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

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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 NFLDcZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvlNZJKSzVyPUCuNFgzOzFiIN88US=> MVTTRW5ITVJ?
SW756 MmTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XFPGlEPTB;MD6xOFAzPCBizszN M1;Z[3NCVkeHUh?=
CTV-1 NHT5NlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPJTWM2OD1yLkG2N|k5KCEQvF2= MX3TRW5ITVJ?
HSC-4 MlXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmmyTWM2OD1yLkG3NVU5KCEQvF2= NXHsRmpjW0GQR1XS
LAMA-84 NFj4NWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TpNWlEPTB;MD6yPFY3PCBizszN NGLLbIFUSU6JRWK=
KU812 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHqTWM2OD1yLkO0NFY5KCEQvF2= M365c3NCVkeHUh?=
HCC1806 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHjZ25MUUN3ME2wMlM2OjF4IDFOwG0> M2f3enNCVkeHUh?=
DOK MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTVN2RbUUN3ME2wMlM4Pzh4IDFOwG0> NGfUZWpUSU6JRWK=
NCI-H209 MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T6bmlEPTB;MD60NFgxQCBizszN NGKzTGtUSU6JRWK=
EoL-1-cell MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwNEG1O|YhKM7:TR?= NHHUOpRUSU6JRWK=
H9 MlHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPKTWM2OD1yLkSzOFY1KCEQvF2= M33G[XNCVkeHUh?=
EM-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXjdnVKSzVyPUCuOFM5QSBizszN MWHTRW5ITVJ?
NCI-H292 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwNESxNFghKM7:TR?= M32zRnNCVkeHUh?=
697 MnfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwNEW2N|MhKM7:TR?= MnHXV2FPT0WU
BHT-101 NEX4UFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mle1TWM2OD1yLkS2OVkhKM7:TR?= MYTTRW5ITVJ?
BE-13 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vqXWlEPTB;MD60PFU4OiBizszN Mn\RV2FPT0WU
RS4-11 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTBwNEi1PFQhKM7:TR?= MmPpV2FPT0WU
IGROV-1 NGruV2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z2ZmlEPTB;MD60PFc6PyBizszN NXHpSI8yW0GQR1XS
KE-37 M4T3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXZcHk6UUN3ME2wMlQ6PTB7IDFOwG0> MYjTRW5ITVJ?
BV-173 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorhTWM2OD1yLkWwO|kzKCEQvF2= NV;He3REW0GQR1XS
MEG-01 NUSzSVNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHFcYxKSzVyPUCuOVEzOTRiIN88US=> NH3WeW5USU6JRWK=
LB2241-RCC M3LiO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj3TWM2OD1yLkWzO|E5KCEQvF2= MVXTRW5ITVJ?
ACHN NFywe4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPuTmFuUUN3ME2wMlU1ODZ7IDFOwG0> Mk\TV2FPT0WU
CTB-1 Mk\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7OTWM2OD1yLkW0PFIhKM7:TR?= MX\TRW5ITVJ?
HT-1080 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M162cmlEPTB;MD61OVM1QSBizszN NXK3T|RpW0GQR1XS
CHL-1 NIHBb2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;4folKSzVyPUCuOVU1PjViIN88US=> NInISHJUSU6JRWK=
EW-3 Mmq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXSUZBKSzVyPUCuOVU6OzViIN88US=> NH;YS4NUSU6JRWK=
ES1 M2fWUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[1TWM2OD1yLk[3OFk5KCEQvF2= M3fqOHNCVkeHUh?=
KASUMI-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGP4R5FKSzVyPUCuO|I{OyBizszN NYTQN2JjW0GQR1XS
SW13 MojXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPLO5FKSzVyPUCuO|M4QThiIN88US=> MnPmV2FPT0WU
A3-KAW NEnxSIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[3Z5dsUUN3ME2wMlc6OjB6IDFOwG0> M3;icHNCVkeHUh?=
LB771-HNC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTBwOEOxNFQhKM7:TR?= NFvmW4lUSU6JRWK=
OC-314 MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwOE[5OlUhKM7:TR?= M{G2cHNCVkeHUh?=
MLMA NWjuOYNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwOUC2O|UhKM7:TR?= NV2x[ohPW0GQR1XS
KARPAS-45 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LhcmlEPTB;MD65NlQ3PiBizszN MmXyV2FPT0WU
CAL-27 M{LiVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDMUWJrUUN3ME2wMlkzQTB4IDFOwG0> M176dHNCVkeHUh?=
SK-NEP-1 M4\3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{K4ZmlEPTB;MD65O|I1QCBizszN M4\ZUHNCVkeHUh?=
COR-L105 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\GeGlEPTB;MT6wNFM6PCBizszN MVHTRW5ITVJ?
TI-73 M1z3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7jdFdKSzVyPUGuNFE3PSBizszN NIDDdotUSU6JRWK=
JVM-3 M1;sfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjhTWM2OD1zLkC1NFE4KCEQvF2= NUnqNWNlW0GQR1XS
HAL-01 NWjXUWhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S2[GlEPTB;MT6wPFgyKCEQvF2= MVvTRW5ITVJ?
QIMR-WIL NEfvdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTFwMEmwOVghKM7:TR?= M4nWeXNCVkeHUh?=
HSC-3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYT2[XdJUUN3ME2xMlEyPzh|IDFOwG0> NE\SXYtUSU6JRWK=
KY821 NE\Y[FZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmizTWM2OD1zLkGzN|UyKCEQvF2= NF;4XVVUSU6JRWK=
5637 M2fM[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjFRpdDUUN3ME2xMlE{QDB|IDFOwG0> MUPTRW5ITVJ?
CAL-33 MlP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPpbJZKSzVyPUGuNVk{ODJiIN88US=> NUPCSlhMW0GQR1XS
ES4 NV7B[oFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTFwMkC3PUAh|ryP NULRU5VFW0GQR1XS
BHY NXrsfFdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwMkK4PVIhKM7:TR?= M4LPUnNCVkeHUh?=
LB1047-RCC MmXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XMdmlEPTB;MT6yN|c5PSBizszN M3q0Z3NCVkeHUh?=
H4 NX\RUXVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK5TWM2OD1zLkK0NlU2KCEQvF2= MnzPV2FPT0WU
RPMI-8866 NUH6Spd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL5TWM2OD1zLkK2NVA3KCEQvF2= M33ZPXNCVkeHUh?=
HO-1-N-1 NFLOZppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4m4WmlEPTB;MT6yOlM3QSBizszN NIfK[lVUSU6JRWK=
BB30-HNC NF:wS3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[xeWlEPTB;MT6yPFcyPCBizszN NGXOXWRUSU6JRWK=
PC-14 MknoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV61flE{UUN3ME2xMlI6OjB3IDFOwG0> MVzTRW5ITVJ?
NUGC-3 NFfBdGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1KxXGlEPTB;MT6yPVM2PiBizszN MV3TRW5ITVJ?
A4-Fuk MoDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUX0RohDUUN3ME2xMlMxPzB2IDFOwG0> M4T5ZXNCVkeHUh?=
MHH-NB-11 NUSz[JNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33aRWlEPTB;MT6zNVM5OyBizszN MlTHV2FPT0WU
KOSC-2 NYDEbXZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlf4TWM2OD1zLkOxO|c2KCEQvF2= MXLTRW5ITVJ?
A498 NHnufHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M173OmlEPTB;MT60NFEyOyBizszN NGDrZlNUSU6JRWK=
KG-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\yTWM2OD1zLkSxNlc{KCEQvF2= M13MNnNCVkeHUh?=
DEL MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFwNEO2OVchKM7:TR?= NYrlNFQ6W0GQR1XS
EW-16 NF70VINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfqTWM2OD1zLkSzPVc{KCEQvF2= MX7TRW5ITVJ?
BPH-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDpTFM3UUN3ME2xMlQ1QDB3IDFOwG0> NFnhfVlUSU6JRWK=
JAR NUTZeGhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwNEmzOkAh|ryP MnrHV2FPT0WU
J-RT3-T3-5 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH5d2xKSzVyPUGuOVE4OjJiIN88US=> MUHTRW5ITVJ?
A375 M4\RXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2W0c2lEPTB;MT61NVc4OiBizszN M2TyWnNCVkeHUh?=
SW954 M3XDdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTFwNUWwNFchKM7:TR?= MWHTRW5ITVJ?
Ca9-22 NHX1OJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEf0UG9KSzVyPUGuOVYzPiBizszN NEPGT2pUSU6JRWK=
D-566MG MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFwNUexOVUhKM7:TR?= Mm\RV2FPT0WU
SCC-15 NVrIfpViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULOWotGUUN3ME2xMlYyQDB2IDFOwG0> MXnTRW5ITVJ?
HD-MY-Z MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGqwbpNKSzVyPUGuOlM2QDRiIN88US=> M1;sW3NCVkeHUh?=
HT-1376 NIDFS2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfGSplQUUN3ME2xMlY1OzZiIN88US=> MYXTRW5ITVJ?
CAL-54 M3H6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW4TXlKSzVyPUGuOlU4ODliIN88US=> NXzzTJEzW0GQR1XS
ONS-76 NFL4WWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDocIdKSzVyPUGuOlc2PTFiIN88US=> MlnXV2FPT0WU
EFO-27 M3K3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j2bWlEPTB;MT62PFkzKCEQvF2= NUXnNYR1W0GQR1XS
769-P MoTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LkeGlEPTB;MT62PVU6PiBizszN MWXTRW5ITVJ?
MV-4-11 M4jnPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL0TnFKSzVyPUGuOlk5PTZiIN88US=> NXnQVmlvW0GQR1XS
NKM-1 NUL3emdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PiR2lEPTB;MT63NVgxOiBizszN MXPTRW5ITVJ?
LOXIMVI MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mli5TWM2OD1zLke0OVk6KCEQvF2= NISySHJUSU6JRWK=
KYSE-140 NGX2OYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnexTWM2OD1zLke1OlU2KCEQvF2= MnzQV2FPT0WU
ES5 MlLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTFwOE[3OFchKM7:TR?= MojmV2FPT0WU
BB65-RCC MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTFwOEm4OFkhKM7:TR?= MWXTRW5ITVJ?
HN Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37sSWlEPTB;MT64PVg4PCBizszN NFHZWGhUSU6JRWK=
A101D M{TJWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXnTZRKSzVyPUGuPVM3OjhiIN88US=> M4fOWHNCVkeHUh?=
LoVo MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TtN2lEPTB;MT65O|Y4QSBizszN MUfTRW5ITVJ?
NCI-H526 MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTJTWM2OD1zLkm5N|I2KCEQvF2= M4n2bHNCVkeHUh?=
NCI-H1693 M1rKfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFwOUm4PFghKM7:TR?= MojLV2FPT0WU
OVCAR-4 M{\tOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDGWVBKSzVyPUKuNFA1OzViIN88US=> M{OzcHNCVkeHUh?=
SK-HEP-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHGO2xKSzVyPUKuNFA4PDViIN88US=> MljLV2FPT0WU
C2BBe1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlr6TWM2OD1{LkCzN|czKCEQvF2= NHj1VlNUSU6JRWK=
MEL-JUSO MoDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGO1[4lKSzVyPUKuNFQ1PjRiIN88US=> M1rqOnNCVkeHUh?=
MOLT-16 NHnxNGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37jcWlEPTB;Mj6wO|A2QCBizszN Ml\sV2FPT0WU
NBsusSR NGqxcIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XYVGlEPTB;Mj6wPVg5QSBizszN NULVWFBlW0GQR1XS
TK10 MojyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jEcmlEPTB;Mj6xN|Q2QCBizszN MXzTRW5ITVJ?
CAL-39 M4PN[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;iTWM2OD1{LkG0OFghKM7:TR?= M4\t[HNCVkeHUh?=
NCI-H2030 NUOzbHhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3RTWM2OD1{LkG4PVc{KCEQvF2= MXzTRW5ITVJ?
HCT-116 MleyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PRO2lEPTB;Mj6yNlk5PCBizszN NVLVcI1{W0GQR1XS
HTC-C3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJwMk[4NlQhKM7:TR?= M1m0THNCVkeHUh?=
TYK-nu M2PacWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJwM{C5NFkhKM7:TR?= M1vLNnNCVkeHUh?=
FADU M1KwdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJwM{KyPVYhKM7:TR?= NVnxSXhvW0GQR1XS
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BT-20 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\lTWM2OD1{OD6zOlg2KCEQvF2= MX\TRW5ITVJ?
DBTRG-05MG NF3YZpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ6LkS4N|ghKM7:TR?= MXPTRW5ITVJ?
HPAF-II MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrxWXU{UUN3ME2yPE44PzliIN88US=> M4XaU3NCVkeHUh?=
SW837 M3\xSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrwVpVKSzVyPUK5MlM{QDViIN88US=> M36xVnNCVkeHUh?=
647-V NXOwNoFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jxT2lEPTB;MkmuO|AxOyBizszN NHPldo9USU6JRWK=
J82 M2\mPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3j6N2lEPTB;MkmuPFAyOyBizszN NVnoOJNUW0GQR1XS
MC116 M2DI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLDTnFKSzVyPUOwMlA4OzNiIN88US=> NF\KWotUSU6JRWK=
NCI-H69 MkPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\rNGlEPTB;M{CuOlA6OyBizszN M1;pPXNCVkeHUh?=
NB6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnjVpNwUUN3ME2zNU4{PjJ7IDFOwG0> M3LwOHNCVkeHUh?=
CAL-120 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T0U2lEPTB;M{KuOFMyPyBizszN NVrweWVqW0GQR1XS
U-87-MG MnLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTN|LkCyOVEhKM7:TR?= M4nzTnNCVkeHUh?=
NCI-H1304 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTN|LkCzOVQhKM7:TR?= MUDTRW5ITVJ?
YH-13 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zKSWlEPTB;M{OuNlU{PSBizszN MXzTRW5ITVJ?
RMG-I NXHi[pBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH20bHlKSzVyPUOzMlQzQDViIN88US=> NFz4[IlUSU6JRWK=
LU-65 NFq3XVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXlUJNKSzVyPUO0MlE1ODhiIN88US=> NE\BUJpUSU6JRWK=
GB-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PuS2lEPTB;M{WuNFczQSBizszN NHvVfIdUSU6JRWK=
DU-4475 MmnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPHfYRnUUN3ME2zOU4yPTV|IDFOwG0> NUnvO4pOW0GQR1XS
SBC-5 NFXmdolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\FSGlEPTB;M{[uOVkxOiBizszN MmLjV2FPT0WU
OE33 MlrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTN5Lke1O|chKM7:TR?= NXrrS|J1W0GQR1XS
C8166 M{K1UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTN6LkWyOlchKM7:TR?= MXzTRW5ITVJ?
COLO-684 M2TCfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nnOWlEPTB;M{iuO|QzQCBizszN MlP3V2FPT0WU
NCI-H1155 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfDTWM2OD1|OT6wOFcyKCEQvF2= NIXDPXdUSU6JRWK=
ATN-1 NETHe|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTN7Lke3PVIhKM7:TR?= MUnTRW5ITVJ?
KARPAS-299 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7OW5NUUUN3ME2zPU45OzliIN88US=> MWPTRW5ITVJ?
KNS-81-FD MlTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;MSVFCUUN3ME20NE4{PjB2IDFOwG0> NFT1eHBUSU6JRWK=
NCI-H1563 NH;EfZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13sW2lEPTB;NEGuOVA{QSBizszN NXn2Z5l7W0GQR1XS
NB14 NWD6[GRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LVRmlEPTB;NEKuO|I3OyBizszN MVvTRW5ITVJ?
COLO-800 NXe4eZlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki5TWM2OD12Mj64OVE4KCEQvF2= MoH5V2FPT0WU
MS-1 MoDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC0dYJKSzVyPUSzMlA1QDNiIN88US=> NF;DZW1USU6JRWK=
OVCAR-8 M{fzdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzBTWM2OD12Mz62PFA6KCEQvF2= MnrLV2FPT0WU
SK-PN-DW NHL4R|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTR|Lki3O|YhKM7:TR?= M2LLU3NCVkeHUh?=
G-402 MmrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrGTHFKSzVyPUSzMlkxODZiIN88US=> M4rwc3NCVkeHUh?=
NCI-H2291 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHQTWM2OD12ND64NFE4KCEQvF2= MVfTRW5ITVJ?
PC-3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C1SWlEPTB;NEWuPFAzOyBizszN NFO3d3hUSU6JRWK=
NCI-H1581 NGfOV2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLHOYY2UUN3ME20OU46QDh7IDFOwG0> MoG5V2FPT0WU
SW1116 NV3KNmRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{mxdGlEPTB;NEeuNFE5OiBizszN M371S3NCVkeHUh?=
ZR-75-30 NWSyU3lxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTR5LkCyN|khKM7:TR?= MojTV2FPT0WU
OCI-AML2 NEDweZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3DUmZKSzVyPUS3MlA6OThiIN88US=> MmK3V2FPT0WU
MDA-MB-231 Ml3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyzXHl2UUN3ME20O{43OjR7IDFOwG0> MmLFV2FPT0WU
ES3 NYjUZWtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTR6LkO1NlkhKM7:TR?= NVHZZ2piW0GQR1XS
NCI-H630 NFPlNHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLVSVBKSzVyPUS5MlE4PDJiIN88US=> NYTGToFxW0GQR1XS
OE19 NIfMS5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1:3c2lEPTB;NEmuNlkxOiBizszN NWfzfnRTW0GQR1XS
NCI-H1573 M3vBO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzwcVJpUUN3ME20PU43QDZzIDFOwG0> M3fEWHNCVkeHUh?=
EW-1 M{CwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1SxZmlEPTB;NEmuPVA5PCBizszN M3mxb3NCVkeHUh?=

... 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

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

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Dilution Calculator

Dilution Calculator

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

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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.

selleck catalog

Src Signaling Pathway Map

Src Inhibitors with Unique Features

  • Most Potent Src Inhibitor

    Dasatinib : Src, IC50=0.8 nM.

  • FDA-approved Src Inhibitor

    Dasatinib : Approved by FDA for CML and Ph+ ALL.

  • Newest Src Inhibitor

    PP1 : Potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • Classic Src Inhibitor

    KX2-391 : The first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

Related Src Products4

  • Dasatinib Monohydrate New

    Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.

  • SU6656 New

    SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

  • PX-478 2HCl New

    PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

  • Saracatinib (AZD0530)

    Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.

    Features:The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.

  • Dasatinib

    Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.

  • KX2-391

    KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.

  • PP1

    PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • PP2

    PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.

  • WH-4-023

    WH-4-023 is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.

  • Ibrutinib (PCI-32765)

    Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID