BMS-754807

製品コードS1124

BMS-754807化学構造

分子量(MW):461.49

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, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.

サイズ 価格(税別) 在庫  
JPY 31800 あり
JPY 46800 あり
JPY 129800 あり
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バルク問合せ

製品安全説明書

IGF-1R阻害剤の選択性比較

生物活性

製品説明 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, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.
特性 Muti-inhibitor of the IGR-1R/IR family.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IGF-Sal M37SW2tqdmG|ZTDhd5NigQ>? NWfLNItqcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDJS2YuOVJiKFnDOVAhRSBzM37NLUBidmRidHjlJIRwf26|dILlZY0hfGG{Z3X0d{BCc3RiKFnDOVAhRSB{Mn7NLUBidmRiTVHQT{ApUUN3MDC9JFE{dk1r NGrub|MyQTd5OECyOC=>
IGF-Sal NIr4bXRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M37OXmlEPTB;NzDuUS=> M{j1VVE6Pzd6MEK0
CCRF-CEM (ALL) M3rY[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYf+OUDPxE1? NYnoSm0xTE2VTx?= M3Wz[mlEPTB;MT6yN|kh|ryP M1q0UFE6QTl4Mkey
PC3 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4D5XZ42KM7:TR?= MV;EUXNQ NFfKTJJKSzVyPUCuPVY2KM7:TR?= NXnwZW9iOTl7OU[yO|I>
JD MlzHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3LkTp42KM7:TR?= M2PnR2ROW09? NGi4eXRKSzVyPUCuN|kyKM7:TR?= NH3xfIoyQTl7NkK3Ni=>
DU145 Mn31S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3[2V542KM7:TR?= NH7ZU|VFVVOR MWfJR|UxRTFwNE[1JO69VQ>? MYexPVk6PjJ5Mh?=
KAG MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlXPglUh|ryP MULEUXNQ M4LsVGlEPTB;MT62OlUh|ryP M2XFclE6QTl4Mkey
K-562 (CML) Ml;JS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NILtU2J,PSEQvF2= MUDEUXNQ M1nKemlEPTB;Mj6zNFIh|ryP MVmxPVk6PjJ5Mh?=
B6-P210 (Murine ALL) MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUfXWXVZhjVizszN MVjEUXNQ M3rudGlEPTB;MT6yPVMh|ryP MnfrNVk6QTZ{N{K=
LN CAP-FGC M1nJbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYr1WHo3hjVizszN M1rybWROW09? MnK4TWM2OD1zLkSzOEDPxE1? MWCxPVk6PjJ5Mh?=
VW M{DPOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVH2OXpLhjVizszN NX21Uo1jTE2VTx?= M2i0ZmlEPTB;MD6wNVkh|ryP MmDmNVk6QTZ{N{K=
MV411 (B Myelomonocytic) MnnUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4LpZZ42KM7:TR?= MonrSG1UVw>? MYnJR|UxRTBwM{Og{txO MoS4NVk6QTZ{N{K=
MDA-PCa-2b NWKwO|k{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGj5cGZ,PSEQvF2= MY\EUXNQ MnnWTWM2OD1yLkC5PEDPxE1? NWnUXnJ7OTl7OU[yO|I>
LG NX3oXWJJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWn+OUDPxE1? MnnySG1UVw>? NEnGb|JKSzVyPUCuNFM5KM7:TR?= MUmxPVk6PjJ5Mh?=
RS411 (B cell precursor-ALL) NUXGPYxwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoPKglUh|ryP NV;zPXg4TE2VTx?= MoTJTWM2OD1yLkGwNkDPxE1? MWqxPVk6PjJ5Mh?=
22-r-1 NVTXdG9HT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1X3TZ42KM7:TR?= NWntVFkyTE2VTx?= M4XwemlEPTB;MD6xO|Uh|ryP NHHLUXAyQTl7NkK3Ni=>
5838 MoLqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1TqZ542KM7:TR?= M2L3bGROW09? Mnj3TWM2OD1yLkCzOEDPxE1? M{\XOVE6QTl4Mkey
P388 (Murine) NFPIR4JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV\HPJZRhjVizszN MW\EUXNQ MlT4TWM2OD12LkK3JO69VQ>? M1XxcVE6QTl4Mkey
A2780/S M1K3WWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXv+OUDPxE1? NVzob2JNTE2VTx?= M3nYdmlEPTB;MD6xNlIh|ryP MmPMNVk6QTZ{N{K=
RDES NEnRbnlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUL+OUDPxE1? M3X4VWROW09? M4q3dWlEPTB;MD6wNVIh|ryP MlP3NVk6QTZ{N{K=
B6-T315I (Murine B-ALL) M162Omdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkHxglUh|ryP NV3Y[WZmTE2VTx?= NVzKZoY2UUN3ME2yMlg{KM7:TR?= NXnod|h[OTl7OU[yO|I>
TOV 112D NI\LfWlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF31R3R,PSEQvF2= NH31R3pFVVOR MlvzTWM2OD1{LkG0OkDPxE1? NWPTe2VqOTl7OU[yO|I>
TC32 NYfnN|FpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVLRd3dthjVizszN MkPSSG1UVw>? Ml6zTWM2OD1yLkCwPEDPxE1? MVKxPVk6PjJ5Mh?=
HL60 (acute myelocytic) NUXuXokzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXTkZXVyhjVizszN M{\XPGROW09? M3zkVmlEPTB;MD6xNkDPxE1? M3L6[VE6QTl4Mkey
TOV 21G NGe4OodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4H0dp42KM7:TR?= NUWzNGdbTE2VTx?= MmTOTWM2OD12LkK3PUDPxE1? MoCzNVk6QTZ{N{K=
TC71 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGP3[IN,PSEQvF2= MnO4SG1UVw>? NYfY[nNyUUN3ME2wMlAyPCEQvF2= NUXpc29POTl7OU[yO|I>
HPN-ALL (T-cell) Mk\5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX7+OUDPxE1? MonOSG1UVw>? MXTJR|UxRTBwNUKg{txO MVexPVk6PjJ5Mh?=
A2780R NY\lTHY3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4nUT542KM7:TR?= MlHzSG1UVw>? NIj4PJhKSzVyPUGuOVY1KM7:TR?= NFX2cZkyQTl7NkK3Ni=>
Rh1 M4DSU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF:1UYR,PSEQvF2= MkfiSG1UVw>? Mnv3TWM2OD1yLkCyO{DPxE1? NIXrUJMyQTl7NkK3Ni=>
Kasumi-1 (acute myeloid) Ml\1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{C3eJ42KM7:TR?= MVnEUXNQ M1fOZ2lEPTB;MD6xOkDPxE1? NXHjT5FkOTl7OU[yO|I>
sk-ov-3 Moe5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2HyO542KM7:TR?= MmX0SG1UVw>? M1rFZ2lEPTB;NT6xJO69VQ>? MmS5NVk6QTZ{N{K=
ME NXfSb|FpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVjGcmRXhjVizszN NIXjXWZFVVOR MYrJR|UxRTBwMEG1JO69VQ>? NVGzPXpnOTl7OU[yO|I>
L1210 (Murine lymphocytic) MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXXkb28{hjVizszN MV;EUXNQ MVrJR|UxRTJwM{mg{txO M3PhTFE6QTl4Mkey
sw-626 NUnhd|JKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4C1eJ42KM7:TR?= MlXISG1UVw>? NHz3TGlKSzVyPUKuN|A3KM7:TR?= M1XTc|E6QTl4Mkey
CTR NFjofVBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MX\+OUDPxE1? MkHySG1UVw>? MX;JR|UxRTBwMkWzJO69VQ>? MmHPNVk6QTZ{N{K=
ML2 (Myelomonocytic) NEj0VmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlLKglUh|ryP MX7EUXNQ M2T0R2lEPTB;MD6wPUDPxE1? NHjrTYkyQTl7NkK3Ni=>
ovcar-3 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2rJUJ42KM7:TR?= NU\iTHlOTE2VTx?= MV;JR|UxRTVizszN M13oNFE6QTl4Mkey
Rh36 M1rvb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF;mR2t,PSEQvF2= MUHEUXNQ NYnyXY8yUUN3ME2xMlQ{OiEQvF2= NGPVOHEyQTl7NkK3Ni=>
MOLM-13 (acute myeloid) MoOyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF3YeWt,PSEQvF2= NFTB[GZFVVOR M4SxSWlEPTB;MD60NkDPxE1? M3m1eVE6QTl4Mkey
ovcar-4 NVnydIh[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWL+OUDPxE1? NFTYSJVFVVOR NYT6UItnUUN3ME2xJO69VQ>? NHvPXmgyQTl7NkK3Ni=>
Rh41 MkixS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVn+OUDPxE1? MWjEUXNQ NXm0RWc6UUN3ME2wMlAxPSEQvF2= NYf1[|VlOTl7OU[yO|I>
Mutz 2 (acute myeloid) MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn7SglUh|ryP NXTwfpRnTE2VTx?= MlLwTWM2OD1zLkG1JO69VQ>? NU\FTnZkOTl7OU[yO|I>
ovcar-5 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGPiO3p,PSEQvF2= NXrrd45KTE2VTx?= NE\GS|RKSzVyPUCuNFUh|ryP MUSxPVk6PjJ5Mh?=
RD1 NWLHPINRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYP+OUDPxE1? MWHEUXNQ M{PjbWlEPTB;MD6wOlgh|ryP Mn3kNVk6QTZ{N{K=
OCI-AML 2 (acute myeloid) NYf1dnpVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIXTNWp,PSEQvF2= NF\GfmtFVVOR NHnaboRKSzVyPUOuN|Mh|ryP NGnKSJAyQTl7NkK3Ni=>
786-O M2PQZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2X6Xp42KM7:TR?= NXjF[JlpTE2VTx?= Ml3YTWM2OD1zLk[0O{DPxE1? NVnY[mlJOTl7OU[yO|I>
A673 Mli5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVfzZnUyhjVizszN M3jwTWROW09? NFjwc4NKSzVyPUCuOFA5KM7:TR?= MW[xPVk6PjJ5Mh?=
TALL-1 (T-cell) NF7NOIxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MojvglUh|ryP MYPEUXNQ MWTJR|UxRTFwMkig{txO NEfHdJUyQTl7NkK3Ni=>
151-B NHXOR5RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2P4VZ42KM7:TR?= NWXFWZRpTE2VTx?= NX\vZmQyUUN3ME2yMlY4KM7:TR?= MlvnNVk6QTZ{N{K=
PFSK-1 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NY\SSI9ihjVizszN Mm\tSG1UVw>? MlPXTWM2OD1yLkGzNkDPxE1? NXPTNVl3OTl7OU[yO|I>
THP-1 MoTUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF7weJF,PSEQvF2= NUTNSWJjTE2VTx?= NIjpcXZKSzVyPU[uOVgh|ryP NWPLTpdLOTl7OU[yO|I>
HEK293 NY[y[YVzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmXYglUh|ryP NVuxNm1yTE2VTx?= NIPVTHVKSzVyPUCuPVE2KM7:TR?= MYGxPVk6PjJ5Mh?=
DAOY MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkHMglUh|ryP NIK5UHZFVVOR NYiwR4FzUUN3ME2xMlk4QSEQvF2= M1fLWFE6QTl4Mkey
SET2 NHHWW5hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHnLPWh,PSEQvF2= M1j2emROW09? NFjqRmRKSzVyPUCuNlk5KM7:TR?= Ml[xNVk6QTZ{N{K=
HTB-46 MkL1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXv2dFhrhjVizszN M3zLXmROW09? NUDxUmlSUUN3ME21MlI2KM7:TR?= NEnnSo8yQTl7NkK3Ni=>
SK-NAS MmjjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkK5glUh|ryP MlnhSG1UVw>? MlHaTWM2OD1yLkS5O{DPxE1? MUexPVk6PjJ5Mh?=
CTLL2 NIL5enJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUThW4M3hjVizszN M{HoZ2ROW09? M4DlTWlEPTB-MT6wNEDPxE1? Mnq1NVk6QTZ{N{K=
HTB-47 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVP+OUDPxE1? MVXEUXNQ MmizTWM2OD1{LkC1OkDPxE1? NFPzboUyQTl7NkK3Ni=>
LAN-1 M1mxPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUL+OUDPxE1? NEiyTZpFVVOR Mn\VTWM2OD1yLkC0JO69VQ>? NX3BOIR4OTl7OU[yO|I>
ST486 NICzemJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1XCdJ42KM7:TR?= M4fpSWROW09? MWTJR|UxRTFwMUmg{txO M3XxPVE6QTl4Mkey
HS766T Ml3aS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1LjfZ42KM7:TR?= MYHEUXNQ NWXUbGFwUUN3ME2yMlAxOSEQvF2= NUj4SnZtOTl7OU[yO|I>
IMR-32 NWqwfHdwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2rZWZ42KM7:TR?= NF3uZohFVVOR MV;JR|UxRTBwMk[xJO69VQ>? NYq0[IJ4OTl7OU[yO|I>
Daudi (Burkitt's) MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGPPXmV,PSEQvF2= MluwSG1UVw>? NIH6TlJKSzVyPUKuOlM4KM7:TR?= NYDZb5BuOTl7OU[yO|I>
Aspc-1 M4LJZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmfSglUh|ryP M33rUGROW09? NWjteVdbUUN3ME2wMlM4QSEQvF2= M3HFTFE6QTl4Mkey
SK-NSH NHvXeoxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHXsZ|h,PSEQvF2= M3O0ZmROW09? MWTJR|UxRTBwMUO5JO69VQ>? MojHNVk6QTZ{N{K=
MEC-1 (Chronic B cell) M17GNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVX+OUDPxE1? MXjEUXNQ NYqyZYNjUUN3ME2yMlY{PyEQvF2= MYGxPVk6PjJ5Mh?=
Capan-2 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWL2S4dYhjVizszN MWnEUXNQ NEi4TZFKSzVyPUGuO|c1KM7:TR?= NYPTN21mOTl7OU[yO|I>
SHSY5Y MkXkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mle1glUh|ryP M1uyOmROW09? MVjJR|UxRTBwMUC2JO69VQ>? NFfwTnEyQTl7NkK3Ni=>
U937 (Histioocytic) MlzwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXT+OUDPxE1? NE[1enhFVVOR NEeyfIpKSzVyPkWuNFAh|ryP NV7X[5NROTl7OU[yO|I>
Bxpc-1 NV\SNXp{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MofZglUh|ryP NU\DfoxiTE2VTx?= NGHOfopKSzVyPUGuPVI1KM7:TR?= MnPDNVk6QTZ{N{K=
Bxpc-3 MkHGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIfJSZp,PSEQvF2= MkHFSG1UVw>? M1jkVWlEPTB-NT6wNEDPxE1? NID4bYUyQTl7NkK3Ni=>
HTB-92 NH7pN2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVS3WW84hjVizszN MoXuSG1UVw>? M3LXNmlEPTB;MT6wNkDPxE1? MlX1NVk6QTZ{N{K=
OCI-LY10 (B-cell) NVTSbWlbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2e2cp42KM7:TR?= NHT0VFNFVVOR M1HjNWlEPTB;MD60OUDPxE1? NHfnblQyQTl7NkK3Ni=>
PANC-1 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M13oXJ42KM7:TR?= NWjRb3E{TE2VTx?= NILU[lBKSzVyPkWuNFAh|ryP MnPDNVk6QTZ{N{K=
To184.T M{XUPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NE\QeG5,PSEQvF2= M{TiN2ROW09? M4PSSGlEPTB;MD60Olkh|ryP NHO2PXkyQTl7NkK3Ni=>
OCI-LY19 (B-cell) M4fUPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXniO|EyhjVizszN NIPzVFFFVVOR NI\V[4JKSzVyPUCuOEDPxE1? NULsSFZCOTl7OU[yO|I>
PANC-1 BM M1nUTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoDyglUh|ryP NXG0SZJWTE2VTx?= MUTJR|UxRjVwMECg{txO MW[xPVk6PjJ5Mh?=
SA-4 M3r0Omdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2TsPZ42KM7:TR?= MnzRSG1UVw>? M{KzbmlEPTB;MT6zNFEh|ryP MY[xPVk6PjJ5Mh?=
RPMI 8226 NIPGN|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH;qfZZ,PSEQvF2= MXHEUXNQ M4O5UWlEPTB;MT6yPVMh|ryP M2LXWFE6QTl4Mkey
HPAF-II M1[5VWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYLl[XVMhjVizszN MW\EUXNQ NV60ZmVrUUN3ME2wMlY1PCEQvF2= NWLNcGg{OTl7OU[yO|I>
SHP-77 M1\PNmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NW\seJN5hjVizszN M37RdGROW09? NXfSc3ZzUUN3ME2xMlg5QCEQvF2= NU\aVYtiOTl7OU[yO|I>
U266 B1 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoSxglUh|ryP Ml\DSG1UVw>? NUPzUJlNUUN3ME2xMlY3QSEQvF2= M2HoW|E6QTl4Mkey
Hs700t M1H0fmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn;0glUh|ryP NYTh[5dxTE2VTx?= NGezdnNKSzVyPUCuNlMyKM7:TR?= MmqwNVk6QTZ{N{K=
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Rh30 NEfzT5dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYH+NVDjiIsQvF2= MVPJR|UxRTBwMUmgxtVO NY\2R2FJOjF{OUi3OFU>
BT-12 MmjmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2Pmep4yOOLCit88US=> NIjqXVVKSzVyPUCuO|ghyrWP NFLIRYMzOTJ7OEe0OS=>
CHLA-266 NXy4WGNsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWr+NVDjiIsQvF2= Mn36TWM2OD1yLki5JOK2VQ>? M1r1dVIyOjl6N{S1
TC-71 NY\aRXJ6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFXs[4h,OTEkgJtOwG0> NFrhfFlKSzVyPUCuNVEhyrWP M{DHVlIyOjl6N{S1
CHLA-9 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYT+NVDjiIsQvF2= M3\3SmlEPTB;MD6xNkDDvU1? M33JeFIyOjl6N{S1
CHLA-10 MmrqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHzHR5d,OTEkgJtOwG0> Ml;tTWM2OD1yLk[yJOK2VQ>? NUDEcnhMOjF{OUi3OFU>
CHLA-258 NYLyfGw5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUfHPWFlhjFy4pEK{txO NX75eYo1UUN3ME2wMlI4KML3TR?= NXLkU4l6OjF{OUi3OFU>
GBM2 NY\POpNJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mmr0glEx6oDMzszN NV3zTWpEUUN3ME2xMlQ4KML3TR?= Mo\SNlEzQTh5NEW=
NB-1643 MkXES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NEfwe|V,OTEkgJtOwG0> MV\JR|UxRTBwMUKgxtVO NEXmcGUzOTJ7OEe0OS=>
NB-EBc1 NGjuZWtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmHXglEx6oDMzszN NHLZTGZKSzVyPUCuN|UhyrWP MlzsNlEzQTh5NEW=
CHLA-90 M3zlUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEDufHB,OTEkgJtOwG0> MoLrTWM2OD1yLke3JOK2VQ>? NWHiZm84OjF{OUi3OFU>
CHLA-136 NGjTc2ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlfjglEx6oDMzszN Ml7CTWM2OD1yLkWyJOK2VQ>? M1TxXlIyOjl6N{S1
NALM-6 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MljyglEx6oDMzszN MoPsTWM2OD1yLkS5JOK2VQ>? MWeyNVI6QDd2NR?=
COG-LL-317 NEnGUG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUf+NVDjiIsQvF2= MYDJR|UxRTFwM{igxtVO NEjEOW0zOTJ7OEe0OS=>
RS4;11 M4X5Zmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml;mglEx6oDMzszN Mo\JTWM2OD1yLkO4JOK2VQ>? NVjJeIs3OjF{OUi3OFU>
MOLT-4 MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHnoWnZ,OTEkgJtOwG0> NFfjblBKSzVyPUCuOVMhyrWP M4D0e|IyOjl6N{S1
CCRF-CEM NF7vbIZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXG0WYhPhjFy4pEK{txO MlOwTWM2OD1zLkGzJOK2VQ>? M{HwPVIyOjl6N{S1
Kasumi-1 Mlr2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MknYglEx6oDMzszN NXP1NXF6UUN3ME2xMlIhyrWP MVmyNVI6QDd2NR?=
Karpas-299 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmXSglEx6oDMzszN M1f5PGlEPTB;MT62OEDDvU1? M1HFXVIyOjl6N{S1
Ramos-RA1 NEfse3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NILKTYl,OTEkgJtOwG0> NHj6eFJKSzVyPUGuN|EhyrWP NFzBboMzOTJ7OEe0OS=>
Rh30  NFnEdnpHfW6ldHnvckBie3OjeR?= MmLDbY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w MU[yOVkzPTN5OB?=
Rh41 M3;McmZ2dmO2aX;uJIF{e2G7 M2r1e4lv\HWlZYOgZY4hcW6lcnXhd4Uhd2ZiU1\LJJBpd3OyaH;yfYxifGmxbh?= MUOyOVkzPTN5OB?=
RD M2r6bWZ2dmO2aX;uJIF{e2G7 NFq1PHJqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:|cHjvdplt[XSrb36= M1HTdFI2QTJ3M{e4
A549 M3\JWGtqdmG|ZTDhd5NigQ>? NYPFWFVkOC534pEK{txO Mmn2SG1UVw>? NGnndJVqdmirYnn0d{BKT0ZvSWKvTXIh[WO2aY\heIlwdg>? MnG3NlY6Ojh3N{i=
NCI-H358 MXPLbY5ie2ViYYPzZZk> NVi5UJpWOC534pEK{txO NVrGTYRQTE2VTx?= MnfvbY5pcWKrdIOgTWdHNUmUL1nSJIFkfGm4YYTpc44> M{\Re|I3QTJ6NUe4
A549 NF[0OFVHfW6ldHnvckBie3OjeR?= NH7xdnAxNjYkgJtOwG0> NV7uS2lVTE2VTx?= MnzqZ4F2e2W|IHGgZ49v[3W{cnXueEBl\WO{ZXHz[UBqdiCyaH;zdIhwenmuYYTl[EBCU1RiYX7kJGVTUw>? NH7KZ4QzPjl{OEW3PC=>
NCI-H358 NIC2dVRHfW6ldHnvckBie3OjeR?= Mlv0NE426oDMzszN NXLW[FNQTE2VTx?= MlLuZ4F2e2W|IHGgZ49v[3W{cnXueEBl\WO{ZXHz[UBqdiCyaH;zdIhwenmuYYTl[EBCU1RiYX7kJGVTUw>? NXnXXnVkOjZ7Mki1O|g>
A549 NF\oNmFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGThTm9,OTEkgJtOwG0> M4jPeWROW09? NGnhNFRKSzVyPUCuO|Yh|ryP M324dlI3QTJ6NUe4
NCI-H358 NFnhcpZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYr+NVDjiIsQvF2= NU[zVIt3TE2VTx?= MVzJR|UxRTFwMEmg{txO NH;aeZIzPjl{OEW3PC=>
A549 MW\BdI9xfG:|aYOgZZN{[Xl? NVHT[Y1WOC534pEK{txO NYrreGxrTE2VTx?= MWTpcoR2[2W|IFHwc5B1d3Orcx?= NGXpe5YzPjl{OEW3PC=>
NCI-H358 M37TSGFxd3C2b4Ppd{Bie3OjeR?= NITGXFQxNjYkgJtOwG0> NXjyO3pwTE2VTx?= M4DlO4lv\HWlZYOgRZBweHSxc3nz MXGyOlkzQDV5OB?=
A549 MV\GeY5kfGmxbjDhd5NigQ>? NHXKXY8xNjYkgJtOwG0> M323V2ROW09? MnrhdoVlfWOnczD3c5Vv\CClbH;zeZJm MkPuNlY6Ojh3N{i=
NCI-H358 MVzGeY5kfGmxbjDhd5NigQ>? NHvNeFMxNjYkgJtOwG0> NGDjfo5FVVOR MorYdoVlfWOnczD3c5Vv\CClbH;zeZJm NX3UWVFLOjZ7Mki1O|g>

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アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

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.
細胞試験: [1]
- 合併
  • 細胞株: IGF-1R-Sal, RH41 and Geo cell lines
  • 濃度: 365 nM
  • 反応時間: 72 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[1]
- 合併
  • 動物モデル: IGF-1R-Sal, GEO, Colo205, JJN3, RD1 or Rh41 tumor–bearing nude mice
  • 製剤: Mixture of polyethylene glycol 400 (PEG400/water (4:1; vol/vol)
  • 投薬量: 150 mg/kg
  • 投与方法: Orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 92 mg/mL (199.35 mM)
Ethanol 92 mg/mL (199.35 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 461.49
化学式

C23H24FN9O

CAS No. 1001350-96-4
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

IGF-1Rシグナル伝達経路

IGF-1R Inhibitors with Unique Features

相関IGF-1R製品

Tags: BMS-754807を買う | BMS-754807 ic50 | BMS-754807供給者 | BMS-754807を購入する | BMS-754807費用 | BMS-754807生産者 | オーダーBMS-754807 | BMS-754807化学構造 | BMS-754807分子量 | BMS-754807代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID