Bosutinib (SKI-606)

For research use only.

Licensed by Pfizer Catalog No.S1014

59 publications

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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Selleck's Bosutinib (SKI-606) has been cited by 59 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 NV\mN3VpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LuOGlEPTB;MD6wPFI{OSBizszN NV32OppkW0GQR1XS
SW756 MnjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPOTWM2OD1yLkG0NFI1KCEQvF2= NIPWc5BUSU6JRWK=
CTV-1 M3\Dcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXUXGtKSzVyPUCuNVY{QThiIN88US=> M4fhSnNCVkeHUh?=
HSC-4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwMUexOVghKM7:TR?= MkPoV2FPT0WU
LAMA-84 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPY[GRKSzVyPUCuNlg3PjRiIN88US=> MVTTRW5ITVJ?
KU812 MmPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwM{SwOlghKM7:TR?= M2P1WnNCVkeHUh?=
HCC1806 MlvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfDTWM2OD1yLkO1NlE3KCEQvF2= M2i0WnNCVkeHUh?=
DOK MkTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXncmdbUUN3ME2wMlM4Pzh4IDFOwG0> M{DmUXNCVkeHUh?=
NCI-H209 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfvemVjUUN3ME2wMlQxQDB6IDFOwG0> NILpT3FUSU6JRWK=
EoL-1-cell MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{i2Z2lEPTB;MD60NVU4PiBizszN MnrYV2FPT0WU
H9 NXnUd3ZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnDSlhIUUN3ME2wMlQ{PDZ2IDFOwG0> NUTNTmQ3W0GQR1XS
EM-2 Ml\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPoTWM2OD1yLkSzPFkhKM7:TR?= M4K4e3NCVkeHUh?=
NCI-H292 NVLwd5FyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\pPGFYUUN3ME2wMlQ1OTB6IDFOwG0> Mm\DV2FPT0WU
697 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTxTWM2OD1yLkS1OlM{KCEQvF2= NIH3b25USU6JRWK=
BHT-101 NV\QfXFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT4TGtjUUN3ME2wMlQ3PTliIN88US=> NWTMSGRrW0GQR1XS
BE-13 NUD1eW41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz6TWM2OD1yLkS4OVczKCEQvF2= M2rscnNCVkeHUh?=
RS4-11 M2G4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITyRlRKSzVyPUCuOFg2QDRiIN88US=> NXroR25xW0GQR1XS
IGROV-1 MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwNEi3PVchKM7:TR?= M4T1e3NCVkeHUh?=
KE-37 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn6wTWM2OD1yLkS5OVA6KCEQvF2= MkHLV2FPT0WU
BV-173 M1\oemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjGOG82UUN3ME2wMlUxPzl{IDFOwG0> NHXGPJdUSU6JRWK=
MEG-01 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwNUGyNVQhKM7:TR?= MorkV2FPT0WU
LB2241-RCC NYXpNW5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwNUO3NVghKM7:TR?= NVq4OY5xW0GQR1XS
ACHN NF\McWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnj1TWM2OD1yLkW0NFY6KCEQvF2= MoTKV2FPT0WU
CTB-1 M4LQfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzyTWM2OD1yLkW0PFIhKM7:TR?= NEnPXoVUSU6JRWK=
HT-1080 NGnNV4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHYTWM2OD1yLkW1N|Q6KCEQvF2= MVTTRW5ITVJ?
CHL-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ntUWlEPTB;MD61OVQ3PSBizszN MlXYV2FPT0WU
EW-3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwNUW5N|UhKM7:TR?= M17XPXNCVkeHUh?=
ES1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvkSXNKSzVyPUCuOlc1QThiIN88US=> MWjTRW5ITVJ?
KASUMI-1 MkXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjhTWM2OD1yLkeyN|MhKM7:TR?= M13RbnNCVkeHUh?=
SW13 NV;VOZE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEW5NFRKSzVyPUCuO|M4QThiIN88US=> NEDZSWFUSU6JRWK=
A3-KAW M4SwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjQT3pjUUN3ME2wMlc6OjB6IDFOwG0> MlLxV2FPT0WU
LB771-HNC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjmVlRlUUN3ME2wMlg{OTB2IDFOwG0> Mm[1V2FPT0WU
OC-314 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYiyfFNHUUN3ME2wMlg3QTZ3IDFOwG0> NELNSlZUSU6JRWK=
MLMA NUK4UpZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwOUC2O|UhKM7:TR?= Ml70V2FPT0WU
KARPAS-45 NX[1cWxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfESWkxUUN3ME2wMlkzPDZ4IDFOwG0> M{C4SXNCVkeHUh?=
CAL-27 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv6VotKSzVyPUCuPVI6ODZiIN88US=> NUnIeop{W0GQR1XS
SK-NEP-1 NFTwVWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPuTWM2OD1yLkm3NlQ5KCEQvF2= MlTvV2FPT0WU
COR-L105 NXu4eIdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjweJNKSzVyPUGuNFA{QTRiIN88US=> NFP1VHRUSU6JRWK=
TI-73 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXEU4FKSzVyPUGuNFE3PSBizszN M{LBeHNCVkeHUh?=
JVM-3 NUPXeodzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFwMEWwNVchKM7:TR?= Ml7ZV2FPT0WU
HAL-01 NYPFdpl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnziTWM2OD1zLkC4PFEhKM7:TR?= NGP1NWFUSU6JRWK=
QIMR-WIL NUfIPFc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXnTWM2OD1zLkC5NFU5KCEQvF2= MVzTRW5ITVJ?
HSC-3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTFwMUG3PFMhKM7:TR?= NWPvTJN7W0GQR1XS
KY821 NU\QdXhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LXcGlEPTB;MT6xN|M2OSBizszN MoniV2FPT0WU
5637 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzyd4xKSzVyPUGuNVM5ODNiIN88US=> NUHWNmZiW0GQR1XS
CAL-33 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHYfpV1UUN3ME2xMlE6OzB{IDFOwG0> MlPjV2FPT0WU
ES4 M4rvb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHiTWM2OD1zLkKwO|khKM7:TR?= MWTTRW5ITVJ?
BHY MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjBTWM2OD1zLkKyPFkzKCEQvF2= MlHYV2FPT0WU
LB1047-RCC M4W3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFwMkO3PFUhKM7:TR?= MWfTRW5ITVJ?
H4 NFXPVI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzVTWM2OD1zLkK0NlU2KCEQvF2= M3fQRnNCVkeHUh?=
RPMI-8866 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFwMk[xNFYhKM7:TR?= MWfTRW5ITVJ?
HO-1-N-1 M2LLNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLsW4RKSzVyPUGuNlY{PjliIN88US=> MXXTRW5ITVJ?
BB30-HNC M4KyS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jBfGlEPTB;MT6yPFcyPCBizszN MUfTRW5ITVJ?
PC-14 M{fH[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nBNmlEPTB;MT6yPVIxPSBizszN NWfvRplHW0GQR1XS
NUGC-3 NEfRXZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTNTWM2OD1zLkK5N|U3KCEQvF2= MU\TRW5ITVJ?
A4-Fuk M{flNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPZR|dVUUN3ME2xMlMxPzB2IDFOwG0> NFLRUGxUSU6JRWK=
MHH-NB-11 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHVUGw6UUN3ME2xMlMyOzh|IDFOwG0> Mnz2V2FPT0WU
KOSC-2 M{Lz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\n[GlEPTB;MT6zNVc4PSBizszN NIXJbZJUSU6JRWK=
A498 MoCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrTTWM2OD1zLkSwNVE{KCEQvF2= Ml7hV2FPT0WU
KG-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwNEGyO|MhKM7:TR?= NIWzfZdUSU6JRWK=
DEL M17Kb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX3ZY5KSzVyPUGuOFM3PTdiIN88US=> MV\TRW5ITVJ?
EW-16 NX;wO5p5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HodWlEPTB;MT60N|k4OyBizszN MV;TRW5ITVJ?
BPH-1 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPwV|JKSzVyPUGuOFQ5ODViIN88US=> MlPhV2FPT0WU
JAR NF7oXZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFv3PIFKSzVyPUGuOFk{PiBizszN MonqV2FPT0WU
J-RT3-T3-5 M1nPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfjTIR5UUN3ME2xMlUyPzJ{IDFOwG0> NV76ZpBPW0GQR1XS
A375 M3rRT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j6U2lEPTB;MT61NVc4OiBizszN NWLjT5c2W0GQR1XS
SW954 NVviOIhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTFwNUWwNFchKM7:TR?= MVHTRW5ITVJ?
Ca9-22 MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTFwNU[yOkAh|ryP NVfRZldXW0GQR1XS
D-566MG Mk\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\0bmFKSzVyPUGuOVcyPTViIN88US=> MW\TRW5ITVJ?
SCC-15 Mly3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTr[YxKSzVyPUGuOlE5ODRiIN88US=> MVXTRW5ITVJ?
HD-MY-Z M4r6emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fJ[WlEPTB;MT62N|U5PCBizszN MYfTRW5ITVJ?
HT-1376 NHLTN3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULSZ2dEUUN3ME2xMlY1OzZiIN88US=> MXPTRW5ITVJ?
CAL-54 NHuyNYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;KPWtKSzVyPUGuOlU4ODliIN88US=> M1r2b3NCVkeHUh?=
ONS-76 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HGVGlEPTB;MT62O|U2OSBizszN MXfTRW5ITVJ?
EFO-27 NHH5bmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIW2PJVKSzVyPUGuOlg6OiBizszN MU\TRW5ITVJ?
769-P Mme0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwNkm1PVYhKM7:TR?= NWnrTGpJW0GQR1XS
MV-4-11 NW\3clB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFG3RpFKSzVyPUGuOlk5PTZiIN88US=> MUTTRW5ITVJ?
NKM-1 NIfNcZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHsUW1KSzVyPUGuO|E5ODJiIN88US=> MXnTRW5ITVJ?
LOXIMVI NYXVXIJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfyTWM2OD1zLke0OVk6KCEQvF2= MkDBV2FPT0WU
KYSE-140 NX3SOYRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWW2ZmFkUUN3ME2xMlc2PjV3IDFOwG0> M1z4OXNCVkeHUh?=
ES5 NIC0bG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrkWmF7UUN3ME2xMlg3PzR5IDFOwG0> NEPlOIpUSU6JRWK=
BB65-RCC MnPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTBPWFKSzVyPUGuPFk5PDliIN88US=> M1\jU3NCVkeHUh?=
HN M3ruXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXKwSIh4UUN3ME2xMlg6QDd2IDFOwG0> NGLw[W1USU6JRWK=
A101D M2jqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\tZWlEPTB;MT65N|YzQCBizszN NHX6WVJUSU6JRWK=
LoVo NVvENY1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr4NWRlUUN3ME2xMlk4Pjd7IDFOwG0> Ml\nV2FPT0WU
NCI-H526 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPLTWM2OD1zLkm5N|I2KCEQvF2= NFz1OJpUSU6JRWK=
NCI-H1693 MoLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPCelVKSzVyPUGuPVk5QDhiIN88US=> NF3Ncm9USU6JRWK=
OVCAR-4 MmjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrITWM2OD1{LkCwOFM2KCEQvF2= NGj5c25USU6JRWK=
SK-HEP-1 NYnxXYRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HndmlEPTB;Mj6wNFc1PSBizszN MVrTRW5ITVJ?
C2BBe1 M1i3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HpPGlEPTB;Mj6wN|M4OiBizszN NY\2WGx4W0GQR1XS
MEL-JUSO NV3sOZB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX0[GZKSzVyPUKuNFQ1PjRiIN88US=> MWLTRW5ITVJ?
MOLT-16 M2TqeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\MN2lEPTB;Mj6wO|A2QCBizszN NF;LUGlUSU6JRWK=
NBsusSR MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXj1VZllUUN3ME2yMlA6QDh7IDFOwG0> MlfsV2FPT0WU
TK10 NGrY[m1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3DPIVKSzVyPUKuNVM1PThiIN88US=> NWCwOFNKW0GQR1XS
CAL-39 M1O1Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjaTWM2OD1{LkG0OFghKM7:TR?= NH;FSnRUSU6JRWK=
NCI-H2030 MoLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DqPGlEPTB;Mj6xPFk4OyBizszN MoDHV2FPT0WU
HCT-116 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTJwMkK5PFQhKM7:TR?= NEfCWGVUSU6JRWK=
HTC-C3 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfyXWtuUUN3ME2yMlI3QDJ2IDFOwG0> NWLTSZE1W0GQR1XS
TYK-nu NG[2T3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDYOVd6UUN3ME2yMlMxQTB7IDFOwG0> M{L1cnNCVkeHUh?=
FADU NFrPO2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTJwM{KyPVYhKM7:TR?= MWTTRW5ITVJ?
A431 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TqcGlEPTB;Mj6zO|AzPSBizszN NWLVTIVFW0GQR1XS
TE-11 NXrUU5VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonCTWM2OD1{LkO4NFE6KCEQvF2= MVnTRW5ITVJ?
CAL-12T M{S3fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHwWGJKSzVyPUKuOFA1OTdiIN88US=> NVq2eIp[W0GQR1XS
DB NUjIRnFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vNW2lEPTB;Mj60Nlg3QSBizszN NVPGOXVXW0GQR1XS
L-363 NILrXVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnkUYVpUUN3ME2yMlQ{PTB5IDFOwG0> NXLMdFlqW0GQR1XS
MSTO-211H MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\wcGJKSzVyPUKuOlY{QTFiIN88US=> NXKwUG1RW0GQR1XS
SK-UT-1 NHzXZVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;wUXBKSzVyPUKuO|E1ODZiIN88US=> NW\RXnIxW0GQR1XS
RPMI-8226 Mn3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJwN{OxOlQhKM7:TR?= NILG[4NUSU6JRWK=
SF295 NF\LfYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnu4TWM2OD1{Lke0N|EhKM7:TR?= MkCzV2FPT0WU
OS-RC-2 NX3sVHlyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2mxbmlEPTB;Mj63OlY4OyBizszN M2rO[nNCVkeHUh?=
SK-MEL-24 MkfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTJwN{iyNlQhKM7:TR?= NXPOOItsW0GQR1XS
COR-L23 Mnz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;0TWM2OD1{Lke5OFY1KCEQvF2= M{fjb3NCVkeHUh?=
MHH-PREB-1 M1HPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJwOECxOlEhKM7:TR?= M2nQb3NCVkeHUh?=
SK-N-DZ MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLmTWM2OD1{LkixOlM5KCEQvF2= NHzMXppUSU6JRWK=
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RMG-I M{fYSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvFe3ZQUUN3ME2zN{41Ojh3IDFOwG0> MmXHV2FPT0WU
LU-65 MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fuXGlEPTB;M{SuNVQxQCBizszN NHHDVZpUSU6JRWK=
GB-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTsTWM2OD1|NT6wO|I6KCEQvF2= Mn;BV2FPT0WU
DU-4475 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jVO2lEPTB;M{WuNVU2OyBizszN NGnl[3pUSU6JRWK=
SBC-5 MmnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33Y[GlEPTB;M{[uOVkxOiBizszN NGDTWmFUSU6JRWK=
OE33 NFWzcW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPjOlhKSzVyPUO3Mlc2PzdiIN88US=> MnP0V2FPT0WU
C8166 M{HiRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTCTWM2OD1|OD61NlY4KCEQvF2= MW\TRW5ITVJ?
COLO-684 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTvdI5KSzVyPUO4Mlc1OjhiIN88US=> MWPTRW5ITVJ?
NCI-H1155 NYXQdG5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTN7LkC0O|EhKM7:TR?= MV7TRW5ITVJ?
ATN-1 NXTuTlJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fPNGlEPTB;M{muO|c6OiBizszN MWTTRW5ITVJ?
KARPAS-299 MnPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDXTWM2OD1|OT64N|khKM7:TR?= NEfGOXFUSU6JRWK=
KNS-81-FD NY\ET2w{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnrTWM2OD12MD6zOlA1KCEQvF2= NX;XdGpzW0GQR1XS
NCI-H1563 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rzVGlEPTB;NEGuOVA{QSBizszN M2LKcnNCVkeHUh?=
NB14 NVTxb4N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13wSGlEPTB;NEKuO|I3OyBizszN NGnEVGxUSU6JRWK=
COLO-800 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{W0eWlEPTB;NEKuPFUyPyBizszN MULTRW5ITVJ?
MS-1 MmTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnEUXRKSzVyPUSzMlA1QDNiIN88US=> NVHjToRIW0GQR1XS
OVCAR-8 NFe4W4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXiTWM2OD12Mz62PFA6KCEQvF2= M{HUVXNCVkeHUh?=
SK-PN-DW NVrpcoJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn6TWM2OD12Mz64O|c3KCEQvF2= Mmr5V2FPT0WU
G-402 M1rqRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLuTWM2OD12Mz65NFA3KCEQvF2= M37hUHNCVkeHUh?=
NCI-H2291 MkjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT6XYFEUUN3ME20OE45ODF5IDFOwG0> NWPuXYVvW0GQR1XS
PC-3 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTR3LkiwNlMhKM7:TR?= M363fnNCVkeHUh?=
NCI-H1581 NFLRdmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTR3Lkm4PFkhKM7:TR?= MoXXV2FPT0WU
SW1116 MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTR5LkCxPFIhKM7:TR?= NVe3V5VQW0GQR1XS
ZR-75-30 M3i0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\qTmtKSzVyPUS3MlAzOzliIN88US=> MYfTRW5ITVJ?
OCI-AML2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\RUpk2UUN3ME20O{4xQTF6IDFOwG0> NED5WHVUSU6JRWK=
MDA-MB-231 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUP6e2tUUUN3ME20O{43OjR7IDFOwG0> NYDZcJZXW0GQR1XS
ES3 MlT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\mTWM2OD12OD6zOVI6KCEQvF2= MXvTRW5ITVJ?
NCI-H630 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTwdXhKSzVyPUS5MlE4PDJiIN88US=> MU\TRW5ITVJ?
OE19 NI\Dc2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[yTWM2OD12OT6yPVAzKCEQvF2= NF3HTWxUSU6JRWK=
NCI-H1573 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTR7Lk[4OlEhKM7:TR?= NFT0PJdUSU6JRWK=
EW-1 M1z5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jS[GlEPTB;NEmuPVA5PCBizszN MWDTRW5ITVJ?

... 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)
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
Smiles COC1=C(Cl)C=C(Cl)C(=C1)NC2=C(C=NC3=CC(=C(OC)C=C23)OCCCN4CCN(C)CC4)C#N

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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
    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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04258943 Not yet 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 March 20 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 January 2020 Phase 1
NCT03888222 Active not 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.

  • * 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID