Bosutinib

別名:SKI-606

Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.

Bosutinib化学構造

CAS No. 380843-75-4

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 52000 国内在庫あり
JPY 104500 国内在庫あり
JPY 220500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(137)

製品安全説明書

現在のバッチを見る: 純度: 99.94%
99.94

Bosutinib関連製品

シグナル伝達経路

Src阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0043 μM. 26814890
HEK293 Function assay 1 hr Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0127 μM. 29941193
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.128 μM. 30137981
HEK293 Function assay 1 hr Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.133 μM. 29941193
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.14 μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.146 μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.177 μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.195 μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.204 μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.243 μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.278 μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.356 μM. 30137981
Ba/F3 Function assay 48 hrs Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.642 μM. 30137981
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.15 μM. 18485715
HT29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.17 μM. 18485715
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay, IC50 = 3.2 μM. 26814890
HeLa Function assay 4.5 hrs Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50 = 3.85 μM. 29624387
HT29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, IC50 = 3.87 μM. 18485715
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, IC50 = 3.91 μM. 18485715
HT29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, TGI = 6.5 μM. 18485715
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, TGI = 7.66 μM. 18485715
Ramos-2G6-4C10 Growth Inhibition Assay IC50=4.16739 μM SANGER
MN-60 Growth Inhibition Assay IC50=4.10501 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=4.09799 μM SANGER
Mewo Growth Inhibition Assay IC50=4.06361 μM SANGER
U-266 Growth Inhibition Assay IC50=3.97481 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=3.9729 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=3.96997 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=3.96971 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=3.74177 μM SANGER
BT-549 Growth Inhibition Assay IC50=3.67854 μM SANGER
NOS-1 Growth Inhibition Assay IC50=3.64276 μM SANGER
DSH1 Growth Inhibition Assay IC50=3.64122 μM SANGER
SW982 Growth Inhibition Assay IC50=3.58829 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=3.58569 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=3.5729 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=3.49802 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=3.48199 μM SANGER
A427 Growth Inhibition Assay IC50=3.46124 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=3.41812 μM SANGER
C-33-A Growth Inhibition Assay IC50=3.41421 μM SANGER
SCH Growth Inhibition Assay IC50=3.40844 μM SANGER
GMS-10 Growth Inhibition Assay IC50=3.34086 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=3.30172 μM SANGER
HL-60 Growth Inhibition Assay IC50=3.2913 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=3.2901 μM SANGER
ME-180 Growth Inhibition Assay IC50=3.26051 μM SANGER
SW48 Growth Inhibition Assay IC50=3.25486 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=3.24829 μM SANGER
HSC-2 Growth Inhibition Assay IC50=3.22232 μM SANGER
T-24 Growth Inhibition Assay IC50=3.21814 μM SANGER
P30-OHK Growth Inhibition Assay IC50=3.20117 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=3.18418 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=3.17263 μM SANGER
YKG-1 Growth Inhibition Assay IC50=3.14706 μM SANGER
EW-11 Growth Inhibition Assay IC50=3.14277 μM SANGER
8505C Growth Inhibition Assay IC50=3.10301 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=3.00235 μM SANGER
SAS Growth Inhibition Assay IC50=2.99415 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=2.89243 μM SANGER
OMC-1 Growth Inhibition Assay IC50=2.85003 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=2.81638 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=2.80161 μM SANGER
COR-L23 Growth Inhibition Assay IC50=2.79464 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=2.78224 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=2.76673 μM SANGER
SF295 Growth Inhibition Assay IC50=2.7431 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=2.73164 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=2.71406 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=2.66391 μM SANGER
L-363 Growth Inhibition Assay IC50=2.43507 μM SANGER
DB Growth Inhibition Assay IC50=2.42869 μM SANGER
CAL-12T Growth Inhibition Assay IC50=2.40417 μM SANGER
TE-11 Growth Inhibition Assay IC50=2.38019 μM SANGER
A431 Growth Inhibition Assay IC50=2.37025 μM SANGER
FADU Growth Inhibition Assay IC50=2.32296 μM SANGER
TYK-nu Growth Inhibition Assay IC50=2.30909 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=2.26824 μM SANGER
HCT-116 Growth Inhibition Assay IC50=2.22984 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=2.18973 μM SANGER
CAL-39 Growth Inhibition Assay IC50=2.1448 μM SANGER
TK10 Growth Inhibition Assay IC50=2.13458 μM SANGER
NBsusSR Growth Inhibition Assay IC50=2.09889 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=2.07058 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=2.04464 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=2.03372 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=2.00745 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=2.00435 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=1.99888 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=1.99325 μM SANGER
LoVo Growth Inhibition Assay IC50=1.97679 μM SANGER
A101D Growth Inhibition Assay IC50=1.93628 μM SANGER
HN Growth Inhibition Assay IC50=1.89874 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=1.89849 μM SANGER
ES5 Growth Inhibition Assay IC50=1.86747 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=1.75655 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=1.74599 μM SANGER
NKM-1 Growth Inhibition Assay IC50=1.71802 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=1.69856 μM SANGER
769-P Growth Inhibition Assay IC50=1.69596 μM SANGER
EFO-27 Growth Inhibition Assay IC50=1.6892 μM SANGER
ONS-76 Growth Inhibition Assay IC50=1.67551 μM SANGER
CAL-54 Growth Inhibition Assay IC50=1.65709 μM SANGER
HT-1376 Growth Inhibition Assay IC50=1.6436 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=1.63584 μM SANGER
SCC-15 Growth Inhibition Assay IC50=1.61804 μM SANGER
D-566MG Growth Inhibition Assay IC50=1.57155 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=1.5626 μM SANGER
SW954 Growth Inhibition Assay IC50=1.55007 μM SANGER
A375 Growth Inhibition Assay IC50=1.51772 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=1.51722 μM SANGER
JAR Growth Inhibition Assay IC50=1.4936 μM SANGER
BPH-1 Growth Inhibition Assay IC50=1.44805 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.43973 μM SANGER
DEL Growth Inhibition Assay IC50=1.43657 μM SANGER
KG-1 Growth Inhibition Assay IC50=1.41273 μM SANGER
A498 Growth Inhibition Assay IC50=1.40113 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=1.31775 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=1.31383 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=1.30704 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=1.29356 μM SANGER
PC-14 Growth Inhibition Assay IC50=1.29205 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=1.28714 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=1.26369 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=1.26106 μM SANGER
H4 Growth Inhibition Assay IC50=1.24255 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=1.23785 μM SANGER
BHY Growth Inhibition Assay IC50=1.22892 μM SANGER
ES4 Growth Inhibition Assay IC50=1.2079 μM SANGER
CAL-33 Growth Inhibition Assay IC50=1.19302 μM SANGER
5637 Growth Inhibition Assay IC50=1.13803 μM SANGER
KY821 Growth Inhibition Assay IC50=1.13351 μM SANGER
HSC-3 Growth Inhibition Assay IC50=1.11783 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=1.09058 μM SANGER
HAL-01 Growth Inhibition Assay IC50=1.0881 μM SANGER
JVM-3 Growth Inhibition Assay IC50=1.05017 μM SANGER
TI-73 Growth Inhibition Assay IC50=1.0165 μM SANGER
COR-L105 Growth Inhibition Assay IC50=1.00394 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=0.97248 μM SANGER
CAL-27 Growth Inhibition Assay IC50=0.92906 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.92466 μM SANGER
MLMA Growth Inhibition Assay IC50=0.90675 μM SANGER
OC-314 Growth Inhibition Assay IC50=0.86965 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=0.83104 μM SANGER
A3-KAW Growth Inhibition Assay IC50=0.79208 μM SANGER
SW13 Growth Inhibition Assay IC50=0.73798 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=0.7233 μM SANGER
ES1 Growth Inhibition Assay IC50=0.67498 μM SANGER
EW-3 Growth Inhibition Assay IC50=0.55935 μM SANGER
CHL-1 Growth Inhibition Assay IC50=0.55465 μM SANGER
HT-1080 Growth Inhibition Assay IC50=0.55349 μM SANGER
CTB-1 Growth Inhibition Assay IC50=0.5482 μM SANGER
ACHN Growth Inhibition Assay IC50=0.54069 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=0.53718 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.51214 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.50792 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.49509 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=0.48797 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.48584 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.48572 μM SANGER
BHT-101 Growth Inhibition Assay IC50=0.4659 μM SANGER
697 Growth Inhibition Assay IC50=0.45633 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=0.44108 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.4389 μM SANGER
H9 Growth Inhibition Assay IC50=0.43464 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.41576 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=0.40808 μM SANGER
DOK Growth Inhibition Assay IC50=0.37786 μM SANGER
HCC1806 Growth Inhibition Assay IC50=0.35216 μM SANGER
KU812 Growth Inhibition Assay IC50=0.34068 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.28664 μM SANGER
HSC-4 Growth Inhibition Assay IC50=0.17158 μM SANGER
CTV-1 Growth Inhibition Assay IC50=0.16398 μM SANGER
SW756 Growth Inhibition Assay IC50=0.14024 μM SANGER
NB7 Growth Inhibition Assay IC50=0.08231 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=4.18695 μM SANGER
ABC-1 Growth Inhibition Assay IC50=4.23333 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=4.24571 μM SANGER
HOS Growth Inhibition Assay IC50=4.29141 μM SANGER
SN12C Growth Inhibition Assay IC50=4.34244 μM SANGER
NB13 Growth Inhibition Assay IC50=4.37355 μM SANGER
M14 Growth Inhibition Assay IC50=4.48792 μM SANGER
GP5d Growth Inhibition Assay IC50=4.5012 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=4.53612 μM SANGER
D-423MG Growth Inhibition Assay IC50=4.53924 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=4.59559 μM SANGER
MEL-HO Growth Inhibition Assay IC50=4.61261 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=4.62411 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=4.65126 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=4.71291 μM SANGER
HOP-92 Growth Inhibition Assay IC50=4.81379 μM SANGER
MKN1 Growth Inhibition Assay IC50=4.83914 μM SANGER
ML-2 Growth Inhibition Assay IC50=4.85626 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=4.9298 μM SANGER
G-361 Growth Inhibition Assay IC50=5.01003 μM SANGER
HC-1 Growth Inhibition Assay IC50=5.03291 μM SANGER
EW-24 Growth Inhibition Assay IC50=5.04038 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=5.14334 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=5.3428 μM SANGER
HGC-27 Growth Inhibition Assay IC50=5.37682 μM SANGER
TE-12 Growth Inhibition Assay IC50=5.41585 μM SANGER
GT3TKB Growth Inhibition Assay IC50=5.44212 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=5.45986 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=5.46115 μM SANGER
A172 Growth Inhibition Assay IC50=5.54925 μM SANGER
EGI-1 Growth Inhibition Assay IC50=5.58938 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=5.61486 μM SANGER
SW1710 Growth Inhibition Assay IC50=5.69091 μM SANGER
HT-144 Growth Inhibition Assay IC50=5.72685 μM SANGER
PA-1 Growth Inhibition Assay IC50=5.81893 μM SANGER
HCC1937 Growth Inhibition Assay IC50=5.83929 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=5.91121 μM SANGER
K5 Growth Inhibition Assay IC50=6.0517 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=6.07797 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=6.09261 μM SANGER
EKVX Growth Inhibition Assay IC50=6.13501 μM SANGER
ES7 Growth Inhibition Assay IC50=6.16115 μM SANGER
KS-1 Growth Inhibition Assay IC50=6.17993 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=6.18081 μM SANGER
ES8 Growth Inhibition Assay IC50=6.18082 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=6.21816 μM SANGER
T47D Growth Inhibition Assay IC50=6.26457 μM SANGER
A2780 Growth Inhibition Assay IC50=6.37701 μM SANGER
SCC-4 Growth Inhibition Assay IC50=6.43561 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=6.97043 μM SANGER
no-11 Growth Inhibition Assay IC50=7.1641 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=7.16476 μM SANGER
MKN45 Growth Inhibition Assay IC50=7.18699 μM SANGER
SCC-25 Growth Inhibition Assay IC50=7.23414 μM SANGER
ETK-1 Growth Inhibition Assay IC50=7.25514 μM SANGER
COR-L88 Growth Inhibition Assay IC50=7.29319 μM SANGER
8305C Growth Inhibition Assay IC50=7.32492 μM SANGER
Detroit562 Growth Inhibition Assay IC50=7.32506 μM SANGER
SNU-449 Growth Inhibition Assay IC50=7.37651 μM SANGER
A704 Growth Inhibition Assay IC50=7.38278 μM SANGER
D-502MG Growth Inhibition Assay IC50=7.38473 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=7.41458 μM SANGER
CHP-212 Growth Inhibition Assay IC50=7.51896 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=7.59066 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=7.70312 μM SANGER
HCC2218 Growth Inhibition Assay IC50=7.72258 μM SANGER
GCT Growth Inhibition Assay IC50=7.82172 μM SANGER
SW780 Growth Inhibition Assay IC50=7.9906 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=8.0407 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=8.08648 μM SANGER
TE-1 Growth Inhibition Assay IC50=8.11057 μM SANGER
OAW-42 Growth Inhibition Assay IC50=8.25496 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=8.28364 μM SANGER
ECC10 Growth Inhibition Assay IC50=8.28397 μM SANGER
SW1573 Growth Inhibition Assay IC50=8.44465 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=8.59774 μM SANGER
ALL-PO Growth Inhibition Assay IC50=8.66597 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=8.77625 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=8.83001 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=8.83101 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=8.84157 μM SANGER
RCM-1 Growth Inhibition Assay IC50=9.08145 μM SANGER
Daoy Growth Inhibition Assay IC50=9.12028 μM SANGER
HCC1395 Growth Inhibition Assay IC50=9.30896 μM SANGER
786-0 Growth Inhibition Assay IC50=9.36026 μM SANGER
GAMG Growth Inhibition Assay IC50=9.65534 μM SANGER
HCC1954 Growth Inhibition Assay IC50=9.85859 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=9.90371 μM SANGER
SW620 Growth Inhibition Assay IC50=9.95357 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=10.4197 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=10.4248 μM SANGER
NCI-H1666 Growth Inhibition Assay IC50=10.4355 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=10.4753 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=10.6396 μM SANGER
COLO-829 Growth Inhibition Assay IC50=10.8004 μM SANGER
RVH-421 Growth Inhibition Assay IC50=11.152 μM SANGER
A549 Growth Inhibition Assay IC50=11.2478 μM SANGER
DJM-1 Growth Inhibition Assay IC50=11.3833 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=11.7319 μM SANGER
BEN Growth Inhibition Assay IC50=11.7402 μM SANGER
KM12 Growth Inhibition Assay IC50=11.9091 μM SANGER
HuO9 Growth Inhibition Assay IC50=12.0666 μM SANGER
U-2-OS Growth Inhibition Assay IC50=12.0893 μM SANGER
RH-1 Growth Inhibition Assay IC50=12.4472 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=12.5506 μM SANGER
Mo-T Growth Inhibition Assay IC50=12.7307 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=12.7455 μM SANGER
A388 Growth Inhibition Assay IC50=12.7713 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=12.8046 μM SANGER
HEL Growth Inhibition Assay IC50=12.8212 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=12.8874 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=13.0267 μM SANGER
SW626 Growth Inhibition Assay IC50=13.2485 μM SANGER
ES6 Growth Inhibition Assay IC50=13.2512 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=13.8108 μM SANGER
RXF393 Growth Inhibition Assay IC50=13.9927 μM SANGER
HMV-II Growth Inhibition Assay IC50=14.078 μM SANGER
EW-22 Growth Inhibition Assay IC50=14.1502 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=14.564 μM SANGER
COLO-678 Growth Inhibition Assay IC50=14.7271 μM SANGER
HCT-15 Growth Inhibition Assay IC50=14.8855 μM SANGER
HCE-T Growth Inhibition Assay IC50=14.8874 μM SANGER
SF539 Growth Inhibition Assay IC50=15.0643 μM SANGER
AU565 Growth Inhibition Assay IC50=15.2096 μM SANGER
JVM-2 Growth Inhibition Assay IC50=15.2681 μM SANGER
CaR-1 Growth Inhibition Assay IC50=15.4412 μM SANGER
23132-87 Growth Inhibition Assay IC50=15.8495 μM SANGER
A673 Growth Inhibition Assay IC50=15.9636 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=16.029 μM SANGER
TE-9 Growth Inhibition Assay IC50=16.062 μM SANGER
LU-139 Growth Inhibition Assay IC50=16.1823 μM SANGER
GCIY Growth Inhibition Assay IC50=16.1916 μM SANGER
JEG-3 Growth Inhibition Assay IC50=16.25 μM SANGER
RT-112 Growth Inhibition Assay IC50=16.4143 μM SANGER
COLO-680N Growth Inhibition Assay IC50=16.5108 μM SANGER
LU-134-A Growth Inhibition Assay IC50=16.9893 μM SANGER
MFM-223 Growth Inhibition Assay IC50=17.1535 μM SANGER
SF126 Growth Inhibition Assay IC50=17.1701 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=17.2066 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=17.4832 μM SANGER
SCC-9 Growth Inhibition Assay IC50=17.6285 μM SANGER
KNS-62 Growth Inhibition Assay IC50=17.6629 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=17.8149 μM SANGER
D-336MG Growth Inhibition Assay IC50=17.8294 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=18.0183 μM SANGER
EFM-19 Growth Inhibition Assay IC50=18.0577 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=18.1021 μM SANGER
HEC-1 Growth Inhibition Assay IC50=18.2918 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=18.5929 μM SANGER
SF268 Growth Inhibition Assay IC50=18.6702 μM SANGER
COLO-792 Growth Inhibition Assay IC50=18.7997 μM SANGER
HLE Growth Inhibition Assay IC50=18.8331 μM SANGER
A204 Growth Inhibition Assay IC50=18.9164 μM SANGER
CAL-72 Growth Inhibition Assay IC50=19.0877 μM SANGER
U031 Growth Inhibition Assay IC50=19.4909 μM SANGER
FTC-133 Growth Inhibition Assay IC50=19.9304 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=20.3761 μM SANGER
KGN Growth Inhibition Assay IC50=20.4699 μM SANGER
HCC2998 Growth Inhibition Assay IC50=21.3926 μM SANGER
GOTO Growth Inhibition Assay IC50=21.485 μM SANGER
AGS Growth Inhibition Assay IC50=21.8451 μM SANGER
EW-13 Growth Inhibition Assay IC50=22.1022 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=22.1603 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=22.2907 μM SANGER
A2058 Growth Inhibition Assay IC50=22.434 μM SANGER
SH-4 Growth Inhibition Assay IC50=22.7045 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=23.6472 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=23.6911 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=23.7939 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=24.146 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=24.242 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=24.4024 μM SANGER
HCC1187 Growth Inhibition Assay IC50=25.0235 μM SANGER
BALL-1 Growth Inhibition Assay IC50=25.2062 μM SANGER
SBC-1 Growth Inhibition Assay IC50=25.2993 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=25.3551 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=25.6744 μM SANGER
SW1990 Growth Inhibition Assay IC50=25.9655 μM SANGER
DK-MG Growth Inhibition Assay IC50=26.0443 μM SANGER
TE-8 Growth Inhibition Assay IC50=26.0668 μM SANGER
Becker Growth Inhibition Assay IC50=26.1574 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=26.5317 μM SANGER
MKN7 Growth Inhibition Assay IC50=27.7479 μM SANGER
D-392MG Growth Inhibition Assay IC50=27.7694 μM SANGER
NH-12 Growth Inhibition Assay IC50=28.1229 μM SANGER
EW-18 Growth Inhibition Assay IC50=28.2218 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=28.2762 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=28.3566 μM SANGER
BT-20 Growth Inhibition Assay IC50=28.3685 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=28.4838 μM SANGER
HPAF-II Growth Inhibition Assay IC50=28.779 μM SANGER
SW837 Growth Inhibition Assay IC50=29.3385 μM SANGER
647-V Growth Inhibition Assay IC50=29.7003 μM SANGER
J82 Growth Inhibition Assay IC50=29.8013 μM SANGER
MC116 Growth Inhibition Assay IC50=30.0733 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=30.6093 μM SANGER
NB6 Growth Inhibition Assay IC50=31.3629 μM SANGER
CAL-120 Growth Inhibition Assay IC50=32.4317 μM SANGER
U-87-MG Growth Inhibition Assay IC50=33.0251 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=33.0354 μM SANGER
YH-13 Growth Inhibition Assay IC50=33.2535 μM SANGER
RMG-I Growth Inhibition Assay IC50=33.4285 μM SANGER
LU-65 Growth Inhibition Assay IC50=34.1408 μM SANGER
GB-1 Growth Inhibition Assay IC50=35.0729 μM SANGER
DU-4475 Growth Inhibition Assay IC50=35.1553 μM SANGER
SBC-5 Growth Inhibition Assay IC50=36.5902 μM SANGER
OE33 Growth Inhibition Assay IC50=37.7577 μM SANGER
C8166 Growth Inhibition Assay IC50=38.5267 μM SANGER
COLO-684 Growth Inhibition Assay IC50=38.7428 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=39.0471 μM SANGER
ATN-1 Growth Inhibition Assay IC50=39.7792 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=39.839 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=40.3604 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=41.5039 μM SANGER
NB14 Growth Inhibition Assay IC50=42.7263 μM SANGER
COLO-800 Growth Inhibition Assay IC50=42.8517 μM SANGER
MS-1 Growth Inhibition Assay IC50=43.0483 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=43.6809 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=43.8776 μM SANGER
G-402 Growth Inhibition Assay IC50=43.9006 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=44.8017 μM SANGER
PC-3 Growth Inhibition Assay IC50=45.8023 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=45.9889 μM SANGER
SW1116 Growth Inhibition Assay IC50=47.0182 μM SANGER
ZR-75-30 Growth Inhibition Assay IC50=47.0239 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=47.0918 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=47.6249 μM SANGER
ES3 Growth Inhibition Assay IC50=48.3529 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=49.1742 μM SANGER
OE19 Growth Inhibition Assay IC50=49.2902 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=49.6861 μM SANGER
EW-1 Growth Inhibition Assay IC50=49.9084 μM SANGER
fibroblast cells Antiproliferative assay Antiproliferative activity against Src-transformed rat2 fibroblast cells, IC50 = 0.1 μM. 17181170
fibroblast cells Function assay Inhibition of human cSrc-vSrc fusion protein expressed in rat fibroblast cells by ELISA, IC50 = 0.1 μM. 17905586
Ba/F3 Function assay Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay, IC50 = 0.15 μM. 16970400
Ba/F3 Antiproliferative assay Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay, IC50 = 0.2 μM. 16970400
Ba/F3 Function assay Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay, IC50 = 0.2 μM. 16970400
fibroblast cells Function assay Inhibitory concentration against Abl transformed rat fibroblast cells, IC50 = 0.49 μM. 16161995
Ba/F3 Antiproliferative assay Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay, IC50 = 1 μM. 16970400
Ba/F3 Cell death assay Induction of cell death of murine BaF3 cells expressing NPM/ALK L256T mutant by trypan blue exclusion assay 16970400
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
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生物活性

製品説明 Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Targets
S6 kinase [7] ERK [7] STAT3 [7] LCK [1] Abl [2]
(Cell-free assay)
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1 nM
In Vitro
In vitro

Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM. [1] Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation. [2] Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin. [3]

Kinase Assay The Src and Abl kinase assays
The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution.
細胞実験 細胞株 Abl-MLV, Rat 2, KU812, K562, and MEG-01 cells
濃度 Dissolved in DMSO, final concentrations ~1 μM
反応時間 72 hours
実験の流れ

Cells are exposed to various concentrations of Bosutinib for 72 hours. Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts is measured in 96-well ultra-low binding plates treated with Sigmacote to block residual cell attachment. Cell proliferation is measured with MTS or Cell-Glo. For the determination of cell cycle or cell death, cells are prepared for FACS analysis in the CycleTest Plus DNA reagent kit and analyzed on a fluorescence-activated cell sorter flow cytometer.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-ABL / ABL p-FAK / FAK / p-Pyk2 / p-p130Cas / p-AKT p-Src / Src / p-c-Abl / c-Abl / p-S6 / S6 / p-ERK / ERK / p-STAT3 / STAT3 28199182
Immunofluorescence p-FAK / p-STAT3 / beta-catenin 18483306
Growth inhibition assay IC50 Cell viability 27903968
In Vivo
In Vivo

Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively. [1] Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity. [2] As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts. [4]

動物実験 動物モデル Nude female mice injected with K562 cells
投与量 ~150 mg/kg/day
投与経路 Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05363488 Completed
Myeloid Leukemia
Pfizer
October 8 2021 --
NCT04258943 Active not recruiting
Philadelphia Chromosome Positive CML|Accelerated Phase Chronic Myelogenous Leukemia|Blastic Phase Chronic Myelogenous Leukemia|Chronic Phase Chronic Myelogenous Leukemia
Children''s Oncology Group|Erasmus Medical Center|Dutch Childhood Oncology Group|Innovative Therapies for Children with Cancer|Pfizer
April 6 2020 Phase 1|Phase 2
NCT03023319 Completed
Carcinoma Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer
Nagla Abdel Karim|Augusta University
December 10 2019 Phase 1
NCT03888222 Completed
Dementia With Lewy Bodies
Georgetown University|Alzheimer''s Association
April 23 2019 Phase 2
NCT03854903 Active not recruiting
Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer
Georgetown University|Pfizer
April 1 2019 Phase 1

化学情報

分子量 530.45 化学式

C26H29Cl2N5O3

CAS No. 380843-75-4 SDF Download Bosutinib SDFをダウンロードする
Smiles CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (188.51 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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よくある質問(FAQ)

質問1:
Can I give S1014 Bosutinib to mice by oral gavage? If so, how to dissolve the drug?

回答
For oral gavage, S1014 Bosutinib can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension.

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