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 NYfxOXFJU2mwYYPlJIF{e2G7 MVvpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEmJRj2xVkApUUN3MDC9JFE{dk1rIHHu[EB1cGViZH;3cpN1emWjbTD0ZZJo\XS|IFHreEApUUN3MDC9JFIzdk1rIHHu[EBOSVCNIDjJR|UxKD1iMUPuUUk> NIi5RZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe3PFAzPCd-MUm3O|gxOjR:L3G+
IGF-Sal NX3O[JJ4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1zmVGlEPTB;NzDuUS=> MoHyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5N{iwNlQoRjF7N{e4NFI1RC:jPh?=
CCRF-CEM (ALL) MnfjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXj+OUDPxE1? M4nlZ2ROW09? NEnqc|JKSzVyPUGuNlM6KM7:TR?= Mk\xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
PC3 NYWz[m5XT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGnVS4Z,PSEQvF2= MV3EUXNQ MoDSTWM2OD1yLkm2OUDPxE1? NE\6eIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
JD NV;mO5pST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2\xb542KM7:TR?= M3PFNWROW09? MkfjTWM2OD1yLkO5NUDPxE1? NFP1UVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
DU145 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFvBO5p,PSEQvF2= NWnvdmNiTE2VTx?= MVTJR|UxRTFwNE[1JO69VQ>? M4r6clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
KAG MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVz+OUDPxE1? M3LvVmROW09? M{fPN2lEPTB;MT62OlUh|ryP NU\WNGJGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
K-562 (CML) M4fsVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mlm4glUh|ryP MUfEUXNQ M1:2bGlEPTB;Mj6zNFIh|ryP MkTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
B6-P210 (Murine ALL) MlHkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{XMXp42KM7:TR?= NYfBTmYyTE2VTx?= MWXJR|UxRTFwMkmzJO69VQ>? M2jk[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
LN CAP-FGC NYSyO|FpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVP+OUDPxE1? NVvqSWJvTE2VTx?= NYHL[JpKUUN3ME2xMlQ{PCEQvF2= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
VW NUW5O254T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3q0ZZ42KM7:TR?= MYfEUXNQ NXvjWlJWUUN3ME2wMlAyQSEQvF2= M3rvUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
MV411 (B Myelomonocytic) NXLoZnE2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHy3UZN,PSEQvF2= MWTEUXNQ NGXkXGVKSzVyPUCuN|Mh|ryP MnnJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
MDA-PCa-2b MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlPXglUh|ryP MnzPSG1UVw>? MWfJR|UxRTBwMEm4JO69VQ>? MnG2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
LG NHTobXZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWq5VJNPhjVizszN NU\FfmVVTE2VTx?= MkfHTWM2OD1yLkCzPEDPxE1? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
RS411 (B cell precursor-ALL) NHvvb25Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWr+OUDPxE1? NFPod5hFVVOR NIW5TXZKSzVyPUCuNVAzKM7:TR?= MoXQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
22-r-1 NVf6bYI6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2TFXJ42KM7:TR?= MnO0SG1UVw>? MmDkTWM2OD1yLkG3OUDPxE1? MnrTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
5838 MnO5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGH6bId,PSEQvF2= NV;XcVZyTE2VTx?= NYj5dlBsUUN3ME2wMlA{PCEQvF2= NFvhN|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
P388 (Murine) NVPnWFNuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlvpglUh|ryP NIPnS5NFVVOR NHXjbXpKSzVyPUSuNlch|ryP MlPoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
A2780/S MnHtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mk\UglUh|ryP MoHBSG1UVw>? M1HMeWlEPTB;MD6xNlIh|ryP MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
RDES NXXL[5dsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXr+OUDPxE1? NYHJTI1wTE2VTx?= NWXPT2lbUUN3ME2wMlAyOiEQvF2= NInwOI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
B6-T315I (Murine B-ALL) NGjQOlBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4\CNJ42KM7:TR?= M{TWOWROW09? NXPEdZZvUUN3ME2yMlg{KM7:TR?= NFThS|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
TOV 112D Mn;NS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVXybVJlhjVizszN NYDIZZBoTE2VTx?= NVL2eI5VUUN3ME2yMlE1PiEQvF2= NEGy[G49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
TC32 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlPqglUh|ryP M4rJR2ROW09? NYS3VVZFUUN3ME2wMlAxQCEQvF2= NIi2W5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
HL60 (acute myelocytic) NF22dXpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{PDO542KM7:TR?= NGfQTohFVVOR NFPlT5RKSzVyPUCuNVIh|ryP NIf1d4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
TOV 21G M{mzNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2rPVp42KM7:TR?= MkjwSG1UVw>? MmrBTWM2OD12LkK3PUDPxE1? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
TC71 MmL2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mm\vglUh|ryP MVrEUXNQ NEn0UZhKSzVyPUCuNFE1KM7:TR?= NH7iSWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
HPN-ALL (T-cell) MlfyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MY\+OUDPxE1? NVnPZ29QTE2VTx?= NWDOWm9sUUN3ME2wMlUzKM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
A2780R M{n2Umdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVvNTZNOhjVizszN MYHEUXNQ NVzUdIFZUUN3ME2xMlU3PCEQvF2= NFTBWXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
Rh1 NH3uVm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYf+OUDPxE1? M3vJOGROW09? MmHNTWM2OD1yLkCyO{DPxE1? M322b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Kasumi-1 (acute myeloid) MorRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUDofXNHhjVizszN MoqxSG1UVw>? NIr5NVhKSzVyPUCuNVYh|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
sk-ov-3 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXT+OUDPxE1? MVnEUXNQ NF\US4RKSzVyPUWuNUDPxE1? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ME NFPaRpBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIjUOVZ,PSEQvF2= MkPiSG1UVw>? M{LxSWlEPTB;MD6wNVUh|ryP Ml;hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
L1210 (Murine lymphocytic) NIjQdXNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1Tve542KM7:TR?= MmPSSG1UVw>? MYPJR|UxRTJwM{mg{txO NVzoToFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
sw-626 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1HsWJ42KM7:TR?= M4ji[GROW09? MXHJR|UxRTJwM{C2JO69VQ>? MnjzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
CTR M13qUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVT+OUDPxE1? Ml7tSG1UVw>? M1L6PWlEPTB;MD6yOVMh|ryP MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ML2 (Myelomonocytic) NHLzW4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmTQglUh|ryP NVHnWohNTE2VTx?= M3LGRmlEPTB;MD6wPUDPxE1? MmHQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
ovcar-3 MmjJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVf+OUDPxE1? NFK0c49FVVOR MWjJR|UxRTVizszN MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Rh36 MkXMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2TROJ42KM7:TR?= MkPHSG1UVw>? MXrJR|UxRTFwNEOyJO69VQ>? NGnkcGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
MOLM-13 (acute myeloid) NIPNUJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWi2OldOhjVizszN NYqzOFlZTE2VTx?= MYXJR|UxRTBwNEKg{txO MmftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
ovcar-4 M3;rRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnXsglUh|ryP NFe3dIhFVVOR NXGwO|ZTUUN3ME2xJO69VQ>? NUe0N255RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Rh41 NIjYeI1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIe5T3h,PSEQvF2= Mm\ZSG1UVw>? MXLJR|UxRTBwMEC1JO69VQ>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Mutz 2 (acute myeloid) NVr5b3VET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYL+OUDPxE1? MXfEUXNQ NXXWdJA2UUN3ME2xMlE2KM7:TR?= MlvZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
ovcar-5 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYHpPXk4hjVizszN Ml7FSG1UVw>? M17LPGlEPTB;MD6wOUDPxE1? MlnRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
RD1 NHzwcHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2LvO542KM7:TR?= MnLxSG1UVw>? M4PFeGlEPTB;MD6wOlgh|ryP M{\rSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
OCI-AML 2 (acute myeloid) NVX1cHROT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXj+OUDPxE1? Mmr4SG1UVw>? MWXJR|UxRTNwM{Og{txO NGjGWW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
786-O Ml\xS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVvjbnpihjVizszN NETSRWlFVVOR M3jCU2lEPTB;MT62OFch|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
A673 M{LJPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEnNd3p,PSEQvF2= MUfEUXNQ NXX5[IZbUUN3ME2wMlQxQCEQvF2= NY[4OHU4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
TALL-1 (T-cell) M1fJZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHL6UXl,PSEQvF2= M2DjVWROW09? NEHwVVRKSzVyPUGuNlgh|ryP Mo\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
151-B NIDoPGtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVz+OUDPxE1? NFrzWWVFVVOR MUjJR|UxRTJwNkeg{txO M1vyZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
PFSK-1 NGC4ZYNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUfZbWFjhjVizszN M1Gzc2ROW09? MWrJR|UxRTBwMUOyJO69VQ>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
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SET2 NUK5[ZBDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn;GglUh|ryP NFHQd4tFVVOR NF3QOVZKSzVyPUCuNlk5KM7:TR?= Ml;SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
HTB-46 NH;lc5VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFLOWJF,PSEQvF2= NHjDcmVFVVOR MmHMTWM2OD13LkK1JO69VQ>? Mk\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
SK-NAS Mni3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3jseZ42KM7:TR?= MWDEUXNQ NGrFSWJKSzVyPUCuOFk4KM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
CTLL2 NV63e5pOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXHHS|JPhjVizszN NH\hWYhFVVOR MlT5TWM2OD5zLkCwJO69VQ>? NYi2VJBqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
HTB-47 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mle0glUh|ryP M1zONWROW09? MUHJR|UxRTJwMEW2JO69VQ>? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
LAN-1 M{DYNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn;tglUh|ryP NYLZOnU5TE2VTx?= MknSTWM2OD1yLkC0JO69VQ>? NFyycnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
ST486 NXfpTIp7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX\1W2t1hjVizszN MXfEUXNQ NETySZRKSzVyPUGuNVkh|ryP MkLLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
HS766T MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHeyfXN,PSEQvF2= NGPmfllFVVOR NYH0N2VpUUN3ME2yMlAxOSEQvF2= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
IMR-32 NXjzV4F[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXj+OUDPxE1? NU\nR445TE2VTx?= NXrEOZJ1UUN3ME2wMlI3OSEQvF2= MmHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Daudi (Burkitt's) NIT6SY9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYX+OUDPxE1? MnK5SG1UVw>? MXzJR|UxRTJwNkO3JO69VQ>? M3z6NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Aspc-1 MnrkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWn+OUDPxE1? NEDyNmtFVVOR MVLJR|UxRTBwM{e5JO69VQ>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
SK-NSH Mof5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIj5fJV,PSEQvF2= M4iweWROW09? NELodpBKSzVyPUCuNVM6KM7:TR?= NGjhfmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
MEC-1 (Chronic B cell) MofCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXS2Z4tqhjVizszN MUfEUXNQ M{XGWmlEPTB;Mj62N|ch|ryP NGPHXXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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SHSY5Y MkT6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MojCglUh|ryP M{\SOGROW09? NV[4eWxPUUN3ME2wMlExPiEQvF2= M3;YdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
U937 (Histioocytic) NFfD[pVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2PyNp42KM7:TR?= NIHLe4RFVVOR NHWzT2hKSzVyPkWuNFAh|ryP M1\hcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Bxpc-1 M2SzWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYr+OUDPxE1? NFjNSnRFVVOR NWK1fIQ6UUN3ME2xMlkzPCEQvF2= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
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HTB-92 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVz+OUDPxE1? NWS0W2pCTE2VTx?= M{\vfGlEPTB;MT6wNkDPxE1? M{TzflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
OCI-LY10 (B-cell) NVHPXFFWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHvvPZZ,PSEQvF2= NYDTeWlOTE2VTx?= MkXjTWM2OD1yLkS1JO69VQ>? NHTDcpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
PANC-1 NHrJdHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlS3glUh|ryP MkHrSG1UVw>? NWrXXYVmUUN3ME61MlAxKM7:TR?= NFryVnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
To184.T NUPPXJJNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUf+OUDPxE1? MnnNSG1UVw>? M1;IZ2lEPTB;MD60Olkh|ryP MnO5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
OCI-LY19 (B-cell) NYXTVWtzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1TWUZ42KM7:TR?= NFLxSolFVVOR MXXJR|UxRTBwNDFOwG0> M4m1OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
PANC-1 BM MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFLNV|d,PSEQvF2= M133OGROW09? NFPJVIxKSzVyPkWuNFAh|ryP NE\jNnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
SA-4 NHn1W|VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4Hxc542KM7:TR?= Mkm1SG1UVw>? MUfJR|UxRTFwM{CxJO69VQ>? MmHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
RPMI 8226 MoC5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVzSXpBMhjVizszN NX7sOmdITE2VTx?= NH7adJJKSzVyPUGuNlk{KM7:TR?= NFX4b|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
HPAF-II MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV\+OUDPxE1? MV7EUXNQ NIXiOnFKSzVyPUCuOlQ1KM7:TR?= MlyyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
SHP-77 M{nhWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYf+OUDPxE1? NV7uT3JZTE2VTx?= NHPlXWdKSzVyPUGuPFg5KM7:TR?= MmH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
U266 B1 MlK3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUf+OUDPxE1? NGntN4NFVVOR MorzTWM2OD1zLk[2PUDPxE1? M3;YR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
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NCI-446 NGDCXnFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVfaVItQhjVizszN M2j6cGROW09? MonOTWM2OD1zLkG1OEDPxE1? NIXidVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
H929 NIn0WWFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3vZb542KM7:TR?= MmHqSG1UVw>? MVrJR|UxRTBwMEG0JO69VQ>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
PL45 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFL3VHN,PSEQvF2= NW\aPGFGTE2VTx?= M4\RWmlEPTB;Mj6yOVUh|ryP NFX3OFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
NCI-H383 NX;3ZmhnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV7zd2Y{hjVizszN Mkj5SG1UVw>? NYrPdVJYUUN3ME61MlAxKM7:TR?= Mor5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
JJN3 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWjYZZp[hjVizszN M1jDc2ROW09? NX;oNnFQUUN3ME2yMlQ{OyEQvF2= NILBR|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
SU.86.86 M4HDb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXPnSVl6hjVizszN M{DWS2ROW09? NVvFZmxXUUN3ME2yMlY4OiEQvF2= NWe0[2tiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
H1299 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmfsglUh|ryP NXjPXldrTE2VTx?= NIT6bIlKSzVyPkWuNFAh|ryP NHjJ[|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
MDA-MB-468 NVHTZoJET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1;6bZ42KM7:TR?= MmXjSG1UVw>? M1S1[mlEPTB;MD61NFQh|ryP NHzwdlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
SW1990 M4H2TGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1;kdJ42KM7:TR?= MnTNSG1UVw>? MkHyTWM2OD1yLkiyOkDPxE1? MmD0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Calu-6 Mn[4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVnDOpZqhjVizszN Mk\aSG1UVw>? M{nMU2lEPTB-NT6wNEDPxE1? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
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TC32 MkT1dWhVWyCjc4PhfS=> MnnUdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? MoLmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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A673 NVe3VWR5eUiWUzDhd5NigQ>? NUDxOI5leUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= M4rIOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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Saos-2 NF7LNnhyUFSVIHHzd4F6 M2\Dc5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MojZdWhVWyCjc4PhfS=> MlvkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 MV3xTHRUKGG|c3H5 NXL1TVZIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> MmCzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 MlPGdWhVWyCjc4PhfS=> M{W4S5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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MG 63 (6-TG R) MnXrdWhVWyCjc4PhfS=> NV3MOIlCeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz MnrXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
wild type fibroblast cells MWrxTHRUKGG|c3H5 NVnVTm9meUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IHPvcpRzd2xiSHige4lt\CC2eYDlJIZq[nKxYnzhd5Qh[2WubIO= NITEfXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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NB1643 M3nvNJFJXFNiYYPzZZk> NUnKOYhReUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| NWrKOpkyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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LAN-5 NWrHNnpkeUiWUzDhd5NigQ>? MknOdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUGFPNTViY3XscJM> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 M1ToSpFJXFNiYYPzZZk> MkLZdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUmIuTUKlMTDj[Yxtew>? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 MljkdWhVWyCjc4PhfS=> NHSyOXZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBDXC1|NzDj[Yxtew>? NGrqcY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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MKN7 NHu0Z4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPR[XE3UW6qaXLpeIlwdiCxZjDoeY1idiCPS163JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1Oi52OUe3JO69VS5? Mne2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc2PDR6Lze+V2FPT0WUPD;hQi=>
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K052 MlrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HESmlvcGmkaYTpc44hd2ZiaIXtZY4hUzB3MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gOFMvODZ7ODFOwG0v NWLlcGM2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
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BE-13 NHLKU4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrScHVqUW6qaXLpeIlwdiCxZjDoeY1idiCERT2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDVwOUO5NkDPxE1w NGfkTo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzV2NEivK|5USU6JRWK8M4E,
SW684 M2T3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJcohq[mm2aX;uJI9nKGi3bXHuJHNYPjh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0O{41QTZ7IN88UU4> NIrPVJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzV2NEivK|5USU6JRWK8M4E,
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.
  • (Only for Reference)
Animal Research:[1]
  • 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 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 2021-09-06)

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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