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BMS-754807

For research use only.

Catalog No.S1124

33 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 (c-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 33 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 (c-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 NHfN[mJMcW6jc3WgZZN{[Xl? MWrpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEmJRj2xVkApUUN3MDC9JFE{dk1rIHHu[EB1cGViZH;3cpN1emWjbTD0ZZJo\XS|IFHreEApUUN3MDC9JFIzdk1rIHHu[EBOSVCNIDjJR|UxKD1iMUPuUUk> NYnhTm1ZOTl5N{iwNlQ>
IGF-Sal M3rTXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NW[yeWkzUUN3ME23JI5O NVfoPFRlOTl5N{iwNlQ>
CCRF-CEM (ALL) NF3pO5NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmXBglUh|ryP MkH5SG1UVw>? M2q4[GlEPTB;MT6yN|kh|ryP NFL0clkyQTl7NkK3Ni=>
PC3 NU\DeXJTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX\+OUDPxE1? NFrRNZpFVVOR MkfNTWM2OD1yLkm2OUDPxE1? MlzJNVk6QTZ{N{K=
JD NEj6clNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUj+OUDPxE1? M1nRNGROW09? M1HuUGlEPTB;MD6zPVEh|ryP M4\3NlE6QTl4Mkey
DU145 M3foT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{i0fp42KM7:TR?= MlnpSG1UVw>? NF62fHpKSzVyPUGuOFY2KM7:TR?= MUmxPVk6PjJ5Mh?=
KAG MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF3lS3l,PSEQvF2= NXjpNWRwTE2VTx?= MnjqTWM2OD1zLk[2OUDPxE1? M3fQWlE6QTl4Mkey
K-562 (CML) MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWf+OUDPxE1? NFK5RpdFVVOR NE\6eIZKSzVyPUKuN|AzKM7:TR?= NHTh[3MyQTl7NkK3Ni=>
B6-P210 (Murine ALL) MoT2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1ewdJ42KM7:TR?= NHjSTpdFVVOR NWTleZdrUUN3ME2xMlI6OyEQvF2= NWHjS286OTl7OU[yO|I>
LN CAP-FGC MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXzvRoVphjVizszN NVHu[|FFTE2VTx?= MmDWTWM2OD1zLkSzOEDPxE1? MWmxPVk6PjJ5Mh?=
VW NIT0[VFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH73dI5,PSEQvF2= Ml;lSG1UVw>? NHf5W5ZKSzVyPUCuNFE6KM7:TR?= MXuxPVk6PjJ5Mh?=
MV411 (B Myelomonocytic) NULRUlBET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NET2UmR,PSEQvF2= M{j4OmROW09? NW\kcphHUUN3ME2wMlM{KM7:TR?= MWCxPVk6PjJ5Mh?=
MDA-PCa-2b NYf5cVRoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn2yglUh|ryP NV;zPJVrTE2VTx?= NULRWFk3UUN3ME2wMlA6QCEQvF2= MWCxPVk6PjJ5Mh?=
LG M4nPeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXrvTHlphjVizszN NVzXcVZxTE2VTx?= NXq1XolXUUN3ME2wMlA{QCEQvF2= M{nGXFE6QTl4Mkey
RS411 (B cell precursor-ALL) NVy2[Ix5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGrJTYJ,PSEQvF2= MnrDSG1UVw>? MoToTWM2OD1yLkGwNkDPxE1? MY[xPVk6PjJ5Mh?=
22-r-1 NVLRTodJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUDpOXc4hjVizszN NH3xc|RFVVOR MXrJR|UxRTBwMUe1JO69VQ>? Mlv2NVk6QTZ{N{K=
5838 MmfBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIXCPWh,PSEQvF2= NYLFdW1UTE2VTx?= NYnWd|JOUUN3ME2wMlA{PCEQvF2= NXTw[mI6OTl7OU[yO|I>
P388 (Murine) MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUj+OUDPxE1? NHvCOnZFVVOR MXXJR|UxRTRwMkeg{txO M37zXlE6QTl4Mkey
A2780/S MkWxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWf+OUDPxE1? MofXSG1UVw>? MnrFTWM2OD1yLkGyNkDPxE1? NUfWbHhQOTl7OU[yO|I>
RDES NIfQPItIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWP+OUDPxE1? M{ThTWROW09? NXXmdZg3UUN3ME2wMlAyOiEQvF2= NIracGIyQTl7NkK3Ni=>
B6-T315I (Murine B-ALL) M{TPN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoDVglUh|ryP M{[xfmROW09? M2[4fGlEPTB;Mj64N{DPxE1? NGf5enUyQTl7NkK3Ni=>
TOV 112D NYrUWGpjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVHsWZB3hjVizszN NU\tXJFPTE2VTx?= MUDJR|UxRTJwMUS2JO69VQ>? M3T6SVE6QTl4Mkey
TC32 NVTrfpdvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml\lglUh|ryP NVLQUY13TE2VTx?= MYnJR|UxRTBwMEC4JO69VQ>? M36ze|E6QTl4Mkey
HL60 (acute myelocytic) NITKWGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{DrZZ42KM7:TR?= M2fQPWROW09? MoTDTWM2OD1yLkGyJO69VQ>? NUfOVFQzOTl7OU[yO|I>
TOV 21G MnvQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXvrWnpthjVizszN MWLEUXNQ Mn3XTWM2OD12LkK3PUDPxE1? NISxZpYyQTl7NkK3Ni=>
TC71 M{LlU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mnf6glUh|ryP MWTEUXNQ NGj5SY9KSzVyPUCuNFE1KM7:TR?= NFPzbHcyQTl7NkK3Ni=>
HPN-ALL (T-cell) NH3aSG1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV\OR3A3hjVizszN MYTEUXNQ Mn30TWM2OD1yLkWyJO69VQ>? MnLhNVk6QTZ{N{K=
A2780R M3K5SGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYCwS4JzhjVizszN NVHwUoc{TE2VTx?= MVXJR|UxRTFwNU[0JO69VQ>? NWXRdpQ4OTl7OU[yO|I>
Rh1 NFXxTGNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWj3NHZXhjVizszN NV;TOmFYTE2VTx?= MYnJR|UxRTBwMEK3JO69VQ>? M4nNNVE6QTl4Mkey
Kasumi-1 (acute myeloid) NFHHSIdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mlf0glUh|ryP NWnNNmpnTE2VTx?= NWr5NWlPUUN3ME2wMlE3KM7:TR?= MonzNVk6QTZ{N{K=
sk-ov-3 MknwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIjDXYh,PSEQvF2= MULEUXNQ M3LJPWlEPTB;NT6xJO69VQ>? M4LaZVE6QTl4Mkey
ME MlzPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1z0ZZ42KM7:TR?= MYfEUXNQ NGLiXlZKSzVyPUCuNFE2KM7:TR?= M{Lyd|E6QTl4Mkey
L1210 (Murine lymphocytic) MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHKwPFF,PSEQvF2= MmnGSG1UVw>? M4XHV2lEPTB;Mj6zPUDPxE1? MYKxPVk6PjJ5Mh?=
sw-626 MkHrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXnxPJZyhjVizszN MUfEUXNQ MX\JR|UxRTJwM{C2JO69VQ>? MYWxPVk6PjJ5Mh?=
CTR NV3MVmNJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NI\uOnB,PSEQvF2= NEfmbYpFVVOR MV;JR|UxRTBwMkWzJO69VQ>? MWCxPVk6PjJ5Mh?=
ML2 (Myelomonocytic) NVe4WIFQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmnHglUh|ryP Ml;4SG1UVw>? MVTJR|UxRTBwMEmg{txO MkXTNVk6QTZ{N{K=
ovcar-3 NVK4NZBzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWH+OUDPxE1? NGfvfW1FVVOR MlvITWM2OD13IN88US=> MXqxPVk6PjJ5Mh?=
Rh36 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIO3TW5,PSEQvF2= MUDEUXNQ Mm[5TWM2OD1zLkSzNkDPxE1? NEXKUI4yQTl7NkK3Ni=>
MOLM-13 (acute myeloid) MkGwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGH3fWF,PSEQvF2= MYXEUXNQ MlTVTWM2OD1yLkSyJO69VQ>? MVuxPVk6PjJ5Mh?=
ovcar-4 NWrhOIhOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnfmglUh|ryP NXrafFQxTE2VTx?= MXvJR|UxRTFizszN MWOxPVk6PjJ5Mh?=
Rh41 NIPNVFRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4P3UZ42KM7:TR?= NYTwO4JOTE2VTx?= MnO3TWM2OD1yLkCwOUDPxE1? NHn1[2gyQTl7NkK3Ni=>
Mutz 2 (acute myeloid) MkHxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUj+OUDPxE1? NWrBPHRCTE2VTx?= Mo\KTWM2OD1zLkG1JO69VQ>? MYCxPVk6PjJ5Mh?=
ovcar-5 NFvM[m5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MknKglUh|ryP M1K0U2ROW09? MWrJR|UxRTBwMEWg{txO NVPPWWtSOTl7OU[yO|I>
RD1 NFrIdYRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVf+OUDPxE1? M3\qT2ROW09? NF7SfoVKSzVyPUCuNFY5KM7:TR?= Mn;qNVk6QTZ{N{K=
OCI-AML 2 (acute myeloid) MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFfhWFJ,PSEQvF2= MkHhSG1UVw>? MUjJR|UxRTNwM{Og{txO NHrjemcyQTl7NkK3Ni=>
786-O NXTZT5JMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFHRdZV,PSEQvF2= MkDDSG1UVw>? M{n6W2lEPTB;MT62OFch|ryP NWL5cYNUOTl7OU[yO|I>
A673 M33JN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn\BglUh|ryP MUfEUXNQ MX7JR|UxRTBwNEC4JO69VQ>? NHPXWGEyQTl7NkK3Ni=>
TALL-1 (T-cell) NVLqdYZzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3Ozd542KM7:TR?= M1PYeWROW09? NG\EVHJKSzVyPUGuNlgh|ryP M{TydVE6QTl4Mkey
151-B MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYfa[Ws{hjVizszN MmjCSG1UVw>? Ml7kTWM2OD1{Lk[3JO69VQ>? NFradHkyQTl7NkK3Ni=>
PFSK-1 NUDsdZdvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVn+OUDPxE1? MmnkSG1UVw>? M3n0UmlEPTB;MD6xN|Ih|ryP M1T6Z|E6QTl4Mkey
THP-1 NF\vZo1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmLXglUh|ryP NVnS[2pHTE2VTx?= Mny2TWM2OD14LkW4JO69VQ>? MmroNVk6QTZ{N{K=
HEK293 M{fKS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVT+OUDPxE1? MV7EUXNQ NEPYSXVKSzVyPUCuPVE2KM7:TR?= NITCZlMyQTl7NkK3Ni=>
DAOY M1zVVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NH7jfIV,PSEQvF2= MnXSSG1UVw>? NYPidFNtUUN3ME2xMlk4QSEQvF2= NUPNSFdiOTl7OU[yO|I>
SET2 NUjmV5VmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIrNNot,PSEQvF2= MYHEUXNQ MYPJR|UxRTBwMkm4JO69VQ>? NVzhWolrOTl7OU[yO|I>
HTB-46 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{\6ZZ42KM7:TR?= NYLqVJBQTE2VTx?= MXHJR|UxRTVwMkWg{txO M4nqelE6QTl4Mkey
SK-NAS MkX1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MY\+OUDPxE1? MXLEUXNQ NFv2d3pKSzVyPUCuOFk4KM7:TR?= M17GblE6QTl4Mkey
CTLL2 NUfMWodWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnHhglUh|ryP MYLEUXNQ NETh[WpKSzVyPkGuNFAh|ryP NX7kV2E1OTl7OU[yO|I>
HTB-47 NV3jWGs2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGXVc4d,PSEQvF2= NW\ub2M3TE2VTx?= MVfJR|UxRTJwMEW2JO69VQ>? MV2xPVk6PjJ5Mh?=
LAN-1 MofTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3\rdJ42KM7:TR?= MnLwSG1UVw>? NIDjPWVKSzVyPUCuNFQh|ryP M4PxOVE6QTl4Mkey
ST486 NIjofYJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXLtW2NzhjVizszN M{\vWWROW09? M2Xt[GlEPTB;MT6xPUDPxE1? MnXRNVk6QTZ{N{K=
HS766T MnizS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmOyglUh|ryP MYXEUXNQ NVnNbodDUUN3ME2yMlAxOSEQvF2= NXLuUXd1OTl7OU[yO|I>
IMR-32 MoXoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1Txd542KM7:TR?= MVHEUXNQ MknETWM2OD1yLkK2NUDPxE1? MnXvNVk6QTZ{N{K=
Daudi (Burkitt's) NHTCdnVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MljCglUh|ryP MlzsSG1UVw>? NYq5NolxUUN3ME2yMlY{PyEQvF2= NH\JeG8yQTl7NkK3Ni=>
Aspc-1 NVj4bYJjT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MU\+OUDPxE1? NW\TS3BGTE2VTx?= NVnXdXJIUUN3ME2wMlM4QSEQvF2= NITGNo4yQTl7NkK3Ni=>
SK-NSH NF7DS5RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFrp[YJ,PSEQvF2= NHPCSllFVVOR NX:y[oZsUUN3ME2wMlE{QSEQvF2= M1TuXlE6QTl4Mkey
MEC-1 (Chronic B cell) NF2xO4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV7uZnk2hjVizszN M4XPTWROW09? NYP5S2dvUUN3ME2yMlY{PyEQvF2= NH:yb2QyQTl7NkK3Ni=>
Capan-2 NXzqOGFGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEC0PXN,PSEQvF2= M{fpd2ROW09? M1rTV2lEPTB;MT63O|Qh|ryP NWDyeWI1OTl7OU[yO|I>
SHSY5Y NWjGWZJPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{X4RZ42KM7:TR?= NVzTZ5JQTE2VTx?= MoPPTWM2OD1yLkGwOkDPxE1? NEPxXIYyQTl7NkK3Ni=>
U937 (Histioocytic) MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYTyTmp3hjVizszN MmTMSG1UVw>? MXzJR|UxRjVwMECg{txO M2\aeFE6QTl4Mkey
Bxpc-1 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYT2PYJjhjVizszN MUDEUXNQ MWnJR|UxRTFwOUK0JO69VQ>? MYKxPVk6PjJ5Mh?=
Bxpc-3 MoLBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHXLWFl,PSEQvF2= M3vZcGROW09? MojlTWM2OD53LkCwJO69VQ>? NILhTIMyQTl7NkK3Ni=>
HTB-92 MoLKS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWfnPWQ6hjVizszN MYrEUXNQ M3P6[2lEPTB;MT6wNkDPxE1? M{XsPFE6QTl4Mkey
OCI-LY10 (B-cell) NF\nc5NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWHMbJlyhjVizszN M{\semROW09? M4DUR2lEPTB;MD60OUDPxE1? NGLtOYgyQTl7NkK3Ni=>
PANC-1 M1SxNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHjaNWF,PSEQvF2= MkKwSG1UVw>? NFLscodKSzVyPkWuNFAh|ryP NYHCZ2ltOTl7OU[yO|I>
To184.T NX7QcWlRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmHmglUh|ryP NHG1WJRFVVOR NX;sN2VsUUN3ME2wMlQ3QSEQvF2= M3y1OFE6QTl4Mkey
OCI-LY19 (B-cell) NUC0NnJpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWf+OUDPxE1? M{D5OWROW09? M3j6UmlEPTB;MD60JO69VQ>? Ml;PNVk6QTZ{N{K=
PANC-1 BM MnWzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWD+OUDPxE1? M3nrUmROW09? MYjJR|UxRjVwMECg{txO NESzOJQyQTl7NkK3Ni=>
SA-4 M4\ETmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWm3UIYxhjVizszN NYm4TGY5TE2VTx?= MVHJR|UxRTFwM{CxJO69VQ>? NICwe3IyQTl7NkK3Ni=>
RPMI 8226 M{Hzc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVXnOWZGhjVizszN NWqxfnV7TE2VTx?= NX7KXpRTUUN3ME2xMlI6OyEQvF2= M3WwSVE6QTl4Mkey
HPAF-II M2DTTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmrYglUh|ryP NGDleoxFVVOR MXTJR|UxRTBwNkS0JO69VQ>? NUPMe4tCOTl7OU[yO|I>
SHP-77 NXz6[YFVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{TUXp42KM7:TR?= MlTySG1UVw>? NGPHRpZKSzVyPUGuPFg5KM7:TR?= M4fzTFE6QTl4Mkey
U266 B1 MmPmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHv6ZVZ,PSEQvF2= NWfEfJhzTE2VTx?= NXy1XpVpUUN3ME2xMlY3QSEQvF2= NUXnT5RrOTl7OU[yO|I>
Hs700t MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmHqglUh|ryP NHjMVYFFVVOR MlzHTWM2OD1yLkKzNUDPxE1? MoDENVk6QTZ{N{K=
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DU4475 2.431 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1O3UZ42KM7:TR?= MkD1SG1UVw>? MXzJR|UxRTJwNEOxJO69VQ>? NGLrdlQyQTl7NkK3Ni=>
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BT549 MkfZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYDLNZVuhjVizszN MVjEUXNQ M4DlWWlEPTB;MT62OFUh|ryP MUCxPVk6PjJ5Mh?=
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Colo205 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2L4OZ42KM7:TR?= MYjEUXNQ NWTMS2N7UUN3ME2wMlExPCEQvF2= MUWxPVk6PjJ5Mh?=
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BT474 (S) NYX6UmR2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVL+OUDPxE1? MY\EUXNQ NWDOWZF1UUN3ME2yMlQxOyEQvF2= M4nBeVE6QTl4Mkey
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SW403 Ml3aS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnjjglUh|ryP MYHEUXNQ MXfJR|UxRTBwMkKg{txO NEXJNIYyQTl7NkK3Ni=>
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H661 0.573 MlvVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXznZpZihjVizszN MYjEUXNQ M{O0WmlEPTB;MD61O|Mh|ryP M{HXRlE6QTl4Mkey
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SW116 NF3WUGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mkm0glUh|ryP NYrY[XpiTE2VTx?= M1HTW2lEPTB;MD6wOlch|ryP MkfPNVk6QTZ{N{K=
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MDA-MB-157 MmP2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1;Fd542KM7:TR?= NImwSVFFVVOR M{fUUWlEPTB;MD6wN|Yh|ryP MkDSNVk6QTZ{N{K=
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RD MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV\BNFJOhjFy4pEK{txO M1TDRmlEPTB;MT6xNkDDvU1? NHnxTWozOTJ7OEe0OS=>
Rh41 MnHJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnrVglEx6oDMzszN MoLJTWM2OD1yLkC3JOK2VQ>? MnG5NlEzQTh5NEW=
Rh18 NGrlUpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYT+NVDjiIsQvF2= NW[1ZlVyUUN3ME20Mlk3KML3TR?= NUPycnA5OjF{OUi3OFU>
Rh30 M1jTeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlrjglEx6oDMzszN MoLUTWM2OD1yLkG5JOK2VQ>? MoD4NlEzQTh5NEW=
BT-12 NIDNWm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mlm0glEx6oDMzszN NGDEdHVKSzVyPUCuO|ghyrWP MlzQNlEzQTh5NEW=
CHLA-266 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmnoglEx6oDMzszN NU\BUpB[UUN3ME2wMlg6KML3TR?= MX2yNVI6QDd2NR?=
TC-71 MnzlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUn+NVDjiIsQvF2= MnnXTWM2OD1yLkGxJOK2VQ>? MXmyNVI6QDd2NR?=
CHLA-9 NGXOenNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1;hWp4yOOLCit88US=> NHT6T|BKSzVyPUCuNVIhyrWP MkT2NlEzQTh5NEW=
CHLA-10 NWK3[2I4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVizNpZmhjFy4pEK{txO MXHJR|UxRTBwNkKgxtVO M3jRRlIyOjl6N{S1
CHLA-258 Mn3uS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIi1VlV,OTEkgJtOwG0> NFjsSWRKSzVyPUCuNlchyrWP NXexVnBQOjF{OUi3OFU>
GBM2 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLtXmdChjFy4pEK{txO NGH5eWdKSzVyPUGuOFchyrWP M2rIWFIyOjl6N{S1
NB-1643 NWD3bWU{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkfLglEx6oDMzszN M{TT[WlEPTB;MD6xNkDDvU1? Ml3tNlEzQTh5NEW=
NB-EBc1 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVXpc4dKhjFy4pEK{txO MnzyTWM2OD1yLkO1JOK2VQ>? M1znRlIyOjl6N{S1
CHLA-90 NXuwWW1{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{\4bZ4yOOLCit88US=> MYfJR|UxRTBwN{egxtVO M3XIO|IyOjl6N{S1
CHLA-136 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnjrglEx6oDMzszN MkD6TWM2OD1yLkWyJOK2VQ>? MXOyNVI6QDd2NR?=
NALM-6 M174eGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1;UXZ4yOOLCit88US=> MYLJR|UxRTBwNEmgxtVO M3LnUlIyOjl6N{S1
COG-LL-317 NWTCW3hWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1jKfp4yOOLCit88US=> MWDJR|UxRTFwM{igxtVO NY\pbmFzOjF{OUi3OFU>
RS4;11 MonES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\hWJ4yOOLCit88US=> NID6WmRKSzVyPUCuN|ghyrWP Mnz0NlEzQTh5NEW=
MOLT-4 NUDEd3dXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYjiVGRnhjFy4pEK{txO NEf3cotKSzVyPUCuOVMhyrWP MV[yNVI6QDd2NR?=
CCRF-CEM NW\lSHJWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYqyUpBJhjFy4pEK{txO MlHYTWM2OD1zLkGzJOK2VQ>? NH64THczOTJ7OEe0OS=>
Kasumi-1 M1vxUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXLzbpVzhjFy4pEK{txO MYDJR|UxRTFwMjFCuW0> M1:1d|IyOjl6N{S1
Karpas-299 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3nUWp4yOOLCit88US=> M2jIZ2lEPTB;MT62OEDDvU1? NFvmdlMzOTJ7OEe0OS=>
Ramos-RA1 NVvDUnVTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn\DglEx6oDMzszN NHe1cVVKSzVyPUGuN|EhyrWP NYmxNHBFOjF{OUi3OFU>
Rh30  MWPGeY5kfGmxbjDhd5NigQ>? NE\UdIlqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:|cHjvdplt[XSrb36= MojtNlU6OjV|N{i=
Rh41 NWjh[JZ3TnWwY4Tpc44h[XO|YYm= NUK1fJpUcW6mdXPld{BidiCrbnPy[YF{\SCxZjDTSmsheGixc4Doc5J6dGG2aX;u MofvNlU6OjV|N{i=
RD MWnGeY5kfGmxbjDhd5NigQ>? NGfSelJqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:|cHjvdplt[XSrb36= MWWyOVkzPTN5OB?=
A549 NYrLeIp5U2mwYYPlJIF{e2G7 MkLiNE426oDMzszN NFXFVI9FVVOR NXLob5RrcW6qaXLpeJMhUUeILVnSM2lTKGGldHn2ZZRqd25? MWSyOlkzQDV5OB?=
NCI-H358 MXjLbY5ie2ViYYPzZZk> NXn5d|dpOC534pEK{txO M4HDemROW09? M2ruXolvcGmkaYTzJGlITi2LUj;JVkBi[3SrdnH0bY9v M1\1Z|I3QTJ6NUe4
A549 MnjQSpVv[3Srb36gZZN{[Xl? NGLNVZoxNjYkgJtOwG0> M37FW2ROW09? MUjjZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM NVPRWFBJOjZ7Mki1O|g>
NCI-H358 Ml3RSpVv[3Srb36gZZN{[Xl? MX6wMlXjiIsQvF2= M{fuXGROW09? M1LxdINifXOnczDhJINwdmO3coLlcpQh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSUuWIHHu[EBGWkt? NHriU3IzPjl{OEW3PC=>
A549 NUHQ[485T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWnlcGVjhjFy4pEK{txO NWLIclluTE2VTx?= MonKTWM2OD1yLke2JO69VQ>? NIrRWY0zPjl{OEW3PC=>
NCI-H358 M37COGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4TENZ4yOOLCit88US=> NITv[GZFVVOR NYXV[45yUUN3ME2xMlA6KM7:TR?= M4PjVFI3QTJ6NUe4
A549 MljFRZBweHSxc3nzJIF{e2G7 NH7qbIQxNjYkgJtOwG0> NG\hXG9FVVOR NYjBVZJCcW6mdXPld{BCeG:ydH;zbZM> MUSyOlkzQDV5OB?=
NCI-H358 MnPqRZBweHSxc3nzJIF{e2G7 MV2wMlXjiIsQvF2= NFnqZm1FVVOR Ml34bY5lfWOnczDBdI9xfG:|aYO= NHrPcmwzPjl{OEW3PC=>
A549 NXzEWItFTnWwY4Tpc44h[XO|YYm= NXvy[2huOC534pEK{txO M3XGTWROW09? NF\ocYJz\WS3Y3XzJJdwfW6mIHPsc5N2emV? NHnLN28zPjl{OEW3PC=>
NCI-H358 MYLGeY5kfGmxbjDhd5NigQ>? NUXlTVJEOC534pEK{txO NFz2c4xFVVOR MVny[YR2[2W|IIfveY5lKGOub4P1doU> MorDNlY6Ojh3N{i=

... 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)
Water Insoluble
Ethanol '''92 mg/mL
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

  • Serial Dilutions

  • 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

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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