BMS-754807

For research use only.

Catalog No.S1124

35 publications

BMS-754807 Chemical Structure

CAS No. 1001350-96-4

BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.

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Selleck's BMS-754807 has been cited by 35 publications

Purity & Quality Control

Choose Selective IGF-1R Inhibitors

Biological Activity

Description BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.
Features Muti-inhibitor of the IGR-1R/IR family.
Targets
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
TrkB [1]
(Cell-free assay)
Met [1]
(Cell-free assay)
TrkA [1]
(Cell-free assay)
1.7 nM 1.8 nM 4.1 nM 5.6 nM 7.4 nM
In vitro

BMS-754807 effectively inhibits the growth of a broad range of human tumor cell lines of different histologic origins including mesenchymal (Ewing's, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreatic, colon, and gastric), and hematopoietic (multiple myeloma and leukemia), the IC50 values range from 5 nM to 365 nM for the most sensitive cell lines. BMS-754807 inhibits proliferation of IGF-1R-Sal cells and RH41 cells with IC50 of 7 nM and 5 nM. BMS-754807 inhibits phosphorylation of IGF-1R in IGF-1R-Sal cells, Rh41 and Geo with IC50 of 13 nM, 6 nM and 21 nM. BMS-754807 inhibits phosphorylation of Akt in IGF-1R-Sal cells, Rh41 and Geo with IC50 of 22 nM, 13 nM and 16 nM. BMS-754807 induces greater apoptosis in Rh41 cells by 24 hours as indicated by an increased sub-G1 peak (23.1%), compared with control (2.4%). [1] BMS-754807 inhibits the phosphorylation of IGF-1R (IC50 = 13nM) and the downstream targets Akt (IC50 = 22nM) and MAPK (IC50 = 13nM) in the IGF-Sal cell line with IC50 consistent with the antiproliferative IC50 (7 nM) in this cell line. The crystal structure of BMS-754807 cocrystallized with the kinase domain of IGF-1R shows that the donor/acceptor/donor hydrogen bond triad with Met1052 and Glu1050 within the hinge region of the kinase. [2] BMS-754807 shows a median EC50 value of 0.62 μM against 23 cell lines in the pediatric preclinical testing program (PPTP). [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IGF-Sal NX\0OGcyU2mwYYPlJIF{e2G7 MonLbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCLR1[tNXIhMEmFNUCgQUAyO26PKTDhcoQhfGinIHTve45{fHKnYX2geIFz\2W2czDBb5QhMEmFNUCgQUAzOm6PKTDhcoQhVUGSSzCoTWM2OCB;IEGzcm0q MnXXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5N{iwNlQoRjF7N{e4NFI1RC:jPh?=
IGF-Sal MlHNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGH3SI5KSzVyPUegcm0> NGLkPXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe3PFAzPCd-MUm3O|gxOjR:L3G+
CCRF-CEM (ALL) M37IN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWToR|VOhjVizszN NV7Pc5RtTE2VTx?= NHrWVGFKSzVyPUGuNlM6KM7:TR?= M1z2flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
PC3 MoTZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnS0glUh|ryP MlmwSG1UVw>? M2HiN2lEPTB;MD65OlUh|ryP Mn:xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
JD MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX7+OUDPxE1? MonESG1UVw>? NGjCR5hKSzVyPUCuN|kyKM7:TR?= NI\JN|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
DU145 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1fQTJ42KM7:TR?= NF\4UG1FVVOR NFjOc45KSzVyPUGuOFY2KM7:TR?= NIK2dWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
KAG Mle3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF;TS|N,PSEQvF2= MoLKSG1UVw>? MkXRTWM2OD1zLk[2OUDPxE1? NVXBfpZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
K-562 (CML) NY\I[nhMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYrSfmhNhjVizszN MWfEUXNQ NIrXPZVKSzVyPUKuN|AzKM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
B6-P210 (Murine ALL) Mk[4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1e4bZ42KM7:TR?= MmHWSG1UVw>? MnHLTWM2OD1zLkK5N{DPxE1? MlzPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
LN CAP-FGC MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVm1dld7hjVizszN NIfWfGZFVVOR MnrNTWM2OD1zLkSzOEDPxE1? NIPGVpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
VW NUHpVpV7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4T3OJ42KM7:TR?= MoLYSG1UVw>? M4f2fmlEPTB;MD6wNVkh|ryP MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
MV411 (B Myelomonocytic) MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn;WglUh|ryP MVzEUXNQ M{fMTWlEPTB;MD6zN{DPxE1? NELRfWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
