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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5 Customer Reviews

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

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

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

    Mol Cancer Ther, 2017, 16(6):1145-1154. 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.

    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.

  • 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 NFPmZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHK4R4JKSzVyPUCuNFgzOzFiIN88US=> NXnTeI9SW0GQR1XS
SW756 MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mon1TWM2OD1yLkG0NFI1KCEQvF2= NFjPdFhUSU6JRWK=
CTV-1 NV3hO3M2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwMU[zPVghKM7:TR?= Mn22V2FPT0WU
HSC-4 NY\lTohVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXexVGs3UUN3ME2wMlE4OTV6IDFOwG0> NFrNS2NUSU6JRWK=
LAMA-84 NULpb2VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPqNYVKSzVyPUCuNlg3PjRiIN88US=> MX\TRW5ITVJ?
KU812 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jIRmlEPTB;MD6zOFA3QCBizszN MmOxV2FPT0WU
HCC1806 NV;1WpZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjFPIdXUUN3ME2wMlM2OjF4IDFOwG0> MlzQV2FPT0WU
DOK NUjDUYV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWOzXWZWUUN3ME2wMlM4Pzh4IDFOwG0> MoTKV2FPT0WU
NCI-H209 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jqUmlEPTB;MD60NFgxQCBizszN M123WXNCVkeHUh?=
EoL-1-cell Ml;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDIbIhKSzVyPUCuOFE2PzZiIN88US=> NHr4VGhUSU6JRWK=
H9 M2n5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWGzVW5lUUN3ME2wMlQ{PDZ2IDFOwG0> NHTDO29USU6JRWK=
EM-2 M2DwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFT2RVJKSzVyPUCuOFM5QSBizszN NYC4NIRHW0GQR1XS
NCI-H292 MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwNESxNFghKM7:TR?= MVXTRW5ITVJ?
697 MkL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\SZ3VFUUN3ME2wMlQ2PjN|IDFOwG0> Mlr4V2FPT0WU
BHT-101 M4K1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS0[ng5UUN3ME2wMlQ3PTliIN88US=> MlLLV2FPT0WU
BE-13 NYfYfIRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjQXJY1UUN3ME2wMlQ5PTd{IDFOwG0> NUm4OHNPW0GQR1XS
RS4-11 MojJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwNEi1PFQhKM7:TR?= Ml7vV2FPT0WU
IGROV-1 NHfob5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zLemlEPTB;MD60PFc6PyBizszN NEfzW21USU6JRWK=
KE-37 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zRfWlEPTB;MD60PVUxQSBizszN NVuxbFlRW0GQR1XS
BV-173 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTpTWM2OD1yLkWwO|kzKCEQvF2= NUi2TIhJW0GQR1XS
MEG-01 NVv0epNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[3Z2lEPTB;MD61NVIyPCBizszN NXLFUodUW0GQR1XS
LB2241-RCC NEXvU4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwNUO3NVghKM7:TR?= NIPTRY9USU6JRWK=
ACHN M4Pvb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwNUSwOlkhKM7:TR?= NWrQUW9pW0GQR1XS
CTB-1 NYf6TXpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXpd2Q1UUN3ME2wMlU1QDJiIN88US=> NU\4dGp1W0GQR1XS
HT-1080 NGrzW2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmmyTWM2OD1yLkW1N|Q6KCEQvF2= NGjq[HVUSU6JRWK=
CHL-1 MmjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUK1NWdpUUN3ME2wMlU2PDZ3IDFOwG0> NXu1[5dHW0GQR1XS
EW-3 NHewNZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTiNYNNUUN3ME2wMlU2QTN3IDFOwG0> MYrTRW5ITVJ?
ES1 NI\mVVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPkfZNWUUN3ME2wMlY4PDl6IDFOwG0> M4W0S3NCVkeHUh?=
KASUMI-1 NFjFc4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvNcZhKSzVyPUCuO|I{OyBizszN NXPaOFlMW0GQR1XS
SW13 NUi5cnlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXSbolDUUN3ME2wMlc{Pzl6IDFOwG0> MoX5V2FPT0WU
A3-KAW MmezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPwTWM2OD1yLke5NlA5KCEQvF2= NVrpTYVpW0GQR1XS
LB771-HNC NXPKU4pTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LzTGlEPTB;MD64N|ExPCBizszN NXnhOZFHW0GQR1XS
OC-314 M1Pjfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LnZmlEPTB;MD64Olk3PSBizszN MoHIV2FPT0WU
MLMA NIDGclZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwOUC2O|UhKM7:TR?= MXnTRW5ITVJ?
KARPAS-45 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwOUK0OlYhKM7:TR?= M2HHOXNCVkeHUh?=
CAL-27 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S0bGlEPTB;MD65NlkxPiBizszN NFLCfHlUSU6JRWK=
SK-NEP-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf1fVhKSzVyPUCuPVczPDhiIN88US=> NH63RmtUSU6JRWK=
COR-L105 NUfxcWVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGqxZ2hKSzVyPUGuNFA{QTRiIN88US=> NIHE[IVUSU6JRWK=
TI-73 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFntNHJKSzVyPUGuNFE3PSBizszN NYSwOVdSW0GQR1XS
JVM-3 NFfBblRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnqTFRXUUN3ME2xMlA2ODF5IDFOwG0> NYDISohUW0GQR1XS
HAL-01 M2nZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;nTWM2OD1zLkC4PFEhKM7:TR?= NX7tVJFuW0GQR1XS
QIMR-WIL NULHVIRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWe3VlRtUUN3ME2xMlA6ODV6IDFOwG0> MmfTV2FPT0WU
HSC-3 M4n2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HrbGlEPTB;MT6xNVc5OyBizszN NH\QPYpUSU6JRWK=
KY821 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TCdWlEPTB;MT6xN|M2OSBizszN MXLTRW5ITVJ?
5637 NGXIUoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF33dmJKSzVyPUGuNVM5ODNiIN88US=> M1KzcXNCVkeHUh?=
CAL-33 NIfrVolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P6Z2lEPTB;MT6xPVMxOiBizszN M2[0[XNCVkeHUh?=
ES4 M4rnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvmTWM2OD1zLkKwO|khKM7:TR?= NIOwR4JUSU6JRWK=
BHY NXm5UWNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrUTWM2OD1zLkKyPFkzKCEQvF2= NXP4OnJzW0GQR1XS
LB1047-RCC M1XEPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHtTWM2OD1zLkKzO|g2KCEQvF2= MkDpV2FPT0WU
H4 NETXSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;0TWM2OD1zLkK0NlU2KCEQvF2= NYGwVGlUW0GQR1XS
RPMI-8866 MlyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3tTWM2OD1zLkK2NVA3KCEQvF2= NH31O|JUSU6JRWK=
HO-1-N-1 NYfSelVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf0dXBSUUN3ME2xMlI3OzZ7IDFOwG0> MlmyV2FPT0WU
BB30-HNC M3\i[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1O0NmlEPTB;MT6yPFcyPCBizszN M2jXTHNCVkeHUh?=
PC-14 NHfRZ5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwMkmyNFUhKM7:TR?= M1Pl[3NCVkeHUh?=
NUGC-3 MmmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFwMkmzOVYhKM7:TR?= NEfXeWRUSU6JRWK=
A4-Fuk MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHOTpBKSzVyPUGuN|A4ODRiIN88US=> NELkZpdUSU6JRWK=
MHH-NB-11 Mkn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvlTWM2OD1zLkOxN|g{KCEQvF2= MoDJV2FPT0WU
KOSC-2 NGm3enZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn20TWM2OD1zLkOxO|c2KCEQvF2= MlP3V2FPT0WU
A498 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXoTWM2OD1zLkSwNVE{KCEQvF2= MVzTRW5ITVJ?
KG-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTseZlGUUN3ME2xMlQyOjd|IDFOwG0> NWj0N4ZOW0GQR1XS
DEL M32xe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTFwNEO2OVchKM7:TR?= MUfTRW5ITVJ?
EW-16 M3TUVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTFwNEO5O|MhKM7:TR?= NXezclRQW0GQR1XS
BPH-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v5W2lEPTB;MT60OFgxPSBizszN NUfISoF3W0GQR1XS
JAR M1vWRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL2bVNKUUN3ME2xMlQ6OzZiIN88US=> M{LlRnNCVkeHUh?=
J-RT3-T3-5 MnywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwNUG3NlIhKM7:TR?= NUXxUI9qW0GQR1XS
A375 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP4OpdKSzVyPUGuOVE4PzJiIN88US=> NEXIdJNUSU6JRWK=
SW954 M3P0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFwNUWwNFchKM7:TR?= NHfzZXlUSU6JRWK=
Ca9-22 MmPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTFwNU[yOkAh|ryP NI\oNWtUSU6JRWK=
D-566MG MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;xbWJ6UUN3ME2xMlU4OTV3IDFOwG0> NX\QcHBJW0GQR1XS
SCC-15 MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH3W2hKSzVyPUGuOlE5ODRiIN88US=> NXLkVYxXW0GQR1XS
HD-MY-Z MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPNSFdKSzVyPUGuOlM2QDRiIN88US=> NFX3d|RUSU6JRWK=
HT-1376 M1jxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS3eXE{UUN3ME2xMlY1OzZiIN88US=> NIDrNFZUSU6JRWK=
CAL-54 NV\hRWxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoroTWM2OD1zLk[1O|A6KCEQvF2= NIT6SHlUSU6JRWK=
ONS-76 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\zNoc2UUN3ME2xMlY4PTVzIDFOwG0> M17jO3NCVkeHUh?=
EFO-27 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LKV2lEPTB;MT62PFkzKCEQvF2= M4rkVHNCVkeHUh?=
769-P MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFwNkm1PVYhKM7:TR?= MkDHV2FPT0WU
MV-4-11 NH;6RpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwNkm4OVYhKM7:TR?= NU\PZ|ZWW0GQR1XS
NKM-1 MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTFwN{G4NFIhKM7:TR?= M172OHNCVkeHUh?=
LOXIMVI NVHLSm8zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTFwN{S1PVkhKM7:TR?= NXjD[pZjW0GQR1XS
KYSE-140 M{TOUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TXcWlEPTB;MT63OVY2PSBizszN NU[4NJY6W0GQR1XS
ES5 M{nUOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nZeWlEPTB;MT64Olc1PyBizszN NIHMU2lUSU6JRWK=
BB65-RCC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTFwOEm4OFkhKM7:TR?= NEKx[pZUSU6JRWK=
HN MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFwOEm4O|QhKM7:TR?= M3;S[XNCVkeHUh?=
A101D Ml7uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwOUO2NlghKM7:TR?= M{DrcHNCVkeHUh?=
LoVo MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPvTWM2OD1zLkm3Olc6KCEQvF2= MXjTRW5ITVJ?
NCI-H526 NXvtU5h3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[4[|hKSzVyPUGuPVk{OjViIN88US=> MU\TRW5ITVJ?
NCI-H1693 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3xRY5KSzVyPUGuPVk5QDhiIN88US=> NUT4N41XW0GQR1XS
OVCAR-4 MomwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTJwMEC0N|UhKM7:TR?= NHm2TY5USU6JRWK=
SK-HEP-1 M2TjcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlSzTWM2OD1{LkCwO|Q2KCEQvF2= NIf0SZBUSU6JRWK=
C2BBe1 M3q1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\CTWM2OD1{LkCzN|czKCEQvF2= NGTZOWZUSU6JRWK=
MEL-JUSO MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmP1TWM2OD1{LkC0OFY1KCEQvF2= NYTrb|cyW0GQR1XS
MOLT-16 M1PkdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHvUmpKSzVyPUKuNFcxPThiIN88US=> NX;q[VUxW0GQR1XS
NBsusSR MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXmWnZzUUN3ME2yMlA6QDh7IDFOwG0> NV7PNG9qW0GQR1XS
TK10 M1\6bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13hbWlEPTB;Mj6xN|Q2QCBizszN NGe0botUSU6JRWK=
CAL-39 NET5RlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnLcZQ4UUN3ME2yMlE1PDhiIN88US=> MUHTRW5ITVJ?
NCI-H2030 NWTlOotVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHjcGtKUUN3ME2yMlE5QTd|IDFOwG0> MVPTRW5ITVJ?
HCT-116 Mni3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlKxTWM2OD1{LkKyPVg1KCEQvF2= MkTFV2FPT0WU
HTC-C3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTJwMk[4NlQhKM7:TR?= MU\TRW5ITVJ?
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LCLC-97TM1 NXTlblBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrNO5NwUUN3ME2yPE4zPzZ{IDFOwG0> NUfEXJlFW0GQR1XS
NCI-H1770 NXnLU4FbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJ6LkO1OlYhKM7:TR?= M4fXenNCVkeHUh?=
BT-20 NF;o[4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHi0eIJKSzVyPUK4MlM3QDViIN88US=> NGTkS5lUSU6JRWK=
DBTRG-05MG MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[4SIgxUUN3ME2yPE41QDN6IDFOwG0> NWTrOnF[W0GQR1XS
HPAF-II M{TVXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;iTWM2OD1{OD63O|khKM7:TR?= NX\mUFJMW0GQR1XS
SW837 M1Hremdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37PXWlEPTB;MkmuN|M5PSBizszN MnjGV2FPT0WU
647-V MnfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJ7LkewNFMhKM7:TR?= M1vhPXNCVkeHUh?=
J82 NEjvbWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTJ7LkiwNVMhKM7:TR?= MoO5V2FPT0WU
MC116 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTNyLkC3N|MhKM7:TR?= NGPNWopUSU6JRWK=
NCI-H69 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTNyLk[wPVMhKM7:TR?= NHu3[lVUSU6JRWK=
NB6 M2jud2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTNzLkO2NlkhKM7:TR?= NUDzPVRRW0GQR1XS
CAL-120 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LURmlEPTB;M{KuOFMyPyBizszN M1\wNnNCVkeHUh?=
U-87-MG MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDwTnVuUUN3ME2zN{4xOjVzIDFOwG0> NXfDT3c{W0GQR1XS
NCI-H1304 M{nLeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTkNnVKSzVyPUOzMlA{PTRiIN88US=> MlPmV2FPT0WU
YH-13 M3;TPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTN|LkK1N|UhKM7:TR?= NVjoVWYzW0GQR1XS
RMG-I MnjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTN|LkSyPFUhKM7:TR?= M2TzUnNCVkeHUh?=
LU-65 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;D[o5KSzVyPUO0MlE1ODhiIN88US=> NEPXcHNUSU6JRWK=
GB-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rqdWlEPTB;M{WuNFczQSBizszN NFnmUZpUSU6JRWK=
DU-4475 NWLuRYhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;WZ2lEPTB;M{WuNVU2OyBizszN M3\UUnNCVkeHUh?=
SBC-5 M4jo[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;QSJRKSzVyPUO2MlU6ODJiIN88US=> NFOx[oxUSU6JRWK=
OE33 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHSxR3FKSzVyPUO3Mlc2PzdiIN88US=> M3\5W3NCVkeHUh?=
C8166 NIXXdphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrzTWM2OD1|OD61NlY4KCEQvF2= NX[yfVdSW0GQR1XS
COLO-684 NFv2WG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HzdWlEPTB;M{iuO|QzQCBizszN NXjRcldEW0GQR1XS
NCI-H1155 M4LxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;0bZdsUUN3ME2zPU4xPDdzIDFOwG0> NGTXWFNUSU6JRWK=
ATN-1 MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrZOVF7UUN3ME2zPU44Pzl{IDFOwG0> MWPTRW5ITVJ?
KARPAS-299 M3vRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TJPWlEPTB;M{muPFM6KCEQvF2= MofEV2FPT0WU
KNS-81-FD M1HkZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1OwWGlEPTB;NECuN|YxPCBizszN NHvjcllUSU6JRWK=
NCI-H1563 NUX1WII6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHOXmlKSzVyPUSxMlUxOzliIN88US=> NF7BZoVUSU6JRWK=
NB14 NHXr[mRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXaTWM2OD12Mj63NlY{KCEQvF2= MoHjV2FPT0WU
COLO-800 NHvnSIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3hXohpUUN3ME20Nk45PTF5IDFOwG0> Mnr3V2FPT0WU
MS-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjTUJlKSzVyPUSzMlA1QDNiIN88US=> MVPTRW5ITVJ?
OVCAR-8 MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nKWmlEPTB;NEOuOlgxQSBizszN MYLTRW5ITVJ?
SK-PN-DW MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnroTWM2OD12Mz64O|c3KCEQvF2= MWjTRW5ITVJ?
G-402 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTR|LkmwNFYhKM7:TR?= NEDLenZUSU6JRWK=
NCI-H2291 NV3jO|M6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPzTWM2OD12ND64NFE4KCEQvF2= MmC1V2FPT0WU
PC-3 M2jwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:zOXJHUUN3ME20OU45ODJ|IDFOwG0> MYDTRW5ITVJ?
NCI-H1581 MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jTbWlEPTB;NEWuPVg5QSBizszN NV7YZ5NnW0GQR1XS
SW1116 M{XpS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTR5LkCxPFIhKM7:TR?= NX;ufHR5W0GQR1XS
ZR-75-30 NGftfHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTR5LkCyN|khKM7:TR?= NUTtN3c5W0GQR1XS
OCI-AML2 Mnq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TSNWlEPTB;NEeuNFkyQCBizszN M3XWPXNCVkeHUh?=
MDA-MB-231 MkPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHlNphKUUN3ME20O{43OjR7IDFOwG0> NXPDemw5W0GQR1XS
ES3 Mne3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTGU3lKSzVyPUS4MlM2OjliIN88US=> M4rT[nNCVkeHUh?=
NCI-H630 NFT3TXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlSwTWM2OD12OT6xO|QzKCEQvF2= MX\TRW5ITVJ?
OE19 M{HjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTR7LkK5NFIhKM7:TR?= NEPBbpdUSU6JRWK=
NCI-H1573 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PaW2lEPTB;NEmuOlg3OSBizszN Mkj1V2FPT0WU
EW-1 Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT3TWM2OD12OT65NFg1KCEQvF2= NWi5[VFrW0GQR1XS

... 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)

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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 )

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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):
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    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

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Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Can I give S1014 Bosutinib to mice by oral gavage? If so, how to dissolve the drug?

  • Answer:

    For oral gavage, S1014 Bosutinib can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID