3wOFBRhjVizszN M4\x[WROW09? M4PXPGlEPTB-MT6wNEDPxE1? NIfBSIcyQTl7NkK3Ni=>
HTB-47 Mke4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlXhglUh|ryP MVPEUXNQ MkHxTWM2OD1{LkC1OkDPxE1? NVG5TZB[OTl7OU[yO|I>
LAN-1 MlvUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV3POpBNhjVizszN NVPlU5R4TE2VTx?= NYDme41pUUN3ME2wMlA1KM7:TR?= MYCxPVk6PjJ5Mh?=
ST486 M{\jUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2DvXp42KM7:TR?= NF7QcJVFVVOR NEH6TXlKSzVyPUGuNVkh|ryP NXXpbGtpOTl7OU[yO|I>
HS766T MmfzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\qV542KM7:TR?= NVPh[YR[TE2VTx?= NGnJW|FKSzVyPUKuNFAyKM7:TR?= M4jzcFE6QTl4Mkey
IMR-32 NGGxZm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIjoO|B,PSEQvF2= MV;EUXNQ MXrJR|UxRTBwMk[xJO69VQ>? M3zycFE6QTl4Mkey
Daudi (Burkitt's) M1HFOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVj+OUDPxE1? Ml3VSG1UVw>? M3nsOmlEPTB;Mj62N|ch|ryP MVWxPVk6PjJ5Mh?=
Aspc-1 Mk\jS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1\WNJ42KM7:TR?= NXrOVI5xTE2VTx?= NVXlW41kUUN3ME2wMlM4QSEQvF2= M3ixTlE6QTl4Mkey
SK-NSH Mn7hS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWf+OUDPxE1? M3;ldmROW09? NUn4Z|Y6UUN3ME2wMlE{QSEQvF2= Mm\NNVk6QTZ{N{K=
MEC-1 (Chronic B cell) M{S4fGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWj+OUDPxE1? NF3xUHlFVVOR NIm5WI9KSzVyPUKuOlM4KM7:TR?= M3GzTVE6QTl4Mkey
Capan-2 NF30d5lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkPlglUh|ryP M1fneGROW09? MYHJR|UxRTFwN{e0JO69VQ>? MkXGNVk6QTZ{N{K=
SHSY5Y MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn\GglUh|ryP MY\EUXNQ NVrLOVlNUUN3ME2wMlExPiEQvF2= NFry[mwyQTl7NkK3Ni=>
U937 (Histioocytic) MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2W0dZ42KM7:TR?= M3LGPGROW09? MoT1TWM2OD53LkCwJO69VQ>? NU\kTWt4OTl7OU[yO|I>
Bxpc-1 NHTrdopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEXpPZJ,PSEQvF2= M1LmSGROW09? NIjHSoZKSzVyPUGuPVI1KM7:TR?= MWSxPVk6PjJ5Mh?=
Bxpc-3 NE\D[mtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MofrglUh|ryP NFHyR41FVVOR MY\JR|UxRjVwMECg{txO MV2xPVk6PjJ5Mh?=
HTB-92 M1PHOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXq2cGtxhjVizszN NITmcppFVVOR Mo\xTWM2OD1zLkCyJO69VQ>? M4\afFE6QTl4Mkey
OCI-LY10 (B-cell) MmjnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXP+OUDPxE1? NHLYZWdFVVOR M3PUOGlEPTB;MD60OUDPxE1? Mnr4NVk6QTZ{N{K=
PANC-1 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWPNR2RQhjVizszN NXrL[pA2TE2VTx?= NXm5WWNbUUN3ME61MlAxKM7:TR?= NELVO2wyQTl7NkK3Ni=>
To184.T MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWL+OUDPxE1? NGXTfIJFVVOR MmDkTWM2OD1yLkS2PUDPxE1? MlLUNVk6QTZ{N{K=
OCI-LY19 (B-cell) NGnjVWNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVf+OUDPxE1? NGXLfXZFVVOR NELmc2dKSzVyPUCuOEDPxE1? MkK3NVk6QTZ{N{K=
PANC-1 BM NFixdFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIfMcIZ,PSEQvF2= M{PXOmROW09? MV;JR|UxRjVwMECg{txO MkDENVk6QTZ{N{K=
SA-4 NIrqfoRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{ixc542KM7:TR?= NWL1NmIyTE2VTx?= M4fkbWlEPTB;MT6zNFEh|ryP MX[xPVk6PjJ5Mh?=
RPMI 8226 Mo\qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIHNcmh,PSEQvF2= MoXISG1UVw>? Mo\XTWM2OD1zLkK5N{DPxE1? NXfYbpFWOTl7OU[yO|I>
HPAF-II MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1PS[542KM7:TR?= M3HIcGROW09? NGD4cHFKSzVyPUCuOlQ1KM7:TR?= NHTZenoyQTl7NkK3Ni=>
SHP-77 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWj+OUDPxE1? Ml;jSG1UVw>? MV;JR|UxRTFwOEi4JO69VQ>? NXTiXYtHOTl7OU[yO|I>
U266 B1 NYHVd2J5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NETye2p,PSEQvF2= MmG4SG1UVw>? NISzSYpKSzVyPUGuOlY6KM7:TR?= Mmf3NVk6QTZ{N{K=
Hs700t NXnO[lNET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1fEfp42KM7:TR?= NIT4WWxFVVOR NH[xOJFKSzVyPUCuNlMyKM7:TR?= NEHqTVIyQTl7NkK3Ni=>
NCI-446 NETCPYFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVTBb4o5hjVizszN M1Pm[WROW09? NYrkT5dNUUN3ME2xMlE2PCEQvF2= M{XkeVE6QTl4Mkey
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Rh30 NVnNcpV5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVO5fGN4hjFy4pEK{txO NVzMVFRIUUN3ME2wMlE6KML3TR?= NFviUXczOTJ7OEe0OS=>
BT-12 NITvdlFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYT+NVDjiIsQvF2= M2K1TmlEPTB;MD63PEDDvU1? MYGyNVI6QDd2NR?=
CHLA-266 Mo\IS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoDtglEx6oDMzszN MWTJR|UxRTBwOEmgxtVO M1rmVVIyOjl6N{S1
TC-71 MnX0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYr+NVDjiIsQvF2= MYPJR|UxRTBwMUGgxtVO MYeyNVI6QDd2NR?=
CHLA-9 NH:xW2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUD+NVDjiIsQvF2= NHH2UopKSzVyPUCuNVIhyrWP MXmyNVI6QDd2NR?=
CHLA-10 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFrjcpJ,OTEkgJtOwG0> NEO2TVVKSzVyPUCuOlIhyrWP Mn7CNlEzQTh5NEW=
CHLA-258 M3\nXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVL+NVDjiIsQvF2= M2DEbWlEPTB;MD6yO{DDvU1? NYjFR|ZqOjF{OUi3OFU>
GBM2 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3ry[Z4yOOLCit88US=> MUnJR|UxRTFwNEegxtVO MXiyNVI6QDd2NR?=
NB-1643 NHzmSHlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlfOglEx6oDMzszN NGXzSVRKSzVyPUCuNVIhyrWP NWjROYd[OjF{OUi3OFU>
NB-EBc1 M4TmW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUDue2tXhjFy4pEK{txO NIqwc5pKSzVyPUCuN|UhyrWP NVvNV3Q6OjF{OUi3OFU>
CHLA-90 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3L6XJ4yOOLCit88US=> Mn;6TWM2OD1yLke3JOK2VQ>? NGi2TVMzOTJ7OEe0OS=>
CHLA-136 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVnVWHA5hjFy4pEK{txO NVH6dZNCUUN3ME2wMlUzKML3TR?= MkfqNlEzQTh5NEW=
NALM-6 NWTlblZvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlzBglEx6oDMzszN MWXJR|UxRTBwNEmgxtVO M13ISFIyOjl6N{S1
COG-LL-317 M13GeWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVjZ[nhZhjFy4pEK{txO MWLJR|UxRTFwM{igxtVO M3TIblIyOjl6N{S1
RS4;11 NYjjOVZIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmX3glEx6oDMzszN M2TCcmlEPTB;MD6zPEDDvU1? MomyNlEzQTh5NEW=
MOLT-4 NH3M[FdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEexOHF,OTEkgJtOwG0> NImxWXpKSzVyPUCuOVMhyrWP NE[2TpIzOTJ7OEe0OS=>
CCRF-CEM NXLWfFdvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEDiZmF,OTEkgJtOwG0> NVPUUVMzUUN3ME2xMlE{KML3TR?= NWjTPIw{OjF{OUi3OFU>
Kasumi-1 M33KUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoK4glEx6oDMzszN M1\VcWlEPTB;MT6yJOK2VQ>? M1\ZfVIyOjl6N{S1
Karpas-299 M3rGeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX3+NVDjiIsQvF2= NYDRWVVZUUN3ME2xMlY1KML3TR?= NXfBRY81OjF{OUi3OFU>
Ramos-RA1 NUWxPJU5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWHnfoZnhjFy4pEK{txO NFLtU2FKSzVyPUGuN|EhyrWP NF[2[3UzOTJ7OEe0OS=>
Rh30  M{H3NGZ2dmO2aX;uJIF{e2G7 M2X6colv\HWlZYOgZY4hcW6lcnXhd4Uhd2ZiU1\LJJBpd3OyaH;yfYxifGmxbh?= MX2yOVkzPTN5OB?=
Rh41 NXrUXlJnTnWwY4Tpc44h[XO|YYm= NHrtcpVqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:|cHjvdplt[XSrb36= Mn:zNlU6OjV|N{i=
RD NV:yfo9JTnWwY4Tpc44h[XO|YYm= Mn[4bY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w M3PDNFI2QTJ3M{e4
A549 NVnWZXhOU2mwYYPlJIF{e2G7 M3r2R|AvPeLCit88US=> NUWwVHBRTE2VTx?= MV3pcohq[mm2czDJS2YuUVJxSWKgZYN1cX[jdHnvci=> MX[yOlkzQDV5OB?=
NCI-H358 NI[wenNMcW6jc3WgZZN{[Xl? MYGwMlXjiIsQvF2= MWTEUXNQ NYOxbm91cW6qaXLpeJMhUUeILVnSM2lTKGGldHn2ZZRqd25? M3XXPFI3QTJ6NUe4
A549 MUjGeY5kfGmxbjDhd5NigQ>? NV;4Opl3OC534pEK{txO NXuyU29jTE2VTx?= MoTtZ4F2e2W|IHGgZ49v[3W{cnXueEBl\WO{ZXHz[UBqdiCyaH;zdIhwenmuYYTl[EBCU1RiYX7kJGVTUw>? MXOyOlkzQDV5OB?=
NCI-H358 NUK1enJGTnWwY4Tpc44h[XO|YYm= NGDOZnExNjYkgJtOwG0> M4rWdWROW09? MXfjZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM NXfxT3VCOjZ7Mki1O|g>
A549 NFPGbZdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV[2PYxJhjFy4pEK{txO NInhRotFVVOR M37iT2lEPTB;MD63OkDPxE1? MX6yOlkzQDV5OB?=
NCI-H358 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1O3Sp4yOOLCit88US=> MUTEUXNQ NIjUR2NKSzVyPUGuNFkh|ryP Mom5NlY6Ojh3N{i=
A549 NFS4[3BCeG:ydH;zbZMh[XO|YYm= NF:zZ3IxNjYkgJtOwG0> NWXX[ZVpTE2VTx?= NXzEcZF7cW6mdXPld{BCeG:ydH;zbZM> NH;FdGIzPjl{OEW3PC=>
NCI-H358 NITMcXhCeG:ydH;zbZMh[XO|YYm= MmruNE426oDMzszN MVvEUXNQ NYjIT3k6cW6mdXPld{BCeG:ydH;zbZM> M2TyWlI3QTJ6NUe4
A549 NYDLdZRNTnWwY4Tpc44h[XO|YYm= MnzGNE426oDMzszN NX;MUphWTE2VTx?= NUDFS5JmemWmdXPld{B4d3WwZDDjcI9{fXKn NY\PXHh[OjZ7Mki1O|g>
NCI-H358 M1LwemZ2dmO2aX;uJIF{e2G7 MVSwMlXjiIsQvF2= M2PIOGROW09? Mo\TdoVlfWOnczD3c5Vv\CClbH;zeZJm M1HwbVI3QTJ6NUe4

... 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=N[N]3C=CC=C3C(=N2)NC4=N[NH]C(=C4)C5CC5)C(=O)NC6=CC=C(F)N=C6

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

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

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    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

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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