MDA-PCa-2b NFi4foVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWDtb|NwhjVizszN NI\vb5JFVVOR NIXBb4ZKSzVyPUCuNFk5KM7:TR?= NIewXWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
LG NFrLO|NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYf+OUDPxE1? MYfEUXNQ NXvqNpJJUUN3ME2wMlA{QCEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
RS411 (B cell precursor-ALL) M4n3[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NG\6c5d,PSEQvF2= NYL3XpI6TE2VTx?= MWLJR|UxRTBwMUCyJO69VQ>? NVW3WYFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
22-r-1 Mn\ZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHXNfYF,PSEQvF2= MW\EUXNQ MULJR|UxRTBwMUe1JO69VQ>? NFPER3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
5838 MmH4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEK4emF,PSEQvF2= NGLOT5BFVVOR NGHzUW9KSzVyPUCuNFM1KM7:TR?= MmfiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
P388 (Murine) MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV\+OUDPxE1? M3fMN2ROW09? NXO1RYp[UUN3ME20MlI4KM7:TR?= M17IeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
A2780/S M33UTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVKwfJl4hjVizszN NUizfm9JTE2VTx?= MY\JR|UxRTBwMUKyJO69VQ>? NIL4UXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
RDES M2LPZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUH+OUDPxE1? NW\XZ2MzTE2VTx?= MVfJR|UxRTBwMEGyJO69VQ>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
B6-T315I (Murine B-ALL) NFX5d3JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mk[5glUh|ryP NFXHSpVFVVOR Ml7pTWM2OD1{LkizJO69VQ>? M{nFVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
TOV 112D NVHVfW8xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlrVglUh|ryP NIewT5lFVVOR MYTJR|UxRTJwMUS2JO69VQ>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
TC32 MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoTQglUh|ryP NYT5bXpUTE2VTx?= NYD1U2tWUUN3ME2wMlAxQCEQvF2= NXW0W2hYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
HL60 (acute myelocytic) NYDVN5J3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYr+OUDPxE1? M2HEeGROW09? M2XacGlEPTB;MD6xNkDPxE1? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
TOV 21G MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIHGUmd,PSEQvF2= NGHod3NFVVOR NGrSSnBKSzVyPUSuNlc6KM7:TR?= MnfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
TC71 NHHFXYhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnLZglUh|ryP MkLYSG1UVw>? MofiTWM2OD1yLkCxOEDPxE1? M37UT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
HPN-ALL (T-cell) NGKxfYRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVz+OUDPxE1? MVHEUXNQ NYDON2FRUUN3ME2wMlUzKM7:TR?= NFHXZlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
A2780R NHG4[4JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIm3R4J,PSEQvF2= MXjEUXNQ M33ZRWlEPTB;MT61OlQh|ryP M2nHelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Rh1 NIS3d5lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVf+OUDPxE1? MXnEUXNQ M1rhNWlEPTB;MD6wNlch|ryP MmjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Kasumi-1 (acute myeloid) NIT2WWpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXnET2lRhjVizszN MXjEUXNQ NY\4flFHUUN3ME2wMlE3KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
sk-ov-3 NFmyZohIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX;+OUDPxE1? NGHhSYpFVVOR NELGS2VKSzVyPUWuNUDPxE1? NUO3eGJmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
ME MoLBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHrSWHB,PSEQvF2= NWf5XItuTE2VTx?= NWry[VBlUUN3ME2wMlAyPSEQvF2= NUTNe4ZCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
L1210 (Murine lymphocytic) MnTIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFn5Vpl,PSEQvF2= NVH2e|NITE2VTx?= Mlv5TWM2OD1{LkO5JO69VQ>? NXTyZ2JwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
sw-626 NXvaOHBFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkL1glUh|ryP NWHRSIN2TE2VTx?= NETv[WVKSzVyPUKuN|A3KM7:TR?= M{fmVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
CTR MlHSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mof4glUh|ryP NIL1ZXNFVVOR NGK2XG1KSzVyPUCuNlU{KM7:TR?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
ML2 (Myelomonocytic) NXXhVYNmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYftXpo6hjVizszN MoPvSG1UVw>? MmTlTWM2OD1yLkC5JO69VQ>? NWXZN|VrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
ovcar-3 NYfFWG5zT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{j5Rp42KM7:TR?= NFeyOIdFVVOR NETmTINKSzVyPUWg{txO NYDDe5V1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
Rh36 Mln6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVv3UGlWhjVizszN MX7EUXNQ NH[0OZFKSzVyPUGuOFMzKM7:TR?= M3XFfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
MOLM-13 (acute myeloid) NYrYeJpqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml3nglUh|ryP NXm3S5BWTE2VTx?= M4\jRWlEPTB;MD60NkDPxE1? NYnrcmlVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
ovcar-4 NVnN[HBCT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEfVcWx,PSEQvF2= NHjve45FVVOR M1uwb2lEPTB;MTFOwG0> MnvNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Rh41 NUHmSFBbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlTNglUh|ryP NIPKSGdFVVOR NHz6UoRKSzVyPUCuNFA2KM7:TR?= Mm\KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
Mutz 2 (acute myeloid) MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIjifVh,PSEQvF2= MlfSSG1UVw>? NGXTdnBKSzVyPUGuNVUh|ryP NYPxc2ljRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
ovcar-5 M4DLbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF7aeWt,PSEQvF2= NVS2d5lPTE2VTx?= NVjkS|ZEUUN3ME2wMlA2KM7:TR?= NUP1SHJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
RD1 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEPUfo1,PSEQvF2= NWLBfnpETE2VTx?= NY\jPGVJUUN3ME2wMlA3QCEQvF2= NF7U[3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
OCI-AML 2 (acute myeloid) NUXUeWNlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2HJOZ42KM7:TR?= NH3wXoJFVVOR M3S2XWlEPTB;Mz6zN{DPxE1? M{Pm[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
786-O NU\DVXd3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MU\+OUDPxE1? NULXOIM2TE2VTx?= NHy2UmtKSzVyPUGuOlQ4KM7:TR?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
A673 NYLvNVlqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4joT542KM7:TR?= NETIT2pFVVOR Mn30TWM2OD1yLkSwPEDPxE1? MmHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
TALL-1 (T-cell) NWDFTlRQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXfoXZF1hjVizszN M4L2N2ROW09? NXHING1xUUN3ME2xMlI5KM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
151-B Ml\KS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXX+OUDPxE1? MYXEUXNQ MXvJR|UxRTJwNkeg{txO M{PaXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
PFSK-1 NWrXR3RwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVT+OUDPxE1? M1LSZWROW09? MojxTWM2OD1yLkGzNkDPxE1? NXTlfYZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
THP-1 M1LnOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXr+OUDPxE1? NFfYbGZFVVOR NWHjUmdZUUN3ME22MlU5KM7:TR?= M4ToUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
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DAOY MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkHoglUh|ryP MU\EUXNQ MXrJR|UxRTFwOUe5JO69VQ>? M1zuZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
SET2 M4PROmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV\+OUDPxE1? M1e0PGROW09? NEDSS4xKSzVyPUCuNlk5KM7:TR?= NVX2NGMzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
HTB-46 NVvVOoJET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIPSSmt,PSEQvF2= NVKzNVc4TE2VTx?= M{HZV2lEPTB;NT6yOUDPxE1? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
SK-NAS M1vKW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkDQglUh|ryP MUjEUXNQ M1nG[2lEPTB;MD60PVch|ryP MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
CTLL2 MkLNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnTtglUh|ryP MYrEUXNQ NUTxdodOUUN3ME6xMlAxKM7:TR?= NGrHVVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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LAN-1 NYLC[I82T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUn+OUDPxE1? M3XCc2ROW09? Mn\HTWM2OD1yLkC0JO69VQ>? NVXPfZA3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
ST486 NEjDW29Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUD+OUDPxE1? NXXONFZMTE2VTx?= MX;JR|UxRTFwMUmg{txO MkLYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
HS766T NVTLcYJ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUTCTHhDhjVizszN M4e0NWROW09? MlnQTWM2OD1{LkCwNUDPxE1? NGTSeoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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Daudi (Burkitt's) NYrzV2ZuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIHTd4Z,PSEQvF2= MlTCSG1UVw>? MUTJR|UxRTJwNkO3JO69VQ>? M3fnUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
Aspc-1 NWCxcG8zT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mki1glUh|ryP MX;EUXNQ NG\Wc4tKSzVyPUCuN|c6KM7:TR?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
SK-NSH MmS3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV33[JQ6hjVizszN MWPEUXNQ MWPJR|UxRTBwMUO5JO69VQ>? M2fVcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
MEC-1 (Chronic B cell) MofhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnOwglUh|ryP NIS2bJFFVVOR NYfhWHRIUUN3ME2yMlY{PyEQvF2= NGGxUZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
Capan-2 M3OxeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUDPUYhChjVizszN NUfHOIdvTE2VTx?= M2XnSWlEPTB;MT63O|Qh|ryP NHS4enY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
SHSY5Y MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXeyU214hjVizszN MYPEUXNQ NXqzSpNyUUN3ME2wMlExPiEQvF2= M2PT[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
U937 (Histioocytic) MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M37IRp42KM7:TR?= MXjEUXNQ M3SwcGlEPTB-NT6wNEDPxE1? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
Bxpc-1 M1;oVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NG\FZ2Z,PSEQvF2= M3T4NmROW09? NEjCT2lKSzVyPUGuPVI1KM7:TR?= NIPQZnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
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HTB-92 NEHKOGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH[zZ2J,PSEQvF2= NYLH[I5rTE2VTx?= NFLjdJNKSzVyPUGuNFIh|ryP MlixQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
OCI-LY10 (B-cell) NVHsUYNST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEX1e3l,PSEQvF2= NI\YWYVFVVOR MXTJR|UxRTBwNEWg{txO MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
PANC-1 M3vVR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXz+OUDPxE1? NU\LXHpCTE2VTx?= MnfMTWM2OD53LkCwJO69VQ>? NF7iVI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
To184.T M1;yOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXv+OUDPxE1? MUjEUXNQ NYTKd3dlUUN3ME2wMlQ3QSEQvF2= MofMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
OCI-LY19 (B-cell) NG\GbY1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1vZVZ42KM7:TR?= MVvEUXNQ M{mzbWlEPTB;MD60JO69VQ>? M3nqT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
PANC-1 BM NGjaR|hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPFfId,PSEQvF2= NEn3OIZFVVOR NES5SIRKSzVyPkWuNFAh|ryP M4jzPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
SA-4 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGTsToh,PSEQvF2= MormSG1UVw>? NFrWXlRKSzVyPUGuN|AyKM7:TR?= M{i4R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
RPMI 8226 NU\6bGFST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX;pPYVZhjVizszN M3XDN2ROW09? M2PqWGlEPTB;MT6yPVMh|ryP MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
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SHP-77 NXLrW484T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUPqeVI5hjVizszN NI\VeFlFVVOR NHHFRpNKSzVyPUGuPFg5KM7:TR?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
U266 B1 M1HGSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2PHfJ42KM7:TR?= NHfZWpVFVVOR NF;FPIFKSzVyPUGuOlY6KM7:TR?= NHHJ[Y89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
Hs700t NXT4cJJWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3rDSp42KM7:TR?= M2G5S2ROW09? NGrYb4RKSzVyPUCuNlMyKM7:TR?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
NCI-446 NWG3PXpZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGT1UlZ,PSEQvF2= NYK5UWpsTE2VTx?= Mo\kTWM2OD1zLkG1OEDPxE1? M3vzSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUm2NlczLz5zOUm5OlI4OjxxYU6=
H929 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGLsNo9,PSEQvF2= NFz2SndFVVOR NFq2enNKSzVyPUCuNFE1KM7:TR?= MnXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
PL45 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3f2[p42KM7:TR?= NWS5SY1RTE2VTx?= M17rVGlEPTB;Mj6yOVUh|ryP NF3MSWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
NCI-H383 M1LkbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUXiPGpMhjVizszN NHe1foJFVVOR Mn7wTWM2OD53LkCwJO69VQ>? NULRd|hZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5PVYzPzJpPkG5PVk3Ojd{PD;hQi=>
JJN3 MlHHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHvQOI1,PSEQvF2= NFK0enhFVVOR MoO5TWM2OD1{LkSzN{DPxE1? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl7NkK3Nkc,OTl7OU[yO|I9N2F-
SU.86.86 Mmm0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MoS5glUh|ryP NF\0eW1FVVOR NVHCVJFDUUN3ME2yMlY4OiEQvF2= NEXyNY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm5OlI4Oid-MUm5PVYzPzJ:L3G+
H1299 NXOyUHRDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH7vbnB,PSEQvF2= M2TENmROW09? MU\JR|UxRjVwMECg{txO MnP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
MDA-MB-468 NXLjW2Q4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3zNep42KM7:TR?= M3\oPWROW09? Mn72TWM2OD1yLkWwOEDPxE1? MnnLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
SW1990 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXj+OUDPxE1? NYPlRYlLTE2VTx?= NHPRc|FKSzVyPUCuPFI3KM7:TR?= MlrZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7OU[yO|IoRjF7OUm2NlczRC:jPh?=
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MFE-280 NWH6NYxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1z2T2lvcGmkaYTpc44hd2ZiaIXtZY4hVU[HLUK4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDFwM{e5OEDPxE1w M4LhXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4PTR2OD:nQnNCVkeHUkyvZV4>
647-V MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nJSmlvcGmkaYTpc44hd2ZiaIXtZY4hPjR5LW[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQyNjh6M{Kg{txONg>? M120WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4PTR2OD:nQnNCVkeHUkyvZV4>
PF-382 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnMTY5pcWKrdHnvckBw\iCqdX3hckBRTi1|OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQzNjB{NEKg{txONg>? NIDmSXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzV2NEivK|5USU6JRWK8M4E,
IST-SL1 M3P1c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJcohq[mm2aX;uJI9nKGi3bXHuJGlUXC2VTEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQzNjN{NEeg{txONg>? MkHaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc2PDR6Lze+V2FPT0WUPD;hQi=>
MKN7 M2\hfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnDTY5pcWKrdHnvckBw\iCqdX3hckBOU055IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0Nk41QTd5IN88UU4> NWfFSJVpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
CP50-MEL-B NXfZR3Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzu[plKdmirYnn0bY9vKG:oIHj1cYFvKEOSNUCtUWVNNUJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IESyMlY6ODFizszNMi=> M3S4NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4PTR2OD:nQnNCVkeHUkyvZV4>
K052 M1f4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M32xeGlvcGmkaYTpc44hd2ZiaIXtZY4hUzB3MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gOFMvODZ7ODFOwG0v MlTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc2PDR6Lze+V2FPT0WUPD;hQi=>
23132-87 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DET2lvcGmkaYTpc44hd2ZiaIXtZY4hOjNzM{KtPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDR|LkWyPFYh|ryPLh?= NUPXb|kxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
GAK M4PwdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\KR2lvcGmkaYTpc44hd2ZiaIXtZY4hT0GNIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0OE4yOjdizszNMi=> NUnvTnVIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
Mewo MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfOTY5pcWKrdHnvckBw\iCqdX3hckBO\XexIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0OU42QDd6IN88UU4> M2\JeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4PTR2OD:nQnNCVkeHUkyvZV4>
RMG-I NELkN|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHnNpFMUW6qaXLpeIlwdiCxZjDoeY1idiCUTVetTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDVwN{O3NkDPxE1w NVvSZVM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?
BE-13 NGPSRpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0OU46Ozl{IN88UU4> M1jtOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4PTR2OD:nQnNCVkeHUkyvZV4>
SW684 MmLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i3WWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4OESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ4NjR7Nkmg{txONg>? NUPMTGM5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd3NES4M{c,W0GQR1XSQE9iRg>?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-IGFIRRβ/InsRβ / IGFIRβ / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 26136493     


(C) T4105 cells were treated with OSI-906 or BMS-754807 at indicated concentrations for 24 hours, lysed, and subjected to immunoblotting.

26136493
Growth inhibition assay
Cell viability; 

PubMed: 30754629     


Response of SK-CO-1 to various drugs and drug combinations.

30754629
In vivo BMS-754807 (12.5mg/kg, orally) inhibits IGF-1R phosphorylation in tumor and serum in IGF-1R-Sal tumor–bearing nude mice. BMS-754807 inhibits tumor growth in a selected group of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3), and mesenchymal (RD1 and Rh41) xenograft tumor models with TGI ranging from 53% to 115%. [1] BMS-754807 (6.25 mg/kg) achieves complete tumor growth inhibition in the transgenic-derived IGF-Sal tumor mouse model with correlated inhibition of pIGF-1R and pAKT. The protein binding for BMS-754807 ranges from of 98.5% in mouse plasma to 95.9% in human plasma. BMS-754807 results in clearance of 113 (mL/min)/kg, 20 (mL/min)/kg, 3.5 (mL/min)/kg and 41 (mL/min)/kg. [2] BMS-754807 (25 mg/kg) significantly inhibits tumor in KT-5 (Wilms), KT-14 (rhabdoid), Rh28 (rhabdomyosarcoma), and OS-1 xenografts mice model. [3]

Protocol

Kinase Assay:[1]
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Kinase inhibition assays:

The primary screen for BMS-754807 is an in vitro kinase assay using recombinant human IGF-1 receptor enzyme in biochemical assays using synthetic peptide KKSRGDYMTMQIG as a phosphoacceptor substrate. The selectivity profile is evaluated against multiple recombinant enzymes that are generated at BMS or purchased externally. The enzymatic assays are performed in Ubottom 384-well plates using a 30 μL reaction volume in assay buffer (100 mM Hepes pH 7.4, 10 mM MgCl2, 0.015% Brij35 and 4 mM DTT). The 60 minute reactions are initiated by combining ATP (concentration equivalent to Km ATP), 1.5 μM fluoresceinlabeled peptide substrate, enzyme and BMS-754807. The reactions are terminated with EDTA. The reaction mixtures are analyzed on the Caliper LabChip 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data are calculated by comparison to enzyme-free control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. Compounds are dissolved in dimethylsulfoxide (DMSO, 10mM stock) and evaluated at eleven concentrations. IC50 values are derived by non-linear regression analysis of the dose response curves.
Cell Research:[1]
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  • Cell lines: IGF-1R-Sal, RH41 and Geo cell lines
  • Concentrations: 365 nM
  • Incubation Time: 72 hours
  • Method: Cells are grown at their optimal density in RPMI +GlutaMax supplemented with 10% heat-inactivated fetal bovine serum (FBS), 10 mM Hepes, penicillin, and streptomycin. Cell proliferation is evaluated by incorporation of 3H-thymidine into DNA after exposure of cells to BMS-754807 for 72 hours. Results are expressed as an IC50, which is the drug concentration required to inhibit cell proliferation by 50% compared with untreated control cells.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: IGF-1R-Sal, GEO, Colo205, JJN3, RD1 or Rh41 tumor–bearing nude mice
  • Dosages: 150 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (199.35 mM)
Water Insoluble
Ethanol '''92 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 461.49
Formula

C23H24FN9O

CAS No. 1001350-96-4
Storage powder
in solvent
Synonyms N/A
Smiles CC1(CCCN1C2=NN3C=CC=C3C(=N2)NC4=NNC(=C4)C5CC5)C(=O)NC6=CN=C(C=C6)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID