Bosutinib (SKI-606)

For research use only.

Licensed by Pfizer Catalog No.S1014

77 publications

Bosutinib (SKI-606) Chemical Structure

CAS No. 380843-75-4

Bosutinib (SKI-606) 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.

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Selleck's Bosutinib (SKI-606) has been cited by 77 publications

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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. 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]
()
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 NYPLWFhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrTTWM2OD1yLkC4NlMyKCEQvF2= NHjEPYZUSU6JRWK=
SW756 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYmyRXN[UUN3ME2wMlE1ODJ2IDFOwG0> NF\YdXNUSU6JRWK=
CTV-1 MoHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlyyTWM2OD1yLkG2N|k5KCEQvF2= NYDadWRRW0GQR1XS
HSC-4 NYLzXVJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzlV2hKSzVyPUCuNVcyPThiIN88US=> NVvrZY17W0GQR1XS
LAMA-84 MmDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTUU4JKSzVyPUCuNlg3PjRiIN88US=> MYPTRW5ITVJ?
KU812 NF;lS4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUP2XXJvUUN3ME2wMlM1ODZ6IDFOwG0> MlzPV2FPT0WU
HCC1806 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGW3eYZKSzVyPUCuN|UzOTZiIN88US=> NUH2dIlMW0GQR1XS
DOK NYXIfYZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fTWmlEPTB;MD6zO|c5PiBizszN M3\KfnNCVkeHUh?=
NCI-H209 NV[3[5ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jqWGlEPTB;MD60NFgxQCBizszN M2[4cXNCVkeHUh?=
EoL-1-cell MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTDTWM2OD1yLkSxOVc3KCEQvF2= NFXpZWVUSU6JRWK=
H9 NX\1SoZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwNEO0OlQhKM7:TR?= MkLjV2FPT0WU
EM-2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTBwNEO4PUAh|ryP NIX5RlJUSU6JRWK=
NCI-H292 MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV33XFAyUUN3ME2wMlQ1OTB6IDFOwG0> MVvTRW5ITVJ?
697 M1HGfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\UR25[UUN3ME2wMlQ2PjN|IDFOwG0> NE\OTZVUSU6JRWK=
BHT-101 M{HSOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwNE[1PUAh|ryP MVrTRW5ITVJ?
BE-13 M1jsS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwNEi1O|IhKM7:TR?= MkXqV2FPT0WU
RS4-11 MlvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTaXZZKSzVyPUCuOFg2QDRiIN88US=> M{PXUnNCVkeHUh?=
IGROV-1 NUfYOpNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4W3UGlEPTB;MD60PFc6PyBizszN M{jZenNCVkeHUh?=
KE-37 Mm\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLUTWM2OD1yLkS5OVA6KCEQvF2= MUHTRW5ITVJ?
BV-173 MnKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqyTWM2OD1yLkWwO|kzKCEQvF2= MUHTRW5ITVJ?
MEG-01 NFnzPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH5TWM2OD1yLkWxNlE1KCEQvF2= MkH4V2FPT0WU
LB2241-RCC M3zGeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITMepNKSzVyPUCuOVM4OThiIN88US=> NVHBNFhMW0GQR1XS
ACHN NX;nNXFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwNUSwOlkhKM7:TR?= Mn76V2FPT0WU
CTB-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rvWmlEPTB;MD61OFgzKCEQvF2= NYjRbpdlW0GQR1XS
HT-1080 MlXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPsO5JXUUN3ME2wMlU2OzR7IDFOwG0> MV7TRW5ITVJ?
CHL-1 Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDMSGM2UUN3ME2wMlU2PDZ3IDFOwG0> NH3icmlUSU6JRWK=
EW-3 M3rwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\Kc3RKSzVyPUCuOVU6OzViIN88US=> M{TlVXNCVkeHUh?=
ES1 NXK5UFhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjqZ3VCUUN3ME2wMlY4PDl6IDFOwG0> MWnTRW5ITVJ?
KASUMI-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj2V4NKSzVyPUCuO|I{OyBizszN MVjTRW5ITVJ?
SW13 Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rodWlEPTB;MD63N|c6QCBizszN NYGwNVI6W0GQR1XS
A3-KAW NWG0THZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjPeW1KSzVyPUCuO|kzODhiIN88US=> Mke0V2FPT0WU
LB771-HNC NUfXc4pjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjJSGtKSzVyPUCuPFMyODRiIN88US=> NUfLW5p{W0GQR1XS
OC-314 NYXFXVNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\YTWM2OD1yLki2PVY2KCEQvF2= MXrTRW5ITVJ?
MLMA Mn3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn5doRKSzVyPUCuPVA3PzViIN88US=> MUTTRW5ITVJ?
KARPAS-45 NUj0WFQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrjTWM2OD1yLkmyOFY3KCEQvF2= M3XVTXNCVkeHUh?=
CAL-27 NVzNSFI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHWUpA3UUN3ME2wMlkzQTB4IDFOwG0> MVjTRW5ITVJ?
SK-NEP-1 NWXpe4xQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHnbXFKSzVyPUCuPVczPDhiIN88US=> Mm\1V2FPT0WU
COR-L105 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\jS2lEPTB;MT6wNFM6PCBizszN MVTTRW5ITVJ?
TI-73 M13tSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljxTWM2OD1zLkCxOlUhKM7:TR?= MlTrV2FPT0WU
JVM-3 NFGwWJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTFwMEWwNVchKM7:TR?= Ml\IV2FPT0WU
HAL-01 NYXHWpFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTFwMEi4NUAh|ryP M2W5SXNCVkeHUh?=
QIMR-WIL MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;mTWM2OD1zLkC5NFU5KCEQvF2= M3;0fnNCVkeHUh?=
HSC-3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKxTWM2OD1zLkGxO|g{KCEQvF2= NIXMVG9USU6JRWK=
KY821 M4\XVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLl[2xMUUN3ME2xMlE{OzVzIDFOwG0> MVjTRW5ITVJ?
5637 NInyU3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFwMUO4NFMhKM7:TR?= MWXTRW5ITVJ?
CAL-33 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHhSWtsUUN3ME2xMlE6OzB{IDFOwG0> NIXJVW9USU6JRWK=
ES4 MmrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXNTlQ5UUN3ME2xMlIxPzliIN88US=> MXLTRW5ITVJ?
BHY MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmGwTWM2OD1zLkKyPFkzKCEQvF2= MknkV2FPT0WU
LB1047-RCC MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTtTWM2OD1zLkKzO|g2KCEQvF2= MVfTRW5ITVJ?
H4 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\oTWM2OD1zLkK0NlU2KCEQvF2= NX7Ie5VtW0GQR1XS
RPMI-8866 NF3LNJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPVTWM2OD1zLkK2NVA3KCEQvF2= M4e2WnNCVkeHUh?=
HO-1-N-1 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjLWndKSzVyPUGuNlY{PjliIN88US=> MofXV2FPT0WU
BB30-HNC M4fkPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFwMki3NVQhKM7:TR?= NEfyOZNUSU6JRWK=
PC-14 M4PuW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;CTWM2OD1zLkK5NlA2KCEQvF2= NUn0ZlQzW0GQR1XS
NUGC-3 M{\iN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moq4TWM2OD1zLkK5N|U3KCEQvF2= MYDTRW5ITVJ?
A4-Fuk NVKzeYF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m3SWlEPTB;MT6zNFcxPCBizszN M37nZ3NCVkeHUh?=
MHH-NB-11 M4r0R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3n1RWlEPTB;MT6zNVM5OyBizszN MUTTRW5ITVJ?
KOSC-2 NVzN[3VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTFwM{G3O|UhKM7:TR?= NInqNJJUSU6JRWK=
A498 NGDxNoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPrZml1UUN3ME2xMlQxOTF|IDFOwG0> MlK0V2FPT0WU
KG-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnrb3ZKSzVyPUGuOFEzPzNiIN88US=> M{D5NHNCVkeHUh?=
DEL MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LFcGlEPTB;MT60N|Y2PyBizszN MmnxV2FPT0WU
EW-16 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFwNEO5O|MhKM7:TR?= NX3qSnhkW0GQR1XS
BPH-1 MnrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFwNES4NFUhKM7:TR?= NYLDcIFxW0GQR1XS
JAR MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fJVWlEPTB;MT60PVM3KCEQvF2= MVPTRW5ITVJ?
J-RT3-T3-5 M{PiR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DCOmlEPTB;MT61NVczOiBizszN MljkV2FPT0WU
A375 NIe2NINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn6NoZKSzVyPUGuOVE4PzJiIN88US=> NFrTN2FUSU6JRWK=
SW954 NYPIOVlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLPfYo1UUN3ME2xMlU2ODB5IDFOwG0> Moe3V2FPT0WU
Ca9-22 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmzdWtKSzVyPUGuOVYzPiBizszN MmfWV2FPT0WU
D-566MG NVP6WI5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7HRopKSzVyPUGuOVcyPTViIN88US=> NF\JTIRUSU6JRWK=
SCC-15 Mlv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TOcWlEPTB;MT62NVgxPCBizszN MkPsV2FPT0WU
HD-MY-Z M4[0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXITWM2OD1zLk[zOVg1KCEQvF2= NIG3emNUSU6JRWK=
HT-1376 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWzTWM2OD1zLk[0N|YhKM7:TR?= MXLTRW5ITVJ?
CAL-54 NHG5VXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\ibG5KSzVyPUGuOlU4ODliIN88US=> NGjk[HBUSU6JRWK=
ONS-76 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTFwNke1OVEhKM7:TR?= MnXtV2FPT0WU
EFO-27 NEi5R2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XNVmlEPTB;MT62PFkzKCEQvF2= MoHvV2FPT0WU
769-P MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFwNkm1PVYhKM7:TR?= NIPZ[2lUSU6JRWK=
MV-4-11 NGXsXlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTFwNkm4OVYhKM7:TR?= MYDTRW5ITVJ?
NKM-1 NYrqNYx5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITs[HNKSzVyPUGuO|E5ODJiIN88US=> NV3HSlRUW0GQR1XS
LOXIMVI NFvhOG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwN{S1PVkhKM7:TR?= MnLSV2FPT0WU
KYSE-140 NWe3[ZZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrv[4JwUUN3ME2xMlc2PjV3IDFOwG0> NHe2WHdUSU6JRWK=
ES5 NVTncGlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XlR2lEPTB;MT64Olc1PyBizszN M2PpN3NCVkeHUh?=
BB65-RCC NIewW5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3mzWGlEPTB;MT64PVg1QSBizszN MXrTRW5ITVJ?
HN Ml\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTFwOEm4O|QhKM7:TR?= MUTTRW5ITVJ?
A101D NWDzcIxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j6NmlEPTB;MT65N|YzQCBizszN M1LQUnNCVkeHUh?=
LoVo MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPBSGhKSzVyPUGuPVc3PzliIN88US=> NE[yNXJUSU6JRWK=
NCI-H526 M3\2W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rFSWlEPTB;MT65PVMzPSBizszN MWPTRW5ITVJ?
NCI-H1693 MlO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTFwOUm4PFghKM7:TR?= NXHzdI1DW0GQR1XS
OVCAR-4 NGXIVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInkfnVKSzVyPUKuNFA1OzViIN88US=> NX;PPXN{W0GQR1XS
SK-HEP-1 M4mzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vyVmlEPTB;Mj6wNFc1PSBizszN MkLqV2FPT0WU
C2BBe1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1joO2lEPTB;Mj6wN|M4OiBizszN NVfnN|d2W0GQR1XS
MEL-JUSO MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoGyTWM2OD1{LkC0OFY1KCEQvF2= M3HBV3NCVkeHUh?=
MOLT-16 MnPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTJwMEewOVghKM7:TR?= MoDCV2FPT0WU
NBsusSR M3LpfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTJwMEm4PFkhKM7:TR?= MkK5V2FPT0WU
TK10 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;EXnhEUUN3ME2yMlE{PDV6IDFOwG0> NFLnZmRUSU6JRWK=
CAL-39 NYTlfIt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\qTWM2OD1{LkG0OFghKM7:TR?= NYPZUpBjW0GQR1XS
NCI-H2030 NVfEbHZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJwMUi5O|MhKM7:TR?= M37IOHNCVkeHUh?=
HCT-116 MmPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTJwMkK5PFQhKM7:TR?= MWHTRW5ITVJ?
HTC-C3 M3;PVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr0TWM2OD1{LkK2PFI1KCEQvF2= M4Hle3NCVkeHUh?=
TYK-nu NIK1cphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTJwM{C5NFkhKM7:TR?= NXfvWnJQW0GQR1XS
FADU NFzOOWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDuR4pKSzVyPUKuN|IzQTZiIN88US=> NXP5RlBPW0GQR1XS
A431 MnPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLlPWFYUUN3ME2yMlM4ODJ3IDFOwG0> M1\RS3NCVkeHUh?=
TE-11 MnfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTnTWM2OD1{LkO4NFE6KCEQvF2= NHLX[llUSU6JRWK=
CAL-12T MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fMfmlEPTB;Mj60NFQyPyBizszN NYjFPXVQW0GQR1XS
DB NGrScJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NID6UlNKSzVyPUKuOFI5PjliIN88US=> Mn3jV2FPT0WU
L-363 MojuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PSNGlEPTB;Mj60N|UxPyBizszN M1fZR3NCVkeHUh?=
MSTO-211H NIXPbFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfONWxXUUN3ME2yMlY3OzlzIDFOwG0> NFnqco5USU6JRWK=
SK-UT-1 NX60UZo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTJwN{G0NFYhKM7:TR?= NWLCS3pkW0GQR1XS
RPMI-8226 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fUcWlEPTB;Mj63N|E3PCBizszN NWflTZBOW0GQR1XS
SF295 NEC2S|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfPbHlOUUN3ME2yMlc1OzFiIN88US=> NYDX[GU1W0GQR1XS
OS-RC-2 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPBV4lKSzVyPUKuO|Y3PzNiIN88US=> Ml\SV2FPT0WU
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COR-L23 M{XiTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\6TWM2OD1{Lke5OFY1KCEQvF2= NETWcFVUSU6JRWK=
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CAL-120 NXnrN|A2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7Td|JKSzVyPUOyMlQ{OTdiIN88US=> MV3TRW5ITVJ?
U-87-MG MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfkTWM2OD1|Mz6wNlUyKCEQvF2= NHHFcpBUSU6JRWK=
NCI-H1304 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DyfmlEPTB;M{OuNFM2PCBizszN NU[0eJNzW0GQR1XS
YH-13 NWrFS|VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTN|LkK1N|UhKM7:TR?= NXXOe|hvW0GQR1XS
RMG-I MnfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jzXGlEPTB;M{OuOFI5PSBizszN MWLTRW5ITVJ?
LU-65 Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\GVGRKSzVyPUO0MlE1ODhiIN88US=> MmjRV2FPT0WU
GB-1 NWjLbotOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXHUG5KSzVyPUO1MlA4OjliIN88US=> NUjpSW5PW0GQR1XS
DU-4475 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPKTWM2OD1|NT6xOVU{KCEQvF2= MULTRW5ITVJ?
SBC-5 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\tZ4ZKSzVyPUO2MlU6ODJiIN88US=> NY\vO4N7W0GQR1XS
OE33 MlnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVH5NHV7UUN3ME2zO{44PTd5IDFOwG0> MUfTRW5ITVJ?
C8166 NXj4dndFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTN6LkWyOlchKM7:TR?= NXPETFBlW0GQR1XS
COLO-684 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLFTWM2OD1|OD63OFI5KCEQvF2= NYrvToozW0GQR1XS
NCI-H1155 NETIempIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;uOmFKSzVyPUO5MlA1PzFiIN88US=> M4T5bHNCVkeHUh?=
ATN-1 MnXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTEcpVKSzVyPUO5Mlc4QTJiIN88US=> NE\y[XRUSU6JRWK=
KARPAS-299 MkX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTCUG82UUN3ME2zPU45OzliIN88US=> M{n4XnNCVkeHUh?=
KNS-81-FD NVjROHl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTRyLkO2NFQhKM7:TR?= M{nTTXNCVkeHUh?=
NCI-H1563 M1rycmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PyOmlEPTB;NEGuOVA{QSBizszN MWjTRW5ITVJ?
NB14 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLhW2N4UUN3ME20Nk44OjZ|IDFOwG0> Mn;RV2FPT0WU
COLO-800 NFHIXG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTR{Lki1NVchKM7:TR?= NF7rUIZUSU6JRWK=
MS-1 NYO5PHh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHvNY17UUN3ME20N{4xPDh|IDFOwG0> NVHFdI5lW0GQR1XS
OVCAR-8 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPjVFdKSzVyPUSzMlY5ODliIN88US=> MlnWV2FPT0WU
SK-PN-DW MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHocIdKSzVyPUSzMlg4PzZiIN88US=> MYnTRW5ITVJ?
G-402 NV[0cZJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD1NW1wUUN3ME20N{46ODB4IDFOwG0> M1rldXNCVkeHUh?=
NCI-H2291 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zzbWlEPTB;NESuPFAyPyBizszN M4joZXNCVkeHUh?=
PC-3 NIDWdmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDCb3hkUUN3ME20OU45ODJ|IDFOwG0> Ml74V2FPT0WU
NCI-H1581 M4fqSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnH1TWM2OD12NT65PFg6KCEQvF2= MXPTRW5ITVJ?
SW1116 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vRV2lEPTB;NEeuNFE5OiBizszN M4fxO3NCVkeHUh?=
ZR-75-30 NGH6T|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTR5LkCyN|khKM7:TR?= MojPV2FPT0WU
OCI-AML2 NV\FW|ZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PQZWlEPTB;NEeuNFkyQCBizszN MmjiV2FPT0WU
MDA-MB-231 NIL2elFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTR5Lk[yOFkhKM7:TR?= MW\TRW5ITVJ?
ES3 MmroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjOXWpbUUN3ME20PE4{PTJ7IDFOwG0> M4La[3NCVkeHUh?=
NCI-H630 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4P1WWlEPTB;NEmuNVc1OiBizszN M1\TOnNCVkeHUh?=
OE19 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr0fYhKSzVyPUS5MlI6ODJiIN88US=> Mm\WV2FPT0WU
NCI-H1573 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\DTWM2OD12OT62PFYyKCEQvF2= NYPRO3dYW0GQR1XS
EW-1 M3H4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPyTWM2OD12OT65NFg1KCEQvF2= M4G5UHNCVkeHUh?=

... 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]

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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]

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  • 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]

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  • Animal Models: Nude female mice injected with K562 cells
  • Dosages: ~150 mg/kg/day
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.51 mM)
Water Insoluble
Ethanol ''''2 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+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
Smiles CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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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    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):
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    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
NCT04258943 Recruiting Drug: Bosutinib Philadelphia Chromosome Positive CML|Accelerated Phase Chronic Myelogenous Leukemia|Blastic Phase Chronic Myelogenous Leukemia|Chronic Phase Chronic Myelogenous Leukemia Children''s Oncology Group|Erasmus MC|Dutch Childhood Oncology Group- Early Clinical Trial Consortium|Innovative Therapies for Children with Cancer|Pfizer April 6 2020 Phase 1|Phase 2
NCT03023319 Recruiting Drug: Bosutinib|Drug: Pemetrexed 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 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

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.

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID