BMS-754807

Catalog No.S1124

For research use only.

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.

BMS-754807 Chemical Structure

CAS No. 1001350-96-4

Selleck's BMS-754807 has been cited by 40 publications

Purity & Quality Control

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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)
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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> NFnyPYZqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFnHSk0yWiBqSVO1NEA:KDF|bl2pJIFv\CC2aHWg[I94dnO2cnXhcUB1[XKpZYTzJGFsfCBqSVO1NEA:KDJ{bl2pJIFv\CCPQWDLJEhKSzVyIE2gNVNvVSl? MnrnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5N{iwNlQoRjF7N{e4NFI1RC:jPh?=
IGF-Sal NV75c3ZET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlW4TWM2OD15IH7N Ml;SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5N{iwNlQoRjF7N{e4NFI1RC:jPh?=
CCRF-CEM (ALL) NX71[5Q{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn7hglUh|ryP NIDZUmVFVVOR MVHJR|UxRTFwMkO5JO69VQ>? NV;Q[nRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
PC3 NWm2UIg4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1jER542KM7:TR?= MnXmSG1UVw>? NETqXZNKSzVyPUCuPVY2KM7:TR?= NEHBVJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
JD NGDOWINIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGXvZY5,PSEQvF2= MnzVSG1UVw>? NIfTeJRKSzVyPUCuN|kyKM7:TR?= NYftc4RwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
DU145 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYD+OUDPxE1? NYfWdnR1TE2VTx?= M4OzV2lEPTB;MT60OlUh|ryP M{fEe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
KAG MnLWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYHmdGIyhjVizszN MUjEUXNQ NV75[WRrUUN3ME2xMlY3PSEQvF2= M2D3ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
K-562 (CML) NEXXWpZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3;GPJ42KM7:TR?= MV3EUXNQ M{\QfWlEPTB;Mj6zNFIh|ryP Mn\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
B6-P210 (Murine ALL) MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH7XWZJ,PSEQvF2= Ml;CSG1UVw>? MofuTWM2OD1zLkK5N{DPxE1? NE[2Om89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
LN CAP-FGC M{nO[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEi5WFl,PSEQvF2= M{D6T2ROW09? NXPScoZwUUN3ME2xMlQ{PCEQvF2= NGrISJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
VW MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MknBglUh|ryP NHXhfW5FVVOR NWrT[oFMUUN3ME2wMlAyQSEQvF2= M1jQUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
MV411 (B Myelomonocytic) MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3;PVJ42KM7:TR?= NVTjUmpMTE2VTx?= MUjJR|UxRTBwM{Og{txO NWjue4N5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
MDA-PCa-2b M2m4[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnTEglUh|ryP M3PiTGROW09? NXXuUVVtUUN3ME2wMlA6QCEQvF2= NFHwcXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
LG NILCZYtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MljwglUh|ryP M1LiNmROW09? MnjTTWM2OD1yLkCzPEDPxE1? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
RS411 (B cell precursor-ALL) MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkPuglUh|ryP NFP0RVBFVVOR MVPJR|UxRTBwMUCyJO69VQ>? M1uzNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
22-r-1 NVuwVoNCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUX+OUDPxE1? MoC2SG1UVw>? M4S3WWlEPTB;MD6xO|Uh|ryP NXrRNldXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
5838 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MU\+OUDPxE1? M2frVGROW09? MoLlTWM2OD1yLkCzOEDPxE1? MmnOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
P388 (Murine) MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHzmb4p,PSEQvF2= Mnr6SG1UVw>? M3vqemlEPTB;ND6yO{DPxE1? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
A2780/S MmTUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYD2cmFlhjVizszN NVG5eZhPTE2VTx?= NWfxTJhXUUN3ME2wMlEzOiEQvF2= NGeyelA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
RDES M4TlTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M13ROJ42KM7:TR?= NXuzOnFzTE2VTx?= MUHJR|UxRTBwMEGyJO69VQ>? M{Lp[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
B6-T315I (Murine B-ALL) NWjQUI5ST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGmzfXR,PSEQvF2= NHjPeWVFVVOR Mki4TWM2OD1{LkizJO69VQ>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
TOV 112D MnLrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkL0glUh|ryP NXTzfGxtTE2VTx?= MmrKTWM2OD1{LkG0OkDPxE1? NV7VPJZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
TC32 MoqwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXPqUmZXhjVizszN NX3x[ldCTE2VTx?= MXPJR|UxRTBwMEC4JO69VQ>? NX;ObIdxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
HL60 (acute myelocytic) MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFG2NYN,PSEQvF2= M{TrfWROW09? MXTJR|UxRTBwMUKg{txO MmK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
TOV 21G NGDrWIlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVHLNYV1hjVizszN M1qySmROW09? NIPvN4NKSzVyPUSuNlc6KM7:TR?= NFTXcFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
TC71 NIrE[VNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{DETp42KM7:TR?= MkHQSG1UVw>? MUPJR|UxRTBwMEG0JO69VQ>? NHLYR2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
HPN-ALL (T-cell) MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIDzSGh,PSEQvF2= NW\adVhZTE2VTx?= MVnJR|UxRTBwNUKg{txO MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
A2780R MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXTo[3pPhjVizszN MUXEUXNQ NVPMbXRkUUN3ME2xMlU3PCEQvF2= M3;xW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Rh1 MoC4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUT+OUDPxE1? Mom3SG1UVw>? NHfYPVhKSzVyPUCuNFI4KM7:TR?= NGfmNXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
Kasumi-1 (acute myeloid) MoXBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWL+OUDPxE1? MWnEUXNQ MV\JR|UxRTBwMU[g{txO M4fWb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
sk-ov-3 MlG3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXf+OUDPxE1? M2XBNWROW09? MWDJR|UxRTVwMTFOwG0> MlPxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
ME NXLsSIxPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NU\1TIdbhjVizszN MXrEUXNQ M365SGlEPTB;MD6wNVUh|ryP NUPpZ|VKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
L1210 (Murine lymphocytic) Mk\sS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUj+OUDPxE1? Ml\KSG1UVw>? NGfhZnFKSzVyPUKuN|kh|ryP M3voO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
sw-626 MnTTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnG3glUh|ryP MkT0SG1UVw>? NI\IcoxKSzVyPUKuN|A3KM7:TR?= NUTvT5FxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
CTR NH\D[|FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MV3+OUDPxE1? MlTwSG1UVw>? NYjscWFVUUN3ME2wMlI2OyEQvF2= M2P6bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
ML2 (Myelomonocytic) MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn7HglUh|ryP NGHtNFJFVVOR NUPmd4lzUUN3ME2wMlA6KM7:TR?= NFyzUm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
ovcar-3 NYHTdWdKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4rZ[p42KM7:TR?= M2XmTGROW09? NUX4RXFFUUN3ME21JO69VQ>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Rh36 M2DtN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{LwTZ42KM7:TR?= MV;EUXNQ MoXiTWM2OD1zLkSzNkDPxE1? NYnM[2lXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
MOLM-13 (acute myeloid) MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2XNUJ42KM7:TR?= MYjEUXNQ M1TkZ2lEPTB;MD60NkDPxE1? MnjUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
ovcar-4 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEO5OYJ,PSEQvF2= NHKy[4FFVVOR NU[yfoQ3UUN3ME2xJO69VQ>? NXO0e|c{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Rh41 NUDQelgxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4LO[Z42KM7:TR?= M1q2b2ROW09? NG\qT4xKSzVyPUCuNFA2KM7:TR?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Mutz 2 (acute myeloid) MnXDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkizglUh|ryP NXvmOFNkTE2VTx?= Mln1TWM2OD1zLkG1JO69VQ>? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ovcar-5 NVrpd|UxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUf3cG1PhjVizszN MlTNSG1UVw>? Mn\aTWM2OD1yLkC1JO69VQ>? M1HYO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
RD1 M2\1Tmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MljIglUh|ryP MmmxSG1UVw>? MYPJR|UxRTBwME[4JO69VQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
OCI-AML 2 (acute myeloid) MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXX+OUDPxE1? NImwNZBFVVOR M4\nXWlEPTB;Mz6zN{DPxE1? Ml:5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
786-O NHjhZY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn3mglUh|ryP M4f6fGROW09? NF;sUYhKSzVyPUGuOlQ4KM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
A673 NFXCcGxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MofaglUh|ryP M{HVVWROW09? NUC0c4VZUUN3ME2wMlQxQCEQvF2= NVnzW3Z{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
