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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In DMSO USD 91 In stock
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USD 270 In stock

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3 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.

    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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NEXw[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIC1cYJKSzVyPUCuNFgzOzFiIN88US=> Mmm0V2FPT0WU
SW756 MmLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vz[WlEPTB;MD6xOFAzPCBizszN NHLxUoRUSU6JRWK=
CTV-1 M3j5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkn4TWM2OD1yLkG2N|k5KCEQvF2= NIDxNItUSU6JRWK=
HSC-4 NVrWU2VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwMUexOVghKM7:TR?= NH7OfGpUSU6JRWK=
LAMA-84 NXPkRndUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwMki2OlQhKM7:TR?= MVnTRW5ITVJ?
KU812 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLUeph1UUN3ME2wMlM1ODZ6IDFOwG0> NYHpXZkyW0GQR1XS
HCC1806 NVrleVg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzl[pIyUUN3ME2wMlM2OjF4IDFOwG0> NFy3PIlUSU6JRWK=
DOK NYrSRYd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;lNWlEPTB;MD6zO|c5PiBizszN NVW1[GZUW0GQR1XS
NCI-H209 M1vm[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwNEC4NFghKM7:TR?= M1zTcHNCVkeHUh?=
EoL-1-cell NGPlc|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGzVpZlUUN3ME2wMlQyPTd4IDFOwG0> MlPmV2FPT0WU
H9 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnsW5E1UUN3ME2wMlQ{PDZ2IDFOwG0> Mm\aV2FPT0WU
EM-2 M{Th[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjVTo9lUUN3ME2wMlQ{QDliIN88US=> M3iw[nNCVkeHUh?=
NCI-H292 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHzW|JKSzVyPUCuOFQyODhiIN88US=> M1viSXNCVkeHUh?=
697 NYG2dIFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWyb2tUUUN3ME2wMlQ2PjN|IDFOwG0> M{X0dnNCVkeHUh?=
BHT-101 M13JS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwNE[1PUAh|ryP NEXBfIdUSU6JRWK=
BE-13 NEjHPIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXO5OnB5UUN3ME2wMlQ5PTd{IDFOwG0> M2G4cnNCVkeHUh?=
RS4-11 M1v2XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEOxTGFKSzVyPUCuOFg2QDRiIN88US=> NXrPT|Q3W0GQR1XS
IGROV-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofuTWM2OD1yLkS4O|k4KCEQvF2= MXzTRW5ITVJ?
KE-37 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPwTWM2OD1yLkS5OVA6KCEQvF2= NEPmV|NUSU6JRWK=
BV-173 MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LrNGlEPTB;MD61NFc6OiBizszN NIfhd5lUSU6JRWK=
MEG-01 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PIVmlEPTB;MD61NVIyPCBizszN M1LrVXNCVkeHUh?=
LB2241-RCC NHTwN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rhVWlEPTB;MD61N|cyQCBizszN NWqzeHZiW0GQR1XS
ACHN MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTBwNUSwOlkhKM7:TR?= MVLTRW5ITVJ?
CTB-1 NYS2UnhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfnU5VKSzVyPUCuOVQ5OiBizszN NFrRPWFUSU6JRWK=
HT-1080 M2DuOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwNUWzOFkhKM7:TR?= MnvXV2FPT0WU
CHL-1 NIP1ZXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwNUW0OlUhKM7:TR?= NEm4foJUSU6JRWK=
EW-3 NYDYTlduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHTTWM2OD1yLkW1PVM2KCEQvF2= MlzwV2FPT0WU
ES1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwNke0PVghKM7:TR?= NWPFVlR6W0GQR1XS
KASUMI-1 NUPGO|VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPmT4pKSzVyPUCuO|I{OyBizszN NUDBd205W0GQR1XS
SW13 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjlWHhnUUN3ME2wMlc{Pzl6IDFOwG0> NFXiXI9USU6JRWK=
A3-KAW MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLQRmhKSzVyPUCuO|kzODhiIN88US=> M2q2NXNCVkeHUh?=
LB771-HNC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTXbG5KSzVyPUCuPFMyODRiIN88US=> MYjTRW5ITVJ?
OC-314 NWfINm1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDyTWM2OD1yLki2PVY2KCEQvF2= M{TYRnNCVkeHUh?=
MLMA NEjLSnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mon4TWM2OD1yLkmwOlc2KCEQvF2= MVXTRW5ITVJ?
KARPAS-45 M{LWOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEeyU5dKSzVyPUCuPVI1PjZiIN88US=> M3zJO3NCVkeHUh?=
CAL-27 NYrFVnJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rke2lEPTB;MD65NlkxPiBizszN MV3TRW5ITVJ?
SK-NEP-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HpRmlEPTB;MD65O|I1QCBizszN NYfNdI5PW0GQR1XS
COR-L105 NUn1NZA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v5dWlEPTB;MT6wNFM6PCBizszN M2\vTXNCVkeHUh?=
TI-73 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTFclBnUUN3ME2xMlAyPjViIN88US=> NX\4cnQxW0GQR1XS
JVM-3 NVXx[|dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXtNJRwUUN3ME2xMlA2ODF5IDFOwG0> NF72OXJUSU6JRWK=
HAL-01 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\heY1KSzVyPUGuNFg5OSBizszN MYnTRW5ITVJ?
QIMR-WIL NE\lW|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvBbmlOUUN3ME2xMlA6ODV6IDFOwG0> M3;3N3NCVkeHUh?=
HSC-3 NGjWclJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFwMUG3PFMhKM7:TR?= MWrTRW5ITVJ?
KY821 NXrGXGJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1G1PGlEPTB;MT6xN|M2OSBizszN NXWwfGN3W0GQR1XS
5637 MnrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fNXmlEPTB;MT6xN|gxOyBizszN NXvKXo9SW0GQR1XS
CAL-33 MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPaTWM2OD1zLkG5N|AzKCEQvF2= M1e2PHNCVkeHUh?=
ES4 MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzkdpdKSzVyPUGuNlA4QSBizszN NFHR[pFUSU6JRWK=
BHY M2\WSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rHeWlEPTB;MT6yNlg6OiBizszN NXHrWlBpW0GQR1XS
LB1047-RCC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v1[2lEPTB;MT6yN|c5PSBizszN NWfZUJdHW0GQR1XS
H4 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDuTHdHUUN3ME2xMlI1OjV3IDFOwG0> MU\TRW5ITVJ?
RPMI-8866 M3HCR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFwMk[xNFYhKM7:TR?= NVL2N4hGW0GQR1XS
HO-1-N-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PQe2lEPTB;MT6yOlM3QSBizszN MVfTRW5ITVJ?
BB30-HNC NF\ET29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHxTWM2OD1zLkK4O|E1KCEQvF2= M17ldnNCVkeHUh?=
PC-14 M1fzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWSyNmZMUUN3ME2xMlI6OjB3IDFOwG0> MVPTRW5ITVJ?
NUGC-3 MmfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLuTWM2OD1zLkK5N|U3KCEQvF2= M{fDWnNCVkeHUh?=
A4-Fuk NF;Le3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\XVXdKSzVyPUGuN|A4ODRiIN88US=> MUnTRW5ITVJ?
MHH-NB-11 NVHxVFZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvlelBKSzVyPUGuN|E{QDNiIN88US=> MVnTRW5ITVJ?
KOSC-2 NWrydGpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13pWmlEPTB;MT6zNVc4PSBizszN M2LIdHNCVkeHUh?=
A498 MmXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3tUXpmUUN3ME2xMlQxOTF|IDFOwG0> MnPBV2FPT0WU
KG-1 NIHQRmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jmd2lEPTB;MT60NVI4OyBizszN NHvve|VUSU6JRWK=
DEL NVzRW4ZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvNSIRFUUN3ME2xMlQ{PjV5IDFOwG0> NHHaNZpUSU6JRWK=
EW-16 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDLPFQyUUN3ME2xMlQ{QTd|IDFOwG0> M1TOSXNCVkeHUh?=
BPH-1 M1G1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;oWmlEPTB;MT60OFgxPSBizszN MkizV2FPT0WU
JAR NH\WeJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHwdlhKSzVyPUGuOFk{PiBizszN MYXTRW5ITVJ?
J-RT3-T3-5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1GwSGlEPTB;MT61NVczOiBizszN MY\TRW5ITVJ?
A375 M{HnS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPMTWM2OD1zLkWxO|czKCEQvF2= NWXrPJBsW0GQR1XS
SW954 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\FbWlEPTB;MT61OVAxPyBizszN MkGzV2FPT0WU
Ca9-22 NV:z[nhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPpTWM2OD1zLkW2NlYhKM7:TR?= MoLzV2FPT0WU
D-566MG NIfIfGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLoTWM2OD1zLkW3NVU2KCEQvF2= M2ric3NCVkeHUh?=
SCC-15 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XtW2lEPTB;MT62NVgxPCBizszN MmrUV2FPT0WU
HD-MY-Z M1rP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTFwNkO1PFQhKM7:TR?= MYLTRW5ITVJ?
HT-1376 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Pjb2lEPTB;MT62OFM3KCEQvF2= NGq0emRUSU6JRWK=
CAL-54 NFPMZ3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHj4OHpKSzVyPUGuOlU4ODliIN88US=> M4npWXNCVkeHUh?=
ONS-76 M4mzN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3vTWM2OD1zLk[3OVUyKCEQvF2= Ml\LV2FPT0WU
EFO-27 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmntTWM2OD1zLk[4PVIhKM7:TR?= NYi4cJFpW0GQR1XS
769-P NXexcphjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\YSnBGUUN3ME2xMlY6PTl4IDFOwG0> NFLmVYtUSU6JRWK=
MV-4-11 M{PIUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDje5p4UUN3ME2xMlY6QDV4IDFOwG0> MojKV2FPT0WU
NKM-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LDU2lEPTB;MT63NVgxOiBizszN MVHTRW5ITVJ?
LOXIMVI Mor3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFwN{S1PVkhKM7:TR?= NYTBc2ZNW0GQR1XS
KYSE-140 M1nPRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4flVmlEPTB;MT63OVY2PSBizszN NVHJOpJ1W0GQR1XS
ES5 NXrjW29RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojZTWM2OD1zLki2O|Q4KCEQvF2= NXvxU2JiW0GQR1XS
BB65-RCC MlLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTGTWM2OD1zLki5PFQ6KCEQvF2= MVjTRW5ITVJ?
HN MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofaTWM2OD1zLki5PFc1KCEQvF2= Moj0V2FPT0WU
A101D MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHiTWM2OD1zLkmzOlI5KCEQvF2= MmXpV2FPT0WU
LoVo NGfabWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLLcZRKSzVyPUGuPVc3PzliIN88US=> M3ni[HNCVkeHUh?=
NCI-H526 Ml73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFwOUmzNlUhKM7:TR?= MnKxV2FPT0WU
NCI-H1693 NUfxcllnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2G4dmlEPTB;MT65PVg5QCBizszN MUnTRW5ITVJ?
OVCAR-4 M3PjdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfiflNKSzVyPUKuNFA1OzViIN88US=> MmPMV2FPT0WU
SK-HEP-1 NGf4O3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTJwMEC3OFUhKM7:TR?= M{HYPXNCVkeHUh?=
C2BBe1 NFq4fppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT0TWM2OD1{LkCzN|czKCEQvF2= NYrwbG9yW0GQR1XS
MEL-JUSO MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvJTWM2OD1{LkC0OFY1KCEQvF2= MlH4V2FPT0WU
MOLT-16 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnPOYVKSzVyPUKuNFcxPThiIN88US=> MUfTRW5ITVJ?
NBsusSR NHvWblJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHMVZJ5UUN3ME2yMlA6QDh7IDFOwG0> NEm4OJBUSU6JRWK=
TK10 NHe3d5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;wUGdRUUN3ME2yMlE{PDV6IDFOwG0> MWrTRW5ITVJ?
CAL-39 M3;4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\STWM2OD1{LkG0OFghKM7:TR?= MXjTRW5ITVJ?
NCI-H2030 MmDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrGcFhWUUN3ME2yMlE5QTd|IDFOwG0> NHHrfHBUSU6JRWK=
HCT-116 M{nDTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M336NWlEPTB;Mj6yNlk5PCBizszN NWrjfXhOW0GQR1XS
HTC-C3 NEjRPZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP3VZZKSzVyPUKuNlY5OjRiIN88US=> M1iwPHNCVkeHUh?=
TYK-nu NGSwbZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJwM{C5NFkhKM7:TR?= Ml;yV2FPT0WU
FADU MoX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTJwM{KyPVYhKM7:TR?= M1ix[nNCVkeHUh?=
A431 MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fzPWlEPTB;Mj6zO|AzPSBizszN M4nTUHNCVkeHUh?=
TE-11 M3XjV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mor3TWM2OD1{LkO4NFE6KCEQvF2= MVzTRW5ITVJ?
CAL-12T NF7vXGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWn5cYRHUUN3ME2yMlQxPDF5IDFOwG0> MUDTRW5ITVJ?
DB MlL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\JfmlEPTB;Mj60Nlg3QSBizszN M33IS3NCVkeHUh?=
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J82 M4X4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHm2SIhKSzVyPUK5MlgxOTNiIN88US=> NYrvfXdpW0GQR1XS
MC116 NIXMbohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\XbnFKSzVyPUOwMlA4OzNiIN88US=> NHixe4hUSU6JRWK=
NCI-H69 NID6Wo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnMdItWUUN3ME2zNE43ODl|IDFOwG0> NFHzbZNUSU6JRWK=
NB6 NFLiOXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjpTWM2OD1|MT6zOlI6KCEQvF2= NIDRbXRUSU6JRWK=
CAL-120 NUHVdmpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj3Om5KSzVyPUOyMlQ{OTdiIN88US=> MnLiV2FPT0WU
U-87-MG NVz4[XRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1i1NWlEPTB;M{OuNFI2OSBizszN NFnmZ3ZUSU6JRWK=
NCI-H1304 NFnhdJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nCXWlEPTB;M{OuNFM2PCBizszN NUTCR3JTW0GQR1XS
YH-13 NH;5cGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTN|LkK1N|UhKM7:TR?= NGL1R4JUSU6JRWK=
RMG-I MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTN|LkSyPFUhKM7:TR?= MnLYV2FPT0WU
LU-65 NUHFN4x[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX2wOoo{UUN3ME2zOE4yPDB6IDFOwG0> NHvrSXFUSU6JRWK=
GB-1 M2T3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTv[IxIUUN3ME2zOU4xPzJ7IDFOwG0> MXXTRW5ITVJ?
DU-4475 NWTiXWk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC4TWM2OD1|NT6xOVU{KCEQvF2= MV\TRW5ITVJ?
SBC-5 MmPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljmTWM2OD1|Nj61PVAzKCEQvF2= NYD1c|lsW0GQR1XS
OE33 NULVSmJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnK0TWM2OD1|Nz63OVc4KCEQvF2= NV;WeXJYW0GQR1XS
C8166 NUTid412T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn61TWM2OD1|OD61NlY4KCEQvF2= MnnTV2FPT0WU
COLO-684 M4LsT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NViwdpFKUUN3ME2zPE44PDJ6IDFOwG0> NITHbm1USU6JRWK=
NCI-H1155 M{[0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTNTWM2OD1|OT6wOFcyKCEQvF2= NUXwfGVEW0GQR1XS
ATN-1 M2\1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfQTWM2OD1|OT63O|kzKCEQvF2= NEjubWVUSU6JRWK=
KARPAS-299 NXPHfoY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTN7LkizPUAh|ryP NYrFOoNSW0GQR1XS
KNS-81-FD M1fSO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPWbIdEUUN3ME20NE4{PjB2IDFOwG0> NUfjeJR[W0GQR1XS
NCI-H1563 NXPTXZdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH5dHBnUUN3ME20NU42ODN7IDFOwG0> M{DDPXNCVkeHUh?=
NB14 M3\vT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnJ[|lSUUN3ME20Nk44OjZ|IDFOwG0> NXnDNVdOW0GQR1XS
COLO-800 MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTR{Lki1NVchKM7:TR?= NHLuN5JUSU6JRWK=
MS-1 NYD6[XMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjvVFJMUUN3ME20N{4xPDh|IDFOwG0> MUnTRW5ITVJ?
OVCAR-8 NH76WlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfvTWM2OD12Mz62PFA6KCEQvF2= NHjGZXZUSU6JRWK=
SK-PN-DW NXLJeIJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTR|Lki3O|YhKM7:TR?= Mn3LV2FPT0WU
G-402 M1\WdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTR|LkmwNFYhKM7:TR?= NXTBNolzW0GQR1XS
NCI-H2291 NVrWTIpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTR2LkiwNVchKM7:TR?= M3W3cnNCVkeHUh?=
PC-3 NXXuPZAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTR3LkiwNlMhKM7:TR?= NFG5VW1USU6JRWK=
NCI-H1581 NH3rSWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjRcZNzUUN3ME20OU46QDh7IDFOwG0> NXTvcm9IW0GQR1XS
SW1116 NYrE[2ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTR5LkCxPFIhKM7:TR?= MlrwV2FPT0WU
ZR-75-30 NUHlUmpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\FR2lEPTB;NEeuNFI{QSBizszN Ml74V2FPT0WU
OCI-AML2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrwfoREUUN3ME20O{4xQTF6IDFOwG0> MUHTRW5ITVJ?
MDA-MB-231 NV\M[GVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HoW2lEPTB;NEeuOlI1QSBizszN NHfNcVBUSU6JRWK=
ES3 NFqwV4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXZTWM2OD12OD6zOVI6KCEQvF2= MkHXV2FPT0WU
NCI-H630 NEDXV3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXVNIs1UUN3ME20PU4yPzR{IDFOwG0> NVHTZYh2W0GQR1XS
OE19 M4mwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR7LkK5NFIhKM7:TR?= MorRV2FPT0WU
NCI-H1573 NFvpTlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvnZWxKSzVyPUS5MlY5PjFiIN88US=> MVnTRW5ITVJ?
EW-1 M{G2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTR7LkmwPFQhKM7:TR?= NIXmWIhUSU6JRWK=

... 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 <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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)

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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
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* 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID