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 41 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 MlrvT4lv[XOnIHHzd4F6 MlXzbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXIhMEmFNUCgQUAyO26PKTDhcoQhfGinIHTve45{fHKnYX2geIFz\2W2czDBb5QhMEmFNUCgQUAzOm6PKTDhcoQhVUGSSzCoTWM2OCB;IEGzcm0q NG\Oc5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe3PFAzPCd-MUm3O|gxOjR:L3G+
IGF-Sal MofPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4r6ZWlEPTB;NzDuUS=> MofoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5N{iwNlQoRjF7N{e4NFI1RC:jPh?=
CCRF-CEM (ALL) M2i0bmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoDQglUh|ryP MkS1SG1UVw>? MojnTWM2OD1zLkKzPUDPxE1? MkDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
PC3 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVz+OUDPxE1? NFjEcpJFVVOR M3zBTGlEPTB;MD65OlUh|ryP NX21WmZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
JD NXHQc3hKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV[2N3E3hjVizszN MnjNSG1UVw>? M{PlT2lEPTB;MD6zPVEh|ryP NW[zcmtFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
DU145 MmXFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1vIZp42KM7:TR?= M3TxXWROW09? M1X2TGlEPTB;MT60OlUh|ryP M{HwTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
KAG M1HRO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUH+OUDPxE1? M3vxbWROW09? M3HGR2lEPTB;MT62OlUh|ryP NF:1e3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
K-562 (CML) M1OwbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmPJglUh|ryP M4n4eGROW09? MYrJR|UxRTJwM{CyJO69VQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
B6-P210 (Murine ALL) MkHVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXX+OUDPxE1? MU\EUXNQ NXTGcmt7UUN3ME2xMlI6OyEQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
LN CAP-FGC NHHYT2NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3:5Zp42KM7:TR?= MWnEUXNQ M1TkcGlEPTB;MT60N|Qh|ryP MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
VW M{DGNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUP+OUDPxE1? NH\L[ZVFVVOR NF3ENJlKSzVyPUCuNFE6KM7:TR?= M2C3fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
MV411 (B Myelomonocytic) MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlXuglUh|ryP M1rpeWROW09? NHXKPGRKSzVyPUCuN|Mh|ryP NF\u[3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
MDA-PCa-2b MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFTMOll,PSEQvF2= MmDJSG1UVw>? NIjRVItKSzVyPUCuNFk5KM7:TR?= NWjGOGZtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
LG NXS0PJFTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXn+OUDPxE1? M37k[GROW09? MVPJR|UxRTBwMEO4JO69VQ>? NX31XVRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
RS411 (B cell precursor-ALL) MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWHlRWFWhjVizszN NH;VfFZFVVOR MWjJR|UxRTBwMUCyJO69VQ>? NWnQd|JFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
22-r-1 NHLpV2lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX;hfZVZhjVizszN NX[xNY8{TE2VTx?= NIjyPJNKSzVyPUCuNVc2KM7:TR?= NFrR[mw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
5838 NGm4SZlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIe5c2Z,PSEQvF2= NF\TTGNFVVOR Mmq0TWM2OD1yLkCzOEDPxE1? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
P388 (Murine) NXjxb5NIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYL+OUDPxE1? NVHNWVBzTE2VTx?= MUXJR|UxRTRwMkeg{txO NULxXotoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
A2780/S M3jrUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYX0bYNKhjVizszN M4\qTGROW09? NG[xeGpKSzVyPUCuNVIzKM7:TR?= MmnoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
RDES M{LX[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{TWUJ42KM7:TR?= M{jQPGROW09? M4jJd2lEPTB;MD6wNVIh|ryP MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
B6-T315I (Murine B-ALL) NGLu[|dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV\VTW9khjVizszN Mon6SG1UVw>? NWnXW4syUUN3ME2yMlg{KM7:TR?= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
TOV 112D NVrNb21wT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUL+OUDPxE1? MXTEUXNQ M{j2ZWlEPTB;Mj6xOFYh|ryP NEH5c209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
TC32 NWm5TYtZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1zSNJ42KM7:TR?= MoL0SG1UVw>? NXy1dVhtUUN3ME2wMlAxQCEQvF2= MnS4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
HL60 (acute myelocytic) MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4fpTZ42KM7:TR?= MY\EUXNQ NVr0UWRTUUN3ME2wMlEzKM7:TR?= NVzxZlFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
TOV 21G NGTxdYFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYD+OUDPxE1? NUHxcZVlTE2VTx?= NHPVPY5KSzVyPUSuNlc6KM7:TR?= NGfvTXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
TC71 NECzUGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml7NglUh|ryP MoXCSG1UVw>? NFv0RXFKSzVyPUCuNFE1KM7:TR?= Mn3BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
HPN-ALL (T-cell) NGjtcWpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2LDOJ42KM7:TR?= NGnPRYxFVVOR NXjFWI9zUUN3ME2wMlUzKM7:TR?= MnnpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
A2780R MmjPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mnm2glUh|ryP NUnmT3ZjTE2VTx?= MULJR|UxRTFwNU[0JO69VQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Rh1 M2rJ[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFHib3p,PSEQvF2= NEW5TldFVVOR M{n3NWlEPTB;MD6wNlch|ryP NYLtSlNzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Kasumi-1 (acute myeloid) MmTHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NELFbYN,PSEQvF2= MkHSSG1UVw>? MoTWTWM2OD1yLkG2JO69VQ>? NGLZdZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
sk-ov-3 NI[yXodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHvCN4p,PSEQvF2= MX;EUXNQ NELTcnhKSzVyPUWuNUDPxE1? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ME MkPtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2PwfJ42KM7:TR?= NGD0VXFFVVOR NHHRcVlKSzVyPUCuNFE2KM7:TR?= M1[wdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
L1210 (Murine lymphocytic) NYLZTmJXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXmwOGRShjVizszN NXHNPY55TE2VTx?= M3;nOmlEPTB;Mj6zPUDPxE1? NV6wXVBrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
sw-626 M{DOcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4HKdp42KM7:TR?= MXHEUXNQ M2XRTmlEPTB;Mj6zNFYh|ryP M2fFSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
CTR MkmwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkLwglUh|ryP NVr3TFdrTE2VTx?= MYfJR|UxRTBwMkWzJO69VQ>? M4HVO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
ML2 (Myelomonocytic) MlTRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUP+OUDPxE1? NH2weWRFVVOR M{SyNmlEPTB;MD6wPUDPxE1? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ovcar-3 NI\nT5lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2TibJ42KM7:TR?= MWnEUXNQ M{eyemlEPTB;NTFOwG0> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Rh36 Mn7VS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmCzglUh|ryP M4DyW2ROW09? M3HHWmlEPTB;MT60N|Ih|ryP M2r4SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
MOLM-13 (acute myeloid) MknzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFXqVJp,PSEQvF2= NX;T[m1ETE2VTx?= NXX0[GlEUUN3ME2wMlQzKM7:TR?= Mn32QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
ovcar-4 MmTES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEGyeoh,PSEQvF2= MoLKSG1UVw>? MlXuTWM2OD1zIN88US=> M1jab|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Rh41 NELQeYNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVP+OUDPxE1? M3XOV2ROW09? M1focmlEPTB;MD6wNFUh|ryP NFvVO4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
Mutz 2 (acute myeloid) NUPPWnZ6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4jiXp42KM7:TR?= NYXNboVmTE2VTx?= MUXJR|UxRTFwMUWg{txO NV;ZNJZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
ovcar-5 NGDnOnRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHfs[49,PSEQvF2= M363SmROW09? MlfpTWM2OD1yLkC1JO69VQ>? NV7vRoN[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
RD1 NY\CS41TT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2iwZZ42KM7:TR?= NFT5dVBFVVOR MmLYTWM2OD1yLkC2PEDPxE1? NGLpO2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
OCI-AML 2 (acute myeloid) NWPJTItuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH:zWFF,PSEQvF2= M1\MNWROW09? NXXXcVN4UUN3ME2zMlM{KM7:TR?= M4fuRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
786-O NEHjOXFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXu5[FZuhjVizszN MVrEUXNQ MVPJR|UxRTFwNkS3JO69VQ>? M{n6RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
A673 M3zWRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYX+OUDPxE1? NYfYd|luTE2VTx?= NWnqRoQ3UUN3ME2wMlQxQCEQvF2= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
TALL-1 (T-cell) M1XsSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVHpW|AyhjVizszN NULaR5cyTE2VTx?= MnTVTWM2OD1zLkK4JO69VQ>? MnT5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
151-B MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4qwTZ42KM7:TR?= NIjvO4NFVVOR MUjJR|UxRTJwNkeg{txO MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
PFSK-1 NXjmRYsxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{XMeJ42KM7:TR?= NIXmWohFVVOR MUXJR|UxRTBwMUOyJO69VQ>? M3PUdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
THP-1 NVPaSIo1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWK5dW5shjVizszN NEfudHRFVVOR M1;hOGlEPTB;Nj61PEDPxE1? NGD3RlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
HEK293 M1Gx[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGXrZ5d,PSEQvF2= NVnVVlJsTE2VTx?= MlzyTWM2OD1yLkmxOUDPxE1? NH3kcWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
DAOY MoG1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHL6Wnp,PSEQvF2= NIX5ZZRFVVOR NU[3dJhbUUN3ME2xMlk4QSEQvF2= MlPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
SET2 M4TaOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYjiTWFvhjVizszN NFLVWm5FVVOR Ml3HTWM2OD1yLkK5PEDPxE1? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
HTB-46 NEjNbW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGLFPWd,PSEQvF2= M4\sZ2ROW09? MVXJR|UxRTVwMkWg{txO MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
SK-NAS NV\wfZRXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVz+OUDPxE1? NH3mfmRFVVOR Mnr0TWM2OD1yLkS5O{DPxE1? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
CTLL2 MkLZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV7+OUDPxE1? M2ntTWROW09? NXzNZ45LUUN3ME6xMlAxKM7:TR?= NFzOWnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
HTB-47 NUf6cJlJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUKxdJFJhjVizszN NV21RpIyTE2VTx?= MkP5TWM2OD1{LkC1OkDPxE1? NHPDZoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
LAN-1 NXnmUnh6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFfyboJ,PSEQvF2= M3faN2ROW09? NWS2XXJKUUN3ME2wMlA1KM7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ST486 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlOxglUh|ryP NGTrVJpFVVOR MmTRTWM2OD1zLkG5JO69VQ>? M4jWT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
HS766T NFXWToJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYn+OUDPxE1? NV3LOIEzTE2VTx?= Mn63TWM2OD1{LkCwNUDPxE1? NGHwSmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
IMR-32 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF2xc2x,PSEQvF2= NFzWUnJFVVOR MYDJR|UxRTBwMk[xJO69VQ>? NGHXVnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
Daudi (Burkitt's) MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXL+OUDPxE1? M4fOe2ROW09? NEXoSGVKSzVyPUKuOlM4KM7:TR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Aspc-1 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHKzdWR,PSEQvF2= NYf4fmRLTE2VTx?= MU\JR|UxRTBwM{e5JO69VQ>? MnHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
SK-NSH MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVr+OUDPxE1? M3rRc2ROW09? MUDJR|UxRTBwMUO5JO69VQ>? NWnxZohZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
MEC-1 (Chronic B cell) NHvrbHBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFjLVpZ,PSEQvF2= MojlSG1UVw>? NI\NNFVKSzVyPUKuOlM4KM7:TR?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Capan-2 NIe2XYhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1PDdJ42KM7:TR?= M1jWSGROW09? M2\5R2lEPTB;MT63O|Qh|ryP MonWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
SHSY5Y NFK5cpdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF3NOnl,PSEQvF2= MW\EUXNQ MlznTWM2OD1yLkGwOkDPxE1? NG\Hc2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
U937 (Histioocytic) MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVr+OUDPxE1? NWTyRYV7TE2VTx?= Ml;STWM2OD53LkCwJO69VQ>? NVmwU|dyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Bxpc-1 NWPUdW8xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXnLNYlohjVizszN MXnEUXNQ MVTJR|UxRTFwOUK0JO69VQ>? MorNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Bxpc-3 MnjYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnvPglUh|ryP NXXGVWMyTE2VTx?= MoT4TWM2OD53LkCwJO69VQ>? M1\KRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
HTB-92 M1vUWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHi2cFF,PSEQvF2= MkPwSG1UVw>? MW\JR|UxRTFwMEKg{txO NFvIUmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
OCI-LY10 (B-cell) NV34b2syT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUj+OUDPxE1? M2nKRmROW09? NUDQbGp6UUN3ME2wMlQ2KM7:TR?= NH7wOJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
PANC-1 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1TWNJ42KM7:TR?= NHW5WlZFVVOR M3;kcWlEPTB-NT6wNEDPxE1? NEG0bm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
To184.T NWTCTFRnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXvydow2hjVizszN NILaT2pFVVOR M1XLUGlEPTB;MD60Olkh|ryP MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
OCI-LY19 (B-cell) M1S0R2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn;IglUh|ryP NVm0ZWt1TE2VTx?= MnSwTWM2OD1yLkSg{txO MmPPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
PANC-1 BM M{jUT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3LnSp42KM7:TR?= MUfEUXNQ Ml3KTWM2OD53LkCwJO69VQ>? NXzERXRURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
SA-4 NEOxbYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYH+OUDPxE1? NEHsfZVFVVOR NYjHS4VMUUN3ME2xMlMxOSEQvF2= NHXpPHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
RPMI 8226 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2L1d542KM7:TR?= MX3EUXNQ M3TsVmlEPTB;MT6yPVMh|ryP M4XIZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
HPAF-II M4HXdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlTHglUh|ryP MkDhSG1UVw>? NYTqXGdQUUN3ME2wMlY1PCEQvF2= Mn;LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
SHP-77 M3;PUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV;+OUDPxE1? MYLEUXNQ NFzFPZdKSzVyPUGuPFg5KM7:TR?= NVnOcINuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
U266 B1 MkOxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYT+OUDPxE1? MUHEUXNQ MnT5TWM2OD1zLk[2PUDPxE1? MljRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Hs700t NHnS[HhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3vNVJ42KM7:TR?= MYHEUXNQ NW\WfpRvUUN3ME2wMlI{OSEQvF2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
NCI-446 NHzNZZZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHnYNlN,PSEQvF2= NV3Hb2t[TE2VTx?= M1Swc2lEPTB;MT6xOVQh|ryP NHLEU5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
H929 Mnz5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXv1S|J[hjVizszN M4fVTGROW09? Mlr4TWM2OD1yLkCxOEDPxE1? M{TaO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
PL45 Mkn2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHG5em9,PSEQvF2= M{OySWROW09? MoHjTWM2OD1{LkK1OUDPxE1? NIX4TVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
NCI-H383 NFnNc|RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{O4fp42KM7:TR?= MX3EUXNQ M2jWdGlEPTB-NT6wNEDPxE1? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
JJN3 NFLIZllIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH23VWF,PSEQvF2= MVjEUXNQ Ml\3TWM2OD1{LkSzN{DPxE1? M4jxNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
SU.86.86 NYrNPZNkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3H2UJ42KM7:TR?= MVjEUXNQ NGL3d5dKSzVyPUKuOlczKM7:TR?= M33POlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
H1299 M4DReGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnjFglUh|ryP NXPzeYlyTE2VTx?= M2K2SGlEPTB-NT6wNEDPxE1? NXz5eVhqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
MDA-MB-468 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWH+OUDPxE1? MX\EUXNQ NGXmV3FKSzVyPUCuOVA1KM7:TR?= NHjGXJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
SW1990 NXPoXGRNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVv+OUDPxE1? M4[5bWROW09? MVPJR|UxRTBwOEK2JO69VQ>? NVz4Snk3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Calu-6 M37HN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGThTWN,PSEQvF2= NVLVZoZjTE2VTx?= M1;OeWlEPTB-NT6wNEDPxE1? MmH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
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23132-87 NGDoN45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XjVWlvcGmkaYTpc44hd2ZiaIXtZY4hOjNzM{KtPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDR|LkWyPFYh|ryPLh?= NU\lfZJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
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RMG-I MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{L3fWlvcGmkaYTpc44hd2ZiaIXtZY4hWk2JLVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ2Njd|N{Kg{txONg>? M13VPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4PTR2OD:nQnNCVkeHUkyvZV4>
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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 2022-08-01)

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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