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 NHroPZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3f2PGlEPTB;MD6wPFI{OSBizszN MnfJV2FPT0WU
SW756 NXzzOWZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXzeZdRUUN3ME2wMlE1ODJ2IDFOwG0> MWjTRW5ITVJ?
CTV-1 M2ruOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlyxTWM2OD1yLkG2N|k5KCEQvF2= NWPKTGU5W0GQR1XS
HSC-4 M2i5dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\oO3FMUUN3ME2wMlE4OTV6IDFOwG0> NWrOTZU3W0GQR1XS
LAMA-84 M{nmeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjSTWM2OD1yLkK4OlY1KCEQvF2= NH3PcVNUSU6JRWK=
KU812 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwM{SwOlghKM7:TR?= NWHUcpJYW0GQR1XS
HCC1806 MlnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[1cmlEPTB;MD6zOVIyPiBizszN M1PmV3NCVkeHUh?=
DOK MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnZbXRoUUN3ME2wMlM4Pzh4IDFOwG0> MX\TRW5ITVJ?
NCI-H209 NU\pbo14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm1bXFjUUN3ME2wMlQxQDB6IDFOwG0> NF;5UIlUSU6JRWK=
EoL-1-cell MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwNEG1O|YhKM7:TR?= MXzTRW5ITVJ?
H9 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLQbHhNUUN3ME2wMlQ{PDZ2IDFOwG0> M1PocHNCVkeHUh?=
EM-2 MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3RTWM2OD1yLkSzPFkhKM7:TR?= M3u1fXNCVkeHUh?=
NCI-H292 Ml3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPVN|RKSzVyPUCuOFQyODhiIN88US=> MmLuV2FPT0WU
697 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PFbmlEPTB;MD60OVY{OyBizszN NIPTbmtUSU6JRWK=
BHT-101 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwNE[1PUAh|ryP M4C1fnNCVkeHUh?=
BE-13 MmGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwNEi1O|IhKM7:TR?= M1frRXNCVkeHUh?=
RS4-11 NGXBWZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1:zZ2lEPTB;MD60PFU5PCBizszN M335d3NCVkeHUh?=
IGROV-1 NU\UTHhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zy[mlEPTB;MD60PFc6PyBizszN NIfqO4RUSU6JRWK=
KE-37 M2rR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwNEm1NFkhKM7:TR?= MY\TRW5ITVJ?
BV-173 NWfmeZNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO3cG9KSzVyPUCuOVA4QTJiIN88US=> M1fiXXNCVkeHUh?=
MEG-01 MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrjTWM2OD1yLkWxNlE1KCEQvF2= MnW5V2FPT0WU
LB2241-RCC NUDOZ|dET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwNUO3NVghKM7:TR?= M2\KOHNCVkeHUh?=
ACHN M{HvTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwNUSwOlkhKM7:TR?= M4XC[nNCVkeHUh?=
CTB-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwNUS4NkAh|ryP NGjBWGFUSU6JRWK=
HT-1080 M1;5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDLSXZKSzVyPUCuOVU{PDliIN88US=> Mm\sV2FPT0WU
CHL-1 NUjMcItvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC5TWM2OD1yLkW1OFY2KCEQvF2= MWLTRW5ITVJ?
EW-3 MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ryRWlEPTB;MD61OVk{PSBizszN MVrTRW5ITVJ?
ES1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTpTWM2OD1yLk[3OFk5KCEQvF2= MV3TRW5ITVJ?
KASUMI-1 M2fncmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwN{KzN{Ah|ryP MmDKV2FPT0WU
SW13 MmX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoW1TWM2OD1yLkezO|k5KCEQvF2= MmfjV2FPT0WU
A3-KAW MoTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwN{myNFghKM7:TR?= MVnTRW5ITVJ?
LB771-HNC NI\weFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3sXG04UUN3ME2wMlg{OTB2IDFOwG0> M{LkUHNCVkeHUh?=
OC-314 NYW5dIt2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwOE[5OlUhKM7:TR?= NFXBeGtUSU6JRWK=
MLMA MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj0S2VKSzVyPUCuPVA3PzViIN88US=> MlS2V2FPT0WU
KARPAS-45 NHfsSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\1UGlEPTB;MD65NlQ3PiBizszN MXLTRW5ITVJ?
CAL-27 MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTQTWM2OD1yLkmyPVA3KCEQvF2= M1zJPHNCVkeHUh?=
SK-NEP-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;PTWM2OD1yLkm3NlQ5KCEQvF2= NUm4[HZzW0GQR1XS
COR-L105 NXrJfXVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTFwMECzPVQhKM7:TR?= M3jGU3NCVkeHUh?=
TI-73 NWL0UYZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH2VYVKSzVyPUGuNFE3PSBizszN MYHTRW5ITVJ?
JVM-3 NYr3WVNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV6x[YpLUUN3ME2xMlA2ODF5IDFOwG0> M1XY[HNCVkeHUh?=
HAL-01 NF\1[VlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrvTWM2OD1zLkC4PFEhKM7:TR?= MYnTRW5ITVJ?
QIMR-WIL M1f4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnnTWM2OD1zLkC5NFU5KCEQvF2= MUfTRW5ITVJ?
HSC-3 M3PvUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DtPGlEPTB;MT6xNVc5OyBizszN M13Ec3NCVkeHUh?=
KY821 NV\ySnE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFwMUOzOVEhKM7:TR?= NGn4N5BUSU6JRWK=
5637 NXjrdXloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;HWHlKSzVyPUGuNVM5ODNiIN88US=> NVrEeJZWW0GQR1XS
CAL-33 MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwMUmzNFIhKM7:TR?= M2fjW3NCVkeHUh?=
ES4 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTFwMkC3PUAh|ryP NYDmbo5OW0GQR1XS
BHY MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzJfJppUUN3ME2xMlIzQDl{IDFOwG0> M1r1dXNCVkeHUh?=
LB1047-RCC Mm\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPLTWM2OD1zLkKzO|g2KCEQvF2= MWfTRW5ITVJ?
H4 NESwOlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTFwMkSyOVUhKM7:TR?= MlroV2FPT0WU
RPMI-8866 M{i1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmmwTWM2OD1zLkK2NVA3KCEQvF2= MmCyV2FPT0WU
HO-1-N-1 NEjENplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYm2[Hd3UUN3ME2xMlI3OzZ7IDFOwG0> NVPkfFhzW0GQR1XS
BB30-HNC M4XucWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn4NFJbUUN3ME2xMlI5PzF2IDFOwG0> M4nLSHNCVkeHUh?=
PC-14 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnlTpVKSzVyPUGuNlkzODViIN88US=> MmqwV2FPT0WU
NUGC-3 MnPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTFwMkmzOVYhKM7:TR?= M2Hpe3NCVkeHUh?=
A4-Fuk NV7kS5dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH5bY51UUN3ME2xMlMxPzB2IDFOwG0> MWXTRW5ITVJ?
MHH-NB-11 MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGzTWM2OD1zLkOxN|g{KCEQvF2= M{Hz[3NCVkeHUh?=
KOSC-2 M2\DRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[4NJl7UUN3ME2xMlMyPzd3IDFOwG0> NUDWNHd3W0GQR1XS
A498 M1vpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInqdmpKSzVyPUGuOFAyOTNiIN88US=> MoLpV2FPT0WU
KG-1 MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfsTWM2OD1zLkSxNlc{KCEQvF2= NVXReVl1W0GQR1XS
DEL NGPEUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHWVVBKSzVyPUGuOFM3PTdiIN88US=> Mmi4V2FPT0WU
EW-16 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL6TWM2OD1zLkSzPVc{KCEQvF2= NXLOfJRHW0GQR1XS
BPH-1 M13hVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHu1SVhKSzVyPUGuOFQ5ODViIN88US=> NIfoR5RUSU6JRWK=
JAR M3jN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHK4ZlBKSzVyPUGuOFk{PiBizszN MlP5V2FPT0WU
J-RT3-T3-5 M1PHbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorsTWM2OD1zLkWxO|IzKCEQvF2= MWDTRW5ITVJ?
A375 Mmj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwNUG3O|IhKM7:TR?= MmK1V2FPT0WU
SW954 MlT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTFwNUWwNFchKM7:TR?= NEHXTlhUSU6JRWK=
Ca9-22 NXzifZpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\tdHJKSzVyPUGuOVYzPiBizszN M1L5XXNCVkeHUh?=
D-566MG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHyZlAxUUN3ME2xMlU4OTV3IDFOwG0> MXHTRW5ITVJ?
SCC-15 NIO2V4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLKTWM2OD1zLk[xPFA1KCEQvF2= NFHmd4RUSU6JRWK=
HD-MY-Z MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLOXGlzUUN3ME2xMlY{PTh2IDFOwG0> M4HhZXNCVkeHUh?=
HT-1376 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnDS4ZrUUN3ME2xMlY1OzZiIN88US=> NF;qO4RUSU6JRWK=
CAL-54 NH3xPFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPXfG1KSzVyPUGuOlU4ODliIN88US=> NXSwZndPW0GQR1XS
ONS-76 NUXWZZUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mke1TWM2OD1zLk[3OVUyKCEQvF2= M{f5O3NCVkeHUh?=
EFO-27 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4qwbGlEPTB;MT62PFkzKCEQvF2= M3K5bnNCVkeHUh?=
769-P Mo\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzNTWM2OD1zLk[5OVk3KCEQvF2= M1LhcHNCVkeHUh?=
MV-4-11 MnzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjzTWM2OD1zLk[5PFU3KCEQvF2= M{TMXHNCVkeHUh?=
NKM-1 NVm2bXp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;Y[WhoUUN3ME2xMlcyQDB{IDFOwG0> M1jyN3NCVkeHUh?=
LOXIMVI M4PkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTFwN{S1PVkhKM7:TR?= NFO5TlZUSU6JRWK=
KYSE-140 NWS0[4E5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr5TWM2OD1zLke1OlU2KCEQvF2= MUPTRW5ITVJ?
ES5 MmrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TBT2lEPTB;MT64Olc1PyBizszN MX\TRW5ITVJ?
BB65-RCC MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTFwOEm4OFkhKM7:TR?= Mn7NV2FPT0WU
HN NHKydJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\ZcJE{UUN3ME2xMlg6QDd2IDFOwG0> NHr5[oxUSU6JRWK=
A101D M4ThT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3oT2RKSzVyPUGuPVM3OjhiIN88US=> MXjTRW5ITVJ?
LoVo NES0NlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwOUe2O|khKM7:TR?= M1GwPHNCVkeHUh?=
NCI-H526 NY\VUII3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zYfmlEPTB;MT65PVMzPSBizszN MUjTRW5ITVJ?
NCI-H1693 NVO1Z4Z{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\JZWlEPTB;MT65PVg5QCBizszN NUnzSpI6W0GQR1XS
OVCAR-4 MlrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvrUFNKSzVyPUKuNFA1OzViIN88US=> MkPpV2FPT0WU
SK-HEP-1 NXf3SXp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTQ[IpJUUN3ME2yMlAxPzR3IDFOwG0> NYDFV|J4W0GQR1XS
C2BBe1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7FbVRKSzVyPUKuNFM{PzJiIN88US=> MUPTRW5ITVJ?
MEL-JUSO MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HYd2lEPTB;Mj6wOFQ3PCBizszN M2HuW3NCVkeHUh?=
MOLT-16 MlrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfQTWM2OD1{LkC3NFU5KCEQvF2= MoX5V2FPT0WU
NBsusSR M{K5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDNTHF6UUN3ME2yMlA6QDh7IDFOwG0> Mlf2V2FPT0WU
TK10 NG[2SnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTJwMUO0OVghKM7:TR?= MlzqV2FPT0WU
CAL-39 NUTpRnduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfLcppVUUN3ME2yMlE1PDhiIN88US=> NICzPZhUSU6JRWK=
NCI-H2030 NXzoUJZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\USIdsUUN3ME2yMlE5QTd|IDFOwG0> MXPTRW5ITVJ?
HCT-116 MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTlV3BEUUN3ME2yMlIzQTh2IDFOwG0> MljvV2FPT0WU
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NCI-H1770 NV;0T|BLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULvZ2pyUUN3ME2yPE4{PTZ4IDFOwG0> NEXOWodUSU6JRWK=
BT-20 Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPqUmNKSzVyPUK4MlM3QDViIN88US=> NWfGb3o2W0GQR1XS
DBTRG-05MG NXXodXZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPZR3REUUN3ME2yPE41QDN6IDFOwG0> MlXGV2FPT0WU
HPAF-II MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTJ6Lke3PUAh|ryP MUjTRW5ITVJ?
SW837 MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHXSnlKSzVyPUK5MlM{QDViIN88US=> M4LMfXNCVkeHUh?=
647-V NXvnPJpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJ7LkewNFMhKM7:TR?= M{Hz[3NCVkeHUh?=
J82 NHHxV2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIK2dYlKSzVyPUK5MlgxOTNiIN88US=> NVTVR204W0GQR1XS
MC116 NVr3RlBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTNyLkC3N|MhKM7:TR?= Ml[wV2FPT0WU
NCI-H69 NWDBUnViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTNyLk[wPVMhKM7:TR?= NX24fFYyW0GQR1XS
NB6 M4Dwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\4Z2lEPTB;M{GuN|YzQSBizszN NYHk[nNNW0GQR1XS
CAL-120 M3;lemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLBTWM2OD1|Mj60N|E4KCEQvF2= MYjTRW5ITVJ?
U-87-MG MnWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFq3XZpKSzVyPUOzMlAzPTFiIN88US=> MV7TRW5ITVJ?
NCI-H1304 NHq1TpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPlOm1LUUN3ME2zN{4xOzV2IDFOwG0> NFfuNo9USU6JRWK=
YH-13 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rkNmlEPTB;M{OuNlU{PSBizszN MoDTV2FPT0WU
RMG-I NE\tcXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDnOFFtUUN3ME2zN{41Ojh3IDFOwG0> M{LFUnNCVkeHUh?=
LU-65 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIm1dlFKSzVyPUO0MlE1ODhiIN88US=> MU\TRW5ITVJ?
GB-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTN3LkC3NlkhKM7:TR?= Mnz6V2FPT0WU
DU-4475 NHHIUolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmG0TWM2OD1|NT6xOVU{KCEQvF2= M2jhcnNCVkeHUh?=
SBC-5 MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTN4LkW5NFIhKM7:TR?= NGP6b|BUSU6JRWK=
OE33 M{LlTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULY[4hYUUN3ME2zO{44PTd5IDFOwG0> M4rOb3NCVkeHUh?=
C8166 MljJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTN6LkWyOlchKM7:TR?= M2HEZXNCVkeHUh?=
COLO-684 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13MdmlEPTB;M{iuO|QzQCBizszN NVrTNYlpW0GQR1XS
NCI-H1155 NFzpR21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zKZmlEPTB;M{muNFQ4OSBizszN M3;qS3NCVkeHUh?=
ATN-1 NFntcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlG5TWM2OD1|OT63O|kzKCEQvF2= NWLtZ4lvW0GQR1XS
KARPAS-299 NUHNVXlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTN7LkizPUAh|ryP M2GwbnNCVkeHUh?=
KNS-81-FD MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfwTWM2OD12MD6zOlA1KCEQvF2= NHfSZplUSU6JRWK=
NCI-H1563 M3L0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDWdItlUUN3ME20NU42ODN7IDFOwG0> MlvWV2FPT0WU
NB14 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jFOmlEPTB;NEKuO|I3OyBizszN M1fGc3NCVkeHUh?=
COLO-800 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTR{Lki1NVchKM7:TR?= MVrTRW5ITVJ?
MS-1 M4\x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTR|LkC0PFMhKM7:TR?= NEXoVIJUSU6JRWK=
OVCAR-8 NUHGTY5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXNTWM2OD12Mz62PFA6KCEQvF2= NYHiUlFTW0GQR1XS
SK-PN-DW M3jGdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DiOWlEPTB;NEOuPFc4PiBizszN MX7TRW5ITVJ?
G-402 NX2zO2NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LodGlEPTB;NEOuPVAxPiBizszN NWL4flh4W0GQR1XS
NCI-H2291 NHfpbHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWC5bWdLUUN3ME20OE45ODF5IDFOwG0> MXzTRW5ITVJ?
PC-3 M3nuemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;jco9KSzVyPUS1MlgxOjNiIN88US=> Moe0V2FPT0WU
NCI-H1581 Mlf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDvNHdKSzVyPUS1Mlk5QDliIN88US=> MmfnV2FPT0WU
SW1116 MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T3[WlEPTB;NEeuNFE5OiBizszN NFvLNmJUSU6JRWK=
ZR-75-30 MmPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj2XZFbUUN3ME20O{4xOjN7IDFOwG0> Ml3aV2FPT0WU
OCI-AML2 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTR5LkC5NVghKM7:TR?= Mn2xV2FPT0WU
MDA-MB-231 NFzkclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3LTWM2OD12Nz62NlQ6KCEQvF2= NWTpPGo2W0GQR1XS
ES3 NYXGfIEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K5dmlEPTB;NEiuN|UzQSBizszN Mn32V2FPT0WU
NCI-H630 MoXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnVTWM2OD12OT6xO|QzKCEQvF2= NX;N[o1IW0GQR1XS
OE19 NELQVHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTR7LkK5NFIhKM7:TR?= NGXSWllUSU6JRWK=
NCI-H1573 NF71[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTR7Lk[4OlEhKM7:TR?= MnPyV2FPT0WU
EW-1 NWKyXWV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTR7LkmwPFQhKM7:TR?= MVjTRW5ITVJ?

... 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
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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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    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

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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
NCT02228382 Active not recruiting Previously Treated PH + CML Pfizer|Developmental Therapeutics Consortium November 7 2014 Phase 4
NCT01903733 Active not recruiting Chronic Myeloid Leukemia Pfizer August 28 2013 Not Applicable
NCT03106779 Recruiting Chronic Myelogenous Leukemia Novartis Pharmaceuticals|Novartis October 26 2017 Phase 3
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
NCT02906696 Recruiting Chronic Myelogenous Leukemia M.D. Anderson Cancer Center|Pfizer October 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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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