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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  • 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, 16(6):1145-1154. Bosutinib (SKI-606) purchased from Selleck.

    Abl kinase phosphorylates MNRR1 in vivo. (A) K562 cells harboring the constitutively active BCR-ABL kinase when treated with 100 nM Bosutinib for 24 h show a reduction in MNRR1 phosphorylation. Lysates from vehicle and Bosutinib treated cells were immunoprecipitated using the anti-phosphotyrosine antibody and analyzed for the levels of MNRR1 in the precipitate. The IgG levels are also shown for an equal pull-down. Bosutinib efficacy was confirmed using antibodies against phospho-Abl kinase and phospho-STAT5, a downstream target of Abl kinase. Tubulin was used as a loading control. (B) Bosutinib treatment reduces the levels of phosphorylated proteins only. The total protein levels (Abl kinase and MNRR1) in vehicle and Bosutinib treated cells were similar. (C) Levels of Abl kinase in the WT and Abl kinase deficient MEFs (Abl−/− MEFs). The doublet is caused by the presence of a non-specific band [28]. (D) The level of oxygen consumption in WT MEFs transfected with either WT or phosphomimetic Y99E mutant MNRR1. Oxygen consumption was measured in intact cells on a Seahorse Bioanalyzer. (E) Y99E mutant MNRR1 stimulates oxidative phosphorylation better than WT MNRR1 in Abl deficient MEFs (Abl−/− MEFs) as measured by intact cellular oxygen consumption. (F) Bosutinib also inhibits BCR-Abl kinase in the mitochondrial fraction. NDUFS3 was used as a mitochondrial marker and GAPDH as a cytoplasmic marker to evaluate purity of the fractions. (G) K562 cells treated with Bosutinib, which show a reduction in the level of MNRR1 tyrosine phosphorylation (A), also have a reduction in the levels of oxygen consumption. (H) MNRR1 is not phosphorylated in the Abl−/− MEFs. WT and Abl−/− cellular lysates were immunoprecipitated with the anti-phosphotyrosine antibody and probed for the presence of MNRR1. The total levels of MNRR1 in the WT and Abl−/− MEFs were similar.

    Biochim Biophys Acta, 2017, 1864(2):440-448. Bosutinib (SKI-606) purchased from Selleck.

  • 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

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 NF2xellIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTBwMEiyN|EhKM7:TR?= NXTXb5FEW0GQR1XS
SW756 NV75fWs6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTBwMUSwNlQhKM7:TR?= M{Pp[XNCVkeHUh?=
CTV-1 NX3oSHlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwMU[zPVghKM7:TR?= MoHxV2FPT0WU
HSC-4 NXixeXQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr5RlNKSzVyPUCuNVcyPThiIN88US=> M3vEUnNCVkeHUh?=
LAMA-84 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2D4fmlEPTB;MD6yPFY3PCBizszN NG\PWHhUSU6JRWK=
KU812 NUGxfY1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrsPGZ6UUN3ME2wMlM1ODZ6IDFOwG0> NWPw[Zk2W0GQR1XS
HCC1806 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTBwM{WyNVYhKM7:TR?= MlfhV2FPT0WU
DOK NIrGdVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTBwM{e3PFYhKM7:TR?= M3zyXXNCVkeHUh?=
NCI-H209 Ml\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwNEC4NFghKM7:TR?= NVfoSW1TW0GQR1XS
EoL-1-cell MlnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLsVJFKSzVyPUCuOFE2PzZiIN88US=> MmX1V2FPT0WU
H9 M2fQfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\GSWZEUUN3ME2wMlQ{PDZ2IDFOwG0> NGLhRZFUSU6JRWK=
EM-2 NULBU5NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofxTWM2OD1yLkSzPFkhKM7:TR?= MYTTRW5ITVJ?
NCI-H292 M17Xc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLNNVJKSzVyPUCuOFQyODhiIN88US=> M1zaWXNCVkeHUh?=
697 NXvpO4FYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwNEW2N|MhKM7:TR?= MnTjV2FPT0WU
BHT-101 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz1RolKSzVyPUCuOFY2QSBizszN NFnOPFlUSU6JRWK=
BE-13 MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXW5[YdsUUN3ME2wMlQ5PTd{IDFOwG0> NFLRVm9USU6JRWK=
RS4-11 NEC5XoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LreWlEPTB;MD60PFU5PCBizszN MmrtV2FPT0WU
IGROV-1 NFWyZoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoP4TWM2OD1yLkS4O|k4KCEQvF2= M1T4SnNCVkeHUh?=
KE-37 MmXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHZUo9KSzVyPUCuOFk2ODliIN88US=> MmXHV2FPT0WU
BV-173 NWfGNoFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nRVGlEPTB;MD61NFc6OiBizszN M2P3e3NCVkeHUh?=
MEG-01 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLiTWM2OD1yLkWxNlE1KCEQvF2= MWrTRW5ITVJ?
LB2241-RCC NHy4bJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofZTWM2OD1yLkWzO|E5KCEQvF2= NHe3dI9USU6JRWK=
ACHN NVi0WXAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoD1TWM2OD1yLkW0NFY6KCEQvF2= NXrOSFBKW0GQR1XS
CTB-1 MlzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDuTnliUUN3ME2wMlU1QDJiIN88US=> MnzqV2FPT0WU
HT-1080 M3PGemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HYWWlEPTB;MD61OVM1QSBizszN MlLLV2FPT0WU
CHL-1 NEHv[25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\n[4c4UUN3ME2wMlU2PDZ3IDFOwG0> M{DzTnNCVkeHUh?=
EW-3 MmPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTkV3h3UUN3ME2wMlU2QTN3IDFOwG0> M3HOR3NCVkeHUh?=
ES1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwNke0PVghKM7:TR?= M2fVe3NCVkeHUh?=
KASUMI-1 M4eyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGe2NYVKSzVyPUCuO|I{OyBizszN MnLDV2FPT0WU
SW13 NVT1dVZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:3em1KSzVyPUCuO|M4QThiIN88US=> MnPUV2FPT0WU
A3-KAW NY\Sc4R2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmqzTWM2OD1yLke5NlA5KCEQvF2= NXPSfm1yW0GQR1XS
LB771-HNC NGrwOY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fE[mlEPTB;MD64N|ExPCBizszN NV\BO25sW0GQR1XS
OC-314 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnKbZpGUUN3ME2wMlg3QTZ3IDFOwG0> MWTTRW5ITVJ?
MLMA NFr0UHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTTO45JUUN3ME2wMlkxPjd3IDFOwG0> NYnOTXJqW0GQR1XS
KARPAS-45 NWjyZ3Z{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTBwOUK0OlYhKM7:TR?= M2TWWnNCVkeHUh?=
CAL-27 M4DOOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T3R2lEPTB;MD65NlkxPiBizszN MYLTRW5ITVJ?
SK-NEP-1 M3i5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PNOGlEPTB;MD65O|I1QCBizszN NGficmpUSU6JRWK=
COR-L105 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTFwMECzPVQhKM7:TR?= MUTTRW5ITVJ?
TI-73 MkS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTFwMEG2OUAh|ryP MYDTRW5ITVJ?
JVM-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PBcmlEPTB;MT6wOVAyPyBizszN NY[wVohQW0GQR1XS
HAL-01 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1H0WmlEPTB;MT6wPFgyKCEQvF2= NUO1OGhjW0GQR1XS
QIMR-WIL MnHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTuXZcyUUN3ME2xMlA6ODV6IDFOwG0> NIC3PVlUSU6JRWK=
HSC-3 NILk[2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;GNYt[UUN3ME2xMlEyPzh|IDFOwG0> MX;TRW5ITVJ?
KY821 M{HhZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULEXHliUUN3ME2xMlE{OzVzIDFOwG0> NFPuS2FUSU6JRWK=
5637 M2rWPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTFwMUO4NFMhKM7:TR?= M17LTXNCVkeHUh?=
CAL-33 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mof5TWM2OD1zLkG5N|AzKCEQvF2= MnTpV2FPT0WU
ES4 Mn;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PqUWlEPTB;MT6yNFc6KCEQvF2= M{HqdXNCVkeHUh?=
BHY MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7CbZNLUUN3ME2xMlIzQDl{IDFOwG0> NV7hcIY3W0GQR1XS
LB1047-RCC NIrmSmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\IbW1KSzVyPUGuNlM4QDViIN88US=> MY\TRW5ITVJ?
H4 NVLJU|FJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2O3RmlEPTB;MT6yOFI2PSBizszN M3;tdHNCVkeHUh?=
RPMI-8866 MmLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\jTWM2OD1zLkK2NVA3KCEQvF2= MWPTRW5ITVJ?
HO-1-N-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\SU2xKSzVyPUGuNlY{PjliIN88US=> MmiwV2FPT0WU
BB30-HNC NFTUbnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTFwMki3NVQhKM7:TR?= MmXkV2FPT0WU
PC-14 MoP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL5fWtKSzVyPUGuNlkzODViIN88US=> M2fLRnNCVkeHUh?=
NUGC-3 M1PYTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nQXmlEPTB;MT6yPVM2PiBizszN M{S3TnNCVkeHUh?=
A4-Fuk MmSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP3VFlvUUN3ME2xMlMxPzB2IDFOwG0> NWLLZopRW0GQR1XS
MHH-NB-11 NInXXmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXJeIlKSzVyPUGuN|E{QDNiIN88US=> M{jJeHNCVkeHUh?=
KOSC-2 Ml7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DxPWlEPTB;MT6zNVc4PSBizszN NV\2emJtW0GQR1XS
A498 NX;JNYd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDreoZOUUN3ME2xMlQxOTF|IDFOwG0> M{nDRXNCVkeHUh?=
KG-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFwNEGyO|MhKM7:TR?= NEnRO|JUSU6JRWK=
DEL NX\rWG1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLtTWM2OD1zLkSzOlU4KCEQvF2= Mnm4V2FPT0WU
EW-16 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYiwXW1oUUN3ME2xMlQ{QTd|IDFOwG0> NXfXRpVTW0GQR1XS
BPH-1 NEXJdpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDvTWM2OD1zLkS0PFA2KCEQvF2= NYjtPHlVW0GQR1XS
JAR MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLsb|hNUUN3ME2xMlQ6OzZiIN88US=> MkTXV2FPT0WU
J-RT3-T3-5 NE\kXXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzQR|BKSzVyPUGuOVE4OjJiIN88US=> MY\TRW5ITVJ?
A375 M3e1bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFwNUG3O|IhKM7:TR?= MVLTRW5ITVJ?
SW954 M{Czc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPwTWM2OD1zLkW1NFA4KCEQvF2= MnTjV2FPT0WU
Ca9-22 NGDNbodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP1dFBKSzVyPUGuOVYzPiBizszN MlTmV2FPT0WU
D-566MG MojZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;VRmFKSzVyPUGuOVcyPTViIN88US=> NHXVdoVUSU6JRWK=
SCC-15 NFH6T3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFwNkG4NFQhKM7:TR?= MVPTRW5ITVJ?
HD-MY-Z M2nBRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTFwNkO1PFQhKM7:TR?= MXfTRW5ITVJ?
HT-1376 MkjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC0S4VKSzVyPUGuOlQ{PiBizszN Ml70V2FPT0WU
CAL-54 M3;GPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3k[ZZKSzVyPUGuOlU4ODliIN88US=> M2fDUnNCVkeHUh?=
ONS-76 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnH[WpGUUN3ME2xMlY4PTVzIDFOwG0> NEe2bIRUSU6JRWK=
EFO-27 NYLzeYNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4W4WWlEPTB;MT62PFkzKCEQvF2= NYP1XpBwW0GQR1XS
769-P NH\5SIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nUNmlEPTB;MT62PVU6PiBizszN NWLqRoVkW0GQR1XS
MV-4-11 NYG4SJNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PrZmlEPTB;MT62PVg2PiBizszN MoXQV2FPT0WU
NKM-1 M1vWfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\0V2lEPTB;MT63NVgxOiBizszN MVjTRW5ITVJ?
LOXIMVI NHS5U4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7SVWRKSzVyPUGuO|Q2QTliIN88US=> NHXvXYZUSU6JRWK=
KYSE-140 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPuTWM2OD1zLke1OlU2KCEQvF2= NXHNcXFCW0GQR1XS
ES5 NIX2UmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwOE[3OFchKM7:TR?= MmrPV2FPT0WU
BB65-RCC MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfTXmdKSzVyPUGuPFk5PDliIN88US=> NW\yNFR1W0GQR1XS
HN MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jkc2lEPTB;MT64PVg4PCBizszN MWDTRW5ITVJ?
A101D NIXTWXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTFwOUO2NlghKM7:TR?= NFO4V21USU6JRWK=
LoVo NXPRNHB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGKxOoJKSzVyPUGuPVc3PzliIN88US=> NWDZU5BZW0GQR1XS
NCI-H526 M2q1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHCTWM2OD1zLkm5N|I2KCEQvF2= NVHXXXczW0GQR1XS
NCI-H1693 MlnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFwOUm4PFghKM7:TR?= MX3TRW5ITVJ?
OVCAR-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJwMEC0N|UhKM7:TR?= NYLnZZhKW0GQR1XS
SK-HEP-1 NGTQUZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jXPWlEPTB;Mj6wNFc1PSBizszN NWHqO2lLW0GQR1XS
C2BBe1 NFzPeI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjx[41pUUN3ME2yMlA{Ozd{IDFOwG0> MUPTRW5ITVJ?
MEL-JUSO MonLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrzSnlbUUN3ME2yMlA1PDZ2IDFOwG0> NWLTNlR2W0GQR1XS
MOLT-16 MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvvTWM2OD1{LkC3NFU5KCEQvF2= NGLjVYFUSU6JRWK=
NBsusSR Ml3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTJwMEm4PFkhKM7:TR?= NYOzSY1lW0GQR1XS
TK10 NXX2dVcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH2ydJBKSzVyPUKuNVM1PThiIN88US=> NWf3ZlI1W0GQR1XS
CAL-39 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzOTWM2OD1{LkG0OFghKM7:TR?= NEnUS5NUSU6JRWK=
NCI-H2030 NYfsSGlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDNNFNYUUN3ME2yMlE5QTd|IDFOwG0> NY\vSnZLW0GQR1XS
HCT-116 NF;BdJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\HeZpKSzVyPUKuNlI6QDRiIN88US=> M{jZRXNCVkeHUh?=
HTC-C3 MnjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGD0S49KSzVyPUKuNlY5OjRiIN88US=> MV3TRW5ITVJ?
TYK-nu MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjZTmtmUUN3ME2yMlMxQTB7IDFOwG0> NE\tO2dUSU6JRWK=
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BT-20 M2ntXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7aTWM2OD1{OD6zOlg2KCEQvF2= MWjTRW5ITVJ?
DBTRG-05MG NGi1dHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LRdmlEPTB;MkiuOFg{QCBizszN MnzwV2FPT0WU
HPAF-II MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e0NmlEPTB;MkiuO|c6KCEQvF2= MVzTRW5ITVJ?
SW837 NF;IU5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTJ7LkOzPFUhKM7:TR?= NGrBUoVUSU6JRWK=
647-V M2TIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTJTWM2OD1{OT63NFA{KCEQvF2= Ml;nV2FPT0WU
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MC116 M3v0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ftcmlEPTB;M{CuNFc{OyBizszN NFznUolUSU6JRWK=
NCI-H69 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGm0enRKSzVyPUOwMlYxQTNiIN88US=> NIK5XG9USU6JRWK=
NB6 M4LaOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XQbmlEPTB;M{GuN|YzQSBizszN NVnYOpJ3W0GQR1XS
CAL-120 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTN{LkSzNVchKM7:TR?= M1fROXNCVkeHUh?=
U-87-MG NILJVHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTN|LkCyOVEhKM7:TR?= Mne2V2FPT0WU
NCI-H1304 NEHGS4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ru[2lEPTB;M{OuNFM2PCBizszN MoLzV2FPT0WU
YH-13 NFLte|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jaTGlEPTB;M{OuNlU{PSBizszN NIK4c21USU6JRWK=
RMG-I NYDpe3JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfjWoV6UUN3ME2zN{41Ojh3IDFOwG0> MV;TRW5ITVJ?
LU-65 MojnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHhR|JKSzVyPUO0MlE1ODhiIN88US=> M3nGWnNCVkeHUh?=
GB-1 NFy3TVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTN3LkC3NlkhKM7:TR?= NVLnfXh7W0GQR1XS
DU-4475 M3;FZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Psc2lEPTB;M{WuNVU2OyBizszN MYXTRW5ITVJ?
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OE33 Ml;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHWXmc2UUN3ME2zO{44PTd5IDFOwG0> NFf5VY5USU6JRWK=
C8166 NXzYfmQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[3eYhKSzVyPUO4MlUzPjdiIN88US=> NF3Wb2tUSU6JRWK=
COLO-684 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPJSYZKSzVyPUO4Mlc1OjhiIN88US=> M{jzdHNCVkeHUh?=
NCI-H1155 MmnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnpbGU3UUN3ME2zPU4xPDdzIDFOwG0> NHHSN2JUSU6JRWK=
ATN-1 M1fzb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTN7Lke3PVIhKM7:TR?= NHnieW1USU6JRWK=
KARPAS-299 NWXEUZdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\5TWM2OD1|OT64N|khKM7:TR?= MXrTRW5ITVJ?
KNS-81-FD MkPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTRyLkO2NFQhKM7:TR?= NXPSdW15W0GQR1XS
NCI-H1563 NVzGbmNrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnsZm5KSzVyPUSxMlUxOzliIN88US=> MnnWV2FPT0WU
NB14 M{Xtb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PKZmlEPTB;NEKuO|I3OyBizszN M4TQe3NCVkeHUh?=
COLO-800 MlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrrWoZ5UUN3ME20Nk45PTF5IDFOwG0> NH20bW5USU6JRWK=
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OVCAR-8 Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjacoFKSzVyPUSzMlY5ODliIN88US=> NFTIUVlUSU6JRWK=
SK-PN-DW NUTRXWpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTR|Lki3O|YhKM7:TR?= NWD6bHcyW0GQR1XS
G-402 NW\ZXFgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnuTWM2OD12Mz65NFA3KCEQvF2= MnzFV2FPT0WU
NCI-H2291 MlfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn6RW5UUUN3ME20OE45ODF5IDFOwG0> Mn\uV2FPT0WU
PC-3 NXzRcIJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXMRVFJUUN3ME20OU45ODJ|IDFOwG0> MWfTRW5ITVJ?
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SW1116 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7mNHZKSzVyPUS3MlAyQDJiIN88US=> NIra[JJUSU6JRWK=
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OCI-AML2 M4TXV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzwOJNZUUN3ME20O{4xQTF6IDFOwG0> MWHTRW5ITVJ?
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ES3 MoSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Ty[mlEPTB;NEiuN|UzQSBizszN Mk\lV2FPT0WU
NCI-H630 M2Tlc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fM[mlEPTB;NEmuNVc1OiBizszN M2KwV3NCVkeHUh?=
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EW-1 MmG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DzUGlEPTB;NEmuPVA5PCBizszN NWD2U2JjW0GQR1XS

... 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
NCT03106779 Recruiting Chronic Myelogenous Leukemia Novartis Pharmaceuticals|Novartis October 26 2017 Phase 3
NCT03297606 Recruiting Lymphoma Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors Canadian Cancer Trials Group|AstraZeneca|Bristol-Myers Squibb|Hoffmann-La Roche|Pfizer October 6 2017 Phase 2
NCT03128411 Active not recruiting Leukemia Chronic Myelogenous Pfizer May 15 2017 Phase 2
NCT02782403 Recruiting Leukemia M.D. Anderson Cancer Center|Pfizer March 20 2017 Phase 1|Phase 2
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 dell''Adulto November 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.

Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID