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 47 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 M1HpRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PEdGlEPTB;MD6wPFI{OSBizszN NECycIdUSU6JRWK=
SW756 M3XCeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPXTJdTUUN3ME2wMlE1ODJ2IDFOwG0> NXP2XmJyW0GQR1XS
CTV-1 NHLTR45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwMU[zPVghKM7:TR?= MnjsV2FPT0WU
HSC-4 MlyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfIXWUyUUN3ME2wMlE4OTV6IDFOwG0> MVjTRW5ITVJ?
LAMA-84 M{i2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37YVmlEPTB;MD6yPFY3PCBizszN NEnXPXZUSU6JRWK=
KU812 M4DhR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfXdmhYUUN3ME2wMlM1ODZ6IDFOwG0> Mk\YV2FPT0WU
HCC1806 NEnTSFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{S4[GlEPTB;MD6zOVIyPiBizszN MWfTRW5ITVJ?
DOK NXrK[5BFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnryTWM2OD1yLkO3O|g3KCEQvF2= MnrpV2FPT0WU
NCI-H209 MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwNEC4NFghKM7:TR?= NFrkTolUSU6JRWK=
EoL-1-cell NW[0eo56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwNEG1O|YhKM7:TR?= M{LEW3NCVkeHUh?=
H9 NV;uXoY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3RTWM2OD1yLkSzOFY1KCEQvF2= MXzTRW5ITVJ?
EM-2 M2jaPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17WPGlEPTB;MD60N|g6KCEQvF2= MYPTRW5ITVJ?
NCI-H292 NInvWWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjlTWM2OD1yLkS0NVA5KCEQvF2= M2rIW3NCVkeHUh?=
697 NXnwRoFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof5TWM2OD1yLkS1OlM{KCEQvF2= MnXPV2FPT0WU
BHT-101 NX7EcYROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwNE[1PUAh|ryP MnvRV2FPT0WU
BE-13 NHjiU5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTiTWM2OD1yLkS4OVczKCEQvF2= NYrqdWo4W0GQR1XS
RS4-11 M1PnTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP3RpM4UUN3ME2wMlQ5PTh2IDFOwG0> Ml\iV2FPT0WU
IGROV-1 MlWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlruTWM2OD1yLkS4O|k4KCEQvF2= NV7zUmdSW0GQR1XS
KE-37 NH\I[2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnGc2pKSzVyPUCuOFk2ODliIN88US=> M4\MbHNCVkeHUh?=
BV-173 M1yxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwNUC3PVIhKM7:TR?= MnXuV2FPT0WU
MEG-01 M{TNdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LBZmlEPTB;MD61NVIyPCBizszN NYPz[oJCW0GQR1XS
LB2241-RCC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrEd2xKSzVyPUCuOVM4OThiIN88US=> M4TSdXNCVkeHUh?=
ACHN MnjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PEUWlEPTB;MD61OFA3QSBizszN MmnrV2FPT0WU
CTB-1 M1zqSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYW1cGNvUUN3ME2wMlU1QDJiIN88US=> MWTTRW5ITVJ?
HT-1080 Mmi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnFTWM2OD1yLkW1N|Q6KCEQvF2= MXnTRW5ITVJ?
CHL-1 NE\yZppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV6xVIo3UUN3ME2wMlU2PDZ3IDFOwG0> NU\VTG8yW0GQR1XS
EW-3 Mm\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwNUW5N|UhKM7:TR?= MX7TRW5ITVJ?
ES1 NGixfHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jZU2lEPTB;MD62O|Q6QCBizszN NHj6eIlUSU6JRWK=
KASUMI-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvaTWM2OD1yLkeyN|MhKM7:TR?= M1v2U3NCVkeHUh?=
SW13 NGLaUJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjGZXhKSzVyPUCuO|M4QThiIN88US=> NHXl[5VUSU6JRWK=
A3-KAW MmDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnJSoJKSzVyPUCuO|kzODhiIN88US=> NFq3TlJUSU6JRWK=
LB771-HNC NHLBUWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\EZmlEPTB;MD64N|ExPCBizszN NELRb45USU6JRWK=
OC-314 MnnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXroOZU2UUN3ME2wMlg3QTZ3IDFOwG0> MmCxV2FPT0WU
MLMA MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjhdZhpUUN3ME2wMlkxPjd3IDFOwG0> NHS4OpFUSU6JRWK=
KARPAS-45 NWL0RYxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjpTWM2OD1yLkmyOFY3KCEQvF2= MU\TRW5ITVJ?
CAL-27 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoT0TWM2OD1yLkmyPVA3KCEQvF2= NFzUdGpUSU6JRWK=
SK-NEP-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW4bZZjUUN3ME2wMlk4OjR6IDFOwG0> M3HDbnNCVkeHUh?=
COR-L105 NWXmNFRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjHTWM2OD1zLkCwN|k1KCEQvF2= MV3TRW5ITVJ?
TI-73 Mnu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T0c2lEPTB;MT6wNVY2KCEQvF2= NVfxXJBnW0GQR1XS
JVM-3 NVvtO5A4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\WTWM2OD1zLkC1NFE4KCEQvF2= NGC0N2xUSU6JRWK=
HAL-01 MnL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVKyTnM3UUN3ME2xMlA5QDFiIN88US=> M{jqfnNCVkeHUh?=
QIMR-WIL NFvuR4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfPdVRLUUN3ME2xMlA6ODV6IDFOwG0> MorVV2FPT0WU
HSC-3 NH3jUGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLaV|B6UUN3ME2xMlEyPzh|IDFOwG0> MnjVV2FPT0WU
KY821 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnJVmtWUUN3ME2xMlE{OzVzIDFOwG0> M2CwNnNCVkeHUh?=
5637 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MluyTWM2OD1zLkGzPFA{KCEQvF2= NXXKd4JNW0GQR1XS
CAL-33 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3L0fGlEPTB;MT6xPVMxOiBizszN MVTTRW5ITVJ?
ES4 NU\W[G1VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFwMkC3PUAh|ryP MoXSV2FPT0WU
BHY NEn0UFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfqUWNKSzVyPUGuNlI5QTJiIN88US=> MojCV2FPT0WU
LB1047-RCC NHG3WWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu5eYx7UUN3ME2xMlI{Pzh3IDFOwG0> NHvtc|NUSU6JRWK=
H4 M{\EW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFwMkSyOVUhKM7:TR?= MXnTRW5ITVJ?
RPMI-8866 M2LN[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4mwZ2lEPTB;MT6yOlExPiBizszN MoL0V2FPT0WU
HO-1-N-1 NWjkTlVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\KcmlEPTB;MT6yOlM3QSBizszN NV7TWol7W0GQR1XS
BB30-HNC NGnlNnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TGVWlEPTB;MT6yPFcyPCBizszN NEHQem9USU6JRWK=
PC-14 M3ryW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17ZTWlEPTB;MT6yPVIxPSBizszN M2D0dnNCVkeHUh?=
NUGC-3 M{WzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkL2TWM2OD1zLkK5N|U3KCEQvF2= MmP1V2FPT0WU
A4-Fuk MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\NWGFKSzVyPUGuN|A4ODRiIN88US=> NFX4dnNUSU6JRWK=
MHH-NB-11 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHiTWM2OD1zLkOxN|g{KCEQvF2= MX;TRW5ITVJ?
KOSC-2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LUcWlEPTB;MT6zNVc4PSBizszN MofWV2FPT0WU
A498 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXQW5pKSzVyPUGuOFAyOTNiIN88US=> NVPGVFZWW0GQR1XS
KG-1 NXrEbGtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTFwNEGyO|MhKM7:TR?= NF\rNmpUSU6JRWK=
DEL NGjad4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwNEO2OVchKM7:TR?= MmHpV2FPT0WU
EW-16 NWXNdJVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XVPWlEPTB;MT60N|k4OyBizszN NUTSO4pVW0GQR1XS
BPH-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\vRXNKSzVyPUGuOFQ5ODViIN88US=> NVnQd4J4W0GQR1XS
JAR NIrzTWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\PTWM2OD1zLkS5N|YhKM7:TR?= NXnu[lBwW0GQR1XS
J-RT3-T3-5 M33CXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjDSJRUUUN3ME2xMlUyPzJ{IDFOwG0> MnfCV2FPT0WU
A375 M3fmZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDzTWM2OD1zLkWxO|czKCEQvF2= MX;TRW5ITVJ?
SW954 NF\MblFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnrO2ZKSzVyPUGuOVUxODdiIN88US=> MojZV2FPT0WU
Ca9-22 NHfLe|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnUVY5xUUN3ME2xMlU3OjZiIN88US=> Ml\RV2FPT0WU
D-566MG NV3Se2ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DET2lEPTB;MT61O|E2PSBizszN MmK3V2FPT0WU
SCC-15 MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPNTWM2OD1zLk[xPFA1KCEQvF2= M33FdnNCVkeHUh?=
HD-MY-Z MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPNTWM2OD1zLk[zOVg1KCEQvF2= M3nMcHNCVkeHUh?=
HT-1376 NXrrR2Y3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXTc5N1UUN3ME2xMlY1OzZiIN88US=> NGTRNHZUSU6JRWK=
CAL-54 NH3nRoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwNkW3NFkhKM7:TR?= NXO1PHFxW0GQR1XS
ONS-76 NFn0NIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfaOHFKSzVyPUGuOlc2PTFiIN88US=> MV7TRW5ITVJ?
EFO-27 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTFwNki5NkAh|ryP NV;vbnBmW0GQR1XS
769-P MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XiTGlEPTB;MT62PVU6PiBizszN M1;SNXNCVkeHUh?=
MV-4-11 NHS1T4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLkepFKSzVyPUGuOlk5PTZiIN88US=> NYOzem9WW0GQR1XS
NKM-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHMTWM2OD1zLkexPFAzKCEQvF2= MXHTRW5ITVJ?
LOXIMVI MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTFwN{S1PVkhKM7:TR?= Ml;kV2FPT0WU
KYSE-140 MoSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTFwN{W2OVUhKM7:TR?= NFftPHVUSU6JRWK=
ES5 M2myVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwOE[3OFchKM7:TR?= MmO5V2FPT0WU
BB65-RCC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvNTWM2OD1zLki5PFQ6KCEQvF2= NEK3WFdUSU6JRWK=
HN MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLoUJBSUUN3ME2xMlg6QDd2IDFOwG0> MnT3V2FPT0WU
A101D MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzSTnpKSzVyPUGuPVM3OjhiIN88US=> MYDTRW5ITVJ?
LoVo NVrSVXdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFwOUe2O|khKM7:TR?= NW[yO|RHW0GQR1XS
NCI-H526 M3fiNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFwOUmzNlUhKM7:TR?= NXP4R|B2W0GQR1XS
NCI-H1693 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvlXlRKSzVyPUGuPVk5QDhiIN88US=> MmjHV2FPT0WU
OVCAR-4 MlrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWf2cGJ[UUN3ME2yMlAxPDN3IDFOwG0> M{e5RXNCVkeHUh?=
SK-HEP-1 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIK2To5KSzVyPUKuNFA4PDViIN88US=> NEjLW4lUSU6JRWK=
C2BBe1 M1rFOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vaXWlEPTB;Mj6wN|M4OiBizszN M2r1ZXNCVkeHUh?=
MEL-JUSO NInZSYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHnb2RKSzVyPUKuNFQ1PjRiIN88US=> NH;INlNUSU6JRWK=
MOLT-16 MnnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NID0fIRKSzVyPUKuNFcxPThiIN88US=> Mn;EV2FPT0WU
NBsusSR NGq2NGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmP6TWM2OD1{LkC5PFg6KCEQvF2= Ml:4V2FPT0WU
TK10 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTJwMUO0OVghKM7:TR?= NWK2UnNxW0GQR1XS
CAL-39 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nTcmlEPTB;Mj6xOFQ5KCEQvF2= MmTKV2FPT0WU
NCI-H2030 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCyTWM2OD1{LkG4PVc{KCEQvF2= NVHjWVZJW0GQR1XS
HCT-116 NUHVeW9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJwMkK5PFQhKM7:TR?= M2DJVnNCVkeHUh?=
HTC-C3 NWLMZXJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;v[Y9KSzVyPUKuNlY5OjRiIN88US=> NE\zNYhUSU6JRWK=
TYK-nu M1\HT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{n5XWlEPTB;Mj6zNFkxQSBizszN M4fTPXNCVkeHUh?=
FADU MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvwZVJKSzVyPUKuN|IzQTZiIN88US=> NIKye3VUSU6JRWK=
A431 M4rvTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXZTWM2OD1{LkO3NFI2KCEQvF2= NEfwdppUSU6JRWK=
TE-11 MmfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFj0NoZKSzVyPUKuN|gxOTliIN88US=> M3jMXnNCVkeHUh?=
CAL-12T NVvSOFYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnKN41tUUN3ME2yMlQxPDF5IDFOwG0> NGTpdm1USU6JRWK=
DB MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\wTWM2OD1{LkSyPFY6KCEQvF2= M3PaSXNCVkeHUh?=
L-363 NF75RVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1S0PGlEPTB;Mj60N|UxPyBizszN M3X1ZXNCVkeHUh?=
MSTO-211H NXjmOXF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXkWFZKSzVyPUKuOlY{QTFiIN88US=> MWTTRW5ITVJ?
SK-UT-1 NVfnTZA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVntNGRyUUN3ME2yMlcyPDB4IDFOwG0> NVTnR4U6W0GQR1XS
RPMI-8226 NFPO[mFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTJwN{OxOlQhKM7:TR?= NH7INVBUSU6JRWK=
SF295 M3yyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3oTlRKSzVyPUKuO|Q{OSBizszN MYfTRW5ITVJ?
OS-RC-2 NWjCRY5WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfLSFlxUUN3ME2yMlc3Pjd|IDFOwG0> MlLQV2FPT0WU
SK-MEL-24 NGnTclBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJwN{iyNlQhKM7:TR?= NWXEfYlPW0GQR1XS
COR-L23 MonQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXYcnhKSzVyPUKuO|k1PjRiIN88US=> NVvDNGRGW0GQR1XS
MHH-PREB-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PWOGlEPTB;Mj64NFE3OSBizszN MWfTRW5ITVJ?
SK-N-DZ NV\JNZZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\GTWxiUUN3ME2yMlgyPjN6IDFOwG0> NXnnSZRtW0GQR1XS
OMC-1 MlSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJwOEWwNFMhKM7:TR?= M1rnU3NCVkeHUh?=
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KYSE-180 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLQWodKSzVyPUiuNFg3PDhiIN88US=> MXfTRW5ITVJ?
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OVCAR-5 Mn7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRThwN{e2NlUhKM7:TR?= Mn33V2FPT0WU
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RMG-I MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moj1TWM2OD1|Mz60Nlg2KCEQvF2= MYTTRW5ITVJ?
LU-65 NHLTTmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjoWFlKSzVyPUO0MlE1ODhiIN88US=> MXnTRW5ITVJ?
GB-1 MkjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rTWGlEPTB;M{WuNFczQSBizszN M2HkRnNCVkeHUh?=
DU-4475 M2jVeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nHbGlEPTB;M{WuNVU2OyBizszN MnzuV2FPT0WU
SBC-5 MkPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\l[2lEPTB;M{[uOVkxOiBizszN MlvZV2FPT0WU
OE33 MlrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfJW45{UUN3ME2zO{44PTd5IDFOwG0> NWHUXJRCW0GQR1XS
C8166 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTN6LkWyOlchKM7:TR?= MmLNV2FPT0WU
COLO-684 NVzXTXNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjZc3BKSzVyPUO4Mlc1OjhiIN88US=> NWH0NGN7W0GQR1XS
NCI-H1155 M1zmTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTN7LkC0O|EhKM7:TR?= M2XFbXNCVkeHUh?=
ATN-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLGTWM2OD1|OT63O|kzKCEQvF2= MWnTRW5ITVJ?
KARPAS-299 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXRflc1UUN3ME2zPU45OzliIN88US=> MV3TRW5ITVJ?
KNS-81-FD NVzmUmd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPqXXVFUUN3ME20NE4{PjB2IDFOwG0> M1j6OXNCVkeHUh?=
NCI-H1563 M3TrXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrBTWM2OD12MT61NFM6KCEQvF2= NVvsPZBYW0GQR1XS
NB14 M3PySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4W0[GlEPTB;NEKuO|I3OyBizszN NWLvVYM2W0GQR1XS
COLO-800 NYjEZ242T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPxOHpKSzVyPUSyMlg2OTdiIN88US=> MlTpV2FPT0WU
MS-1 M{\rfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLIPZBTUUN3ME20N{4xPDh|IDFOwG0> MUnTRW5ITVJ?
OVCAR-8 MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTR|Lk[4NFkhKM7:TR?= M4jnZXNCVkeHUh?=
SK-PN-DW MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL0NYxKSzVyPUSzMlg4PzZiIN88US=> NWX5fGVHW0GQR1XS
G-402 NXXHUW1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknUTWM2OD12Mz65NFA3KCEQvF2= NYrhWWFnW0GQR1XS
NCI-H2291 NVnqZ5g3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTR2LkiwNVchKM7:TR?= NI[yR3BUSU6JRWK=
PC-3 NILLOppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTR3LkiwNlMhKM7:TR?= NFH5S2pUSU6JRWK=
NCI-H1581 NGLMdZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zPfWlEPTB;NEWuPVg5QSBizszN NHHaVlNUSU6JRWK=
SW1116 MmjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\LcJpKSzVyPUS3MlAyQDJiIN88US=> MkjTV2FPT0WU
ZR-75-30 NGXoTIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HtcWlEPTB;NEeuNFI{QSBizszN NIP4NlVUSU6JRWK=
OCI-AML2 NEnZT3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPPTWM2OD12Nz6wPVE5KCEQvF2= NUjFbJhlW0GQR1XS
MDA-MB-231 NIrGVlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfDTWM2OD12Nz62NlQ6KCEQvF2= MlyyV2FPT0WU
ES3 MkjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4CzS2lEPTB;NEiuN|UzQSBizszN MoXpV2FPT0WU
NCI-H630 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\LUYRKSzVyPUS5MlE4PDJiIN88US=> MY\TRW5ITVJ?
OE19 NUfldWVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGKwWJdKSzVyPUS5MlI6ODJiIN88US=> MmXSV2FPT0WU
NCI-H1573 MkPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXZVVRKSzVyPUS5MlY5PjFiIN88US=> NWfDPWpDW0GQR1XS
EW-1 NETsPXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEK3XGRKSzVyPUS5MlkxQDRiIN88US=> NF3zdVFUSU6JRWK=

... 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
  • 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
    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
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