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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In DMSO USD 91 In stock
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USD 270 In stock

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3 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.

    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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NFPQVW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwMEiyN|EhKM7:TR?= NV3TW2JMW0GQR1XS
SW756 MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;GTWM2OD1yLkG0NFI1KCEQvF2= Mo[0V2FPT0WU
CTV-1 NVG0b5RrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HUbWlEPTB;MD6xOlM6QCBizszN NFT1[FBUSU6JRWK=
HSC-4 NITLWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\pblBJUUN3ME2wMlE4OTV6IDFOwG0> MVzTRW5ITVJ?
LAMA-84 MoXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnpWVBVUUN3ME2wMlI5PjZ2IDFOwG0> M3PzdXNCVkeHUh?=
KU812 Ml\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPQO4hKUUN3ME2wMlM1ODZ6IDFOwG0> M4jHVnNCVkeHUh?=
HCC1806 NWjjOIRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETKdFRKSzVyPUCuN|UzOTZiIN88US=> MY\TRW5ITVJ?
DOK MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fHTGlEPTB;MD6zO|c5PiBizszN MVHTRW5ITVJ?
NCI-H209 M1jwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTBwNEC4NFghKM7:TR?= NYTzfFc2W0GQR1XS
EoL-1-cell MnflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFz1T4NKSzVyPUCuOFE2PzZiIN88US=> M{KyVnNCVkeHUh?=
H9 NX24SXVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTL[GJKSzVyPUCuOFM1PjRiIN88US=> MmfPV2FPT0WU
EM-2 NX:5e4ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfDWlZKSzVyPUCuOFM5QSBizszN MXLTRW5ITVJ?
NCI-H292 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;zTWM2OD1yLkS0NVA5KCEQvF2= M3rIXHNCVkeHUh?=
697 NH6xcpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nS[mlEPTB;MD60OVY{OyBizszN M17WTHNCVkeHUh?=
BHT-101 MoPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;UUGlEPTB;MD60OlU6KCEQvF2= M1\zbnNCVkeHUh?=
BE-13 M4n0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWH5XXkzUUN3ME2wMlQ5PTd{IDFOwG0> NUfBU5o3W0GQR1XS
RS4-11 NFvOOI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DZOGlEPTB;MD60PFU5PCBizszN NFP1fYRUSU6JRWK=
IGROV-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MomyTWM2OD1yLkS4O|k4KCEQvF2= NV\Ze2hyW0GQR1XS
KE-37 MmnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHu3WY9KSzVyPUCuOFk2ODliIN88US=> M3nQb3NCVkeHUh?=
BV-173 NGLweHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTBwNUC3PVIhKM7:TR?= MnzvV2FPT0WU
MEG-01 MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwNUGyNVQhKM7:TR?= NHzDfG5USU6JRWK=
LB2241-RCC NHS4OmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj6TWM2OD1yLkWzO|E5KCEQvF2= MmDpV2FPT0WU
ACHN MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnaTWM2OD1yLkW0NFY6KCEQvF2= NUjPZW9mW0GQR1XS
CTB-1 NIfPbVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTBwNUS4NkAh|ryP MYDTRW5ITVJ?
HT-1080 NXXHfFNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjpTWM2OD1yLkW1N|Q6KCEQvF2= NFrSO3pUSU6JRWK=
CHL-1 MmD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDp[YRKSzVyPUCuOVU1PjViIN88US=> MlT6V2FPT0WU
EW-3 M17CXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfjTWM2OD1yLkW1PVM2KCEQvF2= M1\6UnNCVkeHUh?=
ES1 MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLaSWZrUUN3ME2wMlY4PDl6IDFOwG0> NX[wO2R[W0GQR1XS
KASUMI-1 NX3wZlFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\yfJl[UUN3ME2wMlczOzNiIN88US=> NWjWdIpmW0GQR1XS
SW13 NUPVSFhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTBwN{O3PVghKM7:TR?= NWDHO4cxW0GQR1XS
A3-KAW NVHFeWR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3KwRWlEPTB;MD63PVIxQCBizszN NVzifmZOW0GQR1XS
LB771-HNC Ml;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG4doZKSzVyPUCuPFMyODRiIN88US=> NVm2boU1W0GQR1XS
OC-314 M3zoNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkntTWM2OD1yLki2PVY2KCEQvF2= MlXHV2FPT0WU
MLMA MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTBwOUC2O|UhKM7:TR?= NHfEeXRUSU6JRWK=
KARPAS-45 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwOUK0OlYhKM7:TR?= NYLQdHdlW0GQR1XS
CAL-27 Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17HZWlEPTB;MD65NlkxPiBizszN NGqw[mtUSU6JRWK=
SK-NEP-1 Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwOUeyOFghKM7:TR?= Mn\oV2FPT0WU
COR-L105 M{XEbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFwMECzPVQhKM7:TR?= NGjGUJhUSU6JRWK=
TI-73 Mli2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\ReVNKSzVyPUGuNFE3PSBizszN NIW2VItUSU6JRWK=
JVM-3 M{Txemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LtbmlEPTB;MT6wOVAyPyBizszN M1XXSHNCVkeHUh?=
HAL-01 M37OSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPTO2h3UUN3ME2xMlA5QDFiIN88US=> NH\3OYVUSU6JRWK=
QIMR-WIL NFHDS3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTFwMEmwOVghKM7:TR?= M{PNVHNCVkeHUh?=
HSC-3 NVvqO3dzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonXTWM2OD1zLkGxO|g{KCEQvF2= MmT0V2FPT0WU
KY821 NFPKe3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nWWWlEPTB;MT6xN|M2OSBizszN MoH4V2FPT0WU
5637 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzNWoRKSzVyPUGuNVM5ODNiIN88US=> NWi0TWtQW0GQR1XS
CAL-33 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjuZ5VKSzVyPUGuNVk{ODJiIN88US=> MlH2V2FPT0WU
ES4 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPGTWM2OD1zLkKwO|khKM7:TR?= MVXTRW5ITVJ?
BHY M2rmXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFwMkK4PVIhKM7:TR?= NE\2cYpUSU6JRWK=
LB1047-RCC MkTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWK0TnlbUUN3ME2xMlI{Pzh3IDFOwG0> NH7uPXVUSU6JRWK=
H4 Mn;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;MT4plUUN3ME2xMlI1OjV3IDFOwG0> M3rmXXNCVkeHUh?=
RPMI-8866 MkXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkewTWM2OD1zLkK2NVA3KCEQvF2= NUjoe2tnW0GQR1XS
HO-1-N-1 MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr5RVI4UUN3ME2xMlI3OzZ7IDFOwG0> NWPzZWlxW0GQR1XS
BB30-HNC Mkf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLFXlBKSzVyPUGuNlg4OTRiIN88US=> NUi5NYlkW0GQR1XS
PC-14 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\GOYhzUUN3ME2xMlI6OjB3IDFOwG0> MXnTRW5ITVJ?
NUGC-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjIR5BKSzVyPUGuNlk{PTZiIN88US=> MVPTRW5ITVJ?
A4-Fuk MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfGcldKSzVyPUGuN|A4ODRiIN88US=> MXLTRW5ITVJ?
MHH-NB-11 NH\tVVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mof6TWM2OD1zLkOxN|g{KCEQvF2= MVjTRW5ITVJ?
KOSC-2 NUnCUItZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjpN2FwUUN3ME2xMlMyPzd3IDFOwG0> M2jwT3NCVkeHUh?=
A498 MmD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PjZmlEPTB;MT60NFEyOyBizszN MVvTRW5ITVJ?
KG-1 M3fmSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETEZ2VKSzVyPUGuOFEzPzNiIN88US=> Mlr0V2FPT0WU
DEL NVznSHpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwNEO2OVchKM7:TR?= M{fQUXNCVkeHUh?=
EW-16 MnPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFwNEO5O|MhKM7:TR?= MY\TRW5ITVJ?
BPH-1 M4\nb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwNES4NFUhKM7:TR?= MYnTRW5ITVJ?
JAR NXWxXYU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nDUmlEPTB;MT60PVM3KCEQvF2= NX\tZWVtW0GQR1XS
J-RT3-T3-5 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHZOG1NUUN3ME2xMlUyPzJ{IDFOwG0> NI\vSXhUSU6JRWK=
A375 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrMTWM2OD1zLkWxO|czKCEQvF2= MY\TRW5ITVJ?
SW954 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjLOZZ{UUN3ME2xMlU2ODB5IDFOwG0> NVzzVII2W0GQR1XS
Ca9-22 M16yc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFwNU[yOkAh|ryP MmHwV2FPT0WU
D-566MG NXTnO|JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\YTWM2OD1zLkW3NVU2KCEQvF2= MWnTRW5ITVJ?
SCC-15 NE\GN|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTFwNkG4NFQhKM7:TR?= MUTTRW5ITVJ?
HD-MY-Z MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3XVoo3UUN3ME2xMlY{PTh2IDFOwG0> NEPpdoNUSU6JRWK=
HT-1376 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwNkSzOkAh|ryP NFLVZWFUSU6JRWK=
CAL-54 NUPrdHhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\TRXVKSzVyPUGuOlU4ODliIN88US=> MXjTRW5ITVJ?
ONS-76 M3Hi[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFH3dVlKSzVyPUGuOlc2PTFiIN88US=> M2ntPXNCVkeHUh?=
EFO-27 NXzhcWVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle1TWM2OD1zLk[4PVIhKM7:TR?= NFvWdmZUSU6JRWK=
769-P M2rtOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nWeWlEPTB;MT62PVU6PiBizszN M4\B[3NCVkeHUh?=
MV-4-11 NVX1bpJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\LRmlEPTB;MT62PVg2PiBizszN MmW2V2FPT0WU
NKM-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTRTWM2OD1zLkexPFAzKCEQvF2= M4i3[HNCVkeHUh?=
LOXIMVI NGOzdHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjqdXlLUUN3ME2xMlc1PTl7IDFOwG0> M4XtTXNCVkeHUh?=
KYSE-140 NIfaTYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4i4WGlEPTB;MT63OVY2PSBizszN NWTxOYxpW0GQR1XS
ES5 NYnQUGt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\MbGlEPTB;MT64Olc1PyBizszN MVLTRW5ITVJ?
BB65-RCC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXkTW15UUN3ME2xMlg6QDR7IDFOwG0> M3K0W3NCVkeHUh?=
HN MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFwOEm4O|QhKM7:TR?= MmXNV2FPT0WU
A101D MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LsXGlEPTB;MT65N|YzQCBizszN MYDTRW5ITVJ?
LoVo MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYCxSXBCUUN3ME2xMlk4Pjd7IDFOwG0> NIDTNJBUSU6JRWK=
NCI-H526 NV64Xm9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3X3fGlEPTB;MT65PVMzPSBizszN M13IUnNCVkeHUh?=
NCI-H1693 M{TTdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L2b2lEPTB;MT65PVg5QCBizszN MV3TRW5ITVJ?
OVCAR-4 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HN[WlEPTB;Mj6wNFQ{PSBizszN NEHGWGdUSU6JRWK=
SK-HEP-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfCc3NKSzVyPUKuNFA4PDViIN88US=> MVzTRW5ITVJ?
C2BBe1 MnrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HsNGlEPTB;Mj6wN|M4OiBizszN MVHTRW5ITVJ?
MEL-JUSO NFO5fYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXS2PZNEUUN3ME2yMlA1PDZ2IDFOwG0> NGjxN29USU6JRWK=
MOLT-16 NFLCTnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz2U3l7UUN3ME2yMlA4ODV6IDFOwG0> NYTBeoJYW0GQR1XS
NBsusSR NX:5e3ZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTM[|FKSzVyPUKuNFk5QDliIN88US=> MYLTRW5ITVJ?
TK10 M2f0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrkTWM2OD1{LkGzOFU5KCEQvF2= NFLYS2pUSU6JRWK=
CAL-39 MoPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7RemNtUUN3ME2yMlE1PDhiIN88US=> NFi1W3pUSU6JRWK=
NCI-H2030 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJwMUi5O|MhKM7:TR?= MmfNV2FPT0WU
HCT-116 NEDUUmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJwMkK5PFQhKM7:TR?= NIPE[pNUSU6JRWK=
HTC-C3 NWr0foI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJwMk[4NlQhKM7:TR?= M3;ENHNCVkeHUh?=
TYK-nu MonOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVflS3p1UUN3ME2yMlMxQTB7IDFOwG0> NEfDZlRUSU6JRWK=
FADU MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXyTWM2OD1{LkOyNlk3KCEQvF2= MoH0V2FPT0WU
A431 NXz1dmh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1e2XmlEPTB;Mj6zO|AzPSBizszN MoHrV2FPT0WU
TE-11 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\MO|BKSzVyPUKuN|gxOTliIN88US=> Mnv6V2FPT0WU
CAL-12T Mn3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjmWHh2UUN3ME2yMlQxPDF5IDFOwG0> M1zvUnNCVkeHUh?=
DB NID1UXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1viR2lEPTB;Mj60Nlg3QSBizszN NGPUZ3hUSU6JRWK=
L-363 NYLSU4FQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3rU2NKSzVyPUKuOFM2ODdiIN88US=> NVvWcldrW0GQR1XS
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NCI-H69 NV7SXW52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3qV3h3UUN3ME2zNE43ODl|IDFOwG0> Mn7kV2FPT0WU
NB6 NUL0fVBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjOSo0{UUN3ME2zNU4{PjJ7IDFOwG0> MlHTV2FPT0WU
CAL-120 NFzUV5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X4eGlEPTB;M{KuOFMyPyBizszN NFH3SGVUSU6JRWK=
U-87-MG M2LQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV65SZhXUUN3ME2zN{4xOjVzIDFOwG0> M1\ISXNCVkeHUh?=
NCI-H1304 NFriPZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{SzTGlEPTB;M{OuNFM2PCBizszN M4PXb3NCVkeHUh?=
YH-13 NUDUWm17T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HLPWlEPTB;M{OuNlU{PSBizszN NVO5dm12W0GQR1XS
RMG-I MoC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LLRWlEPTB;M{OuOFI5PSBizszN NUKxOHlzW0GQR1XS
LU-65 MkjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTHPXlZUUN3ME2zOE4yPDB6IDFOwG0> MXHTRW5ITVJ?
GB-1 NVu3SZBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\sSWlEPTB;M{WuNFczQSBizszN M{TsSXNCVkeHUh?=
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SBC-5 MmHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXYTnJKSzVyPUO2MlU6ODJiIN88US=> MVfTRW5ITVJ?
OE33 M{HE[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;2eZZKSzVyPUO3Mlc2PzdiIN88US=> NWjB[nllW0GQR1XS
C8166 NF;wfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\5[GlEPTB;M{iuOVI3PyBizszN MWPTRW5ITVJ?
COLO-684 NVrGOZhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3ZbFFFUUN3ME2zPE44PDJ6IDFOwG0> NWPPTZVnW0GQR1XS
NCI-H1155 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrPNYZKSzVyPUO5MlA1PzFiIN88US=> M4TJS3NCVkeHUh?=
ATN-1 NF\jUW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;xUmlEPTB;M{muO|c6OiBizszN NGXkWIRUSU6JRWK=
KARPAS-299 NILqNW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTN7LkizPUAh|ryP MYHTRW5ITVJ?
KNS-81-FD MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle3TWM2OD12MD6zOlA1KCEQvF2= MlrhV2FPT0WU
NCI-H1563 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vzZWlEPTB;NEGuOVA{QSBizszN M1PyPXNCVkeHUh?=
NB14 NITNZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTR{LkeyOlMhKM7:TR?= M3fuUXNCVkeHUh?=
COLO-800 M{\3VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTR{Lki1NVchKM7:TR?= MljQV2FPT0WU
MS-1 NVnpZ4twT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWwb4FHUUN3ME20N{4xPDh|IDFOwG0> M3PmV3NCVkeHUh?=
OVCAR-8 NXnDZVJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTR|Lk[4NFkhKM7:TR?= M2XscHNCVkeHUh?=
SK-PN-DW MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHxeGNKSzVyPUSzMlg4PzZiIN88US=> MVnTRW5ITVJ?
G-402 NGG3PHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTR|LkmwNFYhKM7:TR?= NEDHeY9USU6JRWK=
NCI-H2291 MoHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;ZVItKSzVyPUS0MlgxOTdiIN88US=> Mn\QV2FPT0WU
PC-3 NVjqUmlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTR3LkiwNlMhKM7:TR?= MXrTRW5ITVJ?
NCI-H1581 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrJfpVFUUN3ME20OU46QDh7IDFOwG0> NFHCRmpUSU6JRWK=
SW1116 NUS1N4pOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUO0XoZNUUN3ME20O{4xOTh{IDFOwG0> NHq0emtUSU6JRWK=
ZR-75-30 Mn\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTR5LkCyN|khKM7:TR?= M3LQUHNCVkeHUh?=
OCI-AML2 MnTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzwTWM2OD12Nz6wPVE5KCEQvF2= Mli2V2FPT0WU
MDA-MB-231 MofuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;XU4RKSzVyPUS3MlYzPDliIN88US=> NF\LT3JUSU6JRWK=
ES3 M1L1NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTR6LkO1NlkhKM7:TR?= NFfsN4dUSU6JRWK=
NCI-H630 M2\iOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi2[mlKSzVyPUS5MlE4PDJiIN88US=> NWPHTmdXW0GQR1XS
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... 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 <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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* 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID