Bosutinib (SKI-606)

Licensed by Pfizer Catalog No.S1014

Bosutinib (SKI-606) Chemical Structure

Molecular Weight(MW): 530.45

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.

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Cited by 28 Publications

Purity & Quality Control

Choose Selective Src Inhibitors

Biological Activity

Description Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.
Targets
Abl [2]
(Cell-free assay)
Src [1]
(Cell-free assay)
1 nM 1.2 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB7 NXP6enhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\tb5FSUUN3ME2wMlA5OjNzIDFOwG0> MYLTRW5ITVJ?
SW756 NWnyW4tzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[xTWM2OD1yLkG0NFI1KCEQvF2= NVXDcnJFW0GQR1XS
CTV-1 NFq2[GlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvhR2EyUUN3ME2wMlE3Ozl6IDFOwG0> NFzLSnVUSU6JRWK=
HSC-4 M1exc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\LUlFOUUN3ME2wMlE4OTV6IDFOwG0> M1nFSHNCVkeHUh?=
LAMA-84 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTBwMki2OlQhKM7:TR?= MWjTRW5ITVJ?
KU812 NGnUXlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\rPGlEPTB;MD6zOFA3QCBizszN MkTMV2FPT0WU
HCC1806 NYX4UlRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17G[mlEPTB;MD6zOVIyPiBizszN NWH2TJIxW0GQR1XS
DOK Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rwVmlEPTB;MD6zO|c5PiBizszN NWi1VphiW0GQR1XS
NCI-H209 NED3XmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Ps[mlEPTB;MD60NFgxQCBizszN Mnj1V2FPT0WU
EoL-1-cell NXHlVHRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwNEG1O|YhKM7:TR?= MnrhV2FPT0WU
H9 M37TPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTjW|RKSzVyPUCuOFM1PjRiIN88US=> NInyeFlUSU6JRWK=
EM-2 NUj4NG5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwNEO4PUAh|ryP MkLQV2FPT0WU
NCI-H292 NFXsR4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwNESxNFghKM7:TR?= M{fpbHNCVkeHUh?=
697 MoP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr0UpJ4UUN3ME2wMlQ2PjN|IDFOwG0> MmHyV2FPT0WU
BHT-101 NWHJSHQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7udYlKSzVyPUCuOFY2QSBizszN NG\rSZJUSU6JRWK=
BE-13 NY\tVGVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LRWmlEPTB;MD60PFU4OiBizszN MV;TRW5ITVJ?
RS4-11 Mk\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe5[WhPUUN3ME2wMlQ5PTh2IDFOwG0> NH3Id5JUSU6JRWK=
IGROV-1 NWftb2x7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwNEi3PVchKM7:TR?= MnfQV2FPT0WU
KE-37 M2O5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNEm1NFkhKM7:TR?= NXjaWpE6W0GQR1XS
BV-173 MlXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwNUC3PVIhKM7:TR?= M1u1e3NCVkeHUh?=
MEG-01 NUTNUZM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPDW2xrUUN3ME2wMlUyOjF2IDFOwG0> NFLieZdUSU6JRWK=
LB2241-RCC NHT1XlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfpV|lKSzVyPUCuOVM4OThiIN88US=> NGfod2ZUSU6JRWK=
ACHN MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vxRWlEPTB;MD61OFA3QSBizszN MorNV2FPT0WU
CTB-1 MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{OwVGlEPTB;MD61OFgzKCEQvF2= MnzkV2FPT0WU
HT-1080 MmPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv5WVdpUUN3ME2wMlU2OzR7IDFOwG0> MlfGV2FPT0WU
CHL-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGmwOHFKSzVyPUCuOVU1PjViIN88US=> MlHNV2FPT0WU
EW-3 NY\WfXlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNUW5N|UhKM7:TR?= MW\TRW5ITVJ?
ES1 NFvU[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi4TFRLUUN3ME2wMlY4PDl6IDFOwG0> NXzNNmlIW0GQR1XS
KASUMI-1 NHn2dWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\KW2lEPTB;MD63NlM{KCEQvF2= NYfPUHBiW0GQR1XS
SW13 M4\wN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1m0dWlEPTB;MD63N|c6QCBizszN M2LvbXNCVkeHUh?=
A3-KAW M3TlT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13kfmlEPTB;MD63PVIxQCBizszN MkDaV2FPT0WU
LB771-HNC NYPvc5l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwOEOxNFQhKM7:TR?= M13WcXNCVkeHUh?=
OC-314 NGTDTnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIf4XItKSzVyPUCuPFY6PjViIN88US=> NYjrUm5jW0GQR1XS
MLMA M3jO[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX24ZoIzUUN3ME2wMlkxPjd3IDFOwG0> M{XzbnNCVkeHUh?=
KARPAS-45 NInTcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlK0TWM2OD1yLkmyOFY3KCEQvF2= MXHTRW5ITVJ?
CAL-27 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP2TWM2OD1yLkmyPVA3KCEQvF2= NELvVm5USU6JRWK=
SK-NEP-1 MnvsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFroPXBKSzVyPUCuPVczPDhiIN88US=> NVzkcpVwW0GQR1XS
COR-L105 M1:z[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFwMECzPVQhKM7:TR?= MkDGV2FPT0WU
TI-73 NXiyd202T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LlUmlEPTB;MT6wNVY2KCEQvF2= NXzmeXZ{W0GQR1XS
JVM-3 MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LyfGlEPTB;MT6wOVAyPyBizszN MlvzV2FPT0WU
HAL-01 MnHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1:0O2lEPTB;MT6wPFgyKCEQvF2= NFfVc3NUSU6JRWK=
QIMR-WIL NFTW[oFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoflTWM2OD1zLkC5NFU5KCEQvF2= MYPTRW5ITVJ?
HSC-3 M{XXbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\iWpl6UUN3ME2xMlEyPzh|IDFOwG0> NETmdmNUSU6JRWK=
KY821 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLMcYZKSzVyPUGuNVM{PTFiIN88US=> M1zM[HNCVkeHUh?=
5637 NWDrNYhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTNTWM2OD1zLkGzPFA{KCEQvF2= NHnUZ2xUSU6JRWK=
CAL-33 M1jhN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\YWWlEPTB;MT6xPVMxOiBizszN M3PFUnNCVkeHUh?=
ES4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7MTWM2OD1zLkKwO|khKM7:TR?= NXz4[WZOW0GQR1XS
BHY Mn[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHvTWM2OD1zLkKyPFkzKCEQvF2= M3vrZnNCVkeHUh?=
LB1047-RCC M2C4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXWwcIljUUN3ME2xMlI{Pzh3IDFOwG0> MVLTRW5ITVJ?
H4 NVq2UGZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\tTWM2OD1zLkK0NlU2KCEQvF2= NEHSS21USU6JRWK=
RPMI-8866 NF74UZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v4[GlEPTB;MT6yOlExPiBizszN NYfkWWZrW0GQR1XS
HO-1-N-1 NVXwUJpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Tu[mlEPTB;MT6yOlM3QSBizszN MkfpV2FPT0WU
BB30-HNC NU[zUWF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jOUmlEPTB;MT6yPFcyPCBizszN NYjVW2xRW0GQR1XS
PC-14 Mny4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr4WoZKSzVyPUGuNlkzODViIN88US=> NEj5OHJUSU6JRWK=
NUGC-3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXJNIVKSzVyPUGuNlk{PTZiIN88US=> MlXiV2FPT0WU
A4-Fuk NVLsbIxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTFwM{C3NFQhKM7:TR?= MlzTV2FPT0WU
MHH-NB-11 NXPSdVdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXG[nVKSzVyPUGuN|E{QDNiIN88US=> NYC0NHZNW0GQR1XS
KOSC-2 M1ToNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwM{G3O|UhKM7:TR?= M1f6SHNCVkeHUh?=
A498 M3Lq[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj1TWM2OD1zLkSwNVE{KCEQvF2= MW\TRW5ITVJ?
KG-1 MmSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17rOWlEPTB;MT60NVI4OyBizszN NYH6PYJ1W0GQR1XS
DEL NI[4XFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G2dGlEPTB;MT60N|Y2PyBizszN Mn3pV2FPT0WU
EW-16 NV[0PZpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTFwNEO5O|MhKM7:TR?= M1\DR3NCVkeHUh?=
BPH-1 NF;ubZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTFwNES4NFUhKM7:TR?= NFTQd3NUSU6JRWK=
JAR NU\aV|gzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXZb4FKSzVyPUGuOFk{PiBizszN M2X5PXNCVkeHUh?=
J-RT3-T3-5 NIL5S2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXtZ|dKSzVyPUGuOVE4OjJiIN88US=> NY\2eZE5W0GQR1XS
A375 NV7LWIdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTpRopxUUN3ME2xMlUyPzd{IDFOwG0> NY\HcFhWW0GQR1XS
SW954 NGrISYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{SxXGlEPTB;MT61OVAxPyBizszN MX3TRW5ITVJ?
Ca9-22 M1X5Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fDb2lEPTB;MT61OlI3KCEQvF2= NXvOSmltW0GQR1XS
D-566MG M3vlTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf5TYlKSzVyPUGuOVcyPTViIN88US=> MV7TRW5ITVJ?
SCC-15 M3vncGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTFwNkG4NFQhKM7:TR?= M13CXXNCVkeHUh?=
HD-MY-Z MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3UPIJKSzVyPUGuOlM2QDRiIN88US=> NInvbGJUSU6JRWK=
HT-1376 NX21W3FYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFwNkSzOkAh|ryP MVTTRW5ITVJ?
CAL-54 NUTr[XpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFGzZnFKSzVyPUGuOlU4ODliIN88US=> NWnXc45WW0GQR1XS
ONS-76 M{jUW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{GyeGlEPTB;MT62O|U2OSBizszN NITOemxUSU6JRWK=
EFO-27 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFwNki5NkAh|ryP NGDpNlBUSU6JRWK=
769-P MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIWyUplKSzVyPUGuOlk2QTZiIN88US=> NEHDTXJUSU6JRWK=
MV-4-11 M1TNXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXiTWM2OD1zLk[5PFU3KCEQvF2= MnPuV2FPT0WU
NKM-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP0TWM2OD1zLkexPFAzKCEQvF2= NUH4S3FjW0GQR1XS
LOXIMVI M4WzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFwN{S1PVkhKM7:TR?= MYPTRW5ITVJ?
KYSE-140 NWO0[3VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTFwN{W2OVUhKM7:TR?= MojGV2FPT0WU
ES5 NWmzRZhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17QXWlEPTB;MT64Olc1PyBizszN M3PvdXNCVkeHUh?=
BB65-RCC M37zc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13nSmlEPTB;MT64PVg1QSBizszN M4rlZ3NCVkeHUh?=
HN NGDSbINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;ZVWVJUUN3ME2xMlg6QDd2IDFOwG0> NGfmeplUSU6JRWK=
A101D NFj6em9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnTSYxKSzVyPUGuPVM3OjhiIN88US=> MYTTRW5ITVJ?
LoVo MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzOVmtVUUN3ME2xMlk4Pjd7IDFOwG0> MnjlV2FPT0WU
NCI-H526 NGCySplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwOUmzNlUhKM7:TR?= NFrlU49USU6JRWK=
NCI-H1693 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTFwOUm4PFghKM7:TR?= NVjzPYxmW0GQR1XS
OVCAR-4 M{DUfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHDO4JKSzVyPUKuNFA1OzViIN88US=> MYDTRW5ITVJ?
SK-HEP-1 Ml[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\4OYMxUUN3ME2yMlAxPzR3IDFOwG0> NXzxe45{W0GQR1XS
C2BBe1 NXyz[VBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorOTWM2OD1{LkCzN|czKCEQvF2= NYj3bWJOW0GQR1XS
MEL-JUSO NXe4bWRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTJwMES0OlQhKM7:TR?= NXrKSVlCW0GQR1XS
MOLT-16 MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzrTWM2OD1{LkC3NFU5KCEQvF2= NWHMV5lIW0GQR1XS
NBsusSR NHLhVGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTJwMEm4PFkhKM7:TR?= M4C3THNCVkeHUh?=
TK10 M1XlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJwMUO0OVghKM7:TR?= MUfTRW5ITVJ?
CAL-39 NWH2PFhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH20[|hKSzVyPUKuNVQ1QCBizszN M3zISXNCVkeHUh?=
NCI-H2030 Mme5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJwMUi5O|MhKM7:TR?= MVfTRW5ITVJ?
HCT-116 M{G5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJwMkK5PFQhKM7:TR?= M{fp[XNCVkeHUh?=
HTC-C3 NV\XZpVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jYS2lEPTB;Mj6yOlgzPCBizszN M17QNXNCVkeHUh?=
TYK-nu MkfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnMfoV1UUN3ME2yMlMxQTB7IDFOwG0> MnqxV2FPT0WU
FADU MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnnTWM2OD1{LkOyNlk3KCEQvF2= MUfTRW5ITVJ?
A431 NHfiT4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1GxN2lEPTB;Mj6zO|AzPSBizszN M13ibXNCVkeHUh?=
TE-11 MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFr3bm1KSzVyPUKuN|gxOTliIN88US=> M4Die3NCVkeHUh?=
CAL-12T NF22c2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJwNEC0NVchKM7:TR?= M{j2R3NCVkeHUh?=
DB MojXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{GyPGlEPTB;Mj60Nlg3QSBizszN MV;TRW5ITVJ?
L-363 MkCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\aZlN1UUN3ME2yMlQ{PTB5IDFOwG0> MmWyV2FPT0WU
MSTO-211H MljZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\VW2lEPTB;Mj62OlM6OSBizszN Mn6xV2FPT0WU
SK-UT-1 M4WzeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPETWM2OD1{LkexOFA3KCEQvF2= NIrFeWtUSU6JRWK=
RPMI-8226 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDMTWM2OD1{LkezNVY1KCEQvF2= M13RWnNCVkeHUh?=
SF295 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLXSIVKSzVyPUKuO|Q{OSBizszN NIf0cJJUSU6JRWK=
OS-RC-2 M2Laemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DIRWlEPTB;Mj63OlY4OyBizszN MnfhV2FPT0WU
SK-MEL-24 M2C5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTJwN{iyNlQhKM7:TR?= M1;jfXNCVkeHUh?=
COR-L23 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX23WIRTUUN3ME2yMlc6PDZ2IDFOwG0> M2qxXnNCVkeHUh?=
MHH-PREB-1 NWi1NJM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJwOECxOlEhKM7:TR?= M{jl[HNCVkeHUh?=
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RMG-I M3jtfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTN|LkSyPFUhKM7:TR?= NELwVIlUSU6JRWK=
LU-65 M{S1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknETWM2OD1|ND6xOFA5KCEQvF2= M1jLenNCVkeHUh?=
GB-1 Ml\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmP1TWM2OD1|NT6wO|I6KCEQvF2= NITMNWNUSU6JRWK=
DU-4475 Mn;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLz[3g1UUN3ME2zOU4yPTV|IDFOwG0> NWjWSWg4W0GQR1XS
SBC-5 NGHKUoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPEOIRtUUN3ME2zOk42QTB{IDFOwG0> NGO1XVhUSU6JRWK=
OE33 NH;Ieo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;qVJNKSzVyPUO3Mlc2PzdiIN88US=> M4LuWHNCVkeHUh?=
C8166 NE\6OnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTN6LkWyOlchKM7:TR?= M{fuTHNCVkeHUh?=
COLO-684 MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTN6Lke0NlghKM7:TR?= M3mwenNCVkeHUh?=
NCI-H1155 NWW4d2ZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnm[ItKSzVyPUO5MlA1PzFiIN88US=> MkOyV2FPT0WU
ATN-1 NXi5[ZBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e3cWlEPTB;M{muO|c6OiBizszN MonBV2FPT0WU
KARPAS-299 NYL5cnlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTN7LkizPUAh|ryP M3\SPHNCVkeHUh?=
KNS-81-FD NX6yW2ZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTRyLkO2NFQhKM7:TR?= M121OnNCVkeHUh?=
NCI-H1563 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTRzLkWwN|khKM7:TR?= NWrRSHZyW0GQR1XS
NB14 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjtU|M6UUN3ME20Nk44OjZ|IDFOwG0> MnPrV2FPT0WU
COLO-800 M2q2XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjsbFdKSzVyPUSyMlg2OTdiIN88US=> MVnTRW5ITVJ?
MS-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLWVIRKSzVyPUSzMlA1QDNiIN88US=> NXK2VpVSW0GQR1XS
OVCAR-8 M3zUdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mln1TWM2OD12Mz62PFA6KCEQvF2= NYLS[JdqW0GQR1XS
SK-PN-DW M3uz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7U[nNKSzVyPUSzMlg4PzZiIN88US=> NGLHZXRUSU6JRWK=
G-402 M2\WOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPjTWM2OD12Mz65NFA3KCEQvF2= NXe1RllPW0GQR1XS
NCI-H2291 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTR2LkiwNVchKM7:TR?= NGnCTpBUSU6JRWK=
PC-3 NIfKToFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DCOWlEPTB;NEWuPFAzOyBizszN M2fSNXNCVkeHUh?=
NCI-H1581 NUTGUXV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDrTWM2OD12NT65PFg6KCEQvF2= M1;FTHNCVkeHUh?=
SW1116 NWnteIxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTR5LkCxPFIhKM7:TR?= NX3ZW5pQW0GQR1XS
ZR-75-30 NULDUVc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjNe2pKSzVyPUS3MlAzOzliIN88US=> M37lT3NCVkeHUh?=
OCI-AML2 NXf2eVZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVL0cWpDUUN3ME20O{4xQTF6IDFOwG0> MmD3V2FPT0WU
MDA-MB-231 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Lq[GlEPTB;NEeuOlI1QSBizszN M4nx[3NCVkeHUh?=
ES3 M3XOVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XoVWlEPTB;NEiuN|UzQSBizszN M1[2c3NCVkeHUh?=
NCI-H630 M17pTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTR7LkG3OFIhKM7:TR?= NF3oZWdUSU6JRWK=
OE19 MkfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTR7LkK5NFIhKM7:TR?= MkX1V2FPT0WU
NCI-H1573 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rv[WlEPTB;NEmuOlg3OSBizszN NVm3bYxlW0GQR1XS
EW-1 NXrMeJNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDacJhTUUN3ME20PU46ODh2IDFOwG0> MmDrV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Src / Src / p-c-Abl / c-Abl / p-S6 / S6 / p-ERK / ERK / p-STAT3 / STAT3; 

PubMed: 27903968     


IMR-32, NB-19, SH-SY5Y, and SK-N-AS cells were treated with indicated concentrations of bosutinib for 0-8 hrs and the cells were lysed and subjected to immunoblotting with the indicated antibodies. β-Actin was used as a loading control in all experiments.

p-FAK / FAK / p-Pyk2 / p-p130Cas / p-AKT; 

PubMed: 18483306     


Western blot analysis of MDA-MB-468 whole cell extracts. Cells were treated with SKI-606 or 0.01% DMSO at the indicated concentrations for times up to 3 h prior to extraction. Immunoblots were probed as indicated with antibodies to phospho-Src (pY419), phospho-FAK (pYpY576/577 or pY925), phospho-Pyk2 (pY580), phospho-p130Cas (pY410), phospho-Stat3 (pY705), phospho-Akt (pS473), phospho-MAPK p44/42, beta-catenin, or PARP. Blots were re-probed with total anti-Src, anti-FAK, or anti-Stat3 antibodies, as indicated.

p-ABL / ABL ; 

PubMed: 28199182     


Cells were transfected with human wild-type ABL, and p190 and p210 variants of BCR-ABL, treated with inhibitors for 24 hr and analyzed for activating phosphorylation (p) by immunoblot. Actin and total levels of expressed kinases serve as loading controls. Cells transfected with empty plasmid serve as transfection control. 

27903968 18483306 28199182
Immunofluorescence
p-FAK / p-STAT3 / beta-catenin; 

PubMed: 18483306     


MDA-MB-231 cells were treated with 0.01% DMSO or 1 µM SKI-606 for 48 h then fixed, probed with antibodies to phospho-FAK (pY576/pY577), FAK, phospho-Stat3 (pY705) or beta-catenin as indicated, and stained with DAPI. Images were captured under fluorescence at 40x magnification.

18483306
Growth inhibition assay
Cell viability; 

PubMed: 24812339     


Proliferation curves for bosutinib, gefitinib and sorafenib in (A) H1650 and (B) H1975. 

IC50; 

PubMed: 27903968     


Six NB cell lines, IMR-32, NGP, NB-19, CHLA-255, SH-SY5Y, and SK-N-AS, were treated with increasing concentrations of bosutinib for 48 hrs. Cell viability was measured by performing the Cell Counting Kit-8 (CCK-8) assay.

24812339 27903968
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]

Protocol

Kinase Assay:

[1]

+ Expand

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.
Cell Research:

[2]

+ Expand
  • Cell lines: Abl-MLV, Rat 2, KU812, K562, and MEG-01 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~1 μM
  • Incubation Time: 72 hours
  • Method:

    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.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: Nude female mice injected with K562 cells
  • Formulation: Suspended in 0.5% methocel/0.4% Tween 80
  • Dosages: ~150 mg/kg/day
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.51 mM)
Ethanol 2 mg/mL (3.77 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/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 530.45
Formula

C26H29Cl2N5O3

CAS No. 380843-75-4
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03885830 Not yet recruiting CML Chronic Phase|CML (Chronic Myelogenous Leukemia|CML - Philadelphia Chromosome|Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase UNC Lineberger Comprehensive Cancer Center May 2019 --
NCT03885830 Not yet recruiting CML Chronic Phase|CML (Chronic Myelogenous Leukemia|CML - Philadelphia Chromosome|Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase UNC Lineberger Comprehensive Cancer Center May 2019 --
NCT03888222 Recruiting Dementia With Lewy Bodies Georgetown University|Alzheimer''s Association April 2019 Phase 2
NCT03888222 Recruiting Dementia With Lewy Bodies Georgetown University|Alzheimer''s Association April 2019 Phase 2
NCT03854903 Not yet recruiting Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer March 2019 Phase 1
NCT03854903 Not yet recruiting Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer March 2019 Phase 1

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

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

  • Answer:

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

Src Signaling Pathway Map

Src Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID