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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4 Customer Reviews

  • A,IC50 of Bosutinib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. The effect of inhibitors is presented as the percentage of ANDV-induced permeability of inhibitor-treated monolayers 3 days postinfection and 30 min post-VEGF and FITC-dextran addition. B, VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for Fig. 1 at indicated times in the presence or absence of Bosutinib .

    J Virol 2011 85, 2296–2303. Bosutinib (SKI-606) purchased from Selleck.

    Both parental and HR cell lines were treated with bosutinib (0.01, 0.1, and 1 μmol/L) for 24 hours. Src-related signaling pathway molecules were then analyzed.

    Mol Cancer Ther, 2017. Bosutinib (SKI-606) purchased from Selleck.

  • SFK inhibitors abrogate tyrosine phosphorylation associated with sperm capacitation. Mouse sperm were incubated in the absence or in the presence of SKI606 for 60 min in capacitating (cap, with HCO3) or non-capacitating media (NC, without HCO3). Western blot analyses were performed withanti-pY antibodies.

    J Biol Chem 2010 285, 7977–7985. Bosutinib (SKI-606) purchased from Selleck.

    Rescue ofPKAand tyrosine phosphorylation by Ser/Thr phosphatase inhibitors. A and B, spermwere incubated in capacitating medium supplemented with SFK inhibitors and different concentrations of okadaic acid (OA) (A) or calyculin-A (B), before immunodetection of p-PKA substrates (clone 100G7E). C and D, PVDF membranes used in A and B were stripped as described and used for Western blot immunodetection with anti-PY antibodies (clone 4G10).

    Dr. Pablo E.Visconti from University of Massachusetts. Bosutinib (SKI-606) purchased from Selleck.

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 M3vkXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojZTWM2OD1yLkC4NlMyKCEQvF2= MlHLV2FPT0WU
SW756 NWSxTHY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHP4ZWdKSzVyPUCuNVQxOjRiIN88US=> MV3TRW5ITVJ?
CTV-1 MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn6eXg5UUN3ME2wMlE3Ozl6IDFOwG0> M4DpWHNCVkeHUh?=
HSC-4 NIDrcFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDI[pJuUUN3ME2wMlE4OTV6IDFOwG0> MXrTRW5ITVJ?
LAMA-84 NHXEeJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwMki2OlQhKM7:TR?= MX\TRW5ITVJ?
KU812 NGHPSnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHPWnJKSzVyPUCuN|QxPjhiIN88US=> MnvoV2FPT0WU
HCC1806 M1XKbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfROlFKSzVyPUCuN|UzOTZiIN88US=> MlfqV2FPT0WU
DOK NFPB[Y9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwM{e3PFYhKM7:TR?= M1nVcnNCVkeHUh?=
NCI-H209 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHTWGhKSzVyPUCuOFA5ODhiIN88US=> NEfZdYdUSU6JRWK=
EoL-1-cell NHWwVWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[5eWlEPTB;MD60NVU4PiBizszN NGTwPIFUSU6JRWK=
H9 M2LpOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjlTWM2OD1yLkSzOFY1KCEQvF2= MYDTRW5ITVJ?
EM-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnYfpVKSzVyPUCuOFM5QSBizszN NYLQcGU3W0GQR1XS
NCI-H292 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHQbo9RUUN3ME2wMlQ1OTB6IDFOwG0> NIXNSItUSU6JRWK=
697 NHrGV3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGG4TXVKSzVyPUCuOFU3OzNiIN88US=> NI[xUG9USU6JRWK=
BHT-101 NVfae2JHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;NbGlEPTB;MD60OlU6KCEQvF2= MX\TRW5ITVJ?
BE-13 NV:0eIVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LZ[GlEPTB;MD60PFU4OiBizszN Mk\iV2FPT0WU
RS4-11 MmO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXj5PZhzUUN3ME2wMlQ5PTh2IDFOwG0> MkTJV2FPT0WU
IGROV-1 NEj4Z41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXrTWM2OD1yLkS4O|k4KCEQvF2= MW\TRW5ITVJ?
KE-37 MnSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwNEm1NFkhKM7:TR?= MXzTRW5ITVJ?
BV-173 NYLVPIF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwNUC3PVIhKM7:TR?= NFvHRoRUSU6JRWK=
MEG-01 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXizXnNEUUN3ME2wMlUyOjF2IDFOwG0> Mne0V2FPT0WU
LB2241-RCC Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFz3d5hKSzVyPUCuOVM4OThiIN88US=> NVzXS3hJW0GQR1XS
ACHN Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M32zN2lEPTB;MD61OFA3QSBizszN NUfOPYtFW0GQR1XS
CTB-1 NWf6OHM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn6PG5KSzVyPUCuOVQ5OiBizszN MkHnV2FPT0WU
HT-1080 M2Xm[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwNUWzOFkhKM7:TR?= NHm3[oNUSU6JRWK=
CHL-1 NXPFeGVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPuPZJKSzVyPUCuOVU1PjViIN88US=> NH;LNY9USU6JRWK=
EW-3 NXXlWnRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WwWGlEPTB;MD61OVk{PSBizszN NWfKc4ZFW0GQR1XS
ES1 NF;RbZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfHTWM2OD1yLk[3OFk5KCEQvF2= M1;PUHNCVkeHUh?=
KASUMI-1 M1K4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PzfGlEPTB;MD63NlM{KCEQvF2= Mn;6V2FPT0WU
SW13 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvyW4dKSzVyPUCuO|M4QThiIN88US=> Mn[xV2FPT0WU
A3-KAW NGL3e3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DyVmlEPTB;MD63PVIxQCBizszN NW\sbGlJW0GQR1XS
LB771-HNC M4DBdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLUWlYzUUN3ME2wMlg{OTB2IDFOwG0> MWrTRW5ITVJ?
OC-314 M4izTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn5ZXZKSzVyPUCuPFY6PjViIN88US=> NVvnS|FlW0GQR1XS
MLMA Mlq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwOUC2O|UhKM7:TR?= M4K0S3NCVkeHUh?=
KARPAS-45 Ml;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof2TWM2OD1yLkmyOFY3KCEQvF2= Mnr6V2FPT0WU
CAL-27 M4fYbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[xNGlEPTB;MD65NlkxPiBizszN MVvTRW5ITVJ?
SK-NEP-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr5clB2UUN3ME2wMlk4OjR6IDFOwG0> M171fnNCVkeHUh?=
COR-L105 NHXqSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwMECzPVQhKM7:TR?= NX\4Z4x[W0GQR1XS
TI-73 NVPxZolkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzCTWM2OD1zLkCxOlUhKM7:TR?= NUf0XGpDW0GQR1XS
JVM-3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHBWZl5UUN3ME2xMlA2ODF5IDFOwG0> M4TtZ3NCVkeHUh?=
HAL-01 MlXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILP[I9KSzVyPUGuNFg5OSBizszN MVzTRW5ITVJ?
QIMR-WIL MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnMTWM2OD1zLkC5NFU5KCEQvF2= MYPTRW5ITVJ?
HSC-3 M1nGc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjvcnpSUUN3ME2xMlEyPzh|IDFOwG0> NFzpRoZUSU6JRWK=
KY821 M3fzb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwMUOzOVEhKM7:TR?= NUOzTWpyW0GQR1XS
5637 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTFwMUO4NFMhKM7:TR?= MYjTRW5ITVJ?
CAL-33 M1e3fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFwMUmzNFIhKM7:TR?= M3mwSnNCVkeHUh?=
ES4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXORVBKSzVyPUGuNlA4QSBizszN MYPTRW5ITVJ?
BHY M{S1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH3c4NKSzVyPUGuNlI5QTJiIN88US=> MmPZV2FPT0WU
LB1047-RCC MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\yfXVKSzVyPUGuNlM4QDViIN88US=> M4\jeHNCVkeHUh?=
H4 M3WzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwMkSyOVUhKM7:TR?= MVTTRW5ITVJ?
RPMI-8866 NVPzb2FpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjZTWM2OD1zLkK2NVA3KCEQvF2= NG\DVZBUSU6JRWK=
HO-1-N-1 M2Kwe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\4SWxMUUN3ME2xMlI3OzZ7IDFOwG0> NIPCcpZUSU6JRWK=
BB30-HNC NHTvWGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDXTWM2OD1zLkK4O|E1KCEQvF2= MWDTRW5ITVJ?
PC-14 NFfO[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEOzdIZKSzVyPUGuNlkzODViIN88US=> Ml;VV2FPT0WU
NUGC-3 NYLuSVF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzXTWM2OD1zLkK5N|U3KCEQvF2= NVKyeYl6W0GQR1XS
A4-Fuk NUDlZ4szT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TscWlEPTB;MT6zNFcxPCBizszN MkK5V2FPT0WU
MHH-NB-11 NHLWepFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTFwM{GzPFMhKM7:TR?= M1rTUnNCVkeHUh?=
KOSC-2 NIDBbVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULFPWVmUUN3ME2xMlMyPzd3IDFOwG0> NVjGT4llW0GQR1XS
A498 MnrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7CNHIzUUN3ME2xMlQxOTF|IDFOwG0> MW\TRW5ITVJ?
KG-1 MmP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrJTWM2OD1zLkSxNlc{KCEQvF2= MYjTRW5ITVJ?
DEL MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG5TWM2OD1zLkSzOlU4KCEQvF2= MUjTRW5ITVJ?
EW-16 NYXDRYR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LUVWlEPTB;MT60N|k4OyBizszN MXnTRW5ITVJ?
BPH-1 NYHrTYNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDWdY1SUUN3ME2xMlQ1QDB3IDFOwG0> MnnxV2FPT0WU
JAR NF\XVFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmj0TWM2OD1zLkS5N|YhKM7:TR?= NVHTPZMzW0GQR1XS
J-RT3-T3-5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;QVHBKSzVyPUGuOVE4OjJiIN88US=> NV;mcnZVW0GQR1XS
A375 MoLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnz5TWM2OD1zLkWxO|czKCEQvF2= NEf0PGNUSU6JRWK=
SW954 Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;xVmlEPTB;MT61OVAxPyBizszN NVvobYt2W0GQR1XS
Ca9-22 MmfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTFwNU[yOkAh|ryP M3PZTnNCVkeHUh?=
D-566MG MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLVTndLUUN3ME2xMlU4OTV3IDFOwG0> NFXrcXZUSU6JRWK=
SCC-15 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nnWmlEPTB;MT62NVgxPCBizszN MYLTRW5ITVJ?
HD-MY-Z M{PaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTFwNkO1PFQhKM7:TR?= M3;l[HNCVkeHUh?=
HT-1376 NH\ZT3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfJZ3NKSzVyPUGuOlQ{PiBizszN NEDwZ3RUSU6JRWK=
CAL-54 NWf4[YhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfhUGVMUUN3ME2xMlY2PzB7IDFOwG0> MXnTRW5ITVJ?
ONS-76 NITJSm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjkeWdxUUN3ME2xMlY4PTVzIDFOwG0> M13wRXNCVkeHUh?=
EFO-27 MlXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjxPGtUUUN3ME2xMlY5QTJiIN88US=> NVjrPYl3W0GQR1XS
769-P NFL2WpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3WxXGlEPTB;MT62PVU6PiBizszN M4rzdnNCVkeHUh?=
MV-4-11 NILHTpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFwNkm4OVYhKM7:TR?= MVPTRW5ITVJ?
NKM-1 M3LaRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS0NldxUUN3ME2xMlcyQDB{IDFOwG0> NF[xR29USU6JRWK=
LOXIMVI MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTFwN{S1PVkhKM7:TR?= NUC0V2RUW0GQR1XS
KYSE-140 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP0bpBKSzVyPUGuO|U3PTViIN88US=> M2Tld3NCVkeHUh?=
ES5 NYHhWWRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFwOE[3OFchKM7:TR?= NI\vfVRUSU6JRWK=
BB65-RCC NGPieHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1m3OGlEPTB;MT64PVg1QSBizszN MnrzV2FPT0WU
HN MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrVWJhKSzVyPUGuPFk5PzRiIN88US=> MWLTRW5ITVJ?
A101D MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHpVGoxUUN3ME2xMlk{PjJ6IDFOwG0> MkjEV2FPT0WU
LoVo MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfGRnlKSzVyPUGuPVc3PzliIN88US=> NYnvR2w3W0GQR1XS
NCI-H526 NF;DNHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknSTWM2OD1zLkm5N|I2KCEQvF2= MkfEV2FPT0WU
NCI-H1693 M1vEe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITZO2NKSzVyPUGuPVk5QDhiIN88US=> MnH0V2FPT0WU
OVCAR-4 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HmUmlEPTB;Mj6wNFQ{PSBizszN NU[2XJBZW0GQR1XS
SK-HEP-1 NHrXdJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlv4TWM2OD1{LkCwO|Q2KCEQvF2= MWXTRW5ITVJ?
C2BBe1 M{fwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJwMEOzO|IhKM7:TR?= M3;jfXNCVkeHUh?=
MEL-JUSO M4jacmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGxdVlKUUN3ME2yMlA1PDZ2IDFOwG0> M2D2U3NCVkeHUh?=
MOLT-16 MkHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJwMEewOVghKM7:TR?= MnviV2FPT0WU
NBsusSR NHLwc25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGToZ2JKSzVyPUKuNFk5QDliIN88US=> NVHIO4lbW0GQR1XS
TK10 NUHKXJFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXBOZZKSzVyPUKuNVM1PThiIN88US=> M3fKR3NCVkeHUh?=
CAL-39 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjkPFhKSzVyPUKuNVQ1QCBizszN MVPTRW5ITVJ?
NCI-H2030 NV;DSVRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJwMUi5O|MhKM7:TR?= NFvKUoVUSU6JRWK=
HCT-116 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHPUYVIUUN3ME2yMlIzQTh2IDFOwG0> MVXTRW5ITVJ?
HTC-C3 Ml;WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJwMk[4NlQhKM7:TR?= MkDKV2FPT0WU
TYK-nu MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmWyTWM2OD1{LkOwPVA6KCEQvF2= Ml7sV2FPT0WU
FADU Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTJwM{KyPVYhKM7:TR?= MWXTRW5ITVJ?
A431 Mkf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjtTYFKSzVyPUKuN|cxOjViIN88US=> MYnTRW5ITVJ?
TE-11 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJwM{iwNVkhKM7:TR?= NFO5TpBUSU6JRWK=
CAL-12T MkPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXFT5BjUUN3ME2yMlQxPDF5IDFOwG0> MlvCV2FPT0WU
DB MkH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mln3TWM2OD1{LkSyPFY6KCEQvF2= M4Die3NCVkeHUh?=
L-363 M{DYZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jhSWlEPTB;Mj60N|UxPyBizszN NVTCV4JRW0GQR1XS
MSTO-211H MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofKTWM2OD1{Lk[2N|kyKCEQvF2= MXvTRW5ITVJ?
SK-UT-1 M2fXSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGiyd|lKSzVyPUKuO|E1ODZiIN88US=> NHvqc4VUSU6JRWK=
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SK-N-DZ MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPCbWRKSzVyPUKuPFE3OzhiIN88US=> MUPTRW5ITVJ?
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EW-11 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTNwMUSyO|chKM7:TR?= MVLTRW5ITVJ?
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EC-GI-10 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv2ZWVKSzVyPUOuNVczPjNiIN88US=> NXHQfVdWW0GQR1XS
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ME-180 Ml;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPFT|dKSzVyPUOuNlYxPTFiIN88US=> NFG0eXhUSU6JRWK=
NCI-H2009 MnjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTNwMkmwNUAh|ryP Mn7ZV2FPT0WU
HL-60 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PWU2lEPTB;Mz6yPVE{KCEQvF2= MVHTRW5ITVJ?
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ChaGo-K-1 MlXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrXSGxKSzVyPUSuOVk2PTliIN88US=> MnPqV2FPT0WU
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KYSE-270 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\ufmhKSzVyPUSuOlUyOjZiIN88US=> MVTTRW5ITVJ?
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HOP-92 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXjVFZKSzVyPUSuPFE{PzliIN88US=> MkKwV2FPT0WU
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no-11 NV;CcJE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrQT2lyUUN3ME23MlE3PDFiIN88US=> MWLTRW5ITVJ?
KU-19-19 NHj1SJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDkfXd1UUN3ME23MlE3PDd4IDFOwG0> MonYV2FPT0WU
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Detroit562 M{jIU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\rW4NpUUN3ME23MlMzPTB4IDFOwG0> M4PyVHNCVkeHUh?=
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RPMI-2650 NEP4eGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTdwN{CzNVIhKM7:TR?= NHH5XG1USU6JRWK=
HCC2218 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi2NHNKSzVyPUeuO|IzPThiIN88US=> MlLyV2FPT0WU
GCT NFrBfFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTicHBiUUN3ME23MlgzOTd{IDFOwG0> MoLiV2FPT0WU
SW780 NYHxO3dLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTdwOUmwOkAh|ryP NGLj[5dUSU6JRWK=
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KYSE-180 M3zHVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfBXmlKSzVyPUiuNFg3PDhiIN88US=> MmjnV2FPT0WU
TE-1 MkjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRThwMUGwOVchKM7:TR?= MVXTRW5ITVJ?
OAW-42 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzSTWM2OD16LkK1OFk3KCEQvF2= NVKwb3ZrW0GQR1XS
VM-CUB-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fxTGlEPTB;OD6yPFM3PCBizszN MUfTRW5ITVJ?
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NCI-H69 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTNyLk[wPVMhKM7:TR?= NFrNUXRUSU6JRWK=
NB6 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[xWIFKSzVyPUOxMlM3OjliIN88US=> M2HNfnNCVkeHUh?=
CAL-120 NVnme2R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljRTWM2OD1|Mj60N|E4KCEQvF2= NULBeVBbW0GQR1XS
U-87-MG M{nxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTN|LkCyOVEhKM7:TR?= M3HjVXNCVkeHUh?=
NCI-H1304 M4DHV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTN|LkCzOVQhKM7:TR?= NGGxOoJUSU6JRWK=
YH-13 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1W3T2lEPTB;M{OuNlU{PSBizszN NEPoTYtUSU6JRWK=
RMG-I NUXqTWlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXe1UoREUUN3ME2zN{41Ojh3IDFOwG0> NWLaOo91W0GQR1XS
LU-65 NHPKepJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTIRY9KSzVyPUO0MlE1ODhiIN88US=> NHq1XlNUSU6JRWK=
GB-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnUeIZKSzVyPUO1MlA4OjliIN88US=> NHTF[mhUSU6JRWK=
DU-4475 NF63UYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom5TWM2OD1|NT6xOVU{KCEQvF2= NWn3WoZkW0GQR1XS
SBC-5 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XjTGlEPTB;M{[uOVkxOiBizszN MVrTRW5ITVJ?
OE33 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHkTWM2OD1|Nz63OVc4KCEQvF2= NEPWSmZUSU6JRWK=
C8166 MkjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTN6LkWyOlchKM7:TR?= MnvZV2FPT0WU
COLO-684 NIGycJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTN6Lke0NlghKM7:TR?= M3rmdXNCVkeHUh?=
NCI-H1155 NEGyUFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;mTWM2OD1|OT6wOFcyKCEQvF2= NWHZS5lxW0GQR1XS
ATN-1 MlL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjYc2JKSzVyPUO5Mlc4QTJiIN88US=> M3vwTXNCVkeHUh?=
KARPAS-299 M4rhfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDHTWM2OD1|OT64N|khKM7:TR?= MlLQV2FPT0WU
KNS-81-FD NYPJSWRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTEbGhKSzVyPUSwMlM3ODRiIN88US=> M{PhUHNCVkeHUh?=
NCI-H1563 NIrlfWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\TTWM2OD12MT61NFM6KCEQvF2= MYLTRW5ITVJ?
NB14 NWO4NZBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHEWmlYUUN3ME20Nk44OjZ|IDFOwG0> MY\TRW5ITVJ?
COLO-800 NVXPeFlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILOcGhKSzVyPUSyMlg2OTdiIN88US=> MnjPV2FPT0WU
MS-1 MmrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTR|LkC0PFMhKM7:TR?= NVHtWZk4W0GQR1XS
OVCAR-8 NXjiV2x7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HEZWlEPTB;NEOuOlgxQSBizszN MoKzV2FPT0WU
SK-PN-DW M4fZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES2cJNKSzVyPUSzMlg4PzZiIN88US=> MUjTRW5ITVJ?
G-402 NHvDOo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrqTHBKSzVyPUSzMlkxODZiIN88US=> Mkm4V2FPT0WU
NCI-H2291 NUS0emxlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXqTWM2OD12ND64NFE4KCEQvF2= MWjTRW5ITVJ?
PC-3 NHrBU2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTR3LkiwNlMhKM7:TR?= NG\uNFhUSU6JRWK=
NCI-H1581 NFvZW49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPzXIhlUUN3ME20OU46QDh7IDFOwG0> MkHuV2FPT0WU
SW1116 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XHdmlEPTB;NEeuNFE5OiBizszN Mn:zV2FPT0WU
ZR-75-30 MkHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PPbGlEPTB;NEeuNFI{QSBizszN M3;ub3NCVkeHUh?=
OCI-AML2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDQe4ZKSzVyPUS3MlA6OThiIN88US=> NEjKVZBUSU6JRWK=
MDA-MB-231 NEXERYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\He216UUN3ME20O{43OjR7IDFOwG0> NGq0UFFUSU6JRWK=
ES3 M{i3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTSO4F3UUN3ME20PE4{PTJ7IDFOwG0> M1HNcHNCVkeHUh?=
NCI-H630 Mn\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPCTWM2OD12OT6xO|QzKCEQvF2= NYSwcmpPW0GQR1XS
OE19 MlnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTR7LkK5NFIhKM7:TR?= MW\TRW5ITVJ?
NCI-H1573 MoOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHzTWM2OD12OT62PFYyKCEQvF2= MlO2V2FPT0WU
EW-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\qTWM2OD12OT65NFg1KCEQvF2= NXLwSoVIW0GQR1XS

... 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 individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
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
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

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

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

  • C1
    V1
    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

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

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03023319 Recruiting Carcinoma, Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer Nagla Karim|University of Cincinnati January 2017 Phase 1
NCT02810990 Recruiting Chronic Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto November 2016 Phase 2
NCT02906696 Recruiting Chronic Myelogenous Leukemia M.D. Anderson Cancer Center|Pfizer October 2016 Phase 2
NCT02782403 Not yet recruiting Leukemia M.D. Anderson Cancer Center|Pfizer September 2016 Phase 1|Phase 2
NCT02921477 Enrolling by invitation Mild Cognitive Impairment|Dementia Neurological Associates of West Los Angeles|Pfizer September 2016 Phase 1
NCT02693535 Recruiting Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer March 2016 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID