BMS-754807

Name: BMS-754807
Brand: Selleck Chemicals
SKU: S1124
Rating: 5 (23 reviews)

For research use only.

Catalog No.S1124

23 publications

Molecular Weight(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.

Selleck's BMS-754807 has been cited by 23 publications

Cancer Discov, 2015, 5(9):960-971

PubMed: 26036643 ( click the link to review the publication )

Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2485

PubMed: 31969334 ( click the link to review the publication )

Nat Commun, 2019, 10(1):3201

PubMed: 31324758 ( click the link to review the publication )

Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y

PubMed: 31316177 ( click the link to review the publication )

Cytotherapy, 2019, 21(6):619-630

PubMed: 30956007 ( click the link to review the publication )

Cancer Biol Ther, 2019, 10.1080/15384047.2019.1665952

PubMed: 31559898 ( click the link to review the publication )

Molecules, 2019, 24(3)

PubMed: 30754629 ( click the link to review the publication )

Leuk Res, 2019, 78:12-20

PubMed: 30660961 ( click the link to review the publication )

Cell Mol Gastroenterol Hepatol, 2019, 8(1):37-60

PubMed: 30836148 ( click the link to review the publication )

Cancer Res, 2018, 78(14):3995-4006

PubMed: 29669759 ( click the link to review the publication )

Endocrinology, 2018, 159(1):285-296

PubMed: 29029116 ( click the link to review the publication )

Brain Res, 2018, 1678:407-418

PubMed: 29137974 ( click the link to review the publication )

Oncotarget, 2018, 9(56):30869-30882

PubMed: 30112114 ( click the link to review the publication )

Drug Deliv, 2018, 25(1):241-255

PubMed: 29334272 ( click the link to review the publication )

Mol Cell, 2017, 67(3):512-527

PubMed: 28757207 ( click the link to review the publication )

Genes Dev, 2017, 31(6):553-566

PubMed: 28404630 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(1):88-101

PubMed: 28062706 ( click the link to review the publication )

Int J Mol Sci, 2017, 18(11)

PubMed: 29099049 ( click the link to review the publication )

Cellular Signalling, 2016, 19;28(6):652-662

PubMed: 27006333 ( click the link to review the publication )

Mol Cell Biol, 2015, 35(7):1182-96

PubMed: ( click the link to review the publication )

PLoS One, 2015, 10(5):e0126867

PubMed: 25962155 ( click the link to review the publication )

Cancer Res, 2014, 74(20):5866-77

PubMed: 25168481 ( click the link to review the publication )

Clin Cancer Res, 2013, 19(11):2984-94

PubMed: 23549869 ( click the link to review the publication )

Purity & Quality Control

Choose Selective IGF-1R Inhibitors

Biological Activity

Description

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)	View More
1.7 nM	1.8 nM	4.1 nM	5.6 nM	7.4 nM	View More

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	Formulation	Activity Description	PMID
IGF-Sal	MUPLbY5ie2ViYYPzZZk>			MXrpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEmJRj2xVkApUUN3MDC9JFE{dk1rIHHu[EB1cGViZH;3cpN1emWjbTD0ZZJo\XS\|IFHreEApUUN3MDC9JFIzdk1rIHHu[EBOSVCNIDjJR\|UxKD1iMUPuUUk>	NGfITGMyQTd5OECyOC=>
IGF-Sal	M{jDV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7			M4S1OWlEPTB;NzDuUS=>	NVPTO4ZoOTl5N{iwNlQ>
CCRF-CEM (ALL)	NVqzUVdkT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MmfNglUh\|ryP	NGqze\|BFVVOR	MkDNTWM2OD1zLkKzPUDPxE1?	MkixNVk6QTZ{N{K=
PC3	NXvKeplUT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NVLDTIpPhjVizszN	NWT0NpMyTE2VTx?=	NYLNNHdFUUN3ME2wMlk3PSEQvF2=	MXmxPVk6PjJ5Mh?=
JD	MknkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MXH+OUDPxE1?	NEnmVplFVVOR	MkWwTWM2OD1yLkO5NUDPxE1?	NYLG[4xMOTl7OU[yO\|I>
DU145	MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NVSyeI1IhjVizszN	NUHwdZBSTE2VTx?=	MXXJR\|UxRTFwNE[1JO69VQ>?	NUX6ZYJWOTl7OU[yO\|I>
KAG	NWTuWlR5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MVT+OUDPxE1?	NVLZOWJPTE2VTx?=	MXzJR\|UxRTFwNk[1JO69VQ>?	M3nVU\|E6QTl4Mkey
K-562 (CML)	NYLIZpVpT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NHzKRY5,PSEQvF2=	M3jXemROW09?	MoCyTWM2OD1{LkOwNkDPxE1?	NW\EdnB5OTl7OU[yO\|I>
B6-P210 (Murine ALL)	MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M1SzXp42KM7:TR?=	MWPEUXNQ	NW\ud45xUUN3ME2xMlI6OyEQvF2=	MUixPVk6PjJ5Mh?=
LN CAP-FGC	NIPiUVRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NV;kTVBFhjVizszN	M{XlVWROW09?	M2D0eWlEPTB;MT60N\|Qh\|ryP	MkfmNVk6QTZ{N{K=
VW	MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NHXhZXd,PSEQvF2=	NIrPdGtFVVOR	NUDXPI0yUUN3ME2wMlAyQSEQvF2=	MoHuNVk6QTZ{N{K=
MV411 (B Myelomonocytic)	NIqySGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NYXtfJpPhjVizszN	MlzWSG1UVw>?	NF7jXnBKSzVyPUCuN\|Mh\|ryP	NWmz[pVROTl7OU[yO\|I>
MDA-PCa-2b	MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NIW4fmV,PSEQvF2=	MlXESG1UVw>?	NVzMWppsUUN3ME2wMlA6QCEQvF2=	Mn76NVk6QTZ{N{K=
LG	NY\DZndPT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MniwglUh\|ryP	NVe3V3pHTE2VTx?=	MYDJR\|UxRTBwMEO4JO69VQ>?	MWGxPVk6PjJ5Mh?=
RS411 (B cell precursor-ALL)	MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NWDqXmtwhjVizszN	MlzWSG1UVw>?	NH7qPItKSzVyPUCuNVAzKM7:TR?=	MlvzNVk6QTZ{N{K=
22-r-1	NGTxPVJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NVTqR5U5hjVizszN	MVXEUXNQ	NGDURnlKSzVyPUCuNVc2KM7:TR?=	NEnZNXYyQTl7NkK3Ni=>
5838	MkS2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M{PPPZ42KM7:TR?=	M4LOWWROW09?	NWfQWZFIUUN3ME2wMlA{PCEQvF2=	MojmNVk6QTZ{N{K=
P388 (Murine)	Mm\qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M4f6fZ42KM7:TR?=	NELHdlhFVVOR	MWPJR\|UxRTRwMkeg{txO	Mn3UNVk6QTZ{N{K=
A2780/S	M4\Ufmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NF\aOXN,PSEQvF2=	MYTEUXNQ	NVfIbY55UUN3ME2wMlEzOiEQvF2=	NH7LSmIyQTl7NkK3Ni=>
RDES	MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NYjZbJh7hjVizszN	M1fKRWROW09?	NI\Md\|JKSzVyPUCuNFEzKM7:TR?=	NVfSUFhIOTl7OU[yO\|I>
B6-T315I (Murine B-ALL)	NXLXe\|dNT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NHvle4p,PSEQvF2=	MnTOSG1UVw>?	MVXJR\|UxRTJwOEOg{txO	MkThNVk6QTZ{N{K=
TOV 112D	M{G0Z2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NXrzdVRqhjVizszN	M3;iZmROW09?	MWfJR\|UxRTJwMUS2JO69VQ>?	MonNNVk6QTZ{N{K=
TC32	M3fON2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MYL+OUDPxE1?	MX7EUXNQ	MoHETWM2OD1yLkCwPEDPxE1?	M2L2OFE6QTl4Mkey
HL60 (acute myelocytic)	MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NYHlXXhWhjVizszN	NXWweI1DTE2VTx?=	NFL2b4dKSzVyPUCuNVIh\|ryP	MmrPNVk6QTZ{N{K=
TOV 21G	MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MUT+OUDPxE1?	MoXLSG1UVw>?	MkTsTWM2OD12LkK3PUDPxE1?	MYWxPVk6PjJ5Mh?=
TC71	NGLs[VNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NFLZUXV,PSEQvF2=	MoXLSG1UVw>?	M1rM[GlEPTB;MD6wNVQh\|ryP	NFfoNFIyQTl7NkK3Ni=>
HPN-ALL (T-cell)	NV\5U4RGT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NEfFPFB,PSEQvF2=	MV7EUXNQ	NHzJZnZKSzVyPUCuOVIh\|ryP	NYOyZXpROTl7OU[yO\|I>
A2780R	MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M4n1bp42KM7:TR?=	NV3kOokzTE2VTx?=	MofCTWM2OD1zLkW2OEDPxE1?	NVrUR2lEOTl7OU[yO\|I>
Rh1	NFKwUpdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MoWwglUh\|ryP	NUGwcmtETE2VTx?=	MXPJR\|UxRTBwMEK3JO69VQ>?	NFfQOYIyQTl7NkK3Ni=>
Kasumi-1 (acute myeloid)	M4PWPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NX3aVGNwhjVizszN	M1;lTGROW09?	MVvJR\|UxRTBwMU[g{txO	NHHsd4EyQTl7NkK3Ni=>
sk-ov-3	MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NH\kVWV,PSEQvF2=	NX3Ze\|JWTE2VTx?=	NVjm[VBZUUN3ME21MlEh\|ryP	NGTjdVQyQTl7NkK3Ni=>
ME	M1zxc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	Mo[xglUh\|ryP	MUPEUXNQ	Mm\jTWM2OD1yLkCxOUDPxE1?	NIHhS5UyQTl7NkK3Ni=>
L1210 (Murine lymphocytic)	M3TDN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M3PTV542KM7:TR?=	NX63T3JvTE2VTx?=	NWnKb\|dNUUN3ME2yMlM6KM7:TR?=	MV:xPVk6PjJ5Mh?=
sw-626	MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NVXHNWlohjVizszN	MYPEUXNQ	MUTJR\|UxRTJwM{C2JO69VQ>?	M3y5OFE6QTl4Mkey
CTR	NYDwd4pJT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MkfSglUh\|ryP	MV\EUXNQ	M3;SPWlEPTB;MD6yOVMh\|ryP	MUOxPVk6PjJ5Mh?=
ML2 (Myelomonocytic)	NF\pN3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NUDiSHpihjVizszN	NGjneVdFVVOR	NU\1b4VFUUN3ME2wMlA6KM7:TR?=	MYmxPVk6PjJ5Mh?=
ovcar-3	M{HQZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NFj0b\|N,PSEQvF2=	NIfPNIdFVVOR	NEjJbo1KSzVyPUWg{txO	NXrJUFYzOTl7OU[yO\|I>
Rh36	NUSydopJT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MnPFglUh\|ryP	NFjvR4dFVVOR	M1jINWlEPTB;MT60N\|Ih\|ryP	NXHDbm54OTl7OU[yO\|I>
MOLM-13 (acute myeloid)	M3;DN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	Ml[wglUh\|ryP	Mk\0SG1UVw>?	M{fKOGlEPTB;MD60NkDPxE1?	MXqxPVk6PjJ5Mh?=
ovcar-4	M2LhOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MkntglUh\|ryP	Mkf2SG1UVw>?	NX\3em8xUUN3ME2xJO69VQ>?	NFe3Z3kyQTl7NkK3Ni=>
Rh41	NYqxNpg5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NUjaVZFVhjVizszN	MUXEUXNQ	M4nhSGlEPTB;MD6wNFUh\|ryP	MkjXNVk6QTZ{N{K=
Mutz 2 (acute myeloid)	MmCwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MVX+OUDPxE1?	NIjvdI9FVVOR	NUD2WJVzUUN3ME2xMlE2KM7:TR?=	NYHHNZJFOTl7OU[yO\|I>
ovcar-5	MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NInJZ2R,PSEQvF2=	MoK3SG1UVw>?	NH7LO5lKSzVyPUCuNFUh\|ryP	NVzzS3RWOTl7OU[yO\|I>
RD1	NEnEflJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NIWxR4R,PSEQvF2=	M13HZ2ROW09?	MkWxTWM2OD1yLkC2PEDPxE1?	NXnZPIpIOTl7OU[yO\|I>
OCI-AML 2 (acute myeloid)	MnjjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MYf+OUDPxE1?	M4HQTGROW09?	MnzITWM2OD1\|LkOzJO69VQ>?	Mn7QNVk6QTZ{N{K=
786-O	NX3Fb25ET3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M4PhVp42KM7:TR?=	M3PibWROW09?	NH;xbHdKSzVyPUGuOlQ4KM7:TR?=	MmrSNVk6QTZ{N{K=
A673	NVW4cHpTT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NFTaRZB,PSEQvF2=	NXy4PHhXTE2VTx?=	MVrJR\|UxRTBwNEC4JO69VQ>?	NVu2e3UyOTl7OU[yO\|I>
TALL-1 (T-cell)	MmD1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	Mo[0glUh\|ryP	M13vc2ROW09?	M{C2bmlEPTB;MT6yPEDPxE1?	MWexPVk6PjJ5Mh?=
151-B	MnjuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NXu4NoZ2hjVizszN	NILuNHBFVVOR	Mm\YTWM2OD1{Lk[3JO69VQ>?	NEXycnoyQTl7NkK3Ni=>
PFSK-1	MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M1:wOp42KM7:TR?=	M3nxOGROW09?	NX7IUYJTUUN3ME2wMlE{OiEQvF2=	MVmxPVk6PjJ5Mh?=
THP-1	NFj6PG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MnrxglUh\|ryP	NVztfmw1TE2VTx?=	M1izdGlEPTB;Nj61PEDPxE1?	NFjMPZUyQTl7NkK3Ni=>
HEK293	NXfHWmQ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M2naUZ42KM7:TR?=	MlfSSG1UVw>?	M4T3fGlEPTB;MD65NVUh\|ryP	MYqxPVk6PjJ5Mh?=
DAOY	NX3qcGM6T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MUH+OUDPxE1?	M3PQbmROW09?	NWW2[YlkUUN3ME2xMlk4QSEQvF2=	NX35SYZOOTl7OU[yO\|I>
SET2	MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NEHnTlh,PSEQvF2=	Mnv0SG1UVw>?	NUfvbmZuUUN3ME2wMlI6QCEQvF2=	M{HMU\|E6QTl4Mkey
HTB-46	M13Re2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MmTCglUh\|ryP	NXm2N3JDTE2VTx?=	M3X0OGlEPTB;NT6yOUDPxE1?	NUXTNnVxOTl7OU[yO\|I>
SK-NAS	NWnuc5Z1T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MmfRglUh\|ryP	MYDEUXNQ	NXHtSIppUUN3ME2wMlQ6PyEQvF2=	NEL5epUyQTl7NkK3Ni=>
CTLL2	M1ntOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NX3wOFBRhjVizszN	M4\x[WROW09?	M4PXPGlEPTB-MT6wNEDPxE1?	NIfBSIcyQTl7NkK3Ni=>
HTB-47	Mke4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MlXhglUh\|ryP	MVPEUXNQ	MkHxTWM2OD1{LkC1OkDPxE1?	NVG5TZB[OTl7OU[yO\|I>
LAN-1	MlvUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NV3POpBNhjVizszN	NVPlU5R4TE2VTx?=	NYDme41pUUN3ME2wMlA1KM7:TR?=	MYCxPVk6PjJ5Mh?=
ST486	M{\jUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M2DvXp42KM7:TR?=	NF7QcJVFVVOR	NEH6TXlKSzVyPUGuNVkh\|ryP	NXXpbGtpOTl7OU[yO\|I>
HS766T	MmfzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M2\qV542KM7:TR?=	NVPh[YR[TE2VTx?=	NGnJW\|FKSzVyPUKuNFAyKM7:TR?=	M4jzcFE6QTl4Mkey
IMR-32	NGGxZm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NIjoO\|B,PSEQvF2=	MV;EUXNQ	MXrJR\|UxRTBwMk[xJO69VQ>?	M3zycFE6QTl4Mkey
Daudi (Burkitt's)	M1HFOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MVj+OUDPxE1?	Ml3VSG1UVw>?	M3nsOmlEPTB;Mj62N\|ch\|ryP	MVWxPVk6PjJ5Mh?=
Aspc-1	Mk\jS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1\WNJ42KM7:TR?=	NXrOVI5xTE2VTx?=	NVXlW41kUUN3ME2wMlM4QSEQvF2=	M3ixTlE6QTl4Mkey
SK-NSH	Mn7hS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MWf+OUDPxE1?	M3;ldmROW09?	NUn4Z\|Y6UUN3ME2wMlE{QSEQvF2=	Mm\NNVk6QTZ{N{K=
MEC-1 (Chronic B cell)	M{S4fGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MWj+OUDPxE1?	NF3xUHlFVVOR	NIm5WI9KSzVyPUKuOlM4KM7:TR?=	M3GzTVE6QTl4Mkey
Capan-2	NF30d5lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MkPlglUh\|ryP	M1fneGROW09?	MYHJR\|UxRTFwN{e0JO69VQ>?	MkXGNVk6QTZ{N{K=
SHSY5Y	MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	Mn\GglUh\|ryP	MY\EUXNQ	NVrLOVlNUUN3ME2wMlExPiEQvF2=	NFry[mwyQTl7NkK3Ni=>
U937 (Histioocytic)	MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M2W0dZ42KM7:TR?=	M3LGPGROW09?	MoT1TWM2OD53LkCwJO69VQ>?	NU\kTWt4OTl7OU[yO\|I>
Bxpc-1	NHTrdopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NEXpPZJ,PSEQvF2=	M1LmSGROW09?	NIjHSoZKSzVyPUGuPVI1KM7:TR?=	MWSxPVk6PjJ5Mh?=
Bxpc-3	NE\D[mtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MofrglUh\|ryP	NFHyR41FVVOR	MY\JR\|UxRjVwMECg{txO	MV2xPVk6PjJ5Mh?=
HTB-92	M1PHOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NXq2cGtxhjVizszN	NITmcppFVVOR	Mo\xTWM2OD1zLkCyJO69VQ>?	M4\afFE6QTl4Mkey
OCI-LY10 (B-cell)	MmjnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MXP+OUDPxE1?	NHLYZWdFVVOR	M3PUOGlEPTB;MD60OUDPxE1?	Mnr4NVk6QTZ{N{K=
PANC-1	MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NWPNR2RQhjVizszN	NXrL[pA2TE2VTx?=	NXm5WWNbUUN3ME61MlAxKM7:TR?=	NELVO2wyQTl7NkK3Ni=>
To184.T	MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MWL+OUDPxE1?	NGXTfIJFVVOR	MmDkTWM2OD1yLkS2PUDPxE1?	MlLUNVk6QTZ{N{K=
OCI-LY19 (B-cell)	NGnjVWNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MVf+OUDPxE1?	NGXLfXZFVVOR	NELmc2dKSzVyPUCuOEDPxE1?	MkK3NVk6QTZ{N{K=
PANC-1 BM	NFixdFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NIfMcIZ,PSEQvF2=	M{PXOmROW09?	MV;JR\|UxRjVwMECg{txO	MkDENVk6QTZ{N{K=
SA-4	NIrqfoRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M{ixc542KM7:TR?=	NWL1NmIyTE2VTx?=	M4fkbWlEPTB;MT6zNFEh\|ryP	MX[xPVk6PjJ5Mh?=
RPMI 8226	Mo\qS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NIHNcmh,PSEQvF2=	MoXISG1UVw>?	Mo\XTWM2OD1zLkK5N{DPxE1?	NXfYbpFWOTl7OU[yO\|I>
HPAF-II	MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M1PS[542KM7:TR?=	M3HIcGROW09?	NGD4cHFKSzVyPUCuOlQ1KM7:TR?=	NHTZenoyQTl7NkK3Ni=>
SHP-77	MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MWj+OUDPxE1?	Ml;jSG1UVw>?	MV;JR\|UxRTFwOEi4JO69VQ>?	NXTiXYtHOTl7OU[yO\|I>
U266 B1	NYHVd2J5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NETye2p,PSEQvF2=	MmG4SG1UVw>?	NISzSYpKSzVyPUGuOlY6KM7:TR?=	Mmf3NVk6QTZ{N{K=
Hs700t	NXnO[lNET3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M1fEfp42KM7:TR?=	NIT4WWxFVVOR	NH[xOJFKSzVyPUCuNlMyKM7:TR?=	NEHqTVIyQTl7NkK3Ni=>
NCI-446	NETCPYFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NVTBb4o5hjVizszN	M1Pm[WROW09?	NYrkT5dNUUN3ME2xMlE2PCEQvF2=	M{XkeVE6QTl4Mkey
H929	M3\p[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NWrs[3RlhjVizszN	NH;6SpBFVVOR	NV;vfpJwUUN3ME2wMlAyPCEQvF2=	NFTo[WIyQTl7NkK3Ni=>
PL45	MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M4Tmb542KM7:TR?=	M{HJdmROW09?	MYTJR\|UxRTJwMkW1JO69VQ>?	MYixPVk6PjJ5Mh?=
NCI-H383	M{PvcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NIPJTIx,PSEQvF2=	NXHVZlloTE2VTx?=	NHHMU4dKSzVyPkWuNFAh\|ryP	NHzhd\|QyQTl7NkK3Ni=>
JJN3	NVXyZ3dQT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NFrDeHZ,PSEQvF2=	NGntW4RFVVOR	NXXaOo1LUUN3ME2yMlQ{OyEQvF2=	M3vCUVE6QTl4Mkey
SU.86.86	M1PtVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MmDEglUh\|ryP	M1LYXWROW09?	MnO5TWM2OD1{Lk[3NkDPxE1?	NI[zdnYyQTl7NkK3Ni=>
H1299	NFrES4JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NUjxe2NGhjVizszN	NVzaNpExTE2VTx?=	NV3wSGJJUUN3ME61MlAxKM7:TR?=	NIjGXlEyQTl7NkK3Ni=>
MDA-MB-468	M1XZPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MnPhglUh\|ryP	MVfEUXNQ	MnrqTWM2OD1yLkWwOEDPxE1?	M3TaTFE6QTl4Mkey
SW1990	MmrSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MlHzglUh\|ryP	NIXweINFVVOR	MmDuTWM2OD1yLkiyOkDPxE1?	NGmwbmkyQTl7NkK3Ni=>
Calu-6	M37kdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NWfTO3Q4hjVizszN	MUfEUXNQ	MkXUTWM2OD53LkCwJO69VQ>?	MnfhNVk6QTZ{N{K=
MDA-MB-231	M{PtNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MonuglUh\|ryP	M1juVmROW09?	MXfJR\|UxRTFwNkS4JO69VQ>?	Mnr2NVk6QTZ{N{K=
SW-684	MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M4qwW542KM7:TR?=	MoDRSG1UVw>?	M1\FNGlEPTB-NT6wNEDPxE1?	MknmNVk6QTZ{N{K=
H209	MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MnLqglUh\|ryP	NHzyOmlFVVOR	MVHJR\|UxRTFwMUmzJO69VQ>?	MUexPVk6PjJ5Mh?=
MDA-MB-231T	MmXIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NFTJdWd,PSEQvF2=	MXfEUXNQ	M1nNTWlEPTB-NT6wNEDPxE1?	MVSxPVk6PjJ5Mh?=
HT1080/S	MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	Mke0glUh\|ryP	MmHVSG1UVw>?	MWnJR\|UxRTBwNUOxJO69VQ>?	MkLzNVk6QTZ{N{K=
H526 0.044	MoHIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1\2XJ42KM7:TR?=	NVH3WWNnTE2VTx?=	M3jVN2lEPTB;MD6wOFQh\|ryP	M1[3NVE6QTl4Mkey
DU4475 2.431	MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MUX+OUDPxE1?	NYnZeZg{TE2VTx?=	M{DxUmlEPTB;Mj60N\|Eh\|ryP	MmD2NVk6QTZ{N{K=
HCT116	NXPiPY9iT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MoHvglUh\|ryP	NX\r[ZU1TE2VTx?=	M37KN2lEPTB;MD64OVIh\|ryP	MV[xPVk6PjJ5Mh?=
M109	MkPHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MoLFglUh\|ryP	NUPBNZBjTE2VTx?=	NYmwd2tVUUN3ME2xMlA2PSEQvF2=	MofONVk6QTZ{N{K=
BT549	NWe4RWNzT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWrsSodShjVizszN	MV\EUXNQ	NVnHPWlZUUN3ME2xMlY1PSEQvF2=	M37OdlE6QTl4Mkey
HCT116/VM46	MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M4Xudp42KM7:TR?=	M3OyOGROW09?	M2PaW2lEPTB;MT63NFIh\|ryP	MX2xPVk6PjJ5Mh?=
H460	NHra[JhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MYT+OUDPxE1?	M4PmcGROW09?	NXe4WYZKUUN3ME2wMlc6PSEQvF2=	Mn72NVk6QTZ{N{K=
MCF-7	NVTHfmM6T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MonUglUh\|ryP	NH;QS2NFVVOR	NWrxUoZLUUN3ME2wMlAyPiEQvF2=	NYK3Z3FNOTl7OU[yO\|I>
GEO	NX;RU49kT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M2TvTJ42KM7:TR?=	NVOzbXpFTE2VTx?=	NXvYXlRDUUN3ME2wMlM2PiEQvF2=	MX2xPVk6PjJ5Mh?=
H441 0.646	M{HSV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NWLvbnJnhjVizszN	MkHNSG1UVw>?	MVHJR\|UxRTBwNkS2JO69VQ>?	NWXLSGJ7OTl7OU[yO\|I>
MCF-7-807R	MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NXHNXIo{hjVizszN	NEnsOlVFVVOR	MkfPTWM2OD1yLkS5JO69VQ>?	MlrNNVk6QTZ{N{K=
Colo205	NUHPN4hrT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M4nFbZ42KM7:TR?=	MknySG1UVw>?	M{P4T2lEPTB;MD6xNFQh\|ryP	MUixPVk6PjJ5Mh?=
H292	MkTYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NV2zS4NDhjVizszN	NUfLRlB2TE2VTx?=	NE\XdXhKSzVyPUCuO\|g5KM7:TR?=	MkLPNVk6QTZ{N{K=
BT474 (S)	NVLRclJ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MYj+OUDPxE1?	MYjEUXNQ	MlPSTWM2OD1{LkSwN{DPxE1?	MkG1NVk6QTZ{N{K=
HT-29	MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NFjtdXB,PSEQvF2=	NFj0cVhFVVOR	M1HDWmlEPTB;Mj6xNFMh\|ryP	MoXPNVk6QTZ{N{K=
A549	NWHpNVhUT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWfQfmo5hjVizszN	NHu1enRFVVOR	NW\Lb29LUUN3ME2wMlY4PSEQvF2=	M{HteVE6QTl4Mkey
BT474-M1	M1zsRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NWfydWxbhjVizszN	MX;EUXNQ	NVK4boJTUUN3ME2yMlM3PSEQvF2=	M1zQVFE6QTl4Mkey
SW480	MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MlS3glUh\|ryP	M2PwVmROW09?	M3j2PWlEPTB-NT6wNEDPxE1?	NXjJXVNHOTl7OU[yO\|I>
L2987	NUPJR3JFT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MkfMglUh\|ryP	NF3YRnlFVVOR	M2X3eGlEPTB;MD60OFIh\|ryP	NIXnOFIyQTl7NkK3Ni=>
AU565	NGnXTo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MmHEglUh\|ryP	MWXEUXNQ	NXqwbJJDUUN3ME20Mlk4KM7:TR?=	MkfQNVk6QTZ{N{K=
SW403	MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NV7WUmpNhjVizszN	MkPxSG1UVw>?	NFnGNZZKSzVyPUCuNlIh\|ryP	M2DCS\|E6QTl4Mkey
H1437	MlnVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NWTKTZJZhjVizszN	M4H4RWROW09?	M4C4b2lEPTB;MD61NlMh\|ryP	NFexb3kyQTl7NkK3Ni=>
BT-20	MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NIDJVmd,PSEQvF2=	M{POfmROW09?	NV\oO3Q1UUN3ME2zMlU3OiEQvF2=	NEHxTG8yQTl7NkK3Ni=>
Colo320HSR	NY\UOXFJT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MoLLglUh\|ryP	MkDVSG1UVw>?	M1:0PWlEPTB;MD6wNVEh\|ryP	M4HKWFE6QTl4Mkey
H2087	NG\S[\|VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NXnZdpQyhjVizszN	NHywVVlFVVOR	NF3VZodKSzVyPkGuNFAh\|ryP	NEPq[YMyQTl7NkK3Ni=>
HCC1419	M1znTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NX7oZ2JwhjVizszN	MXXEUXNQ	MWfJR\|UxRTJwNUG3JO69VQ>?	NWXNXWZCOTl7OU[yO\|I>
WiDr	NFfKcJJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M1LabJ42KM7:TR?=	MXPEUXNQ	M{O3c2lEPTB;MD6wO\|Yh\|ryP	NH3odWUyQTl7NkK3Ni=>
H661 0.573	NGfn[HZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M2fU[p42KM7:TR?=	M3XITGROW09?	M4H2VmlEPTB;MD61O\|Mh\|ryP	MX:xPVk6PjJ5Mh?=
HCC-38	MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NGK5e4R,PSEQvF2=	M4nlNGROW09?	M{XnRmlEPTB-NT6wNEDPxE1?	MlTGNVk6QTZ{N{K=
LS174T	NGLneplIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NXq4fGNlhjVizszN	M3PxdWROW09?	NHLsSmZKSzVyPUCuOVM2KM7:TR?=	MljQNVk6QTZ{N{K=
H211	MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MWX+OUDPxE1?	MXHEUXNQ	NXzMOVk6UUN3ME2wMlc{OyEQvF2=	M3XSclE6QTl4Mkey
HCC70	NGrCW\|VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MoKxglUh\|ryP	MlXoSG1UVw>?	NWL6SYg4UUN3ME2xMlU2KM7:TR?=	NEXyN2wyQTl7NkK3Ni=>
SW116	NVP1VFh[T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M2S5c542KM7:TR?=	MVjEUXNQ	MX3JR\|UxRTBwME[3JO69VQ>?	NV3SfWNZOTl7OU[yO\|I>
H513	MoXYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NVO2Z21NhjVizszN	M{XGbGROW09?	NVTab29kUUN3ME20MlQ1QCEQvF2=	MkO0NVk6QTZ{N{K=
MDA-MB-157	M4XRR2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MWr+OUDPxE1?	NWrQd5BsTE2VTx?=	NFrNbVlKSzVyPUCuNFM3KM7:TR?=	MmjmNVk6QTZ{N{K=
H2052	NX3IZWNrT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NGW2VYN,PSEQvF2=	MWTEUXNQ	NYnT[GZzUUN3ME2xMlA2KM7:TR?=	M{nqdlE6QTl4Mkey
MDA-MB-415	M{PtZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M2\zVJ42KM7:TR?=	NXi1flU5TE2VTx?=	MVvJR\|UxRjVwMECg{txO	MYKxPVk6PjJ5Mh?=
DLD-1	NVTtOXhzT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NXTjPHJGhjVizszN	MkDtSG1UVw>?	MY\JR\|UxRTBwOUC5JO69VQ>?	NH;hOG0yQTl7NkK3Ni=>
H2595	NIDOUpVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M{Ltep42KM7:TR?=	MXrEUXNQ	NXrYPGdkUUN3ME20MlQ4PSEQvF2=	MmewNVk6QTZ{N{K=
MDA-MB-435S	NUmwb3F5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M1HPOp42KM7:TR?=	M2O4NGROW09?	NUf4cnM2UUN3ME2xMlg3QSEQvF2=	MmC0NVk6QTZ{N{K=
HCT15	MoLwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1LiSZ42KM7:TR?=	Mm\oSG1UVw>?	MV;JR\|UxRjFwMECg{txO	MVqxPVk6PjJ5Mh?=
SK-Hep1	NXizTFM4T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NVfQTohvhjVizszN	NYP1bXFUTE2VTx?=	MUXJR\|UxRTBwMUS2JO69VQ>?	NETxU\|kyQTl7NkK3Ni=>
MDA-MB-436	NE\1fJNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NW[ydIRqhjVizszN	MnezSG1UVw>?	NWrjc3hPUUN3ME21MlUxOiEQvF2=	MVixPVk6PjJ5Mh?=
KM12C	NYfOdopTT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M3jJZ542KM7:TR?=	MXnEUXNQ	MXPJR\|UxRTBwMEW0JO69VQ>?	NYHNdJR3OTl7OU[yO\|I>
HEPG2	NYjV[JZ[T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWn4UJpLhjVizszN	M2fkd2ROW09?	MV\JR\|UxRTBwMEK1JO69VQ>?	M{\FcVE6QTl4Mkey
MDA-MB-453	MkPOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NELOdoF,PSEQvF2=	MmKwSG1UVw>?	MXnJR\|UxRTFwOE[5JO69VQ>?	M3LVXVE6QTl4Mkey
KM12SM	MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NV7WW4l{hjVizszN	NHXNWnhFVVOR	M4PMNmlEPTB;MD6wOVkh\|ryP	M3LPTVE6QTl4Mkey
1483	M4jxe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NITXOpV,PSEQvF2=	NYLsb3RxTE2VTx?=	M4O1TmlEPTB;Mj6xPUDPxE1?	MYixPVk6PjJ5Mh?=
Hs578t	MnTXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M3LUb542KM7:TR?=	MYLEUXNQ	MV\JR\|UxRTFwMki3JO69VQ>?	MVexPVk6PjJ5Mh?=
LS180	NHTncmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M3zibZ42KM7:TR?=	MUHEUXNQ	M4P4SmlEPTB;MD62PVYh\|ryP	M{fwdlE6QTl4Mkey
FaDu	MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MoW2glUh\|ryP	Mk\ySG1UVw>?	MV;JR\|UxRTFwMkeg{txO	MnnPNVk6QTZ{N{K=
ZR-75-1	MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M4H4bZ42KM7:TR?=	NHPxWWtFVVOR	NVjiPHFJUUN3ME2yMlA5PCEQvF2=	MW[xPVk6PjJ5Mh?=
LS513	MmrmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MnjJglUh\|ryP	MYnEUXNQ	MUfJR\|UxRTBwMUO1JO69VQ>?	NGnSUVUyQTl7NkK3Ni=>
Detroit.562	M4n1N2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M3TLV542KM7:TR?=	NVfhVXl3TE2VTx?=	MXHJR\|UxRTFwMUSg{txO	MkSyNVk6QTZ{N{K=
ZR-75-30	MlTES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MV7+OUDPxE1?	NF7XOpFFVVOR	MVLJR\|UxRjVwMECg{txO	M{XoUlE6QTl4Mkey
RKO-PM	NHfqTVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NHuyTnR,PSEQvF2=	MljVSG1UVw>?	NVzJW4tWUUN3ME2wMlI{OiEQvF2=	M3jQ[VE6QTl4Mkey
Cal.27	MmjnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MUD+OUDPxE1?	M{nTSWROW09?	M2nEd2lEPTB;MjFOwG0>	MoHXNVk6QTZ{N{K=
KPL4	M3ixb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M{HRTZ42KM7:TR?=	NEnPNZZFVVOR	MVjJR\|UxRTFwMkWyJO69VQ>?	MYWxPVk6PjJ5Mh?=
PKO-RM13	M4PDSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NEf0dYx,PSEQvF2=	NFWybGJFVVOR	NETWV5JKSzVyPUCuOFI2KM7:TR?=	NXjm[VRWOTl7OU[yO\|I>
HS.53.T	MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MX\+OUDPxE1?	M3rOOWROW09?	M1;XeGlEPTB;MD63PUDPxE1?	MkDKNVk6QTZ{N{K=
EMT6	MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M3vL[J42KM7:TR?=	M3exNWROW09?	M{fyWGlEPTB;MD64NFYh\|ryP	M1i2bFE6QTl4Mkey
SNU-C1	NVH0PZYzT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M4r1dZ42KM7:TR?=	NEfROYxFVVOR	MWfJR\|UxRTBwMEC3JO69VQ>?	NWPrUphUOTl7OU[yO\|I>
SQCCY1	M{[y[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NXXyXYU4hjVizszN	M2G0XGROW09?	NEXoc5FKSzVyPUCuO\|kh\|ryP	NFn4e5IyQTl7NkK3Ni=>
SW480	NHnwdG5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NX61WpA5hjVizszN	NFPMdldFVVOR	NIHu[GxKSzVyPUCuNFM4KM7:TR?=	M2jyZVE6QTl4Mkey
SCC9	NXT4ZnlsT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NYTZfXNOhjVizszN	NWDOUVlPTE2VTx?=	M4nH[mlEPTB;MD63OUDPxE1?	MY[xPVk6PjJ5Mh?=
SK-LMS-1	NH\ObYdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M3L0Tp42KM7:TR?=	M2Hv[mROW09?	MnzkTWM2OD1yLk[4O{DPxE1?	NIXzTHQyQTl7NkK3Ni=>
SCC25	NVTYblUyT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MW\+OUDPxE1?	NXGwO4s3TE2VTx?=	M4\sN2lEPTB;MD62PEDPxE1?	MUOxPVk6PjJ5Mh?=
U87	MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MVT+OUDPxE1?	MXXEUXNQ	MV\JR\|UxRTBwOUWg{txO	NUDRV4xLOTl7OU[yO\|I>
SCC15	MmHMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MlSzglUh\|ryP	MlvCSG1UVw>?	MoDvTWM2OD1yLk[3JO69VQ>?	MkPLNVk6QTZ{N{K=
T98G	NXnEbW1zT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWnlc3ByhjVizszN	Mlj5SG1UVw>?	M{TZXmlEPTB;MT6yNVgh\|ryP	MWexPVk6PjJ5Mh?=
SCC4	NGrBXodIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MUn+OUDPxE1?	M2DYTmROW09?	MnLTTWM2OD1yLk[zJO69VQ>?	NFPUNWYyQTl7NkK3Ni=>
U118	MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NF7VdWp,PSEQvF2=	NWC4fXNpTE2VTx?=	M1PGS2lEPTB;MT62NVgh\|ryP	M4OwTVE6QTl4Mkey
TU167	NHH4S3BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MmnhglUh\|ryP	MmrjSG1UVw>?	MlXHTWM2OD12LkWyJO69VQ>?	NIHlfXcyQTl7NkK3Ni=>
NCI-H727	M4K0Tmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MnfGglEx6oDMzszN	NISxbGNFVVOR	MnPQTWM2OD12Mkigcm0>	M4Dhb\|IxOzh3N{S3
NCI-H720	M2fTPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NEnJWIV,OTEkgJtOwG0>	MnT0SG1UVw>?	MXvJR\|UxRTJwODFOwG0>	M3rXdFIxOzh3N{S3
NCI-H835	NFHIR4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NVHJSYxGhjFy4pEK{txO	MnnoSG1UVw>?	MXHJR\|UxRTFizszN	MUWyNFM5PTd2Nx?=
NCI-H727	NFPlXY5McW6jc3WgZZN{[Xl?	MnvWglEx6oDMzszN	NHf3fHBFVVOR	MVTpcohq[mm2czDjc45{fGm2dYTpeoUhUUeIMWKgZZV1d3Cqb4PwbI9zgWyjdHnvci=>	MYmyNFM5PTd2Nx?=
RD	Mn;SS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MneyglEx6oDMzszN		MXzJR\|UxRTFwMUKgxtVO	MoDlNlEzQTh5NEW=
Rh41	NYTwZlBbT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MmHiglEx6oDMzszN		NEPzcoZKSzVyPUCuNFchyrWP	MVWyNVI6QDd2NR?=
Rh18	NFXFboNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MlLDglEx6oDMzszN		NUjkSW04UUN3ME20Mlk3KML3TR?=	M2\ZZlIyOjl6N{S1
Rh30	NVnNcpV5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NVO5fGN4hjFy4pEK{txO		NVzMVFRIUUN3ME2wMlE6KML3TR?=	NFviUXczOTJ7OEe0OS=>
BT-12	NITvdlFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MYT+NVDjiIsQvF2=		M2K1TmlEPTB;MD63PEDDvU1?	MYGyNVI6QDd2NR?=
CHLA-266	Mo\IS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MoDtglEx6oDMzszN		MWTJR\|UxRTBwOEmgxtVO	M1rmVVIyOjl6N{S1
TC-71	MnX0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MYr+NVDjiIsQvF2=		MYPJR\|UxRTBwMUGgxtVO	MYeyNVI6QDd2NR?=
CHLA-9	NH:xW2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MUD+NVDjiIsQvF2=		NHH2UopKSzVyPUCuNVIhyrWP	MXmyNVI6QDd2NR?=
CHLA-10	MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NFrjcpJ,OTEkgJtOwG0>		NEO2TVVKSzVyPUCuOlIhyrWP	Mn7CNlEzQTh5NEW=
CHLA-258	M3\nXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MVL+NVDjiIsQvF2=		M2DEbWlEPTB;MD6yO{DDvU1?	NYjFR\|ZqOjF{OUi3OFU>
GBM2	MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M3ry[Z4yOOLCit88US=>		MUnJR\|UxRTFwNEegxtVO	MXiyNVI6QDd2NR?=
NB-1643	NHzmSHlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MlfOglEx6oDMzszN		NGXzSVRKSzVyPUCuNVIhyrWP	NWjROYd[OjF{OUi3OFU>
NB-EBc1	M4TmW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NUDue2tXhjFy4pEK{txO		NIqwc5pKSzVyPUCuN\|UhyrWP	NVvNV3Q6OjF{OUi3OFU>
CHLA-90	MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M3L6XJ4yOOLCit88US=>		Mn;6TWM2OD1yLke3JOK2VQ>?	NGi2TVMzOTJ7OEe0OS=>
CHLA-136	MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NVnVWHA5hjFy4pEK{txO		NVH6dZNCUUN3ME2wMlUzKML3TR?=	MkfqNlEzQTh5NEW=
NALM-6	NWTlblZvT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MlzBglEx6oDMzszN		MWXJR\|UxRTBwNEmgxtVO	M13ISFIyOjl6N{S1
COG-LL-317	M13GeWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NVjZ[nhZhjFy4pEK{txO		MWLJR\|UxRTFwM{igxtVO	M3TIblIyOjl6N{S1
RS4;11	NYjjOVZIT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MmX3glEx6oDMzszN		M2TCcmlEPTB;MD6zPEDDvU1?	MomyNlEzQTh5NEW=
MOLT-4	NH3M[FdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NEexOHF,OTEkgJtOwG0>		NImxWXpKSzVyPUCuOVMhyrWP	NE[2TpIzOTJ7OEe0OS=>
CCRF-CEM	NXLWfFdvT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NEDiZmF,OTEkgJtOwG0>		NVPUUVMzUUN3ME2xMlE{KML3TR?=	NWjTPIw{OjF{OUi3OFU>
Kasumi-1	M33KUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MoK4glEx6oDMzszN		M1\VcWlEPTB;MT6yJOK2VQ>?	M1\ZfVIyOjl6N{S1
Karpas-299	M3rGeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MX3+NVDjiIsQvF2=		NYDRWVVZUUN3ME2xMlY1KML3TR?=	NXfBRY81OjF{OUi3OFU>
Ramos-RA1	NUWxPJU5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWHnfoZnhjFy4pEK{txO		NFLtU2FKSzVyPUGuN\|EhyrWP	NF[2[3UzOTJ7OEe0OS=>
Rh30	M{H3NGZ2dmO2aX;uJIF{e2G7			M2X6colv\HWlZYOgZY4hcW6lcnXhd4Uhd2ZiU1\LJJBpd3OyaH;yfYxifGmxbh?=	MX2yOVkzPTN5OB?=
Rh41	NXrUXlJnTnWwY4Tpc44h[XO\|YYm=			NHrtcpVqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:\|cHjvdplt[XSrb36=	Mn:zNlU6OjV\|N{i=
RD	NV:yfo9JTnWwY4Tpc44h[XO\|YYm=			Mn[4bY5lfWOnczDhckBqdmO{ZXHz[UBw\iCVRlugdIhwe3Cqb4L5cIF1cW:w	M3PDNFI2QTJ3M{e4
A549	NVnWZXhOU2mwYYPlJIF{e2G7	M3r2R\|AvPeLCit88US=>	NUWwVHBRTE2VTx?=	MV3pcohq[mm2czDJS2YuUVJxSWKgZYN1cX[jdHnvci=>	MX[yOlkzQDV5OB?=
NCI-H358	NI[wenNMcW6jc3WgZZN{[Xl?	MYGwMlXjiIsQvF2=	MWTEUXNQ	NYOxbm91cW6qaXLpeJMhUUeILVnSM2lTKGGldHn2ZZRqd25?	M3XXPFI3QTJ6NUe4
A549	MUjGeY5kfGmxbjDhd5NigQ>?	NV;4Opl3OC534pEK{txO	NXuyU29jTE2VTx?=	MoTtZ4F2e2W\|IHGgZ49v[3W{cnXueEBl\WO{ZXHz[UBqdiCyaH;zdIhwenmuYYTl[EBCU1RiYX7kJGVTUw>?	MXOyOlkzQDV5OB?=
NCI-H358	NUK1enJGTnWwY4Tpc44h[XO\|YYm=	NGDOZnExNjYkgJtOwG0>	M4rWdWROW09?	MXfjZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM	NXfxT3VCOjZ7Mki1O\|g>
A549	NFPGbZdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NV[2PYxJhjFy4pEK{txO	NInhRotFVVOR	M37iT2lEPTB;MD63OkDPxE1?	MX6yOlkzQDV5OB?=
NCI-H358	MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M1O3Sp4yOOLCit88US=>	MUTEUXNQ	NIjUR2NKSzVyPUGuNFkh\|ryP	Mom5NlY6Ojh3N{i=
A549	NFS4[3BCeG:ydH;zbZMh[XO\|YYm=	NF:zZ3IxNjYkgJtOwG0>	NWXX[ZVpTE2VTx?=	NXzEcZF7cW6mdXPld{BCeG:ydH;zbZM>	NH;FdGIzPjl{OEW3PC=>
NCI-H358	NITMcXhCeG:ydH;zbZMh[XO\|YYm=	MmruNE426oDMzszN	MVvEUXNQ	NYjIT3k6cW6mdXPld{BCeG:ydH;zbZM>	M2TyWlI3QTJ6NUe4
A549	NYDLdZRNTnWwY4Tpc44h[XO\|YYm=	MnzGNE426oDMzszN	NX;MUphWTE2VTx?=	NUDFS5JmemWmdXPld{B4d3WwZDDjcI9{fXKn	NY\PXHh[OjZ7Mki1O\|g>
NCI-H358	M1LwemZ2dmO2aX;uJIF{e2G7	MVSwMlXjiIsQvF2=	M2PIOGROW09?	Mo\TdoVlfWOnczD3c5Vv\CClbH;zeZJm	M1HwbVI3QTJ6NUe4

... 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 Neuro Oncol (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 Molecules 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]	- Collapse 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 K_m 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]	- Collapse 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]	- Collapse Animal Models: IGF-1R-Sal, GEO, Colo205, JJN3, RD1 or Rh41 tumor–bearing nude mice Dosages: 150 mg/kg Administration: Orally (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	92 mg/mL (199.35 mM)
	Ethanol	92 mg/mL (199.35 mM)
	Water	Insoluble
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 Download BMS-754807 SDF

Molecular Weight	461.49
Formula	C₂₃H₂₄FN₉O
CAS No.	1001350-96-4
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CC1(CCCN1C2=N[N]3C=CC=C3C(=N2)NC4=N[NH]C(=C4)C5CC5)C(=O)NC6=CC=C(F)N=C6

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，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.

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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.

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IGF-1R Signaling Pathway Map

IGF-1R Inhibitors with Unique Features

Selective IGF-1R Inhibitor

NVP-AEW541 : IGF-1R-selective, IC50=86 nM.
IGF-1R Inhibitor in Clinical Trial

OSI-906 (Linsitinib) : Phase II for Advanced Solid Tumors.
Newest IGF-1R Inhibitor

PQ 401 : Inhibitor of autophosphorylation of IGF-1R domain with IC50 of <1 μM.
Classic IGF-1R Inhibitor

BMS-536924 : ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.

Related IGF-1R Products

Picropodophyllin (PPP) ^New

Picropodophyllin (PPP) is a IGF-1R inhibitor with IC50 of 1 nM. It displays selectivity for IGF-1R and does not coinhibit tyrosine phosphorylation the IR, or of a selected panel of receptors less related to IGF-IR(FGF-R, PDGF-R, OR EGF-R).
Erlotinib ^New

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Bemcentinib（R428) ^New

R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).
BMS-536924

BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.
NVP-AEW541

NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, greater potency and selectivity for IGF-1R in a cell-based assay.
NVP-ADW742

NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
Linsitinib (OSI-906)

Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.
GSK1904529A

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM in cell-free assays, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.
AG-1024

AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).
PQ 401

PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.

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BMS-754807