BMS-754807

Name: BMS-754807
Brand: Selleck Chemicals
SKU: S1124
Rating: 5 (33 reviews)

For research use only.

Catalog No.S1124

33 publications

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.

Selleck's BMS-754807 has been cited by 33 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 )

Sci Signal, 2020, 26;13(633):eaba3176

PubMed: 32457113 ( click the link to review the publication )

Cancers (Basel), 2020, 12(12)E3717

PubMed: 33322337 ( click the link to review the publication )

Cancers (Basel), 2020, 27;12(5)pii: E1087

PubMed: 32349331 ( click the link to review the publication )

Cancers (Basel), 2020, 13;12(2) pii: E436

PubMed: 32069833 ( click the link to review the publication )

Mol Neurobiol, 2020, 57(3):1570-1593

PubMed: 31797328 ( click the link to review the publication )

J Biol Chem, 2020, jbc.RA120.014960

PubMed: 33273014 ( click the link to review the publication )

Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05927-5

PubMed: 32940848 ( click the link to review the publication )

Nat Commun, 2019, 10(1):3201

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

Cell Rep, 2019, 28(12):3224-3237

PubMed: 31533043 ( 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 )

Endocrinology, 2018, 159(4):1547-1560

PubMed: 29390112 ( 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 )

JCI Insight, 2018, 3(8)97398

PubMed: 29669935 ( 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	NHfN[mJMcW6jc3WgZZN{[Xl?			MWrpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEmJRj2xVkApUUN3MDC9JFE{dk1rIHHu[EB1cGViZH;3cpN1emWjbTD0ZZJo\XS\|IFHreEApUUN3MDC9JFIzdk1rIHHu[EBOSVCNIDjJR\|UxKD1iMUPuUUk>	NYnhTm1ZOTl5N{iwNlQ>
IGF-Sal	M3rTXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7			NW[yeWkzUUN3ME23JI5O	NVfoPFRlOTl5N{iwNlQ>
CCRF-CEM (ALL)	NF3pO5NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MmXBglUh\|ryP	MkH5SG1UVw>?	M2q4[GlEPTB;MT6yN\|kh\|ryP	NFL0clkyQTl7NkK3Ni=>
PC3	NU\DeXJTT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MX\+OUDPxE1?	NFrRNZpFVVOR	MkfNTWM2OD1yLkm2OUDPxE1?	MlzJNVk6QTZ{N{K=
JD	NEj6clNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MUj+OUDPxE1?	M1nRNGROW09?	M1HuUGlEPTB;MD6zPVEh\|ryP	M4\3NlE6QTl4Mkey
DU145	M3foT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M{i0fp42KM7:TR?=	MlnpSG1UVw>?	NF62fHpKSzVyPUGuOFY2KM7:TR?=	MUmxPVk6PjJ5Mh?=
KAG	MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NF3lS3l,PSEQvF2=	NXjpNWRwTE2VTx?=	MnjqTWM2OD1zLk[2OUDPxE1?	M3fQWlE6QTl4Mkey
K-562 (CML)	MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MWf+OUDPxE1?	NFK5RpdFVVOR	NE\6eIZKSzVyPUKuN\|AzKM7:TR?=	NHTh[3MyQTl7NkK3Ni=>
B6-P210 (Murine ALL)	MoT2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1ewdJ42KM7:TR?=	NHjSTpdFVVOR	NWTleZdrUUN3ME2xMlI6OyEQvF2=	NWHjS286OTl7OU[yO\|I>
LN CAP-FGC	MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NXzvRoVphjVizszN	NVHu[\|FFTE2VTx?=	MmDWTWM2OD1zLkSzOEDPxE1?	MWmxPVk6PjJ5Mh?=
VW	NIT0[VFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NH73dI5,PSEQvF2=	Ml;lSG1UVw>?	NHf5W5ZKSzVyPUCuNFE6KM7:TR?=	MXuxPVk6PjJ5Mh?=
MV411 (B Myelomonocytic)	NULRUlBET3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NET2UmR,PSEQvF2=	M{j4OmROW09?	NW\kcphHUUN3ME2wMlM{KM7:TR?=	MWCxPVk6PjJ5Mh?=
MDA-PCa-2b	NYf5cVRoT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	Mn2yglUh\|ryP	NV;zPJVrTE2VTx?=	NULRWFk3UUN3ME2wMlA6QCEQvF2=	MWCxPVk6PjJ5Mh?=
LG	M4nPeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NXrvTHlphjVizszN	NVzXcVZxTE2VTx?=	NXq1XolXUUN3ME2wMlA{QCEQvF2=	M{nGXFE6QTl4Mkey
RS411 (B cell precursor-ALL)	NVy2[Ix5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NGrJTYJ,PSEQvF2=	MnrDSG1UVw>?	MoToTWM2OD1yLkGwNkDPxE1?	MY[xPVk6PjJ5Mh?=
22-r-1	NVLRTodJT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NUDpOXc4hjVizszN	NH3xc\|RFVVOR	MXrJR\|UxRTBwMUe1JO69VQ>?	Mlv2NVk6QTZ{N{K=
5838	MmfBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NIXCPWh,PSEQvF2=	NYLFdW1UTE2VTx?=	NYnWd\|JOUUN3ME2wMlA{PCEQvF2=	NXTw[mI6OTl7OU[yO\|I>
P388 (Murine)	MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MUj+OUDPxE1?	NHvCOnZFVVOR	MXXJR\|UxRTRwMkeg{txO	M37zXlE6QTl4Mkey
A2780/S	MkWxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MWf+OUDPxE1?	MofXSG1UVw>?	MnrFTWM2OD1yLkGyNkDPxE1?	NUfWbHhQOTl7OU[yO\|I>
RDES	NIfQPItIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MWP+OUDPxE1?	M{ThTWROW09?	NXXmdZg3UUN3ME2wMlAyOiEQvF2=	NIracGIyQTl7NkK3Ni=>
B6-T315I (Murine B-ALL)	M{TPN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MoDVglUh\|ryP	M{[xfmROW09?	M2[4fGlEPTB;Mj64N{DPxE1?	NGf5enUyQTl7NkK3Ni=>
TOV 112D	NYrUWGpjT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NVHsWZB3hjVizszN	NU\tXJFPTE2VTx?=	MUDJR\|UxRTJwMUS2JO69VQ>?	M3T6SVE6QTl4Mkey
TC32	NVTrfpdvT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	Ml\lglUh\|ryP	NVLQUY13TE2VTx?=	MYnJR\|UxRTBwMEC4JO69VQ>?	M36ze\|E6QTl4Mkey
HL60 (acute myelocytic)	NITKWGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M{DrZZ42KM7:TR?=	M2fQPWROW09?	MoTDTWM2OD1yLkGyJO69VQ>?	NUfOVFQzOTl7OU[yO\|I>
TOV 21G	MnvQS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NXvrWnpthjVizszN	MWLEUXNQ	Mn3XTWM2OD12LkK3PUDPxE1?	NISxZpYyQTl7NkK3Ni=>
TC71	M{LlU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	Mnf6glUh\|ryP	MWTEUXNQ	NGj5SY9KSzVyPUCuNFE1KM7:TR?=	NFPzbHcyQTl7NkK3Ni=>
HPN-ALL (T-cell)	NH3aSG1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NV\OR3A3hjVizszN	MYTEUXNQ	Mn30TWM2OD1yLkWyJO69VQ>?	MnLhNVk6QTZ{N{K=
A2780R	M3K5SGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NYCwS4JzhjVizszN	NVHwUoc{TE2VTx?=	MVXJR\|UxRTFwNU[0JO69VQ>?	NWXRdpQ4OTl7OU[yO\|I>
Rh1	NFXxTGNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NWj3NHZXhjVizszN	NV;TOmFYTE2VTx?=	MYnJR\|UxRTBwMEK3JO69VQ>?	M4nNNVE6QTl4Mkey
Kasumi-1 (acute myeloid)	NFHHSIdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	Mlf0glUh\|ryP	NWnNNmpnTE2VTx?=	NWr5NWlPUUN3ME2wMlE3KM7:TR?=	MonzNVk6QTZ{N{K=
sk-ov-3	MknwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NIjDXYh,PSEQvF2=	MULEUXNQ	M3LJPWlEPTB;NT6xJO69VQ>?	M4LaZVE6QTl4Mkey
ME	MlzPS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1z0ZZ42KM7:TR?=	MYfEUXNQ	NGLiXlZKSzVyPUCuNFE2KM7:TR?=	M{Lyd\|E6QTl4Mkey
L1210 (Murine lymphocytic)	MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NHKwPFF,PSEQvF2=	MmnGSG1UVw>?	M4XHV2lEPTB;Mj6zPUDPxE1?	MYKxPVk6PjJ5Mh?=
sw-626	MkHrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NXnxPJZyhjVizszN	MUfEUXNQ	MX\JR\|UxRTJwM{C2JO69VQ>?	MYWxPVk6PjJ5Mh?=
CTR	NV3MVmNJT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NI\uOnB,PSEQvF2=	NEfmbYpFVVOR	MV;JR\|UxRTBwMkWzJO69VQ>?	MWCxPVk6PjJ5Mh?=
ML2 (Myelomonocytic)	NVe4WIFQT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MmnHglUh\|ryP	Ml;4SG1UVw>?	MVTJR\|UxRTBwMEmg{txO	MkXTNVk6QTZ{N{K=
ovcar-3	NVK4NZBzT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MWH+OUDPxE1?	NGfvfW1FVVOR	MlvITWM2OD13IN88US=>	MXqxPVk6PjJ5Mh?=
Rh36	MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NIO3TW5,PSEQvF2=	MUDEUXNQ	Mm[5TWM2OD1zLkSzNkDPxE1?	NEXKUI4yQTl7NkK3Ni=>
MOLM-13 (acute myeloid)	MkGwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NGH3fWF,PSEQvF2=	MYXEUXNQ	MlTVTWM2OD1yLkSyJO69VQ>?	MVuxPVk6PjJ5Mh?=
ovcar-4	NWrhOIhOT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MnfmglUh\|ryP	NXrafFQxTE2VTx?=	MXvJR\|UxRTFizszN	MWOxPVk6PjJ5Mh?=
Rh41	NIPNVFRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M4P3UZ42KM7:TR?=	NYTwO4JOTE2VTx?=	MnO3TWM2OD1yLkCwOUDPxE1?	NHn1[2gyQTl7NkK3Ni=>
Mutz 2 (acute myeloid)	MkHxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MUj+OUDPxE1?	NWrBPHRCTE2VTx?=	Mo\KTWM2OD1zLkG1JO69VQ>?	MYCxPVk6PjJ5Mh?=
ovcar-5	NFvM[m5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MknKglUh\|ryP	M1K0U2ROW09?	MWrJR\|UxRTBwMEWg{txO	NVPPWWtSOTl7OU[yO\|I>
RD1	NFrIdYRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MVf+OUDPxE1?	M3\qT2ROW09?	NF7SfoVKSzVyPUCuNFY5KM7:TR?=	Mn;qNVk6QTZ{N{K=
OCI-AML 2 (acute myeloid)	MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NFfhWFJ,PSEQvF2=	MkHhSG1UVw>?	MUjJR\|UxRTNwM{Og{txO	NHrjemcyQTl7NkK3Ni=>
786-O	NXTZT5JMT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NFHRdZV,PSEQvF2=	MkDDSG1UVw>?	M{n6W2lEPTB;MT62OFch\|ryP	NWL5cYNUOTl7OU[yO\|I>
A673	M33JN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	Mn\BglUh\|ryP	MUfEUXNQ	MX7JR\|UxRTBwNEC4JO69VQ>?	NHPXWGEyQTl7NkK3Ni=>
TALL-1 (T-cell)	NVLqdYZzT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M3Ozd542KM7:TR?=	M1PYeWROW09?	NG\EVHJKSzVyPUGuNlgh\|ryP	M{TydVE6QTl4Mkey
151-B	MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NYfa[Ws{hjVizszN	MmjCSG1UVw>?	Ml7kTWM2OD1{Lk[3JO69VQ>?	NFradHkyQTl7NkK3Ni=>
PFSK-1	NUDsdZdvT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MVn+OUDPxE1?	MmnkSG1UVw>?	M3n0UmlEPTB;MD6xN\|Ih\|ryP	M1T6Z\|E6QTl4Mkey
THP-1	NF\vZo1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MmLXglUh\|ryP	NVnS[2pHTE2VTx?=	Mny2TWM2OD14LkW4JO69VQ>?	MmroNVk6QTZ{N{K=
HEK293	M{fKS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MVT+OUDPxE1?	MV7EUXNQ	NEPYSXVKSzVyPUCuPVE2KM7:TR?=	NITCZlMyQTl7NkK3Ni=>
DAOY	M1zVVWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NH7jfIV,PSEQvF2=	MnXSSG1UVw>?	NYPidFNtUUN3ME2xMlk4QSEQvF2=	NUPNSFdiOTl7OU[yO\|I>
SET2	NUjmV5VmT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NIrNNot,PSEQvF2=	MYHEUXNQ	MYPJR\|UxRTBwMkm4JO69VQ>?	NVzhWolrOTl7OU[yO\|I>
HTB-46	MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M{\6ZZ42KM7:TR?=	NYLqVJBQTE2VTx?=	MXHJR\|UxRTVwMkWg{txO	M4nqelE6QTl4Mkey
SK-NAS	MkX1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MY\+OUDPxE1?	MXLEUXNQ	NFv2d3pKSzVyPUCuOFk4KM7:TR?=	M17GblE6QTl4Mkey
CTLL2	NUfMWodWT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MnHhglUh\|ryP	MYLEUXNQ	NETh[WpKSzVyPkGuNFAh\|ryP	NX7kV2E1OTl7OU[yO\|I>
HTB-47	NV3jWGs2T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NGXVc4d,PSEQvF2=	NW\ub2M3TE2VTx?=	MVfJR\|UxRTJwMEW2JO69VQ>?	MV2xPVk6PjJ5Mh?=
LAN-1	MofTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M3\rdJ42KM7:TR?=	MnLwSG1UVw>?	NIDjPWVKSzVyPUCuNFQh\|ryP	M4PxOVE6QTl4Mkey
ST486	NIjofYJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NXLtW2NzhjVizszN	M{\vWWROW09?	M2Xt[GlEPTB;MT6xPUDPxE1?	MnXRNVk6QTZ{N{K=
HS766T	MnizS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MmOyglUh\|ryP	MYXEUXNQ	NVnNbodDUUN3ME2yMlAxOSEQvF2=	NXLuUXd1OTl7OU[yO\|I>
IMR-32	MoXoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1Txd542KM7:TR?=	MVHEUXNQ	MknETWM2OD1yLkK2NUDPxE1?	MnXvNVk6QTZ{N{K=
Daudi (Burkitt's)	NHTCdnVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MljCglUh\|ryP	MlzsSG1UVw>?	NYq5NolxUUN3ME2yMlY{PyEQvF2=	NH\JeG8yQTl7NkK3Ni=>
Aspc-1	NVj4bYJjT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MU\+OUDPxE1?	NW\TS3BGTE2VTx?=	NVnXdXJIUUN3ME2wMlM4QSEQvF2=	NITGNo4yQTl7NkK3Ni=>
SK-NSH	NF7DS5RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NFrp[YJ,PSEQvF2=	NHPCSllFVVOR	NX:y[oZsUUN3ME2wMlE{QSEQvF2=	M1TuXlE6QTl4Mkey
MEC-1 (Chronic B cell)	NF2xO4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NV7uZnk2hjVizszN	M4XPTWROW09?	NYP5S2dvUUN3ME2yMlY{PyEQvF2=	NH:yb2QyQTl7NkK3Ni=>
Capan-2	NXzqOGFGT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NEC0PXN,PSEQvF2=	M{fpd2ROW09?	M1rTV2lEPTB;MT63O\|Qh\|ryP	NWDyeWI1OTl7OU[yO\|I>
SHSY5Y	NWjGWZJPT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M{X4RZ42KM7:TR?=	NVzTZ5JQTE2VTx?=	MoPPTWM2OD1yLkGwOkDPxE1?	NEPxXIYyQTl7NkK3Ni=>
U937 (Histioocytic)	MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NYTyTmp3hjVizszN	MmTMSG1UVw>?	MXzJR\|UxRjVwMECg{txO	M2\aeFE6QTl4Mkey
Bxpc-1	MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NYT2PYJjhjVizszN	MUDEUXNQ	MWnJR\|UxRTFwOUK0JO69VQ>?	MYKxPVk6PjJ5Mh?=
Bxpc-3	MoLBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NHXLWFl,PSEQvF2=	M3vZcGROW09?	MojlTWM2OD53LkCwJO69VQ>?	NILhTIMyQTl7NkK3Ni=>
HTB-92	MoLKS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NWfnPWQ6hjVizszN	MYrEUXNQ	M3P6[2lEPTB;MT6wNkDPxE1?	M{XsPFE6QTl4Mkey
OCI-LY10 (B-cell)	NF\nc5NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NWHMbJlyhjVizszN	M{\semROW09?	M4DUR2lEPTB;MD60OUDPxE1?	NGLtOYgyQTl7NkK3Ni=>
PANC-1	M1SxNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NHjaNWF,PSEQvF2=	MkKwSG1UVw>?	NFLscodKSzVyPkWuNFAh\|ryP	NYHCZ2ltOTl7OU[yO\|I>
To184.T	NX7QcWlRT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MmHmglUh\|ryP	NHG1WJRFVVOR	NX;sN2VsUUN3ME2wMlQ3QSEQvF2=	M3y1OFE6QTl4Mkey
OCI-LY19 (B-cell)	NUC0NnJpT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MWf+OUDPxE1?	M{D5OWROW09?	M3j6UmlEPTB;MD60JO69VQ>?	Ml;PNVk6QTZ{N{K=
PANC-1 BM	MnWzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MWD+OUDPxE1?	M3nrUmROW09?	MYjJR\|UxRjVwMECg{txO	NESzOJQyQTl7NkK3Ni=>
SA-4	M4\ETmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NWm3UIYxhjVizszN	NYm4TGY5TE2VTx?=	MVHJR\|UxRTFwM{CxJO69VQ>?	NICwe3IyQTl7NkK3Ni=>
RPMI 8226	M{Hzc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NVXnOWZGhjVizszN	NWqxfnV7TE2VTx?=	NX7KXpRTUUN3ME2xMlI6OyEQvF2=	M3WwSVE6QTl4Mkey
HPAF-II	M2DTTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MmrYglUh\|ryP	NGDleoxFVVOR	MXTJR\|UxRTBwNkS0JO69VQ>?	NUPMe4tCOTl7OU[yO\|I>
SHP-77	NXz6[YFVT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M{TUXp42KM7:TR?=	MlTySG1UVw>?	NGPHRpZKSzVyPUGuPFg5KM7:TR?=	M4fzTFE6QTl4Mkey
U266 B1	MmPmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NHv6ZVZ,PSEQvF2=	NWfEfJhzTE2VTx?=	NXy1XpVpUUN3ME2xMlY3QSEQvF2=	NUXnT5RrOTl7OU[yO\|I>
Hs700t	MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MmHqglUh\|ryP	NHjMVYFFVVOR	MlzHTWM2OD1yLkKzNUDPxE1?	MoDENVk6QTZ{N{K=
NCI-446	MkjHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NV6zVI95hjVizszN	NUfjWJNbTE2VTx?=	Mm\TTWM2OD1zLkG1OEDPxE1?	MV:xPVk6PjJ5Mh?=
H929	MlLIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	Mmj0glUh\|ryP	M2PYSmROW09?	MX;JR\|UxRTBwMEG0JO69VQ>?	M3fRSlE6QTl4Mkey
PL45	NYm0dZZOT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MnfhglUh\|ryP	M{fweWROW09?	MnvTTWM2OD1{LkK1OUDPxE1?	NInteWMyQTl7NkK3Ni=>
NCI-H383	MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NH:3W\|d,PSEQvF2=	MXXEUXNQ	MkXRTWM2OD53LkCwJO69VQ>?	NXj6cXY2OTl7OU[yO\|I>
JJN3	NVT3NVl[T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M2nFOJ42KM7:TR?=	MUTEUXNQ	NEm5UG9KSzVyPUKuOFM{KM7:TR?=	MV:xPVk6PjJ5Mh?=
SU.86.86	MkT0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NWmzZ3Q3hjVizszN	MoLkSG1UVw>?	NX[0N453UUN3ME2yMlY4OiEQvF2=	Ml\uNVk6QTZ{N{K=
H1299	MoTyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NFy2dIh,PSEQvF2=	MWrEUXNQ	MVPJR\|UxRjVwMECg{txO	MkD1NVk6QTZ{N{K=
MDA-MB-468	NULjVoZoT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NHr2dWJ,PSEQvF2=	NWGwcop6TE2VTx?=	M3L4R2lEPTB;MD61NFQh\|ryP	NHXtfXcyQTl7NkK3Ni=>
SW1990	NELhc2FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MkPiglUh\|ryP	Mnu5SG1UVw>?	MVzJR\|UxRTBwOEK2JO69VQ>?	M33KblE6QTl4Mkey
Calu-6	MmnsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NF7mdXh,PSEQvF2=	Mk[zSG1UVw>?	NIHtc\|JKSzVyPkWuNFAh\|ryP	M13jRVE6QTl4Mkey
MDA-MB-231	NH\NcotIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NYXXXphOhjVizszN	Mn7kSG1UVw>?	NXz2S4ZQUUN3ME2xMlY1QCEQvF2=	M2HVSVE6QTl4Mkey
SW-684	NETKNGVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MUP+OUDPxE1?	M{mzdGROW09?	NWnI[\|I3UUN3ME61MlAxKM7:TR?=	NXXHOlBzOTl7OU[yO\|I>
H209	MnKyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NFnhbWJ,PSEQvF2=	NXr6b\|E{TE2VTx?=	M4rrNmlEPTB;MT6xPVMh\|ryP	MkK1NVk6QTZ{N{K=
MDA-MB-231T	M{HpV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MkjmglUh\|ryP	M1O1OWROW09?	M1S0bGlEPTB-NT6wNEDPxE1?	NYn6dnlOOTl7OU[yO\|I>
HT1080/S	NVL2bZlqT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M1exZZ42KM7:TR?=	NGn6[4NFVVOR	NIHWcGpKSzVyPUCuOVMyKM7:TR?=	NYHmS4RXOTl7OU[yO\|I>
H526 0.044	Mk\iS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NHXXXI5,PSEQvF2=	NI\Wb2xFVVOR	MVrJR\|UxRTBwMES0JO69VQ>?	NH6zNI4yQTl7NkK3Ni=>
DU4475 2.431	MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M1O3UZ42KM7:TR?=	MkD1SG1UVw>?	MXzJR\|UxRTJwNEOxJO69VQ>?	NGLrdlQyQTl7NkK3Ni=>
HCT116	MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NFXPRpV,PSEQvF2=	MWnEUXNQ	NY[2dmwxUUN3ME2wMlg2OiEQvF2=	NXj2PW9kOTl7OU[yO\|I>
M109	MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NG\5O2J,PSEQvF2=	MVvEUXNQ	NXHEcGpwUUN3ME2xMlA2PSEQvF2=	MX2xPVk6PjJ5Mh?=
BT549	MkfZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NYDLNZVuhjVizszN	MVjEUXNQ	M4DlWWlEPTB;MT62OFUh\|ryP	MUCxPVk6PjJ5Mh?=
HCT116/VM46	NYD6TGd[T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M2e4cp42KM7:TR?=	MX\EUXNQ	NYm1OoZlUUN3ME2xMlcxOiEQvF2=	MUSxPVk6PjJ5Mh?=
H460	NVLGTVI4T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWK1[WpGhjVizszN	MkXISG1UVw>?	M17sNWlEPTB;MD63PVUh\|ryP	MlLXNVk6QTZ{N{K=
MCF-7	NX:5fHQ{T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NYi3dmNWhjVizszN	NE[xN2pFVVOR	MVHJR\|UxRTBwMEG2JO69VQ>?	NYi3UItMOTl7OU[yO\|I>
GEO	M4K3Tmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M{LScZ42KM7:TR?=	MVPEUXNQ	M4D4cWlEPTB;MD6zOVYh\|ryP	MYGxPVk6PjJ5Mh?=
H441 0.646	NXP1V25pT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NGD5SXV,PSEQvF2=	MUPEUXNQ	M2jvR2lEPTB;MD62OFYh\|ryP	M2jONVE6QTl4Mkey
MCF-7-807R	MoHDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NWq4[\|VvhjVizszN	M1:4W2ROW09?	Mkf4TWM2OD1yLkS5JO69VQ>?	NWjxcJRlOTl7OU[yO\|I>
Colo205	MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M2L4OZ42KM7:TR?=	MYjEUXNQ	NWTMS2N7UUN3ME2wMlExPCEQvF2=	MUWxPVk6PjJ5Mh?=
H292	MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MnHOglUh\|ryP	MWDEUXNQ	MWPJR\|UxRTBwN{i4JO69VQ>?	NYrtWXI6OTl7OU[yO\|I>
BT474 (S)	NYX6UmR2T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MVL+OUDPxE1?	MY\EUXNQ	NWDOWZF1UUN3ME2yMlQxOyEQvF2=	M4nBeVE6QTl4Mkey
HT-29	MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NX\sN5lFhjVizszN	NEfiPGpFVVOR	MnmyTWM2OD1{LkGwN{DPxE1?	MnzJNVk6QTZ{N{K=
A549	NYq4[4VlT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NXLMfnNihjVizszN	MXPEUXNQ	NXy1SGNpUUN3ME2wMlY4PSEQvF2=	M2[0VlE6QTl4Mkey
BT474-M1	MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M4XITp42KM7:TR?=	M{GxSWROW09?	MkjhTWM2OD1{LkO2OUDPxE1?	MXyxPVk6PjJ5Mh?=
SW480	M2XoXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NEPJVXl,PSEQvF2=	Mn7iSG1UVw>?	M13PR2lEPTB-NT6wNEDPxE1?	M3vjS\|E6QTl4Mkey
L2987	M1Xq[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MWT+OUDPxE1?	NY\BSY5OTE2VTx?=	M{jkZmlEPTB;MD60OFIh\|ryP	NVizblFCOTl7OU[yO\|I>
AU565	MmjVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MV;+OUDPxE1?	M3Pnc2ROW09?	MYrJR\|UxRTRwOUeg{txO	NXjlcmZrOTl7OU[yO\|I>
SW403	Ml3aS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MnjjglUh\|ryP	MYHEUXNQ	MXfJR\|UxRTBwMkKg{txO	NEXJNIYyQTl7NkK3Ni=>
H1437	M2[xbGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NFKydYl,PSEQvF2=	NVfqNJJsTE2VTx?=	MXjJR\|UxRTBwNUKzJO69VQ>?	M3vYdlE6QTl4Mkey
BT-20	NYSzbWZPT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NVPHXmVGhjVizszN	M3LFRWROW09?	MmLBTWM2OD1\|LkW2NkDPxE1?	NVHqNpAyOTl7OU[yO\|I>
Colo320HSR	NIr4eWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NXfGVJM{hjVizszN	M4HGOWROW09?	M1rEdWlEPTB;MD6wNVEh\|ryP	MV2xPVk6PjJ5Mh?=
H2087	MmfTS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NWD6dWhHhjVizszN	NIjD[HFFVVOR	M3i3N2lEPTB-MT6wNEDPxE1?	NHHOeFMyQTl7NkK3Ni=>
HCC1419	NWTPRnNkT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MnnuglUh\|ryP	M1;vNmROW09?	MlTFTWM2OD1{LkWxO{DPxE1?	NHnLO2YyQTl7NkK3Ni=>
WiDr	MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MonQglUh\|ryP	NFPVR2JFVVOR	MnXtTWM2OD1yLkC3OkDPxE1?	NUTGTYNuOTl7OU[yO\|I>
H661 0.573	MlvVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NXznZpZihjVizszN	MYjEUXNQ	M{O0WmlEPTB;MD61O\|Mh\|ryP	M{HXRlE6QTl4Mkey
HCC-38	NVXv[VBvT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MX7+OUDPxE1?	M{HTU2ROW09?	NXnxRol1UUN3ME61MlAxKM7:TR?=	Mly1NVk6QTZ{N{K=
LS174T	NGe2SYxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MmTWglUh\|ryP	MnzWSG1UVw>?	MWfJR\|UxRTBwNUO1JO69VQ>?	M1vCXFE6QTl4Mkey
H211	NWTEVHV4T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NEDZe\|Z,PSEQvF2=	M2rneWROW09?	NVS0T4ZuUUN3ME2wMlc{OyEQvF2=	MmnVNVk6QTZ{N{K=
HCC70	MljqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NEnIfHN,PSEQvF2=	NVPKO4lHTE2VTx?=	MVTJR\|UxRTFwNUWg{txO	NW\ze2pGOTl7OU[yO\|I>
SW116	NF3WUGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	Mkm0glUh\|ryP	NYrY[XpiTE2VTx?=	M1HTW2lEPTB;MD6wOlch\|ryP	MkfPNVk6QTZ{N{K=
H513	NFPEN2ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MkDDglUh\|ryP	MVXEUXNQ	NHXhfmJKSzVyPUSuOFQ5KM7:TR?=	NVTJWYRSOTl7OU[yO\|I>
MDA-MB-157	MmP2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1;Fd542KM7:TR?=	NImwSVFFVVOR	M{fUUWlEPTB;MD6wN\|Yh\|ryP	MkDSNVk6QTZ{N{K=
H2052	MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MnHNglUh\|ryP	MULEUXNQ	NHHFS4JKSzVyPUGuNFUh\|ryP	Mkf1NVk6QTZ{N{K=
MDA-MB-415	MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NYC4b4FqhjVizszN	MWXEUXNQ	MljWTWM2OD53LkCwJO69VQ>?	NIXqb28yQTl7NkK3Ni=>
DLD-1	MoizS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MWf+OUDPxE1?	NYDK[Zc{TE2VTx?=	NXrzVIFHUUN3ME2wMlkxQSEQvF2=	MUKxPVk6PjJ5Mh?=
H2595	MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	Mlq2glUh\|ryP	M1HHNGROW09?	Mnj3TWM2OD12LkS3OUDPxE1?	NXvFNnN{OTl7OU[yO\|I>
MDA-MB-435S	M{jYO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NXrifIVwhjVizszN	M1nkd2ROW09?	NU\DeoY{UUN3ME2xMlg3QSEQvF2=	NGTGZVIyQTl7NkK3Ni=>
HCT15	M1\q[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NY\xdJNJhjVizszN	NXe1PVNbTE2VTx?=	NYTsUZM4UUN3ME6xMlAxKM7:TR?=	NXriTndIOTl7OU[yO\|I>
SK-Hep1	NUTQTYhWT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MnL1glUh\|ryP	NUHSVHRqTE2VTx?=	MV\JR\|UxRTBwMUS2JO69VQ>?	MW[xPVk6PjJ5Mh?=
MDA-MB-436	NWnXO45JT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M13QUp42KM7:TR?=	MmnlSG1UVw>?	Mmf2TWM2OD13LkWwNkDPxE1?	MXGxPVk6PjJ5Mh?=
KM12C	NYniVHhtT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	Ml7zglUh\|ryP	Mkj1SG1UVw>?	NHT5eppKSzVyPUCuNFU1KM7:TR?=	MYGxPVk6PjJ5Mh?=
HEPG2	NF3Wc\|dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NG\mS\|B,PSEQvF2=	MV7EUXNQ	MVvJR\|UxRTBwMEK1JO69VQ>?	NFW0PYMyQTl7NkK3Ni=>
MDA-MB-453	NYrsR\|B6T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NYrMS3NmhjVizszN	NXLCOoxrTE2VTx?=	M33lemlEPTB;MT64Olkh\|ryP	NYnFfWxPOTl7OU[yO\|I>
KM12SM	MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MV3+OUDPxE1?	NH64WGxFVVOR	NYmz[Yw6UUN3ME2wMlA2QSEQvF2=	NF;XPIYyQTl7NkK3Ni=>
1483	NUnUV5BZT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M2HXfJ42KM7:TR?=	NHu1VGNFVVOR	M{[2UmlEPTB;Mj6xPUDPxE1?	MnvENVk6QTZ{N{K=
Hs578t	NVzZO4VHT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M171[542KM7:TR?=	NUW2fZJyTE2VTx?=	MlGyTWM2OD1zLkK4O{DPxE1?	Ml;WNVk6QTZ{N{K=
LS180	M1u3Omdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NFqxUoN,PSEQvF2=	M1nQc2ROW09?	NEPVUmxKSzVyPUCuOlk3KM7:TR?=	M1zt[FE6QTl4Mkey
FaDu	MlfyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NV;XPXJwhjVizszN	NHfpfIdFVVOR	NGL5[HlKSzVyPUGuNlch\|ryP	M33pXlE6QTl4Mkey
ZR-75-1	MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NIqzRVJ,PSEQvF2=	NFPIcIpFVVOR	M2nTSmlEPTB;Mj6wPFQh\|ryP	NHTHVWwyQTl7NkK3Ni=>
LS513	MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NXfMUIRqhjVizszN	NVvaW2lpTE2VTx?=	Mn;qTWM2OD1yLkGzOUDPxE1?	Mm\ZNVk6QTZ{N{K=
Detroit.562	NH;jeI9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M4DHd542KM7:TR?=	NV3pZ491TE2VTx?=	NEW0W3JKSzVyPUGuNVQh\|ryP	M1PLXFE6QTl4Mkey
ZR-75-30	M3q2XGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MmHxglUh\|ryP	M{WyW2ROW09?	NWHsdWhJUUN3ME61MlAxKM7:TR?=	Ml7pNVk6QTZ{N{K=
RKO-PM	NVzIO2NqT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NFLuTWl,PSEQvF2=	MlLySG1UVw>?	M4HlWmlEPTB;MD6yN\|Ih\|ryP	Mn\ZNVk6QTZ{N{K=
Cal.27	MoLBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NWDWOHJRhjVizszN	MoPtSG1UVw>?	NYfaboZLUUN3ME2yJO69VQ>?	MYqxPVk6PjJ5Mh?=
KPL4	NGDZOo9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NXnMcndFhjVizszN	MkO3SG1UVw>?	MnvaTWM2OD1zLkK1NkDPxE1?	M{PaRVE6QTl4Mkey
PKO-RM13	MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MkfYglUh\|ryP	NUm4dlAxTE2VTx?=	NUniZ\|N6UUN3ME2wMlQzPSEQvF2=	NEXJbJkyQTl7NkK3Ni=>
HS.53.T	NVH1UId5T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWLUcY16hjVizszN	Ml;mSG1UVw>?	MYjJR\|UxRTBwN{mg{txO	NIj2Nm8yQTl7NkK3Ni=>
EMT6	Ml\QS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M4\CSJ42KM7:TR?=	NWfyVoxZTE2VTx?=	NHfMNGhKSzVyPUCuPFA3KM7:TR?=	NYHwWZJROTl7OU[yO\|I>
SNU-C1	NFHqRm5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NF3RcnJ,PSEQvF2=	MoW4SG1UVw>?	NV3TcW5ZUUN3ME2wMlAxPyEQvF2=	M2K1dlE6QTl4Mkey
SQCCY1	NWjINlh1T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NVLNbFVlhjVizszN	NWC4S4M2TE2VTx?=	NIjjSGlKSzVyPUCuO\|kh\|ryP	NHP2dmoyQTl7NkK3Ni=>
SW480	MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M1\jPJ42KM7:TR?=	MX3EUXNQ	M2j3bGlEPTB;MD6wN\|ch\|ryP	MoHRNVk6QTZ{N{K=
SCC9	M2PJe2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NX7hSW9lhjVizszN	NEmxRXdFVVOR	NFLBS\|hKSzVyPUCuO\|Uh\|ryP	NVPPRYw1OTl7OU[yO\|I>
SK-LMS-1	NF;LWFRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MWH+OUDPxE1?	NHTrfnVFVVOR	NHq1eGxKSzVyPUCuOlg4KM7:TR?=	M3u5TlE6QTl4Mkey
SCC25	MnrZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M1OwZp42KM7:TR?=	NVnVOVVmTE2VTx?=	NICwcIxKSzVyPUCuOlgh\|ryP	MljVNVk6QTZ{N{K=
U87	M1vkcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NV;2dXY1hjVizszN	M124T2ROW09?	MmrUTWM2OD1yLkm1JO69VQ>?	NV7oc214OTl7OU[yO\|I>
SCC15	M2TpT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NEfEdFZ,PSEQvF2=	Mnr3SG1UVw>?	MYTJR\|UxRTBwNkeg{txO	M2HQZlE6QTl4Mkey
T98G	MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M1y4UJ42KM7:TR?=	MX;EUXNQ	NUjZd2E2UUN3ME2xMlIyQCEQvF2=	MW[xPVk6PjJ5Mh?=
SCC4	M1jOTWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MlfaglUh\|ryP	M{jNZ2ROW09?	NU\ncFFTUUN3ME2wMlY{KM7:TR?=	NVPVfmwyOTl7OU[yO\|I>
U118	M{LYTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MYf+OUDPxE1?	NYrLXm82TE2VTx?=	NV\oOJA4UUN3ME2xMlYyQCEQvF2=	NUnI[pR[OTl7OU[yO\|I>
TU167	M{TvSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NHnCRlZ,PSEQvF2=	MXLEUXNQ	MlnCTWM2OD12LkWyJO69VQ>?	NYfSNos2OTl7OU[yO\|I>
NCI-H727	NG\vfpRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MVT+NVDjiIsQvF2=	NYm5cZd[TE2VTx?=	MYTJR\|UxRTR{ODDuUS=>	MV:yNFM5PTd2Nx?=
NCI-H720	MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MWP+NVDjiIsQvF2=	NIOxZWxFVVOR	NGjETWdKSzVyPUKuPEDPxE1?	M3PSUlIxOzh3N{S3
NCI-H835	NGK1[25Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MnjuglEx6oDMzszN	M2XPUWROW09?	MWfJR\|UxRTFizszN	NFrWfmUzODN6NUe0Oy=>
NCI-H727	NVfoNVU2U2mwYYPlJIF{e2G7	NEK5WoR,OTEkgJtOwG0>	M3nlSWROW09?	NFnB[mNqdmirYnn0d{Bkd26\|dHn0eZRqfmViSVfGNXIh[XW2b4Doc5NxcG:{eXzheIlwdg>?	MWiyNFM5PTd2Nx?=
RD	MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NV\BNFJOhjFy4pEK{txO		M1TDRmlEPTB;MT6xNkDDvU1?	NHnxTWozOTJ7OEe0OS=>
Rh41	MnHJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MnrVglEx6oDMzszN		MoLJTWM2OD1yLkC3JOK2VQ>?	MnG5NlEzQTh5NEW=
Rh18	NGrlUpNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MYT+NVDjiIsQvF2=		NW[1ZlVyUUN3ME20Mlk3KML3TR?=	NUPycnA5OjF{OUi3OFU>
Rh30	M1jTeGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MlrjglEx6oDMzszN		MoLUTWM2OD1yLkG5JOK2VQ>?	MoD4NlEzQTh5NEW=
BT-12	NIDNWm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	Mlm0glEx6oDMzszN		NGDEdHVKSzVyPUCuO\|ghyrWP	MlzQNlEzQTh5NEW=
CHLA-266	MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MmnoglEx6oDMzszN		NU\BUpB[UUN3ME2wMlg6KML3TR?=	MX2yNVI6QDd2NR?=
TC-71	MnzlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MUn+NVDjiIsQvF2=		MnnXTWM2OD1yLkGxJOK2VQ>?	MXmyNVI6QDd2NR?=
CHLA-9	NGXOenNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M1;hWp4yOOLCit88US=>		NHT6T\|BKSzVyPUCuNVIhyrWP	MkT2NlEzQTh5NEW=
CHLA-10	NWK3[2I4T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NVizNpZmhjFy4pEK{txO		MXHJR\|UxRTBwNkKgxtVO	M3jRRlIyOjl6N{S1
CHLA-258	Mn3uS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NIi1VlV,OTEkgJtOwG0>		NFjsSWRKSzVyPUCuNlchyrWP	NXexVnBQOjF{OUi3OFU>
GBM2	MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NVLtXmdChjFy4pEK{txO		NGH5eWdKSzVyPUGuOFchyrWP	M2rIWFIyOjl6N{S1
NB-1643	NWD3bWU{T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MkfLglEx6oDMzszN		M{TT[WlEPTB;MD6xNkDDvU1?	Ml3tNlEzQTh5NEW=
NB-EBc1	MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NVXpc4dKhjFy4pEK{txO		MnzyTWM2OD1yLkO1JOK2VQ>?	M1znRlIyOjl6N{S1
CHLA-90	NXuwWW1{T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M{\4bZ4yOOLCit88US=>		MYfJR\|UxRTBwN{egxtVO	M3XIO\|IyOjl6N{S1
CHLA-136	MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MnjrglEx6oDMzszN		MkD6TWM2OD1yLkWyJOK2VQ>?	MXOyNVI6QDd2NR?=
NALM-6	M174eGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M1;UXZ4yOOLCit88US=>		MYLJR\|UxRTBwNEmgxtVO	M3LnUlIyOjl6N{S1
COG-LL-317	NWTCW3hWT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M1jKfp4yOOLCit88US=>		MWDJR\|UxRTFwM{igxtVO	NY\pbmFzOjF{OUi3OFU>
RS4;11	MonES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M2\hWJ4yOOLCit88US=>		NID6WmRKSzVyPUCuN\|ghyrWP	Mnz0NlEzQTh5NEW=
MOLT-4	NUDEd3dXT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NYjiVGRnhjFy4pEK{txO		NEf3cotKSzVyPUCuOVMhyrWP	MV[yNVI6QDd2NR?=
CCRF-CEM	NW\lSHJWT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NYqyUpBJhjFy4pEK{txO		MlHYTWM2OD1zLkGzJOK2VQ>?	NH64THczOTJ7OEe0OS=>
Kasumi-1	M1vxUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NXLzbpVzhjFy4pEK{txO		MYDJR\|UxRTFwMjFCuW0>	M1:1d\|IyOjl6N{S1
Karpas-299	MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M3nUWp4yOOLCit88US=>		M2jIZ2lEPTB;MT62OEDDvU1?	NFvmdlMzOTJ7OEe0OS=>
Ramos-RA1	NVvDUnVTT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	Mn\DglEx6oDMzszN		NHe1cVVKSzVyPUGuN\|EhyrWP	NYmxNHBFOjF{OUi3OFU>
Rh30	MWPGeY5kfGmxbjDhd5NigQ>?			NE\UdIlqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:\|cHjvdplt[XSrb36=	MojtNlU6OjV\|N{i=
Rh41	NWjh[JZ3TnWwY4Tpc44h[XO\|YYm=			NUK1fJpUcW6mdXPld{BidiCrbnPy[YF{\SCxZjDTSmsheGixc4Doc5J6dGG2aX;u	MofvNlU6OjV\|N{i=
RD	MWnGeY5kfGmxbjDhd5NigQ>?			NGfSelJqdmS3Y3XzJIFvKGmwY4LlZZNmKG:oIGPGT{BxcG:\|cHjvdplt[XSrb36=	MWWyOVkzPTN5OB?=
A549	NYrLeIp5U2mwYYPlJIF{e2G7	MkLiNE426oDMzszN	NFXFVI9FVVOR	NXLob5RrcW6qaXLpeJMhUUeILVnSM2lTKGGldHn2ZZRqd25?	MWSyOlkzQDV5OB?=
NCI-H358	MXjLbY5ie2ViYYPzZZk>	NXn5d\|dpOC534pEK{txO	M4HDemROW09?	M2ruXolvcGmkaYTzJGlITi2LUj;JVkBi[3SrdnH0bY9v	M1\1Z\|I3QTJ6NUe4
A549	MnjQSpVv[3Srb36gZZN{[Xl?	NGLNVZoxNjYkgJtOwG0>	M37FW2ROW09?	MUjjZZV{\XNiYTDjc45kfXK{ZX70JIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJGFMXCCjbnSgSXJM	NVPRWFBJOjZ7Mki1O\|g>
NCI-H358	Ml3RSpVv[3Srb36gZZN{[Xl?	MX6wMlXjiIsQvF2=	M{fuXGROW09?	M1LxdINifXOnczDhJINwdmO3coLlcpQh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSUuWIHHu[EBGWkt?	NHriU3IzPjl{OEW3PC=>
A549	NUHQ[485T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWnlcGVjhjFy4pEK{txO	NWLIclluTE2VTx?=	MonKTWM2OD1yLke2JO69VQ>?	NIrRWY0zPjl{OEW3PC=>
NCI-H358	M37COGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M4TENZ4yOOLCit88US=>	NITv[GZFVVOR	NYXV[45yUUN3ME2xMlA6KM7:TR?=	M4PjVFI3QTJ6NUe4
A549	MljFRZBweHSxc3nzJIF{e2G7	NH7qbIQxNjYkgJtOwG0>	NG\hXG9FVVOR	NYjBVZJCcW6mdXPld{BCeG:ydH;zbZM>	MUSyOlkzQDV5OB?=
NCI-H358	MnPqRZBweHSxc3nzJIF{e2G7	MV2wMlXjiIsQvF2=	NFnqZm1FVVOR	Ml34bY5lfWOnczDBdI9xfG:\|aYO=	NHrPcmwzPjl{OEW3PC=>
A549	NXzEWItFTnWwY4Tpc44h[XO\|YYm=	NXvy[2huOC534pEK{txO	M3XGTWROW09?	NF\ocYJz\WS3Y3XzJJdwfW6mIHPsc5N2emV?	NHnLN28zPjl{OEW3PC=>
NCI-H358	MYLGeY5kfGmxbjDhd5NigQ>?	NUXlTVJEOC534pEK{txO	NFz2c4xFVVOR	MVny[YR2[2W\|IIfveY5lKGOub4P1doU>	MorDNlY6Ojh3N{i=

... 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)
	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 Download BMS-754807 SDF

Molecular Weight	461.49
Formula	C₂₃H₂₄FN₉O
CAS No.	1001350-96-4
Storage	3 years-20°C powder 2 years-80°C 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)

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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 μL 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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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, AXL1717) 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). Picropodophyllin (PPP) induces apoptosis with antineoplastic activity.
Erlotinib ^New

Erlotinib (CP358774, NSC 718781) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Bemcentinib (R428) ^New

Bemcentinib (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 (CS-0117) 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 (GSK 552602A) 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 (GSK 4529) 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, AGS 200) 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