TALL-1 (T-cell) NFH4[WFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1LSTZ42KM7:TR?= MW\EUXNQ M1\FTWlEPTB;MT6yPEDPxE1? NV:2UGZoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
151-B NGH6ZVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYP+OUDPxE1? MkXPSG1UVw>? M4\MfGlEPTB;Mj62O{DPxE1? NEm4Zmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
PFSK-1 NWS1SHBTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVH+OUDPxE1? Mm\BSG1UVw>? NFXmPJlKSzVyPUCuNVMzKM7:TR?= NV7hbno6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
THP-1 M4rxfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn\QglUh|ryP MmDzSG1UVw>? MXnJR|UxRTZwNUig{txO MmXLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
HEK293 NUT0dopLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXj+OUDPxE1? M33rSmROW09? MkLXTWM2OD1yLkmxOUDPxE1? MkfNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
DAOY MmXSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX3odJFrhjVizszN MV\EUXNQ NYHFVm9QUUN3ME2xMlk4QSEQvF2= Ml;1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
SET2 Mn;LS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFHSXmV,PSEQvF2= M4LkXGROW09? M4HmTmlEPTB;MD6yPVgh|ryP MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
HTB-46 Mk[3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NECzc41,PSEQvF2= NYXO[YtzTE2VTx?= NW\XeVY5UUN3ME21MlI2KM7:TR?= M2rWfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
SK-NAS NXTWeoE6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkL4glUh|ryP M33mfWROW09? M3TLeGlEPTB;MD60PVch|ryP NVfRO|dQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
CTLL2 NXf2bVFqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV;+OUDPxE1? M3;WN2ROW09? M1jrTWlEPTB-MT6wNEDPxE1? NYnZbIt2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
HTB-47 NYfTc|IzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoT1glUh|ryP NWG3OJpxTE2VTx?= NXfFbWR2UUN3ME2yMlA2PiEQvF2= NGnENIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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ST486 M1jTPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF7QS2h,PSEQvF2= MUjEUXNQ NIHaXpZKSzVyPUGuNVkh|ryP MmnXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
HS766T MnzIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmXrglUh|ryP M4TV[WROW09? Mn;jTWM2OD1{LkCwNUDPxE1? MkeyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
IMR-32 M1voU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXvsOZNohjVizszN M1ToV2ROW09? MVPJR|UxRTBwMk[xJO69VQ>? MmDEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Daudi (Burkitt's) MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFPCWYJ,PSEQvF2= NFrUPG9FVVOR MnzRTWM2OD1{Lk[zO{DPxE1? NXrNbll5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Aspc-1 Mle3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1:xUZ42KM7:TR?= MVnEUXNQ NHXiZodKSzVyPUCuN|c6KM7:TR?= NFHwPGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
SK-NSH NV;nRVNbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIfNXm1,PSEQvF2= M{TQN2ROW09? MYPJR|UxRTBwMUO5JO69VQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
MEC-1 (Chronic B cell) Mnm5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkfiglUh|ryP MlPnSG1UVw>? NWLyXHZOUUN3ME2yMlY{PyEQvF2= MnnsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Capan-2 MnLES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1TKd542KM7:TR?= MU\EUXNQ MnS0TWM2OD1zLke3OEDPxE1? M{DtWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
SHSY5Y Ml64S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkDiglUh|ryP MV3EUXNQ M{P3dmlEPTB;MD6xNFYh|ryP NUj0TGFqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
U937 (Histioocytic) M1\BV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVLBNFJ{hjVizszN M2DFSmROW09? MnvFTWM2OD53LkCwJO69VQ>? MnvFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Bxpc-1 NX3YfIlYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYXscGVMhjVizszN NFnOPYNFVVOR MkfOTWM2OD1zLkmyOEDPxE1? NV3RPVVLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Bxpc-3 M1e4V2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{\1SJ42KM7:TR?= M{LmemROW09? M3j0U2lEPTB-NT6wNEDPxE1? NGS1[Wc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
HTB-92 Mor5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWL+OUDPxE1? NGn6VnZFVVOR NYPG[YFYUUN3ME2xMlAzKM7:TR?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
OCI-LY10 (B-cell) M1ywTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV3+OUDPxE1? NIXqN2ZFVVOR M4Cz[WlEPTB;MD60OUDPxE1? Mlm2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
PANC-1 MljjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoL5glUh|ryP NEXnNVdFVVOR NFTYdo1KSzVyPkWuNFAh|ryP MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
To184.T NGfsNWlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3;wUp42KM7:TR?= MVTEUXNQ MYjJR|UxRTBwNE[5JO69VQ>? M2\GUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
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PANC-1 BM Ml;zS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX\+OUDPxE1? MUTEUXNQ NUDI[o9pUUN3ME61MlAxKM7:TR?= M3\YVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
SA-4 M4L2W2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn3hglUh|ryP NUWwdGJzTE2VTx?= NXrNd3FCUUN3ME2xMlMxOSEQvF2= NEPKWo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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HPAF-II Mn\SS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVP+OUDPxE1? M3H4cWROW09? MXTJR|UxRTBwNkS0JO69VQ>? M3HsRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
SHP-77 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnX0glUh|ryP NF\Wc3BFVVOR MmjBTWM2OD1zLki4PEDPxE1? NGnPbFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
U266 B1 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXP+OUDPxE1? NYXDNplkTE2VTx?= NHP1eXlKSzVyPUGuOlY6KM7:TR?= NYjnWWZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Hs700t M3v5b2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NX\4OXJYhjVizszN MlLKSG1UVw>? MonHTWM2OD1yLkKzNUDPxE1? M33sNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
NCI-446 Ml3PS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3fTdp42KM7:TR?= MYfEUXNQ NX;ocphDUUN3ME2xMlE2PCEQvF2= MonYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
H929 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYr+OUDPxE1? NGTZRWdFVVOR MXvJR|UxRTBwMEG0JO69VQ>? NHLPXVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
PL45 NV3JSmJOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NI\FRZR,PSEQvF2= MorrSG1UVw>? NX7kdo1lUUN3ME2yMlI2PSEQvF2= NHq4[nk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
NCI-H383 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3\1c542KM7:TR?= NGLUUlNFVVOR NXP3RmlSUUN3ME61MlAxKM7:TR?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
JJN3 M4HobWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXK3UnZPhjVizszN MXTEUXNQ NELJeHJKSzVyPUKuOFM{KM7:TR?= M3j6VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
SU.86.86 M3[yUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEm1[3F,PSEQvF2= MojySG1UVw>? NWexbGkxUUN3ME2yMlY4OiEQvF2= NUTUTZR1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
H1299 MkX4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkH3glUh|ryP MW\EUXNQ NWTJeXZoUUN3ME61MlAxKM7:TR?= M4LKfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
MDA-MB-468 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF63bFN,PSEQvF2= M3:wWGROW09? MUPJR|UxRTBwNUC0JO69VQ>? NHTKbJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
SW1990 NIfyS|hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUD5WJU5hjVizszN NGH1[mFFVVOR Mof1TWM2OD1yLkiyOkDPxE1? M{XweVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Calu-6 M1[4RWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXH2eG1lhjVizszN NWnaelJZTE2VTx?= MV;JR|UxRjVwMECg{txO M{TuWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
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A549 NHLEd|lHfW6ldHnvckBie3OjeR?= MlXoNE426oDMzszN M{HzRWROW09? M13SNoNifXOnczDhJINwdmO3coLlcpQh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSUuWIHHu[EBGWkt? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{OEW3PEc,OjZ7Mki1O|g9N2F-
NCI-H358 Mk\lSpVv[3Srb36gZZN{[Xl? NHXBUWUxNjYkgJtOwG0> M1LNUmROW09? M1;WN4NifXOnczDhJINwdmO3coLlcpQh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSUuWIHHu[EBGWkt? NE\vNFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkmyPFU4QCd-Mk[5Nlg2Pzh:L3G+
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A549 MULGeY5kfGmxbjDhd5NigQ>? NEe0WIcxNjYkgJtOwG0> NUHHeI1vTE2VTx?= MVPy[YR2[2W|IIfveY5lKGOub4P1doU> MmXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7Mki1O|goRjJ4OUK4OVc5RC:jPh?=
NCI-H358 MYfGeY5kfGmxbjDhd5NigQ>? MonhNE426oDMzszN MXTEUXNQ M1;zPJJm\HWlZYOge492dmRiY3zvd5Vz\Q>? NEnuVJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkmyPFU4QCd-Mk[5Nlg2Pzh:L3G+
IGF1R-SAL NI\WTWdHfW6ldHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKEmJRkHSJIlvKEmJRkHSMXNCVCClZXzsd{whUUN3MDC9JFAvODB{MTFOwG0v NX7wc21MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2O|UyOzdpPkKwOlc2OTN5PD;hQi=>
TC32 NXj4OGljeUiWUzDhd5NigQ>? NH3sS4dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?= M3;FSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 M1vudpFJXFNiYYPzZZk> MoLzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= M13HdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 MnPmdWhVWyCjc4PhfS=> NV7ZZ3NReUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= M1PrUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC M2XwNZFJXFNiYYPzZZk> MnnrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NX;BcXBkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 NFPIfoZyUFSVIHHzd4F6 NWnGS|h6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 M2fU[ZFJXFNiYYPzZZk> MWLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MnG0dWhVWyCjc4PhfS=> NUDnfIxkeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> NWW5WGFyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 NV3KSIt{eUiWUzDhd5NigQ>? MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| NGXXbmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MYXxTHRUKGG|c3H5 MlG4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| M4HrfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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OHS-50 MVHxTHRUKGG|c3H5 MoXVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= M1vm[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) NH;oWoVyUFSVIHHzd4F6 NWTEdoU{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NUTMdGZSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
wild type fibroblast cells NGjrZWFyUFSVIHHzd4F6 NX[2WlY5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IHPvcpRzd2xiSHige4lt\CC2eYDlJIZq[nKxYnzhd5Qh[2WubIO= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 NWnxbFVUeUiWUzDhd5NigQ>? MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? MoD0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 M33FfJFJXFNiYYPzZZk> Mmi5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUmIyPjR|IHPlcIx{ MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 M2TnV5FJXFNiYYPzZZk> NHXadmZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBCPjd|IHPlcIx{MQ>? M1rqWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 MoHHdWhVWyCjc4PhfS=> NEXDfotyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBNSU5vNTDj[Yxtew>? NGHBWWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 M{XZ[JFJXFNiYYPzZZk> MXrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORk1GSmNzIHPlcIx{ NXTLTo5HRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 NUDVT2NIeUiWUzDhd5NigQ>? MVfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0{PyClZXzsdy=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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RCC10RGB NE\neJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfrbmNjUW6qaXLpeIlwdiCxZjDoeY1idiCUQ1OxNHJISiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iNz61OFAyPCEQvF2u NEPG[GY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzV2NEivK|5USU6JRWK8M4E,
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CP50-MEL-B M3;HSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13vUmlvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iNEKuOlkxOSEQvF2u NVzHWI9wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
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Assay
Methods Test Index PMID
Western blot p-IGFIRRβ/InsRβ / IGFIRβ / p-AKT / AKT / p-ERK / ERK 26136493
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: IGF-1R-Sal, GEO, Colo205, JJN3, RD1 or Rh41 tumor–bearing nude mice
  • Dosages: 150 mg/kg
  • Administration: Orally

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 461.49
Formula

C23H24FN9O

CAS No. 1001350-96-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01525823 Completed Drug: BMS-754807 (IGR-IR/IR Inhibitor)|Drug: Metformin Healthy Volunteers Bristol-Myers Squibb February 2012 Phase 1
NCT00908024 Terminated Drug: BMS-754807|Drug: cetuximab (Erbitux®) Colorectal Cancer|Head and Neck Cancer|Neoplasm Metastasis Bristol-Myers Squibb October 2009 Phase 1|Phase 2
NCT00898716 Completed Drug: BMS-754807 Neoplasms Bristol-Myers Squibb September 2009 Phase 1
NCT00788333 Completed Drug: BMS-754807|Drug: trastuzumab (Herceptin®) Breast Cancer Bristol-Myers Squibb July 2009 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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