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 31 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 M{fhVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3z3d2lEPTB;MD6wPFI{OSBizszN MlLnV2FPT0WU
SW756 Ml7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;QNmlEPTB;MD6xOFAzPCBizszN MXPTRW5ITVJ?
CTV-1 MlLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXBUWpmUUN3ME2wMlE3Ozl6IDFOwG0> M1XCd3NCVkeHUh?=
HSC-4 NEDPNHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17CfGlEPTB;MD6xO|E2QCBizszN NF\2TnVUSU6JRWK=
LAMA-84 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLMTWM2OD1yLkK4OlY1KCEQvF2= NWHxVHRFW0GQR1XS
KU812 NV;wXZdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PM[mlEPTB;MD6zOFA3QCBizszN M{HLUnNCVkeHUh?=
HCC1806 M4XObmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfNTVA3UUN3ME2wMlM2OjF4IDFOwG0> MXXTRW5ITVJ?
DOK M4DhXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;xTmxKSzVyPUCuN|c4QDZiIN88US=> NXW3PJJqW0GQR1XS
NCI-H209 M3nVcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzsTWM2OD1yLkSwPFA5KCEQvF2= M3zTRnNCVkeHUh?=
EoL-1-cell NFnTNIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwNEG1O|YhKM7:TR?= MnzNV2FPT0WU
H9 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDjZ3NKSzVyPUCuOFM1PjRiIN88US=> MYjTRW5ITVJ?
EM-2 NIHQZo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwNEO4PUAh|ryP NV3Lb4ZMW0GQR1XS
NCI-H292 MorIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3DZm9JUUN3ME2wMlQ1OTB6IDFOwG0> MYHTRW5ITVJ?
697 MoPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjNXXFnUUN3ME2wMlQ2PjN|IDFOwG0> NF\tcIFUSU6JRWK=
BHT-101 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T0RmlEPTB;MD60OlU6KCEQvF2= NUPxe3JOW0GQR1XS
BE-13 NGfLNpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGxUoFYUUN3ME2wMlQ5PTd{IDFOwG0> NFrLSnBUSU6JRWK=
RS4-11 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL2bFJDUUN3ME2wMlQ5PTh2IDFOwG0> MWXTRW5ITVJ?
IGROV-1 MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwNEi3PVchKM7:TR?= MnHiV2FPT0WU
KE-37 M4r6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXLN|ZKSzVyPUCuOFk2ODliIN88US=> NYHC[XV2W0GQR1XS
BV-173 M3fQN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTXTWM2OD1yLkWwO|kzKCEQvF2= M3HOWHNCVkeHUh?=
MEG-01 NVfVU4tTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\WTWM2OD1yLkWxNlE1KCEQvF2= NUT4cW81W0GQR1XS
LB2241-RCC NF3JO4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTJTWM2OD1yLkWzO|E5KCEQvF2= NFfYS3RUSU6JRWK=
ACHN MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXDZm5LUUN3ME2wMlU1ODZ7IDFOwG0> MV7TRW5ITVJ?
CTB-1 Mln3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moq4TWM2OD1yLkW0PFIhKM7:TR?= MlHEV2FPT0WU
HT-1080 M1zGXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfNbXhKSzVyPUCuOVU{PDliIN88US=> NWnpWIFIW0GQR1XS
CHL-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHjRmtPUUN3ME2wMlU2PDZ3IDFOwG0> NVzUVnNXW0GQR1XS
EW-3 NWryc4cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf0WYlKUUN3ME2wMlU2QTN3IDFOwG0> M4fMWnNCVkeHUh?=
ES1 NXLYWlRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTzbnZnUUN3ME2wMlY4PDl6IDFOwG0> NEW2XlVUSU6JRWK=
KASUMI-1 MlXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{SwN2lEPTB;MD63NlM{KCEQvF2= Mn;WV2FPT0WU
SW13 NID6cmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTBwN{O3PVghKM7:TR?= MoPJV2FPT0WU
A3-KAW NVXQUY1ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HL[2lEPTB;MD63PVIxQCBizszN MlziV2FPT0WU
LB771-HNC NI\BdIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrSZ5ZKSzVyPUCuPFMyODRiIN88US=> M{LlVHNCVkeHUh?=
OC-314 NXXLOllzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILyeXFKSzVyPUCuPFY6PjViIN88US=> MV3TRW5ITVJ?
MLMA Ml60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zBS2lEPTB;MD65NFY4PSBizszN NGHkPJpUSU6JRWK=
KARPAS-45 NIPGblVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDOU4hDUUN3ME2wMlkzPDZ4IDFOwG0> NHT2[IFUSU6JRWK=
CAL-27 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwOUK5NFYhKM7:TR?= NYjI[nR5W0GQR1XS
SK-NEP-1 MnXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXP1d4F6UUN3ME2wMlk4OjR6IDFOwG0> NWjkS29bW0GQR1XS
COR-L105 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7tNHhKSzVyPUGuNFA{QTRiIN88US=> M1PETnNCVkeHUh?=
TI-73 M4PvS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfF[FVKSzVyPUGuNFE3PSBizszN Mne3V2FPT0WU
JVM-3 MnzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jhPGlEPTB;MT6wOVAyPyBizszN M2\DO3NCVkeHUh?=
HAL-01 NHe3V4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFwMEi4NUAh|ryP MUDTRW5ITVJ?
QIMR-WIL M4O3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnWwTWM2OD1zLkC5NFU5KCEQvF2= MlLaV2FPT0WU
HSC-3 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f4WWlEPTB;MT6xNVc5OyBizszN NFjjbG5USU6JRWK=
KY821 Mn\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzCNIo6UUN3ME2xMlE{OzVzIDFOwG0> NY\VSIJ2W0GQR1XS
5637 NFjyOHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HQNGlEPTB;MT6xN|gxOyBizszN MUPTRW5ITVJ?
CAL-33 NGXkO4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL1TWM2OD1zLkG5N|AzKCEQvF2= NFi2cYtUSU6JRWK=
ES4 MoCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFwMkC3PUAh|ryP MkjWV2FPT0WU
BHY MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Th[mlEPTB;MT6yNlg6OiBizszN Mn3wV2FPT0WU
LB1047-RCC M3LOV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzFXVFKSzVyPUGuNlM4QDViIN88US=> Mn3TV2FPT0WU
H4 NFLw[4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTFwMkSyOVUhKM7:TR?= NY[5e5d[W0GQR1XS
RPMI-8866 MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFwMk[xNFYhKM7:TR?= MV\TRW5ITVJ?
HO-1-N-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTFwMk[zOlkhKM7:TR?= M{fX[XNCVkeHUh?=
BB30-HNC NVLPdmR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLBTWM2OD1zLkK4O|E1KCEQvF2= M3vXU3NCVkeHUh?=
PC-14 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXR[41TUUN3ME2xMlI6OjB3IDFOwG0> M1r4UXNCVkeHUh?=
NUGC-3 NF3SWmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHFd2FKSzVyPUGuNlk{PTZiIN88US=> MVLTRW5ITVJ?
A4-Fuk NYTlflBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDhZ5lPUUN3ME2xMlMxPzB2IDFOwG0> NGnMSJdUSU6JRWK=
MHH-NB-11 NV22cXRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nvXWlEPTB;MT6zNVM5OyBizszN NXP0T481W0GQR1XS
KOSC-2 M1;5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFwM{G3O|UhKM7:TR?= NWXOcoVkW0GQR1XS
A498 NVXF[2d2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7DTWM2OD1zLkSwNVE{KCEQvF2= NF3mTHVUSU6JRWK=
KG-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjRc|dKSzVyPUGuOFEzPzNiIN88US=> NY\FZoxHW0GQR1XS
DEL MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33CbWlEPTB;MT60N|Y2PyBizszN MmD2V2FPT0WU
EW-16 MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHyyN4NKSzVyPUGuOFM6PzNiIN88US=> MYrTRW5ITVJ?
BPH-1 NE\JdYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILaPXVKSzVyPUGuOFQ5ODViIN88US=> MUjTRW5ITVJ?
JAR NXL0[pp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LpfmlEPTB;MT60PVM3KCEQvF2= MkfSV2FPT0WU
J-RT3-T3-5 MknES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PpNWlEPTB;MT61NVczOiBizszN MlvjV2FPT0WU
A375 NFL4T5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G1SWlEPTB;MT61NVc4OiBizszN NVvCW5FyW0GQR1XS
SW954 M1fHUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlK4TWM2OD1zLkW1NFA4KCEQvF2= MXrTRW5ITVJ?
Ca9-22 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTFwNU[yOkAh|ryP MXvTRW5ITVJ?
D-566MG NIP5WIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrMTWM2OD1zLkW3NVU2KCEQvF2= M37FOHNCVkeHUh?=
SCC-15 NUHJW|d7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TUVmlEPTB;MT62NVgxPCBizszN MXLTRW5ITVJ?
HD-MY-Z NFrwZ4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDmTWM2OD1zLk[zOVg1KCEQvF2= MmHaV2FPT0WU
HT-1376 NEfWeY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVn3UXY{UUN3ME2xMlY1OzZiIN88US=> MlPkV2FPT0WU
CAL-54 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlizTWM2OD1zLk[1O|A6KCEQvF2= NUS0dIhxW0GQR1XS
ONS-76 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFwNke1OVEhKM7:TR?= NXLKcG9oW0GQR1XS
EFO-27 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\FbWlEPTB;MT62PFkzKCEQvF2= NVLo[WozW0GQR1XS
769-P NXHEbYVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPTfm5HUUN3ME2xMlY6PTl4IDFOwG0> NYLXNoZQW0GQR1XS
MV-4-11 NHnIdmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTFwNkm4OVYhKM7:TR?= Mly0V2FPT0WU
NKM-1 MlPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mom3TWM2OD1zLkexPFAzKCEQvF2= NFqxWXFUSU6JRWK=
LOXIMVI M1\yVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3i3TGlEPTB;MT63OFU6QSBizszN M1zo[XNCVkeHUh?=
KYSE-140 NVq2fVBTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPBVZc4UUN3ME2xMlc2PjV3IDFOwG0> MUXTRW5ITVJ?
ES5 NYjJbmpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTFwOE[3OFchKM7:TR?= NU[ycYd1W0GQR1XS
BB65-RCC M{XUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLXOYpKSzVyPUGuPFk5PDliIN88US=> MU\TRW5ITVJ?
HN M{LD[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP0eIN2UUN3ME2xMlg6QDd2IDFOwG0> NVL6eVgzW0GQR1XS
A101D MkPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnTfZhKSzVyPUGuPVM3OjhiIN88US=> NF\PfVBUSU6JRWK=
LoVo NETsR3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwOUe2O|khKM7:TR?= M1;yfXNCVkeHUh?=
NCI-H526 NUC0RWpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrRUlhKSzVyPUGuPVk{OjViIN88US=> M1roe3NCVkeHUh?=
NCI-H1693 NXfO[ndZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvsTWM2OD1zLkm5PFg5KCEQvF2= MlSwV2FPT0WU
OVCAR-4 NGrqfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJwMEC0N|UhKM7:TR?= NUfaNHl3W0GQR1XS
SK-HEP-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzjTWM2OD1{LkCwO|Q2KCEQvF2= NWDXR4pDW0GQR1XS
C2BBe1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HRZWlEPTB;Mj6wN|M4OiBizszN MoXhV2FPT0WU
MEL-JUSO MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXjNldjUUN3ME2yMlA1PDZ2IDFOwG0> MX7TRW5ITVJ?
MOLT-16 NX\WfWFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWf2booyUUN3ME2yMlA4ODV6IDFOwG0> MlHrV2FPT0WU
NBsusSR M1;5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjxdHVKSzVyPUKuNFk5QDliIN88US=> NILYdJVUSU6JRWK=
TK10 NIjrW5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;YbXczUUN3ME2yMlE{PDV6IDFOwG0> NG\ae3hUSU6JRWK=
CAL-39 M2K5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELmdIlKSzVyPUKuNVQ1QCBizszN MV3TRW5ITVJ?
NCI-H2030 MofnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnVcGQ4UUN3ME2yMlE5QTd|IDFOwG0> MWLTRW5ITVJ?
HCT-116 NX;RXIxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJwMkK5PFQhKM7:TR?= M1fUSXNCVkeHUh?=
HTC-C3 M1TOO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWj6SWpwUUN3ME2yMlI3QDJ2IDFOwG0> NU\BOphQW0GQR1XS
TYK-nu MoLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnkTWM2OD1{LkOwPVA6KCEQvF2= M4Xpe3NCVkeHUh?=
FADU MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXHZndKSzVyPUKuN|IzQTZiIN88US=> MUHTRW5ITVJ?
A431 M{PXNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW5TXNKSzVyPUKuN|cxOjViIN88US=> M1SxPXNCVkeHUh?=
TE-11 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnVVW9OUUN3ME2yMlM5ODF7IDFOwG0> MXXTRW5ITVJ?
CAL-12T M{\6SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTPTWM2OD1{LkSwOFE4KCEQvF2= NF\UZohUSU6JRWK=
DB NID1e2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkP4TWM2OD1{LkSyPFY6KCEQvF2= MlHpV2FPT0WU
L-363 NVXE[4ZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jyfGlEPTB;Mj60N|UxPyBizszN NEjiR2ZUSU6JRWK=
MSTO-211H NFu1epJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnweFRKUUN3ME2yMlY3OzlzIDFOwG0> MknhV2FPT0WU
SK-UT-1 M4DzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\wXGlEPTB;Mj63NVQxPiBizszN M{TYdnNCVkeHUh?=
RPMI-8226 Mn7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;xeYFWUUN3ME2yMlc{OTZ2IDFOwG0> Mn23V2FPT0WU
SF295 M{HZZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTGTWM2OD1{Lke0N|EhKM7:TR?= MkiwV2FPT0WU
OS-RC-2 NViwOoJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ewZWlEPTB;Mj63OlY4OyBizszN MVLTRW5ITVJ?
SK-MEL-24 Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rKUmlEPTB;Mj63PFIzPCBizszN NU\OdFN[W0GQR1XS
COR-L23 Ml\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjDTWM2OD1{Lke5OFY1KCEQvF2= NITNUJRUSU6JRWK=
MHH-PREB-1 M4r5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELTN2NKSzVyPUKuPFAyPjFiIN88US=> M{XzdXNCVkeHUh?=
SK-N-DZ NFfidopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW1TWM2OD1{LkixOlM5KCEQvF2= MoXxV2FPT0WU
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RMG-I MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTN|LkSyPFUhKM7:TR?= MULTRW5ITVJ?
LU-65 M1;0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTN2LkG0NFghKM7:TR?= NGPMdm5USU6JRWK=
GB-1 NI[zbHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vjc2lEPTB;M{WuNFczQSBizszN M1Lh[XNCVkeHUh?=
DU-4475 M37ENWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTN3LkG1OVMhKM7:TR?= NGjjbGVUSU6JRWK=
SBC-5 NHW2bndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi5cWtKUUN3ME2zOk42QTB{IDFOwG0> NWHFem9GW0GQR1XS
OE33 M2\QWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPBXpBKSzVyPUO3Mlc2PzdiIN88US=> Mlr3V2FPT0WU
C8166 MmDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HqRmlEPTB;M{iuOVI3PyBizszN MkDIV2FPT0WU
COLO-684 NGPuXGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHTVWpKSzVyPUO4Mlc1OjhiIN88US=> MX3TRW5ITVJ?
NCI-H1155 NHS0RnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3vTWM2OD1|OT6wOFcyKCEQvF2= Ml\tV2FPT0WU
ATN-1 MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XXTmlEPTB;M{muO|c6OiBizszN MYnTRW5ITVJ?
KARPAS-299 M1j5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fXTWlEPTB;M{muPFM6KCEQvF2= NXLyc2JsW0GQR1XS
KNS-81-FD NUDTXlBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn22TWM2OD12MD6zOlA1KCEQvF2= NUfC[ZpIW0GQR1XS
NCI-H1563 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF61fWdKSzVyPUSxMlUxOzliIN88US=> MVTTRW5ITVJ?
NB14 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojGTWM2OD12Mj63NlY{KCEQvF2= M2TBc3NCVkeHUh?=
COLO-800 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3UPFJKSzVyPUSyMlg2OTdiIN88US=> NIXVNINUSU6JRWK=
MS-1 NXzUd5NOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTR|LkC0PFMhKM7:TR?= MUnTRW5ITVJ?
OVCAR-8 M3nHbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFG5bY5KSzVyPUSzMlY5ODliIN88US=> NVH2b29PW0GQR1XS
SK-PN-DW NX\oR5NxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTR|Lki3O|YhKM7:TR?= MlTuV2FPT0WU
G-402 MlHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDuTWM2OD12Mz65NFA3KCEQvF2= NWLU[2UxW0GQR1XS
NCI-H2291 MkHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUS1VoVwUUN3ME20OE45ODF5IDFOwG0> M2L5Z3NCVkeHUh?=
PC-3 NE\JZmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzrXZpOUUN3ME20OU45ODJ|IDFOwG0> MY\TRW5ITVJ?
NCI-H1581 MoC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTwUmVKSzVyPUS1Mlk5QDliIN88US=> M3Xz[nNCVkeHUh?=
SW1116 NIjCT2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\LSmlEPTB;NEeuNFE5OiBizszN NU\Nd4d4W0GQR1XS
ZR-75-30 MkHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTR5LkCyN|khKM7:TR?= MnnoV2FPT0WU
OCI-AML2 Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTR5LkC5NVghKM7:TR?= MYXTRW5ITVJ?
MDA-MB-231 M2jXc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTR5Lk[yOFkhKM7:TR?= NEHWWHNUSU6JRWK=
ES3 NVfoZYNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjnTWM2OD12OD6zOVI6KCEQvF2= NH3DPVNUSU6JRWK=
NCI-H630 M3zOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3XTWM2OD12OT6xO|QzKCEQvF2= NFPoV4lUSU6JRWK=
OE19 NXjJRoVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTR7LkK5NFIhKM7:TR?= NX7aNIFlW0GQR1XS
NCI-H1573 Ml;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\jTWM2OD12OT62PFYyKCEQvF2= M4jKNnNCVkeHUh?=
EW-1 M1KxN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjROm9iUUN3ME20PU46ODh2IDFOwG0> Ml:3V2FPT0WU

... 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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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*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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03888222 Recruiting Drug: Placebo Oral Tablet|Drug: Bosutinib Oral Tablet Dementia With Lewy Bodies Georgetown University|Alzheimer''s Association April 23 2019 Phase 2
NCT03854903 Recruiting Drug: Palbociclib|Drug: Bosutinib|Drug: Fulvestrant 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
NCT03831776 Recruiting Drug: Bosutinib|Drug: Ropeginterferon Chronic Myeloid Leukemia St. Olavs Hospital|Haukeland University Hospital|Oslo University Hospital|University Hospital of North Norway|Helse Stavanger HF|Henri Mondor University Hospital|Hôpital René Huguenin|Hôpital Mignot Versailles Paris|Uppsala University Hospital|Odense University Hospital March 25 2019 Phase 2
NCT03128411 Active not recruiting Drug: Bosutinib Leukemia Chronic Myelogenous Pfizer May 15 2017 Phase 2
NCT01903733 Active not recruiting Drug: bosutinib Chronic Myeloid Leukemia Pfizer August 28 2013 Not Applicable
NCT01374139 Completed Drug: Bosutinib Philadelphia Chromosome Positive (Ph+) Chronic Myeloid Leukemia (CML) Pfizer August 2011 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID