BI-D1870

For research use only.

Catalog No.S2843

29 publications

BI-D1870 Chemical Structure

CAS No. 501437-28-1

BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.

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Selleck's BI-D1870 has been cited by 29 publications

Purity & Quality Control

Choose Selective S6 Kinase Inhibitors

Biological Activity

Description BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
Targets
RSK4 [1]
(Cell-free assay)
RSK3 [1]
(Cell-free assay)
RSK2 [1]
(Cell-free assay)
RSK1 [1]
(Cell-free assay)
15 nM 18 nM 24 nM 31 nM
In vitro

BI-D1870 inhibits RSK1, RSK2, RSK3 and RSK4 with an IC50 of 10–30 nM, but does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. BI-D1870 is cell permeant and prevents the RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in human embry-onic kidney 293 cells and Rat-2 cells. BI-D1870 does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Moreover, BI-D1870 does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EW-3 Mn\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPoTWM2OD1yLkCzOVgh|ryP MUPTRW5ITVJ?
H9 MkjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nWSGlEPTB;MD6wOlAyQSEQvF2= M3fxWHNCVkeHUh?=
KARPAS-45 MkfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVqzdVFFUUN3ME2wMlE3PTJ3IN88US=> NFjL[HpUSU6JRWK=
NCI-H720 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[2c41EUUN3ME2wMlE4OTl2IN88US=> NGrte4hUSU6JRWK=
CTV-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLWPGNIUUN3ME2wMlQ4QDd{IN88US=> MmGyV2FPT0WU
DU-4475 MoW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwNUC0NVch|ryP NUj1VopNW0GQR1XS
A172 MkHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwNUG3NFUh|ryP NGnVXHJUSU6JRWK=
EW-18 NUPVW4E5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwNkKyNVEh|ryP M4LLUXNCVkeHUh?=
KU812 MmfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwNkK2NlMh|ryP NFz0cWFUSU6JRWK=
KP-N-YS MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fsTmlEPTB;MD62PFIzOyEQvF2= MUHTRW5ITVJ?
SBC-1 MlPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHITWM2OD1yLk[5OVI1KM7:TR?= MUHTRW5ITVJ?
ECC10 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmL2TWM2OD1yLkewNFk1KM7:TR?= M1rKOHNCVkeHUh?=
GAMG Mm\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TVXWlEPTB;MD63OFcyPyEQvF2= MoDJV2FPT0WU
NCI-H209 Ml71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\lOmFOUUN3ME2wMlc3QDJizszN NULoNJQzW0GQR1XS
MC-IXC NVHvRnR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn32TWM2OD1yLke5OVg6KM7:TR?= NIC3[oZUSU6JRWK=
HSC-3 M16w[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrxZm1WUUN3ME2wMlgyPzZ7IN88US=> NFPEPFJUSU6JRWK=
IST-SL1 NEXmTXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnTPZFKSzVyPUCuPFQ2PzRizszN M{jQOHNCVkeHUh?=
LU-139 NF3sWWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFixdXBKSzVyPUCuPFQ6PThizszN NUm2N5NiW0GQR1XS
ML-2 NVTHRpVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17FWWlEPTB;MD64OVU4PSEQvF2= M3PzbnNCVkeHUh?=
CAL-62 M1XKU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrMc4RKSzVyPUCuPFgyPTJizszN MVLTRW5ITVJ?
HL-60 NUDvXo9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUT1Ro9mUUN3ME2wMlg5OzZ{IN88US=> MW\TRW5ITVJ?
KY821 NHzmeY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF35T4FKSzVyPUCuPFg5OTJizszN M{X2[3NCVkeHUh?=
ES7 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwOUG2NFch|ryP M3TVOHNCVkeHUh?=
MV-4-11 M3\Wfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUCxcZl[UUN3ME2wMlk4QDl5IN88US=> MmjoV2FPT0WU
Daoy MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;kTWM2OD1yLkm4O|Y4KM7:TR?= NUHVTmRZW0GQR1XS
EoL-1-cell NFvkdlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzkbnRKSzVyPUGuNFE5PzhizszN MnTmV2FPT0WU
TGW MnzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTFwMEWxNlQh|ryP M2LXW3NCVkeHUh?=
LAMA-84 NE\JUZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7wTWM2OD1zLkGyO|k1KM7:TR?= NWH5dWFKW0GQR1XS
KOSC-2 M1jqS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTNUHI5UUN3ME2xMlE{Ozh3IN88US=> MWrTRW5ITVJ?
A549 Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTFwM{C5OVUh|ryP M3\qe3NCVkeHUh?=
CTB-1 NH;2bndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PmTmlEPTB;MT60OFY4QSEQvF2= NFTNTmtUSU6JRWK=
NCI-H292 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXsR2VKSzVyPUGuOFYxPjlizszN Mm\HV2FPT0WU
LoVo MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFwNE[3OVUh|ryP M{TzNHNCVkeHUh?=
BFTC-905 NGnkd4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoftTWM2OD1zLkW2N|MzKM7:TR?= MVLTRW5ITVJ?
BE-13 NWTkNZRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M125V2lEPTB;MT61PFcxQSEQvF2= NXfxdoxMW0GQR1XS
KE-37 MlixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1joe2lEPTB;MT61PVQ4QCEQvF2= Mo\vV2FPT0WU
HN MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFwNkGzOlgh|ryP NVXDN4xFW0GQR1XS
A3-KAW Ml;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfkSY9KSzVyPUGuOlI5OzRizszN NX;RdYFRW0GQR1XS
NEC8 M1XEOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTZTZprUUN3ME2xMlcxOTF3IN88US=> NGK5UXVUSU6JRWK=
Ramos-2G6-4C10 M{S1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3lTWM2OD1zLkewOFQ1KM7:TR?= M4HwO3NCVkeHUh?=
NB10 M4fVVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fLPWlEPTB;MT63O|Y{KM7:TR?= Mkj1V2FPT0WU
NBsusSR NHTodWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETnWI1KSzVyPUGuPFI6PjFizszN MnHtV2FPT0WU
ES4 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDN[|dKSzVyPUGuPFUyPDNizszN NF7FVW5USU6JRWK=
ES8 NEnDd5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTFwOEe3NlQh|ryP M2PUOnNCVkeHUh?=
CHL-1 M{\BcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fmWmlEPTB;MT65OVc6OiEQvF2= NULKb4VQW0GQR1XS
NCI-H2029 M4nke2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFwOUeyOFEh|ryP MUfTRW5ITVJ?
YKG-1 M1zBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfGcopKSzVyPUGuPVg1OzJizszN MWLTRW5ITVJ?
BV-173 MoHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mne5TWM2OD1zLkm4OlY3KM7:TR?= NWroO2dlW0GQR1XS
697 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jTWWlEPTB;Mj6wNlIzQCEQvF2= Mnf1V2FPT0WU
SK-NEP-1 NYrETVBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly0TWM2OD1{LkC0OEDPxE1? MWfTRW5ITVJ?
LOXIMVI M2i0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJwMES0N|Qh|ryP MXPTRW5ITVJ?
QIMR-WIL M{naV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\2[GlEPTB;Mj6wO|g1QSEQvF2= M{\N[3NCVkeHUh?=
DU-145 MmG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XxWmlEPTB;Mj6xNVA2PiEQvF2= NF62[4dUSU6JRWK=
NB14 Ml\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJwMUGzNlEh|ryP M2C1XXNCVkeHUh?=
G-361 NXLQdoQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTGTWM2OD1{LkGyNlEh|ryP Mn\mV2FPT0WU
BPH-1 NV3zV3RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rSOWlEPTB;Mj6xNlk2PyEQvF2= M{mzeXNCVkeHUh?=
KYSE-150 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTJwMUWyN|Qh|ryP MnS4V2FPT0WU
HMV-II MoD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjnb3hKSzVyPUKuNVY3OzNizszN MUHTRW5ITVJ?
TE-9 NGnPPZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTJwMUezO|Yh|ryP NH\LdXlUSU6JRWK=
8-MG-BA MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfPZmtKSzVyPUKuNlM1PjFizszN NU\oN4pwW0GQR1XS
ES5 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXnSHB2UUN3ME2yMlI{PjN|IN88US=> MUTTRW5ITVJ?
D-283MED NF6zOoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDBVZNKSzVyPUKuNlM3QTVizszN MUnTRW5ITVJ?
SK-N-AS MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfWeJRiUUN3ME2yMlI6ODV7IN88US=> NYfNO4Z1W0GQR1XS
SW1710 M1;DXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLiTWM2OD1{LkOwOlYyKM7:TR?= NUfzZmFJW0GQR1XS
GCT NVyyUlhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O0[mlEPTB;Mj6zNVM2QCEQvF2= MYfTRW5ITVJ?
AGS MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzvTWM2OD1{LkO0OFA1KM7:TR?= NYGyfINRW0GQR1XS
HuO9 NXL0VYI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\WTWM2OD1{LkO2PFI1KM7:TR?= MnvzV2FPT0WU
MN-60 NYK0eVhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJwNES4PFMh|ryP MX;TRW5ITVJ?
NB6 M3zkOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJwNEW3O|kh|ryP MWLTRW5ITVJ?
NCI-H1395 NIDr[mtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\uPHFjUUN3ME2yMlQ4OTJzIN88US=> M{TGcHNCVkeHUh?=
H4 NFv0fVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7zcVJyUUN3ME2yMlQ5Ozl|IN88US=> NFHYRXZUSU6JRWK=
HT-3 MorLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrWOHRXUUN3ME2yMlUyODJ2IN88US=> M2jQVHNCVkeHUh?=
P12-ICHIKAWA NVHybVJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmP1TWM2OD1{LkWyOVU6KM7:TR?= M{jo[XNCVkeHUh?=
COLO-800 MnXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlO4TWM2OD1{LkW0NVY3KM7:TR?= MWDTRW5ITVJ?
DB MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJwNUWwNVMh|ryP NH;WZ2tUSU6JRWK=
LCLC-97TM1 MlH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJwNkCwNlgh|ryP M{G4bnNCVkeHUh?=
Ca9-22 NFnaNnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUL4dJlCUUN3ME2yMlY2QTN|IN88US=> MXjTRW5ITVJ?
Becker Mk\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPsTWM2OD1{Lk[2NFc5KM7:TR?= M1fwN3NCVkeHUh?=
ACN NH;zbFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL6VopKSzVyPUKuOlY4QSEQvF2= NYDCeolxW0GQR1XS
SJSA-1 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJwNk[4O{DPxE1? MXHTRW5ITVJ?
NCI-H1048 M1zEUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TRd2lEPTB;Mj62PFMzOSEQvF2= M2LjfXNCVkeHUh?=
HEL Mn7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PZb2lEPTB;Mj63NFI2PCEQvF2= NXP1Rlh[W0GQR1XS
NCI-H69 Ml;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7lO|VKSzVyPUKuO|E3ODFizszN NWrRfm14W0GQR1XS
639-V NF3XNZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYix[FRRUUN3ME2yMlcyPzB|IN88US=> NGjaXXRUSU6JRWK=
U251 Mm\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHziNGRKSzVyPUKuO|MxOzJizszN MlHkV2FPT0WU
NCI-H1792 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vyVGlEPTB;Mj63N|c{QCEQvF2= NEj3SFVUSU6JRWK=
EW-1 NUHYdJZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPuTWM2OD1{Lke1N|I5KM7:TR?= NVjBW3VYW0GQR1XS
ME-180 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DnO2lEPTB;Mj63O|c{PiEQvF2= MnT3V2FPT0WU
HH NGDWOZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHXTWM2OD1{LkiwNFAyKM7:TR?= M3\GWHNCVkeHUh?=
SW954 M1fqNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJwOEW4N{DPxE1? MknSV2FPT0WU
SF268 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXhRVhbUUN3ME2yMlg4OjJ3IN88US=> NFjG[4FUSU6JRWK=
D-566MG NWLQ[|F5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3rdW5bUUN3ME2yMlkyOjl3IN88US=> NXn4T4Z1W0GQR1XS
EM-2 NF;lUlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJwOUKxPVMh|ryP MV3TRW5ITVJ?
NCI-H1299 MnTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M365UWlEPTB;Mj65N|c{PiEQvF2= MXTTRW5ITVJ?
PSN1 NHHtXm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTNwMEW3PFYh|ryP MlfoV2FPT0WU
JVM-3 NX\uS3pvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTNwME[3OVYh|ryP MWPTRW5ITVJ?
D-502MG M1izN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rNRmlEPTB;Mz6wO|AyQSEQvF2= M3m0XnNCVkeHUh?=
SCC-4 MkPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV63b3pqUUN3ME2zMlA6Ojd4IN88US=> NVTT[YZKW0GQR1XS
GMS-10 NV3SSWpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrs[ZZKSzVyPUOuNFk{QDhizszN MXfTRW5ITVJ?
A427 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:3WlNKSzVyPUOuNVA5PzNizszN MYnTRW5ITVJ?
NH-12 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\hTFNJUUN3ME2zMlEyPDV4IN88US=> M{e0TXNCVkeHUh?=
KM12 Mn60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHoT4tKSzVyPUOuNVIzPzNizszN M1LPdHNCVkeHUh?=
GI-1 Mm[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\ZTWM2OD1|LkG1NlU2KM7:TR?= NUn6TGY1W0GQR1XS
TE-8 NVv1UJcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTNwMUmyN|Eh|ryP NHHGNWxUSU6JRWK=
MKN1 M{TLNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K2VmlEPTB;Mz6yNFg4PSEQvF2= MVTTRW5ITVJ?
NCI-H810 M2LHOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTNwMkKxOVUh|ryP Mlj1V2FPT0WU
GOTO NX6xSYtPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13WNWlEPTB;Mz6yPFAxPCEQvF2= NEO2[WtUSU6JRWK=
T98G MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTNwMkiyNVYh|ryP NFjS[nNUSU6JRWK=
HD-MY-Z M{fpdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVm1PWZEUUN3ME2zMlM3PTR{IN88US=> NV\uSXp{W0GQR1XS
SNU-C2B MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1THZmlEPTB;Mz6zPVA6PyEQvF2= M{fJT3NCVkeHUh?=
MOLT-4 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvBfVYyUUN3ME2zMlM6ODl6IN88US=> NXrXVnZZW0GQR1XS
RPMI-7951 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\1TWM2OD1|LkO5O|Mh|ryP NVHzTnRrW0GQR1XS
EW-11 MlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTNwNEGyNlQh|ryP MWPTRW5ITVJ?
RD M{XsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDwTWM2OD1|LkSzNVMzKM7:TR?= NUnl[3ZMW0GQR1XS
SW48 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7sTWM2OD1|LkSzN|U5KM7:TR?= MX7TRW5ITVJ?
BB65-RCC NWPZTGtLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTNwNEWzPVYh|ryP MV3TRW5ITVJ?
Ca-Ski MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;mPWlEPTB;Mz60O|UyPCEQvF2= Ml3tV2FPT0WU
CHP-134 NH\VSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm4TWM2OD1|LkS4O|U5KM7:TR?= M{H4NnNCVkeHUh?=
CAL-33 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nXN2lEPTB;Mz61N|M3OiEQvF2= MX\TRW5ITVJ?
TYK-nu Mlu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTNwNUO2O|Yh|ryP NXHwPJZjW0GQR1XS
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KU-19-19 NEDje2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTHN4Q3UUN3ME2zMlYxOzB2IN88US=> NETk[I9USU6JRWK=
KG-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTNwNkGxNFYh|ryP M1n3[HNCVkeHUh?=
COLO-829 NYHhZXdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTNwNk[2NVgh|ryP NIHDPJRUSU6JRWK=
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NCI-H446 MkTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTNwNkizOEDPxE1? M{TDXXNCVkeHUh?=
LB2241-RCC M3jUfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmC0TWM2OD1|Lk[4OlI2KM7:TR?= NXTVW|U5W0GQR1XS
JEG-3 NFXFTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTNwNkmxPUDPxE1? M2j5b3NCVkeHUh?=
LNCaP-Clone-FGC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfQSIpqUUN3ME2zMlcxODRzIN88US=> Mnv2V2FPT0WU
M059J M1G0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTNwN{G0Olgh|ryP M13PcHNCVkeHUh?=
SK-MES-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTNwN{OwN{DPxE1? M1ztXnNCVkeHUh?=
GT3TKB MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[1NmlEPTB;Mz63OVYxPCEQvF2= MnzyV2FPT0WU
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MZ1-PC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDrN5FCUUN3ME2zMlgzQDh|IN88US=> M3jlVnNCVkeHUh?=
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LU-134-A MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfBbJgzUUN3ME2zMlk2PDJ{IN88US=> M1zxN3NCVkeHUh?=
C32 NFLmWYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TPeGlEPTB;Mz65OlU5OSEQvF2= Mlq0V2FPT0WU
MOLT-13 MkHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3jOnBKSzVyPUOuPVY5PTZizszN NHLDXYhUSU6JRWK=
A375 NGficYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrDUmh4UUN3ME20MlA2OTZ{IN88US=> M375TXNCVkeHUh?=
CAL-12T MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVKzNJU{UUN3ME20MlA2Pzl3IN88US=> NGrnToZUSU6JRWK=
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BHT-101 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXToflZtUUN3ME20MlExPjh|IN88US=> NV7pXVlKW0GQR1XS
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EPLC-272H MlHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTRwMUe1PVYh|ryP NXq1dYs{W0GQR1XS
HT-1376 NF;uUmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPjTWM2OD12LkKzNFU6KM7:TR?= NGL1VXZUSU6JRWK=
HCC1954 MkPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTRwMkW3OFYh|ryP NHPuR49USU6JRWK=
KYSE-510 NXXtUYx3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDKe49KSzVyPUSuNlYxQSEQvF2= M3ToV3NCVkeHUh?=
PANC-03-27 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjqVnZKSzVyPUSuN|AxQDNizszN NF;QPFNUSU6JRWK=
MDA-MB-157 MonSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXuwRW1IUUN3ME20MlMxPjV4IN88US=> NYjJT2p{W0GQR1XS
HOP-62 Ml3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XxfGlEPTB;ND6zNFg2PiEQvF2= MYfTRW5ITVJ?
ETK-1 NHXxfVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLEW5BpUUN3ME20MlM3OjB|IN88US=> Mn:zV2FPT0WU
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MHH-PREB-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi5cIVGUUN3ME20MlM6Pzd|IN88US=> MX;TRW5ITVJ?
LXF-289 Mm\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGX2RoFKSzVyPUSuOFAzODJizszN MVjTRW5ITVJ?
ATN-1 M4fFdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7RTWM2OD12LkSyN|QyKM7:TR?= NVzZcIpuW0GQR1XS
8505C MkHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTRwNEW4NlUh|ryP M1fH[XNCVkeHUh?=
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U-266 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXwRoZNUUN3ME20MlYyODN{IN88US=> NFf3VnBUSU6JRWK=
5637 MkHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnOTWM2OD12Lk[xOFQ1KM7:TR?= NETxSGZUSU6JRWK=
GCIY MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1L4PWlEPTB;ND63NVAyPSEQvF2= M1zpTHNCVkeHUh?=
MDA-MB-231 MnvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTJSZJjUUN3ME20MlczOTF3IN88US=> NFq4[|RUSU6JRWK=
RKO MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7VTWM2OD12LkeyPFE4KM7:TR?= Mkf1V2FPT0WU
COR-L23 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTRwN{SyOVYh|ryP Mk\IV2FPT0WU
DJM-1 MkfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4K5S2lEPTB;ND63PVczQSEQvF2= Mn\TV2FPT0WU
D-423MG Mn\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\BdmlEPTB;ND64NFgxOyEQvF2= MWPTRW5ITVJ?
DMS-114 M4G0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTRwOEGzPFYh|ryP NYTyb5FzW0GQR1XS
MHH-ES-1 Mn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv0U3N6UUN3ME20MlgzPTB2IN88US=> M1nq[3NCVkeHUh?=
CAL-51 MoTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTRwOE[4OFMh|ryP MWnTRW5ITVJ?
SW626 NIG3R4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jh[GlEPTB;ND64PVY6PyEQvF2= MXHTRW5ITVJ?
COLO-824 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnVd5p1UUN3ME20MlkxPDB6IN88US=> NVT6XVN7W0GQR1XS
NCI-H1437 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG5U4RuUUN3ME20MlkzQTNizszN M1HJRnNCVkeHUh?=
CAL-39 MkLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLYTWM2OD12LkmzPVg5KM7:TR?= MX3TRW5ITVJ?
PC-3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke3TWM2OD12Lkm0OlQ5KM7:TR?= MljaV2FPT0WU
A101D NV\IWItLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHO[ol1UUN3ME20Mlk3QDZ3IN88US=> NEHKVopUSU6JRWK=
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EFO-27 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrYSItKSzVyPUWuNFY{OjlizszN M1HMe3NCVkeHUh?=
BT-549 MlzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\1UXBUUUN3ME21MlA4PzN4IN88US=> M4\ke3NCVkeHUh?=
HLE Ml3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPjTWM2OD13LkGxO|M1KM7:TR?= NHz0ZWlUSU6JRWK=
SW982 NHm1fplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfpTWM2OD13LkGzN|c1KM7:TR?= MmXxV2FPT0WU
SCC-25 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmS0TWM2OD13LkG5NFQ3KM7:TR?= NVflZZFYW0GQR1XS
SK-MEL-28 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3UZ21KSzVyPUWuNlA{OTNizszN MXTTRW5ITVJ?
CaR-1 M4jyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnsWZZyUUN3ME21MlIxPzJ4IN88US=> MYjTRW5ITVJ?
MLMA MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;2WIZKSzVyPUWuNlM1OzZizszN MULTRW5ITVJ?
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KNS-42 MkL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofSTWM2OD13LkK2NVYh|ryP MonDV2FPT0WU
TK10 NF7KXY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTVwM{[wPFYh|ryP M2LwZXNCVkeHUh?=
MEG-01 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV2xU5NmUUN3ME21MlM3Ojd2IN88US=> NIjNepJUSU6JRWK=
DEL NIG5cXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLkTFFKSzVyPUWuN|kxOjNizszN MXrTRW5ITVJ?
SJRH30 M1zId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHIdG9YUUN3ME21MlM6OjF|IN88US=> Mlr5V2FPT0WU
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KNS-81-FD Mn:yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrTTI5YUUN3ME21MlUxODl{IN88US=> NEnpO4VUSU6JRWK=
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SCH NFjsNZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTVwN{S3Olch|ryP MWLTRW5ITVJ?
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HT-144 NXrFOoFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;mR5BXUUN3ME21Mlg3QDN{IN88US=> MlnwV2FPT0WU
CAL-54 NIO1O4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PYbWlEPTB;NT65N|MyPCEQvF2= M1LJUHNCVkeHUh?=
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GB-1 NGT4VWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTZwMEKwOlgh|ryP NGnjWZZUSU6JRWK=
HSC-2 NV3IT|B{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HOdWlEPTB;Nj6xNlM2OyEQvF2= NYn5eZRZW0GQR1XS
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OMC-1 Mo\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rjdmlEPTB;Nj6zOVQ1OSEQvF2= NV7Ncno2W0GQR1XS
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HT-1080 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTZwNUSwOFIh|ryP M4XWS3NCVkeHUh?=
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OCUB-M MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTZwNkC3O{DPxE1? M3jHS3NCVkeHUh?=
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U-87-MG NGXiSZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[yWoxtUUN3ME22Mlg{QDJ4IN88US=> MVHTRW5ITVJ?
Detroit562 NF7yPHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr3TWM2OD14Lki1PVkyKM7:TR?= NGPJNotUSU6JRWK=
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NOS-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D0XWlEPTB;Nz6yNFQyPSEQvF2= M{KzTnNCVkeHUh?=
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OVCAR-4 MnTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD3TWM2OD15LkW1NlYh|ryP MXrTRW5ITVJ?
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OVCAR-5 M3HES2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmToTWM2OD15LkiyN|I6KM7:TR?= NEPEXnJUSU6JRWK=
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SW780 MlrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRThwMUi4NlEh|ryP M2qzNnNCVkeHUh?=
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NCI-H2228 M4j4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFzLkS5Nlgh|ryP MYHTRW5ITVJ?
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SK-HEP-1 MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF{LkK2NVMh|ryP MYjTRW5ITVJ?
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NCI-H23 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDJWHc1UUN3ME2xNk4{OTJ3IN88US=> Mn[4V2FPT0WU
NCI-H596 NFvnTY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTF{LkS3PVgh|ryP MYHTRW5ITVJ?
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D-247MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq1ZlZkUUN3ME2xOU45PTN|IN88US=> MULTRW5ITVJ?
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LCLC-103H MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;BT4JKSzVyPUG4MlA2OSEQvF2= NIjQbldUSU6JRWK=
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NCI-H1651 Ml\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHMd2xHUUN3ME2yPU45PTB|IN88US=> MnTVV2FPT0WU
OE33 NIP6SIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\xeWlEPTB;M{CuNVM1OiEQvF2= NHrPOXpUSU6JRWK=
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SN12C MoGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzh[WRKSzVyPUOyMlg5OTVizszN NY\RR3ZCW0GQR1XS
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LU-135 M{PnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoThTWM2OD1|Mz63NFg3KM7:TR?= MnPYV2FPT0WU
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NCI-H1755 M1z0VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTN|LkixNUDPxE1? NYHvfI5HW0GQR1XS
Mo-T NHXMd4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1:0d2lEPTB;M{OuPFU6OyEQvF2= NVLlUllxW0GQR1XS
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COLO-680N NH:xeYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjz[WZKSzVyPUO0MlE{QTdizszN M3zCeHNCVkeHUh?=
KURAMOCHI MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf6TWM2OD1|ND62OFI2KM7:TR?= M3XLbHNCVkeHUh?=
NCI-H661 MnfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDBTWM2OD1|ND64OFQ5KM7:TR?= MXHTRW5ITVJ?
YAPC MmrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFq0[FRKSzVyPUO1Mlk2OzNizszN MmrXV2FPT0WU
NCI-H526 M1rBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3YeI1WUUN3ME2zO{4zPzd{IN88US=> Mn3KV2FPT0WU
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RMG-I NEjGWVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvpNINKSzVyPUSyMlQ6OjFizszN MmGxV2FPT0WU
D-336MG MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;6NWlEPTB;NEOuNVE2OiEQvF2= MmrPV2FPT0WU
SHP-77 M4LzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nuR2lEPTB;NEOuNVgzQCEQvF2= M1jUS3NCVkeHUh?=
SW872 NVK4dWpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfte3dKSzVyPUSzMlIyOjNizszN NEmwTphUSU6JRWK=
DBTRG-05MG MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv2TWM2OD12ND62PVk3KM7:TR?= NUHNW5JCW0GQR1XS
COLO-678 M4TNT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fUSGlEPTB;NEWuO|A{OiEQvF2= MlLkV2FPT0WU
EGI-1 NYjSUoVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvzSplKSzVyPUS3MlE5OzNizszN Mkn1V2FPT0WU
KYSE-70 M2XvUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTR5LkeyNlIh|ryP M{nj[3NCVkeHUh?=
BALL-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;iXIlKSzVyPUS3MlgzPTRizszN NXi1c4VlW0GQR1XS
MDA-MB-361 MkW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nDb2lEPTB;NEiuNFQ3KM7:TR?= MlX4V2FPT0WU
NCI-H1838 MoHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37vZWlEPTB;NEiuN|Q2QCEQvF2= MnvoV2FPT0WU
NCI-H1573 NIDtRYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTR6Lk[3PFUh|ryP NGHEUZhUSU6JRWK=
HCC1395 NEDnUmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3K[GtCUUN3ME20PE46QTJizszN NEjpd5NUSU6JRWK=
NCI-H2291 NXHPN4k3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPLTXFEUUN3ME20PU42QTh6IN88US=> MULTRW5ITVJ?
RH-18 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HHeGlEPTB;NUCuNFg5PCEQvF2= MYDTRW5ITVJ?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-GSK3 / p-ERK / ERK / p-CREB / CREB / p-S6 / p-LKB1 / LKB1 ; 

PubMed: 17040210     


(A) HEK-293 cells that had been deprived of serum for 16 h, were incubated in the absence or presence of 10 μM BI-D1870 for the indicated times, then stimulated with 400 ng/ml PMA (TPA) for 20 min. The cells were lysed and the lysates were immunoblotted with the indicated antibodies as described in the Materials and methods section. (B) As in (A), except that cells were incubated for 30 min with the indicated concentrations of BI-D1870 prior to stimulation with PMA. Similar results were obtained in two separate experiments.

p-YB1 / YB1 / p-Bad / Bad / p-RSK / RSK ; 

PubMed: 28415756     


Western Blot analysis of RSK activity (PS102-YB-1, PS112-Bad) of double resistant SKMel28 RR after treatment with increasing concentrations of BI-D1870 for 24 h. GAPDH was detected as a loading control.

IRF4 / MYC / MCL-1 / PARP ; 

PubMed: 25395420     


(B) H929 cells were incubated with BI-D1870 (BI, 3 μM) at indicated time points, followed by immunoblotting analysis. (C) JJN3 cells were incubated with BI-D1870 at indicated doses for 6 hours, followed by immunoblotting analysis.

p-GSK3 / p-ERK / ERK / p-CREB / CREB / p-S6 / p-LKB1 / LKB1; 

PubMed: 17040210     


(A) HEK-293 cells that had been deprived of serum for 16 h, were incubated in the absence or presence of 10 μM BI-D1870 for the indicated times, then stimulated with 400 ng/ml PMA (TPA) for 20 min. The cells were lysed and the lysates were immunoblotted with the indicated antibodies as described in the Materials and methods section. (B) As in (A), except that cells were incubated for 30 min with the indicated concentrations of BI-D1870 prior to stimulation with PMA. Similar results were obtained in two separate experiments.

p-YB1 / YB1 / p-Bad / Bad / p-RSK / RSK ; 

PubMed: 28415756     


Western Blot analysis of RSK activity (P(S102)-YB-1, P(S112)-Bad) of double resistant SKMel28 RR after treatment with increasing concentrations of BI-D1870 for 24 h. GAPDH was detected as a loading control.

IRF4 / MYC / MCL-1 / PARP ; 

PubMed: 25395420     


(B) H929 cells were incubated with BI-D1870 (BI, 3 μM) at indicated time points, followed by immunoblotting analysis. (C) JJN3 cells were incubated with BI-D1870 at indicated doses for 6 hours, followed by immunoblotting analysis.

17040210 28415756 25395420
Immunofluorescence
PDCD4 / F-actin ; 

PubMed: 25002506     


A375 cells treated as in E were imaged using immunofluorescence microscopy. Cells were stained with anti-PDCD4 antibodies to visualize endogenous PDCD4, phalloidin to visualize F-actin, and DAPI to visualize nuclei.

PDCD4 / F-actin ; 

PubMed: 25002506     


A375 cells treated as in (E) were imaged using immunofluorescence microscopy. Cells were stained with anti-PDCD4 antibodies to visualize endogenous PDCD4, phalloidin to visualize F-actin, and DAPI to visualize nuclei.

25002506
Growth inhibition assay
Cell viability; 

PubMed: 28415756     


(D–F) Cell viability (MUH assay) of double resistant melanoma cells after a 72 h-treatment with increasing concentrations of vemurafenib (D), trametinib (E) or vemurafenib and trametinib (F), as well as of BI-D1870 and the combination of MAPK inhibitors and BI-D1870 (n = 6; mean ± SD). Signals were normalized to the DMSO-treated controls.

Cell viability; 

PubMed: 28415756     


(D–F) Cell viability (MUH assay) of double resistant melanoma cells after a 72 h-treatment with increasing concentrations of vemurafenib (D), trametinib (E) or vemurafenib and trametinib (F), as well as of BI-D1870 and the combination of MAPK inhibitors and BI-D1870 (n = 6; mean ± SD). Signals were normalized to the DMSO-treated controls.

28415756

Protocol

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.27 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

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

Chemical Information

Molecular Weight 391.42
Formula

C19H23F2N5O2

CAS No. 501437-28-1
Storage powder
in solvent
Synonyms N/A
Smiles CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C

In vivo Formulation Calculator (Clear solution)

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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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Frequently Asked Questions

  • Question 1:

    BI-D1870 (catalog No.S2843) is found as a racemic mixture?

  • Answer:

    Yes, BI-D1870 (catalog No.S2843) is found as a racemic mixture.

S6 Kinase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID