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 19 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 MljuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwMEiyN|EhKM7:TR?= M1zue3NCVkeHUh?=
SW756 NInuXY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XWTGlEPTB;MD6xOFAzPCBizszN MUXTRW5ITVJ?
CTV-1 MnywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjFTWM2OD1yLkG2N|k5KCEQvF2= MVfTRW5ITVJ?
HSC-4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\FU5FKSzVyPUCuNVcyPThiIN88US=> M1\zSnNCVkeHUh?=
LAMA-84 NYjiS4h2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXafFFKSzVyPUCuNlg3PjRiIN88US=> NFO2b4VUSU6JRWK=
KU812 M3LldWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwM{SwOlghKM7:TR?= MmO2V2FPT0WU
HCC1806 NIHtVnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwM{WyNVYhKM7:TR?= MnzqV2FPT0WU
DOK MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwM{e3PFYhKM7:TR?= Ml\PV2FPT0WU
NCI-H209 NVPZVI1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPwTWM2OD1yLkSwPFA5KCEQvF2= NXvyb4g{W0GQR1XS
EoL-1-cell MlnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mon2TWM2OD1yLkSxOVc3KCEQvF2= NV7yWHJ2W0GQR1XS
H9 NYX5flFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK1TWM2OD1yLkSzOFY1KCEQvF2= NFjTd3lUSU6JRWK=
EM-2 NFjUbnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TET2lEPTB;MD60N|g6KCEQvF2= MnvpV2FPT0WU
NCI-H292 NYO5ZmdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVG2UXNTUUN3ME2wMlQ1OTB6IDFOwG0> NVi2OotOW0GQR1XS
697 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XjcmlEPTB;MD60OVY{OyBizszN MnG2V2FPT0WU
BHT-101 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwNE[1PUAh|ryP M4fQbXNCVkeHUh?=
BE-13 NIHafmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTXTHd4UUN3ME2wMlQ5PTd{IDFOwG0> MnfIV2FPT0WU
RS4-11 NHrkbVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LyOmlEPTB;MD60PFU5PCBizszN NULqTHlsW0GQR1XS
IGROV-1 M2G0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPVTWM2OD1yLkS4O|k4KCEQvF2= NVnxXHgzW0GQR1XS
KE-37 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLoUpNKSzVyPUCuOFk2ODliIN88US=> NHnZ[WRUSU6JRWK=
BV-173 NVOyVWg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISzTXZKSzVyPUCuOVA4QTJiIN88US=> NYDTbW1OW0GQR1XS
MEG-01 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;1emxKSzVyPUCuOVEzOTRiIN88US=> NHHtWGxUSU6JRWK=
LB2241-RCC NEi0U|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\j[Hp2UUN3ME2wMlU{PzF6IDFOwG0> M3TmVXNCVkeHUh?=
ACHN M1;Td2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3WSopKSzVyPUCuOVQxPjliIN88US=> MX\TRW5ITVJ?
CTB-1 M3\afmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwNUS4NkAh|ryP MlLaV2FPT0WU
HT-1080 NIfhNFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TKVmlEPTB;MD61OVM1QSBizszN NHrFe3hUSU6JRWK=
CHL-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwNUW0OlUhKM7:TR?= Mn;ZV2FPT0WU
EW-3 M370S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVKxeXlWUUN3ME2wMlU2QTN3IDFOwG0> M4Oz[3NCVkeHUh?=
ES1 MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfRXm9jUUN3ME2wMlY4PDl6IDFOwG0> MoXiV2FPT0WU
KASUMI-1 NXvs[JgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXaO4Q3UUN3ME2wMlczOzNiIN88US=> M3WwRXNCVkeHUh?=
SW13 M1K5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwN{O3PVghKM7:TR?= NFq3OJJUSU6JRWK=
A3-KAW M1fINmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUi4fpNFUUN3ME2wMlc6OjB6IDFOwG0> NE\O[olUSU6JRWK=
LB771-HNC MnjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHGxbJJKSzVyPUCuPFMyODRiIN88US=> NUfEV4VJW0GQR1XS
OC-314 NXHKdXllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2i3d2lEPTB;MD64Olk3PSBizszN NYXUc3M{W0GQR1XS
MLMA NXXhWXN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHGTWM2OD1yLkmwOlc2KCEQvF2= MXXTRW5ITVJ?
KARPAS-45 Mn[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M165e2lEPTB;MD65NlQ3PiBizszN MVLTRW5ITVJ?
CAL-27 MnK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwOUK5NFYhKM7:TR?= NX;Ydo5wW0GQR1XS
SK-NEP-1 NGjxO3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwOUeyOFghKM7:TR?= NULoZ5B5W0GQR1XS
COR-L105 M1z1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe0TVduUUN3ME2xMlAxOzl2IDFOwG0> M4nmd3NCVkeHUh?=
TI-73 NVjYN5lmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPyTWM2OD1zLkCxOlUhKM7:TR?= NH7ReZhUSU6JRWK=
JVM-3 NIGxXmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGflO4ZKSzVyPUGuNFUxOTdiIN88US=> M1XmSHNCVkeHUh?=
HAL-01 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTFwMEi4NUAh|ryP MnjrV2FPT0WU
QIMR-WIL M2HZUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXEZ5BKSzVyPUGuNFkxPThiIN88US=> NX7RWZBxW0GQR1XS
HSC-3 M2LFeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKxTWM2OD1zLkGxO|g{KCEQvF2= Mn7lV2FPT0WU
KY821 NHLMNGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLNTYJMUUN3ME2xMlE{OzVzIDFOwG0> M{[wVnNCVkeHUh?=
5637 MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTFwMUO4NFMhKM7:TR?= MnztV2FPT0WU
CAL-33 NVvTcYVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTFwMUmzNFIhKM7:TR?= MWjTRW5ITVJ?
ES4 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknoTWM2OD1zLkKwO|khKM7:TR?= NWm5c2ZVW0GQR1XS
BHY NUfpenlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXBUY02UUN3ME2xMlIzQDl{IDFOwG0> M1;zRXNCVkeHUh?=
LB1047-RCC Mne3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPmTWM2OD1zLkKzO|g2KCEQvF2= NFq4eZdUSU6JRWK=
H4 NYL1emhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLmSYxrUUN3ME2xMlI1OjV3IDFOwG0> NW\R[otSW0GQR1XS
RPMI-8866 MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFwMk[xNFYhKM7:TR?= NHHaPFdUSU6JRWK=
HO-1-N-1 MmSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHRTWM2OD1zLkK2N|Y6KCEQvF2= NIfucHBUSU6JRWK=
BB30-HNC MnPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\6N2hTUUN3ME2xMlI5PzF2IDFOwG0> NGPmWmNUSU6JRWK=
PC-14 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi3PG5sUUN3ME2xMlI6OjB3IDFOwG0> Mn2yV2FPT0WU
NUGC-3 M3HBXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFwMkmzOVYhKM7:TR?= M1\oenNCVkeHUh?=
A4-Fuk NIm2bG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDrO2VrUUN3ME2xMlMxPzB2IDFOwG0> NIH3RoNUSU6JRWK=
MHH-NB-11 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjwbYZKSzVyPUGuN|E{QDNiIN88US=> M{noVHNCVkeHUh?=
KOSC-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu3TWM2OD1zLkOxO|c2KCEQvF2= Ml;YV2FPT0WU
A498 Mkf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLLTWM2OD1zLkSwNVE{KCEQvF2= MXLTRW5ITVJ?
KG-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFwNEGyO|MhKM7:TR?= M2PlbXNCVkeHUh?=
DEL MmTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jSVGlEPTB;MT60N|Y2PyBizszN NV;jRVA4W0GQR1XS
EW-16 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjsO5VKSzVyPUGuOFM6PzNiIN88US=> M2C3[nNCVkeHUh?=
BPH-1 M3Kwe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFwNES4NFUhKM7:TR?= NUXSPWJIW0GQR1XS
JAR M1jSO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLXTWM2OD1zLkS5N|YhKM7:TR?= NELLb4ZUSU6JRWK=
J-RT3-T3-5 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlO5TWM2OD1zLkWxO|IzKCEQvF2= MlfQV2FPT0WU
A375 MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnuyTWM2OD1zLkWxO|czKCEQvF2= MnvsV2FPT0WU
SW954 NVftSpJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:ybpBZUUN3ME2xMlU2ODB5IDFOwG0> MmC2V2FPT0WU
Ca9-22 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYG5V3REUUN3ME2xMlU3OjZiIN88US=> MkTwV2FPT0WU
D-566MG Ml7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\VS2lEPTB;MT61O|E2PSBizszN NEXTUYdUSU6JRWK=
SCC-15 M3:5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HUPGlEPTB;MT62NVgxPCBizszN M1u3fnNCVkeHUh?=
HD-MY-Z NF;Ybm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFwNkO1PFQhKM7:TR?= MmOwV2FPT0WU
HT-1376 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\xcI1nUUN3ME2xMlY1OzZiIN88US=> MnLhV2FPT0WU
CAL-54 M2mxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPwNZl4UUN3ME2xMlY2PzB7IDFOwG0> NI\lPYxUSU6JRWK=
ONS-76 M2T6Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37rdWlEPTB;MT62O|U2OSBizszN MlXTV2FPT0WU
EFO-27 M1TtNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfVTG0yUUN3ME2xMlY5QTJiIN88US=> NUTaTnNVW0GQR1XS
769-P M{PFT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP4ZplKSzVyPUGuOlk2QTZiIN88US=> MV3TRW5ITVJ?
MV-4-11 M4PhbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P1OGlEPTB;MT62PVg2PiBizszN MlvqV2FPT0WU
NKM-1 NWG0PWFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVK3SJFGUUN3ME2xMlcyQDB{IDFOwG0> NGHubVRUSU6JRWK=
LOXIMVI M4XUfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\ONIFKSzVyPUGuO|Q2QTliIN88US=> MnTaV2FPT0WU
KYSE-140 M{nhXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIOzPVRKSzVyPUGuO|U3PTViIN88US=> MkTCV2FPT0WU
ES5 NEGzSFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTFwOE[3OFchKM7:TR?= NVPCeZRPW0GQR1XS
BB65-RCC NH;xS2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFwOEm4OFkhKM7:TR?= MkKyV2FPT0WU
HN MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrpVVVUUUN3ME2xMlg6QDd2IDFOwG0> MmfRV2FPT0WU
A101D NYS0[3JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFwOUO2NlghKM7:TR?= NX:w[Hg6W0GQR1XS
LoVo M2HvXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHTTWM2OD1zLkm3Olc6KCEQvF2= M2TTWXNCVkeHUh?=
NCI-H526 M{PkXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVq3WJQ6UUN3ME2xMlk6OzJ3IDFOwG0> MWPTRW5ITVJ?
NCI-H1693 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\WXmhKSzVyPUGuPVk5QDhiIN88US=> NHTOVGFUSU6JRWK=
OVCAR-4 NGfZZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTJwMEC0N|UhKM7:TR?= M{fQe3NCVkeHUh?=
SK-HEP-1 NIDsOGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13qPGlEPTB;Mj6wNFc1PSBizszN NFLUOWtUSU6JRWK=
C2BBe1 M4DIOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTJwMEOzO|IhKM7:TR?= MlviV2FPT0WU
MEL-JUSO M{THcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoWxTWM2OD1{LkC0OFY1KCEQvF2= MWjTRW5ITVJ?
MOLT-16 M1nqRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTJwMEewOVghKM7:TR?= NWOwUmpDW0GQR1XS
NBsusSR NUDHcVJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJwMEm4PFkhKM7:TR?= M{j2e3NCVkeHUh?=
TK10 NHHCTW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\6PWlvUUN3ME2yMlE{PDV6IDFOwG0> NFPoc4pUSU6JRWK=
CAL-39 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fZUmlEPTB;Mj6xOFQ5KCEQvF2= MY\TRW5ITVJ?
NCI-H2030 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYKyPWo3UUN3ME2yMlE5QTd|IDFOwG0> NYS2U3p5W0GQR1XS
HCT-116 NXrKe4pHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJwMkK5PFQhKM7:TR?= NWe0WJlHW0GQR1XS
HTC-C3 NXXOUHgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Ljb2lEPTB;Mj6yOlgzPCBizszN M{\3NHNCVkeHUh?=
TYK-nu NWniVGM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXVTWM2OD1{LkOwPVA6KCEQvF2= NInKeXJUSU6JRWK=
FADU Mm\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHv2TFhKSzVyPUKuN|IzQTZiIN88US=> MlLkV2FPT0WU
A431 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\abVUzUUN3ME2yMlM4ODJ3IDFOwG0> NGjl[5VUSU6JRWK=
TE-11 MoLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJwM{iwNVkhKM7:TR?= M4\Zb3NCVkeHUh?=
CAL-12T MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPnN3B4UUN3ME2yMlQxPDF5IDFOwG0> M4Dvb3NCVkeHUh?=
DB NXzjc5Z4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;obmlEPTB;Mj60Nlg3QSBizszN NE\SfmxUSU6JRWK=
L-363 Mm[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TNUmlEPTB;Mj60N|UxPyBizszN MkXpV2FPT0WU
MSTO-211H NX3UNVkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f6ZWlEPTB;Mj62OlM6OSBizszN MV;TRW5ITVJ?
SK-UT-1 NIfKPYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\qTWM2OD1{LkexOFA3KCEQvF2= M1HFZ3NCVkeHUh?=
RPMI-8226 Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUi0[o5uUUN3ME2yMlc{OTZ2IDFOwG0> M3PwOHNCVkeHUh?=
SF295 MnfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHibXhKSzVyPUKuO|Q{OSBizszN M1PFZXNCVkeHUh?=
OS-RC-2 MoXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTJwN{[2O|MhKM7:TR?= MlfJV2FPT0WU
SK-MEL-24 MmjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7mWo1LUUN3ME2yMlc5OjJ2IDFOwG0> MVnTRW5ITVJ?
COR-L23 NUX4emJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1L4cmlEPTB;Mj63PVQ3PCBizszN M1HvO3NCVkeHUh?=
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LU-65 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO5d4JOUUN3ME2zOE4yPDB6IDFOwG0> M3Hk[3NCVkeHUh?=
GB-1 NEnoU4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLq[oxKSzVyPUO1MlA4OjliIN88US=> M1WyVnNCVkeHUh?=
DU-4475 M3XRd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TrPGlEPTB;M{WuNVU2OyBizszN NGPQXnRUSU6JRWK=
SBC-5 M2jE[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTN4LkW5NFIhKM7:TR?= NIi1[ZlUSU6JRWK=
OE33 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXjcoFIUUN3ME2zO{44PTd5IDFOwG0> MU\TRW5ITVJ?
C8166 NXfqbodXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnf2TWM2OD1|OD61NlY4KCEQvF2= MYjTRW5ITVJ?
COLO-684 M1HJWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnOZ2tKSzVyPUO4Mlc1OjhiIN88US=> NXjO[YdxW0GQR1XS
NCI-H1155 M{XuOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXUSXpUUUN3ME2zPU4xPDdzIDFOwG0> NGXqUpNUSU6JRWK=
ATN-1 NGXtb4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjoTWM2OD1|OT63O|kzKCEQvF2= MX3TRW5ITVJ?
KARPAS-299 NY\vXVkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTN7LkizPUAh|ryP NU\zSnVSW0GQR1XS
KNS-81-FD NHWzOGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvmXnZKSzVyPUSwMlM3ODRiIN88US=> MkjqV2FPT0WU
NCI-H1563 MofSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPJTXRKSzVyPUSxMlUxOzliIN88US=> M33SSXNCVkeHUh?=
NB14 NWnRcVNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTR{LkeyOlMhKM7:TR?= NV3aWmc1W0GQR1XS
COLO-800 MkO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHifXZKSzVyPUSyMlg2OTdiIN88US=> NVzIfWtHW0GQR1XS
MS-1 NGW0eGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGO5OY9KSzVyPUSzMlA1QDNiIN88US=> M4e1XHNCVkeHUh?=
OVCAR-8 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH34OoNKSzVyPUSzMlY5ODliIN88US=> M17R[3NCVkeHUh?=
SK-PN-DW NULzWpVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO0TJFKSzVyPUSzMlg4PzZiIN88US=> MYjTRW5ITVJ?
G-402 NUnVdVJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR|LkmwNFYhKM7:TR?= NFviPIZUSU6JRWK=
NCI-H2291 NIHOO5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkS0TWM2OD12ND64NFE4KCEQvF2= NFX0dHFUSU6JRWK=
PC-3 NHTuZo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXw[ZlTUUN3ME20OU45ODJ|IDFOwG0> MUfTRW5ITVJ?
NCI-H1581 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHKwZW5KSzVyPUS1Mlk5QDliIN88US=> MVnTRW5ITVJ?
SW1116 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXk[3V6UUN3ME20O{4xOTh{IDFOwG0> NG\JNJJUSU6JRWK=
ZR-75-30 NEXnOXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37yWmlEPTB;NEeuNFI{QSBizszN MXfTRW5ITVJ?
OCI-AML2 NGXtdJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVS5eIM5UUN3ME20O{4xQTF6IDFOwG0> Mlu5V2FPT0WU
MDA-MB-231 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TUSmlEPTB;NEeuOlI1QSBizszN NXXOT2kzW0GQR1XS
ES3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz6UWJKSzVyPUS4MlM2OjliIN88US=> MVTTRW5ITVJ?
NCI-H630 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjmV4Z{UUN3ME20PU4yPzR{IDFOwG0> M4jNeXNCVkeHUh?=
OE19 NH7JSYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvTTWM2OD12OT6yPVAzKCEQvF2= M{fZOnNCVkeHUh?=
NCI-H1573 NXvSUWY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rpdGlEPTB;NEmuOlg3OSBizszN M2i1THNCVkeHUh?=
EW-1 NH\BOXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;JS2t3UUN3ME20PU46ODh2IDFOwG0> NETMc4ZUSU6JRWK=

... Click to View More Cell Line Experimental Data

In vivo Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively. [1] Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity. [2] As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts. [4]

Protocol

Kinase Assay:

[1]

+ Expand

The Src and Abl kinase assays:

The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution.
Cell Research:

[2]

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

    Cells are exposed to various concentrations of Bosutinib for 72 hours. Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts is measured in 96-well ultra-low binding plates treated with Sigmacote to block residual cell attachment. Cell proliferation is measured with MTS or Cell-Glo. For the determination of cell cycle or cell death, cells are prepared for FACS analysis in the CycleTest Plus DNA reagent kit and analyzed on a fluorescence-activated cell sorter flow cytometer.


    (Only for Reference)
Animal Research:

[2]

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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 530.45
Formula

C26H29Cl2N5O3

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

  • Mass
    Concentration
    Volume
    Molecular Weight

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

Dilution Calculator

Dilution Calculator

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

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

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

  • C1
    V1
    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

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

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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

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

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

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

  • Answer:

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

Src Signaling Pathway Map

Src Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID