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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4 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. 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 NUDTT3Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;BZW9IUUN3ME2wMlA5OjNzIDFOwG0> MnnnV2FPT0WU
SW756 NFzj[3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr5N5A6UUN3ME2wMlE1ODJ2IDFOwG0> M1\TeHNCVkeHUh?=
CTV-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfYTWM2OD1yLkG2N|k5KCEQvF2= NV3tXJFNW0GQR1XS
HSC-4 NUnYU2l6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4L1NWlEPTB;MD6xO|E2QCBizszN M1nmOHNCVkeHUh?=
LAMA-84 Mm\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwMki2OlQhKM7:TR?= MVHTRW5ITVJ?
KU812 MlLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\3TWM2OD1yLkO0NFY5KCEQvF2= NFfIVnJUSU6JRWK=
HCC1806 M2DEWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP1UJJKSzVyPUCuN|UzOTZiIN88US=> NEDrdGxUSU6JRWK=
DOK M1WwXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXuT|NKSzVyPUCuN|c4QDZiIN88US=> M2Kze3NCVkeHUh?=
NCI-H209 NIDN[HZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DjOmlEPTB;MD60NFgxQCBizszN NGrhT5FUSU6JRWK=
EoL-1-cell MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rUdGlEPTB;MD60NVU4PiBizszN M3jMdXNCVkeHUh?=
H9 NHO2bnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TJW2lEPTB;MD60N|Q3PCBizszN M{i4O3NCVkeHUh?=
EM-2 NX;oVHM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwNEO4PUAh|ryP MnPYV2FPT0WU
NCI-H292 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwNESxNFghKM7:TR?= M1X1SXNCVkeHUh?=
697 Mo\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXINJRKSzVyPUCuOFU3OzNiIN88US=> MnK1V2FPT0WU
BHT-101 M2DaPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzBWpBKSzVyPUCuOFY2QSBizszN NFizWJlUSU6JRWK=
BE-13 M{\iTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfKTWM2OD1yLkS4OVczKCEQvF2= M{K4[nNCVkeHUh?=
RS4-11 MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D3dmlEPTB;MD60PFU5PCBizszN NHvBeYNUSU6JRWK=
IGROV-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrBTm1KSzVyPUCuOFg4QTdiIN88US=> NFziO4ZUSU6JRWK=
KE-37 Mn7US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofxTWM2OD1yLkS5OVA6KCEQvF2= Ml;nV2FPT0WU
BV-173 NGTB[opIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3u2cGlEPTB;MD61NFc6OiBizszN M4r0e3NCVkeHUh?=
MEG-01 M1nz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNUGyNVQhKM7:TR?= NFP1cpdUSU6JRWK=
LB2241-RCC MmC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHhVohHUUN3ME2wMlU{PzF6IDFOwG0> M1zzfHNCVkeHUh?=
ACHN MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXUPVNKSzVyPUCuOVQxPjliIN88US=> NV6ycYxlW0GQR1XS
CTB-1 NHLHWmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETveXhKSzVyPUCuOVQ5OiBizszN NEOxcGpUSU6JRWK=
HT-1080 NYfWNFdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[2OoxKSzVyPUCuOVU{PDliIN88US=> Mn3kV2FPT0WU
CHL-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1O2SmlEPTB;MD61OVQ3PSBizszN NYXmb4ZHW0GQR1XS
EW-3 MnvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonsTWM2OD1yLkW1PVM2KCEQvF2= MnrRV2FPT0WU
ES1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlG4TWM2OD1yLk[3OFk5KCEQvF2= NEX0WoRUSU6JRWK=
KASUMI-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2iwWGlEPTB;MD63NlM{KCEQvF2= NF76NGtUSU6JRWK=
SW13 M1fQ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33IdmlEPTB;MD63N|c6QCBizszN NYr3XW12W0GQR1XS
A3-KAW NUH3R|Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MomyTWM2OD1yLke5NlA5KCEQvF2= M3iybXNCVkeHUh?=
LB771-HNC NE\KVJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHrepk5UUN3ME2wMlg{OTB2IDFOwG0> M2ftV3NCVkeHUh?=
OC-314 NYnYbWRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjiSFlSUUN3ME2wMlg3QTZ3IDFOwG0> NHzRU5hUSU6JRWK=
MLMA MmDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;ITWM2OD1yLkmwOlc2KCEQvF2= M2fnVHNCVkeHUh?=
KARPAS-45 NFqwOolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwOUK0OlYhKM7:TR?= NVPiSVdlW0GQR1XS
CAL-27 M{PVc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvvVmNKSzVyPUCuPVI6ODZiIN88US=> M2qzV3NCVkeHUh?=
SK-NEP-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTHTWM2OD1yLkm3NlQ5KCEQvF2= NX25TVBpW0GQR1XS
COR-L105 NGjTepFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwMECzPVQhKM7:TR?= MUnTRW5ITVJ?
TI-73 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\LTWM2OD1zLkCxOlUhKM7:TR?= MonHV2FPT0WU
JVM-3 M2DjNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXq2XZZiUUN3ME2xMlA2ODF5IDFOwG0> MWrTRW5ITVJ?
HAL-01 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPoUlY3UUN3ME2xMlA5QDFiIN88US=> MofKV2FPT0WU
QIMR-WIL NUHNTo11T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwMEmwOVghKM7:TR?= Mn3JV2FPT0WU
HSC-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3JPGxKSzVyPUGuNVE4QDNiIN88US=> MmPIV2FPT0WU
KY821 NGO2fmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW0dVV2UUN3ME2xMlE{OzVzIDFOwG0> M4LHO3NCVkeHUh?=
5637 M3fDb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrR[W4yUUN3ME2xMlE{QDB|IDFOwG0> NFLWV4xUSU6JRWK=
CAL-33 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXkUZllUUN3ME2xMlE6OzB{IDFOwG0> NEjEe49USU6JRWK=
ES4 M1P2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXSOlJKSzVyPUGuNlA4QSBizszN MXTTRW5ITVJ?
BHY MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3yy[GlEPTB;MT6yNlg6OiBizszN MWPTRW5ITVJ?
LB1047-RCC NH73PGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz5TWM2OD1zLkKzO|g2KCEQvF2= MVHTRW5ITVJ?
H4 NEWxZpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjPTWM2OD1zLkK0NlU2KCEQvF2= MXfTRW5ITVJ?
RPMI-8866 M2nOeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGP6[lhKSzVyPUGuNlYyODZiIN88US=> MU\TRW5ITVJ?
HO-1-N-1 Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTpTWM2OD1zLkK2N|Y6KCEQvF2= M2nNUnNCVkeHUh?=
BB30-HNC M2\3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXnS4dIUUN3ME2xMlI5PzF2IDFOwG0> NU\afGZpW0GQR1XS
PC-14 NGnFV5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfvWHlKSzVyPUGuNlkzODViIN88US=> NX7YWVI1W0GQR1XS
NUGC-3 Mkj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;RTWM2OD1zLkK5N|U3KCEQvF2= NHX4ZXpUSU6JRWK=
A4-Fuk MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W4UGlEPTB;MT6zNFcxPCBizszN MV3TRW5ITVJ?
MHH-NB-11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rkdWlEPTB;MT6zNVM5OyBizszN NXjlc5FMW0GQR1XS
KOSC-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnjOHlKSzVyPUGuN|E4PzViIN88US=> M1fwb3NCVkeHUh?=
A498 Ml74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vVcWlEPTB;MT60NFEyOyBizszN NF62PIlUSU6JRWK=
KG-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzJc446UUN3ME2xMlQyOjd|IDFOwG0> NWrwb257W0GQR1XS
DEL NYO4VnZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TyfWlEPTB;MT60N|Y2PyBizszN Mn\rV2FPT0WU
EW-16 NWLCSIRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvYdYlbUUN3ME2xMlQ{QTd|IDFOwG0> MXzTRW5ITVJ?
BPH-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13MfWlEPTB;MT60OFgxPSBizszN MV7TRW5ITVJ?
JAR MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzaTWM2OD1zLkS5N|YhKM7:TR?= NX\OXnlzW0GQR1XS
J-RT3-T3-5 NVv5SXVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[wO206UUN3ME2xMlUyPzJ{IDFOwG0> MXXTRW5ITVJ?
A375 M3fXOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TwVGlEPTB;MT61NVc4OiBizszN M4Du[nNCVkeHUh?=
SW954 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfzdI14UUN3ME2xMlU2ODB5IDFOwG0> NFvMfFFUSU6JRWK=
Ca9-22 M4H6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnHTWM2OD1zLkW2NlYhKM7:TR?= MnvYV2FPT0WU
D-566MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFwNUexOVUhKM7:TR?= MVfTRW5ITVJ?
SCC-15 NFnaSIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnf5TWM2OD1zLk[xPFA1KCEQvF2= NILz[YJUSU6JRWK=
HD-MY-Z MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\1VnJKSzVyPUGuOlM2QDRiIN88US=> MWLTRW5ITVJ?
HT-1376 M1nrWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrKTWM2OD1zLk[0N|YhKM7:TR?= M3LjZnNCVkeHUh?=
CAL-54 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHu3SVNKSzVyPUGuOlU4ODliIN88US=> Mn7CV2FPT0WU
ONS-76 NXX2bIZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHrcoJvUUN3ME2xMlY4PTVzIDFOwG0> NXPaUZcyW0GQR1XS
EFO-27 NUTIO4NsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXuOYNKSzVyPUGuOlg6OiBizszN NX;BeHo6W0GQR1XS
769-P NIXHV2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTFwNkm1PVYhKM7:TR?= M37kfHNCVkeHUh?=
MV-4-11 NFjW[pRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTFwNkm4OVYhKM7:TR?= M1T1cnNCVkeHUh?=
NKM-1 NIPsZXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXjNWd2UUN3ME2xMlcyQDB{IDFOwG0> MUXTRW5ITVJ?
LOXIMVI MoDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFwN{S1PVkhKM7:TR?= M{WzPHNCVkeHUh?=
KYSE-140 M4KwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGwOGtoUUN3ME2xMlc2PjV3IDFOwG0> NH[3TYNUSU6JRWK=
ES5 MoPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnoSIRKSzVyPUGuPFY4PDdiIN88US=> MX3TRW5ITVJ?
BB65-RCC M2\veGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXaUZR3UUN3ME2xMlg6QDR7IDFOwG0> MmXsV2FPT0WU
HN NIjSUHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojpTWM2OD1zLki5PFc1KCEQvF2= MoPzV2FPT0WU
A101D NYLaNZkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL1WYNUUUN3ME2xMlk{PjJ6IDFOwG0> NIroZ|ZUSU6JRWK=
LoVo NF\ocmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;S[GFUUUN3ME2xMlk4Pjd7IDFOwG0> NEHjXIdUSU6JRWK=
NCI-H526 NWXJfZNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTFwOUmzNlUhKM7:TR?= NEn3VG5USU6JRWK=
NCI-H1693 MnL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rITWlEPTB;MT65PVg5QCBizszN NHTaV3JUSU6JRWK=
OVCAR-4 NFPiPWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTJwMEC0N|UhKM7:TR?= NIjIZ45USU6JRWK=
SK-HEP-1 NHH0V3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTJwMEC3OFUhKM7:TR?= M1XF[XNCVkeHUh?=
C2BBe1 MmPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfpU|JlUUN3ME2yMlA{Ozd{IDFOwG0> MmDhV2FPT0WU
MEL-JUSO NGW0ZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTJwMES0OlQhKM7:TR?= MXXTRW5ITVJ?
MOLT-16 NHnt[|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXkO5BKSzVyPUKuNFcxPThiIN88US=> NVjKR4p1W0GQR1XS
NBsusSR MoPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTJwMEm4PFkhKM7:TR?= MXjTRW5ITVJ?
TK10 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorkTWM2OD1{LkGzOFU5KCEQvF2= Mm[zV2FPT0WU
CAL-39 M3LBemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfJO3RKSzVyPUKuNVQ1QCBizszN NFXIdGpUSU6JRWK=
NCI-H2030 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJwMUi5O|MhKM7:TR?= MljyV2FPT0WU
HCT-116 NWLNR5lWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTJwMkK5PFQhKM7:TR?= NWH3c4VGW0GQR1XS
HTC-C3 NXfLbFlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTJwMk[4NlQhKM7:TR?= NYGwSlFjW0GQR1XS
TYK-nu M2DEUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJwM{C5NFkhKM7:TR?= MWnTRW5ITVJ?
FADU NYDOW5FbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe0OndKSzVyPUKuN|IzQTZiIN88US=> M2\aWHNCVkeHUh?=
A431 MnX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHrS4pKSzVyPUKuN|cxOjViIN88US=> NWrpdIN[W0GQR1XS
TE-11 MmrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDPdGVUUUN3ME2yMlM5ODF7IDFOwG0> MVzTRW5ITVJ?
CAL-12T NYPQcFZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j3fWlEPTB;Mj60NFQyPyBizszN MlX0V2FPT0WU
DB MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlflTWM2OD1{LkSyPFY6KCEQvF2= NFnU[plUSU6JRWK=
L-363 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7LTWM2OD1{LkSzOVA4KCEQvF2= NVnRUnBtW0GQR1XS
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NCI-H69 MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXvXZdSUUN3ME2zNE43ODl|IDFOwG0> NYC4Z2dLW0GQR1XS
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RMG-I NH3ibHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETlNJJKSzVyPUOzMlQzQDViIN88US=> M{CyO3NCVkeHUh?=
LU-65 M3fMfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTN2LkG0NFghKM7:TR?= NUm4R3hPW0GQR1XS
GB-1 NEXERYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7OO5VKSzVyPUO1MlA4OjliIN88US=> NHznWZpUSU6JRWK=
DU-4475 NIL6ZZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTW[FYzUUN3ME2zOU4yPTV|IDFOwG0> MlrJV2FPT0WU
SBC-5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[1TWM2OD1|Nj61PVAzKCEQvF2= MnHrV2FPT0WU
OE33 NX\nNWc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTN5Lke1O|chKM7:TR?= M1nwNXNCVkeHUh?=
C8166 M{\mcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTN6LkWyOlchKM7:TR?= NWnndnp7W0GQR1XS
COLO-684 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3Z[XpCUUN3ME2zPE44PDJ6IDFOwG0> NUDZenBOW0GQR1XS
NCI-H1155 Mn7hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe0fnFKSzVyPUO5MlA1PzFiIN88US=> Ml\hV2FPT0WU
ATN-1 NInYc4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrBTWM2OD1|OT63O|kzKCEQvF2= M{HkNXNCVkeHUh?=
KARPAS-299 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIP5UGZKSzVyPUO5Mlg{QSBizszN NF7mSGZUSU6JRWK=
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OVCAR-8 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTR|Lk[4NFkhKM7:TR?= M3TSXXNCVkeHUh?=
SK-PN-DW MkHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moq5TWM2OD12Mz64O|c3KCEQvF2= M{C1WXNCVkeHUh?=
G-402 MnOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{GycmlEPTB;NEOuPVAxPiBizszN M{S2e3NCVkeHUh?=
NCI-H2291 M3PpcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDsUolXUUN3ME20OE45ODF5IDFOwG0> MkDNV2FPT0WU
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EW-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPyTWM2OD12OT65NFg1KCEQvF2= MULTRW5ITVJ?

... 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 individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
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
    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
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