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 M3PVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELxRmFKSzVyPUCuNFgzOzFiIN88US=> MUHTRW5ITVJ?
SW756 MknYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XtbGlEPTB;MD6xOFAzPCBizszN NVHlTm83W0GQR1XS
CTV-1 NW\hVIFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwMU[zPVghKM7:TR?= MXLTRW5ITVJ?
HSC-4 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7FTWM2OD1yLkG3NVU5KCEQvF2= Mn3nV2FPT0WU
LAMA-84 M{PWWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTxTWM2OD1yLkK4OlY1KCEQvF2= NILJTm9USU6JRWK=
KU812 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHX1XlJKSzVyPUCuN|QxPjhiIN88US=> NGTEZY9USU6JRWK=
HCC1806 M{\MWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\QcnBKSzVyPUCuN|UzOTZiIN88US=> NEHVN29USU6JRWK=
DOK MkPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkO5TWM2OD1yLkO3O|g3KCEQvF2= NIqzZ4JUSU6JRWK=
NCI-H209 M3rEXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS1TWM2OD1yLkSwPFA5KCEQvF2= NF3ETohUSU6JRWK=
EoL-1-cell M1mwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwNEG1O|YhKM7:TR?= MX7TRW5ITVJ?
H9 M4TmUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\zZXVRUUN3ME2wMlQ{PDZ2IDFOwG0> M1XxW3NCVkeHUh?=
EM-2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LzbmlEPTB;MD60N|g6KCEQvF2= MoTDV2FPT0WU
NCI-H292 M2jVfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjybIpKSzVyPUCuOFQyODhiIN88US=> MWTTRW5ITVJ?
697 MnexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLkTWM2OD1yLkS1OlM{KCEQvF2= NEjMZWJUSU6JRWK=
BHT-101 NUCzN4RvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwNE[1PUAh|ryP NH[yO4FUSU6JRWK=
BE-13 NEDPO5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M32yeGlEPTB;MD60PFU4OiBizszN M1PKNHNCVkeHUh?=
RS4-11 NVrzWXRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnK1TWM2OD1yLkS4OVg1KCEQvF2= NXTzelNJW0GQR1XS
IGROV-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTBwNEi3PVchKM7:TR?= NYrofpR2W0GQR1XS
KE-37 NUnXOW9UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwNEm1NFkhKM7:TR?= MYnTRW5ITVJ?
BV-173 NIjZeGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUe1bIpyUUN3ME2wMlUxPzl{IDFOwG0> NYTqd4lkW0GQR1XS
MEG-01 NGPZXGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjnN2RKSzVyPUCuOVEzOTRiIN88US=> NF3yfW9USU6JRWK=
LB2241-RCC M3PKb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3H4Z2lEPTB;MD61N|cyQCBizszN MnrNV2FPT0WU
ACHN MmqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELzVXZKSzVyPUCuOVQxPjliIN88US=> M3\kbXNCVkeHUh?=
CTB-1 NHr3SoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTBwNUS4NkAh|ryP M{njRnNCVkeHUh?=
HT-1080 NWTQWYRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwNUWzOFkhKM7:TR?= M{\5ZnNCVkeHUh?=
CHL-1 NHfhZoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTBwNUW0OlUhKM7:TR?= MUTTRW5ITVJ?
EW-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvyZ49KSzVyPUCuOVU6OzViIN88US=> NWXQSoZOW0GQR1XS
ES1 NYDPVHg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\0bpRKSzVyPUCuOlc1QThiIN88US=> MXTTRW5ITVJ?
KASUMI-1 NHTI[ZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPuTWM2OD1yLkeyN|MhKM7:TR?= M1PXZXNCVkeHUh?=
SW13 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwN{O3PVghKM7:TR?= MmDCV2FPT0WU
A3-KAW M1y1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwN{myNFghKM7:TR?= NFXMZW9USU6JRWK=
LB771-HNC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwOEOxNFQhKM7:TR?= NVrzZmxPW0GQR1XS
OC-314 NIXz[|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXPUldKSzVyPUCuPFY6PjViIN88US=> Mnq2V2FPT0WU
MLMA NVzvdmZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnRTWM2OD1yLkmwOlc2KCEQvF2= Mk\BV2FPT0WU
KARPAS-45 NVHvTWM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwOUK0OlYhKM7:TR?= MlLDV2FPT0WU
CAL-27 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe0TFNmUUN3ME2wMlkzQTB4IDFOwG0> M3rLV3NCVkeHUh?=
SK-NEP-1 NWPwTHpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;FOZQ5UUN3ME2wMlk4OjR6IDFOwG0> NWDvVWg4W0GQR1XS
COR-L105 M4\nbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlT6TWM2OD1zLkCwN|k1KCEQvF2= M{SzbHNCVkeHUh?=
TI-73 NH33U3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTFwMEG2OUAh|ryP MkjpV2FPT0WU
JVM-3 NHXsXZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwMEWwNVchKM7:TR?= MYLTRW5ITVJ?
HAL-01 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\uT2lEPTB;MT6wPFgyKCEQvF2= MULTRW5ITVJ?
QIMR-WIL NVz6U41HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFwMEmwOVghKM7:TR?= MVTTRW5ITVJ?
HSC-3 Ml;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPTNllKSzVyPUGuNVE4QDNiIN88US=> MmrHV2FPT0WU
KY821 Mn\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPQZVhKSzVyPUGuNVM{PTFiIN88US=> MX3TRW5ITVJ?
5637 M2jHdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\aPWtKSzVyPUGuNVM5ODNiIN88US=> M3L2R3NCVkeHUh?=
CAL-33 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTFwMUmzNFIhKM7:TR?= M132b3NCVkeHUh?=
ES4 NIHYeYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVuwdIdoUUN3ME2xMlIxPzliIN88US=> M{nHNHNCVkeHUh?=
BHY NHzzb|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFwMkK4PVIhKM7:TR?= MX7TRW5ITVJ?
LB1047-RCC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS1WYFmUUN3ME2xMlI{Pzh3IDFOwG0> NVXoc4l1W0GQR1XS
H4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULWXFk4UUN3ME2xMlI1OjV3IDFOwG0> MYTTRW5ITVJ?
RPMI-8866 NHSzPZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTFwMk[xNFYhKM7:TR?= MmnsV2FPT0WU
HO-1-N-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[wfWlEPTB;MT6yOlM3QSBizszN MVjTRW5ITVJ?
BB30-HNC NH;RO5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLJSm5sUUN3ME2xMlI5PzF2IDFOwG0> M4\XTXNCVkeHUh?=
PC-14 Ml7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP6TWM2OD1zLkK5NlA2KCEQvF2= NWLFXYp2W0GQR1XS
NUGC-3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTFwMkmzOVYhKM7:TR?= NUDPTYNlW0GQR1XS
A4-Fuk MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPvdmhKSzVyPUGuN|A4ODRiIN88US=> NWXwO|QxW0GQR1XS
MHH-NB-11 M2Hldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnm4TWM2OD1zLkOxN|g{KCEQvF2= NVfldZppW0GQR1XS
KOSC-2 NXjxNnJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPwbmlKSzVyPUGuN|E4PzViIN88US=> MYLTRW5ITVJ?
A498 NHy5dG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGSyWWZKSzVyPUGuOFAyOTNiIN88US=> NFXpb41USU6JRWK=
KG-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUW2fY1LUUN3ME2xMlQyOjd|IDFOwG0> MU\TRW5ITVJ?
DEL Ml[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPPRlc5UUN3ME2xMlQ{PjV5IDFOwG0> MVXTRW5ITVJ?
EW-16 M1XiV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwNEO5O|MhKM7:TR?= NX3ocYExW0GQR1XS
BPH-1 M{mwSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M32xRWlEPTB;MT60OFgxPSBizszN MlyzV2FPT0WU
JAR MorrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFntXWhKSzVyPUGuOFk{PiBizszN NHv3V3BUSU6JRWK=
J-RT3-T3-5 M37yc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XKXmlEPTB;MT61NVczOiBizszN M3qzcXNCVkeHUh?=
A375 NILH[JVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXFN2xKSzVyPUGuOVE4PzJiIN88US=> NUn5[IhOW0GQR1XS
SW954 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;sTWM2OD1zLkW1NFA4KCEQvF2= MV3TRW5ITVJ?
Ca9-22 NE\KSmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrM[WlKSzVyPUGuOVYzPiBizszN MYXTRW5ITVJ?
D-566MG NUftXIdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7zTWM2OD1zLkW3NVU2KCEQvF2= NGjhbFZUSU6JRWK=
SCC-15 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzFRmY2UUN3ME2xMlYyQDB2IDFOwG0> M3zDOHNCVkeHUh?=
HD-MY-Z NHfld5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPHdVBKSzVyPUGuOlM2QDRiIN88US=> M{f1T3NCVkeHUh?=
HT-1376 M{KxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\tfHRpUUN3ME2xMlY1OzZiIN88US=> MYfTRW5ITVJ?
CAL-54 MoPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTFwNkW3NFkhKM7:TR?= MUXTRW5ITVJ?
ONS-76 M{LsWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLaTWM2OD1zLk[3OVUyKCEQvF2= NXzle4NLW0GQR1XS
EFO-27 NYq3UWJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPpb2tjUUN3ME2xMlY5QTJiIN88US=> NV;iNZFYW0GQR1XS
769-P MnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;tUWRbUUN3ME2xMlY6PTl4IDFOwG0> NXr5PHVzW0GQR1XS
MV-4-11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnXcpN4UUN3ME2xMlY6QDV4IDFOwG0> NHjKbGZUSU6JRWK=
NKM-1 M2\zU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfKcoZKSzVyPUGuO|E5ODJiIN88US=> Ml3LV2FPT0WU
LOXIMVI M4O4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\3TWM2OD1zLke0OVk6KCEQvF2= NFn4eZZUSU6JRWK=
KYSE-140 NX\5VIZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTFwN{W2OVUhKM7:TR?= MYjTRW5ITVJ?
ES5 MmPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jlUWlEPTB;MT64Olc1PyBizszN MmD5V2FPT0WU
BB65-RCC NWHTfllXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFwOEm4OFkhKM7:TR?= NHrLcWtUSU6JRWK=
HN MmPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELSXYlKSzVyPUGuPFk5PzRiIN88US=> NWWydnNVW0GQR1XS
A101D MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFwOUO2NlghKM7:TR?= M3LmenNCVkeHUh?=
LoVo Ml\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnlcpVTUUN3ME2xMlk4Pjd7IDFOwG0> NVvwb3hEW0GQR1XS
NCI-H526 M12xcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTFwOUmzNlUhKM7:TR?= NF64R|NUSU6JRWK=
NCI-H1693 MojQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjrTWM2OD1zLkm5PFg5KCEQvF2= NVzUSGhOW0GQR1XS
OVCAR-4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LmbmlEPTB;Mj6wNFQ{PSBizszN M2eyNHNCVkeHUh?=
SK-HEP-1 NVPpPXZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rleWlEPTB;Mj6wNFc1PSBizszN M{nhOHNCVkeHUh?=
C2BBe1 NILYS|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zMWmlEPTB;Mj6wN|M4OiBizszN NHr3R4xUSU6JRWK=
MEL-JUSO MlfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJwMES0OlQhKM7:TR?= MV;TRW5ITVJ?
MOLT-16 M4rreGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2faeGlEPTB;Mj6wO|A2QCBizszN MVHTRW5ITVJ?
NBsusSR MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLCTWM2OD1{LkC5PFg6KCEQvF2= NG\BXHVUSU6JRWK=
TK10 MnX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfsUItKSzVyPUKuNVM1PThiIN88US=> NF[0eZdUSU6JRWK=
CAL-39 MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJwMUS0PEAh|ryP MUTTRW5ITVJ?
NCI-H2030 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTJwMUi5O|MhKM7:TR?= NVHTc4tyW0GQR1XS
HCT-116 NHfabVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTJwMkK5PFQhKM7:TR?= NWHh[YlbW0GQR1XS
HTC-C3 NV\0fm1kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HLN2lEPTB;Mj6yOlgzPCBizszN M{T1PHNCVkeHUh?=
TYK-nu MkH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;Ybo5SUUN3ME2yMlMxQTB7IDFOwG0> NE\vRVNUSU6JRWK=
FADU MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJwM{KyPVYhKM7:TR?= M4G3S3NCVkeHUh?=
A431 NFe2NJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTJwM{ewNlUhKM7:TR?= NWX1OlRLW0GQR1XS
TE-11 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\1TWM2OD1{LkO4NFE6KCEQvF2= NWrBVFBQW0GQR1XS
CAL-12T NYS4THF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYW0N2ZqUUN3ME2yMlQxPDF5IDFOwG0> NFizSWJUSU6JRWK=
DB MnHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXGXnhKSzVyPUKuOFI5PjliIN88US=> NYfHOFVwW0GQR1XS
L-363 MmHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJwNEO1NFchKM7:TR?= MWPTRW5ITVJ?
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MC116 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTNyLkC3N|MhKM7:TR?= M1f1SXNCVkeHUh?=
NCI-H69 NH3NXINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3yyTWlEPTB;M{CuOlA6OyBizszN MYLTRW5ITVJ?
NB6 NXfacpFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTNzLkO2NlkhKM7:TR?= NHuxUoVUSU6JRWK=
CAL-120 MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mne3TWM2OD1|Mj60N|E4KCEQvF2= M1fucXNCVkeHUh?=
U-87-MG NXzHZ484T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorvTWM2OD1|Mz6wNlUyKCEQvF2= MXnTRW5ITVJ?
NCI-H1304 M2OyUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYe3Xod6UUN3ME2zN{4xOzV2IDFOwG0> MmT6V2FPT0WU
YH-13 NGjTb3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{D1[mlEPTB;M{OuNlU{PSBizszN MY\TRW5ITVJ?
RMG-I NF3KPVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTITWM2OD1|Mz60Nlg2KCEQvF2= NHzYUZVUSU6JRWK=
LU-65 NGLNc2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjBTWM2OD1|ND6xOFA5KCEQvF2= M1zHRXNCVkeHUh?=
GB-1 NIGxUpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTN3LkC3NlkhKM7:TR?= MXrTRW5ITVJ?
DU-4475 NH3aUGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHmTWM2OD1|NT6xOVU{KCEQvF2= M2jxU3NCVkeHUh?=
SBC-5 NGOzSYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHkWJRJUUN3ME2zOk42QTB{IDFOwG0> MmXYV2FPT0WU
OE33 NEHLXlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\y[2lEPTB;M{euO|U4PyBizszN MWnTRW5ITVJ?
C8166 MnTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\RVmlEPTB;M{iuOVI3PyBizszN NYjjUoU2W0GQR1XS
COLO-684 NVvRbIpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfyfHd6UUN3ME2zPE44PDJ6IDFOwG0> MXLTRW5ITVJ?
NCI-H1155 M3\Xfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTN7LkC0O|EhKM7:TR?= M4r4b3NCVkeHUh?=
ATN-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnZTWM2OD1|OT63O|kzKCEQvF2= NFv0RnBUSU6JRWK=
KARPAS-299 NILReWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fCS2lEPTB;M{muPFM6KCEQvF2= MlPHV2FPT0WU
KNS-81-FD NXjNdnVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHkTVNUUUN3ME20NE4{PjB2IDFOwG0> MYrTRW5ITVJ?
NCI-H1563 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[4N2lEPTB;NEGuOVA{QSBizszN MXPTRW5ITVJ?
NB14 NH\YWnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPHTWM2OD12Mj63NlY{KCEQvF2= NUjOdXlYW0GQR1XS
COLO-800 MoHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrFd|FKSzVyPUSyMlg2OTdiIN88US=> NWr5UWN6W0GQR1XS
MS-1 NFLkfHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;2foRKSzVyPUSzMlA1QDNiIN88US=> MXLTRW5ITVJ?
OVCAR-8 NXfLZmNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki3TWM2OD12Mz62PFA6KCEQvF2= MlnyV2FPT0WU
SK-PN-DW NYPHN3BWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTR|Lki3O|YhKM7:TR?= NYC2U|dKW0GQR1XS
G-402 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjaZmJKSzVyPUSzMlkxODZiIN88US=> NWXjS3g2W0GQR1XS
NCI-H2291 NV76OZp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv3RpRjUUN3ME20OE45ODF5IDFOwG0> MYDTRW5ITVJ?
PC-3 Mn7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\nXJNJUUN3ME20OU45ODJ|IDFOwG0> NV\aRY83W0GQR1XS
NCI-H1581 M{WzUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDPc|QxUUN3ME20OU46QDh7IDFOwG0> MonIV2FPT0WU
SW1116 NFfscZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTR5LkCxPFIhKM7:TR?= MlvDV2FPT0WU
ZR-75-30 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTR5LkCyN|khKM7:TR?= MWXTRW5ITVJ?
OCI-AML2 MkjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTR5LkC5NVghKM7:TR?= M3rrTHNCVkeHUh?=
MDA-MB-231 Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLrOGtKSzVyPUS3MlYzPDliIN88US=> M4PYVHNCVkeHUh?=
ES3 NEjabG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTR6LkO1NlkhKM7:TR?= M4C3WXNCVkeHUh?=
NCI-H630 MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PQc2lEPTB;NEmuNVc1OiBizszN M1\DbHNCVkeHUh?=
OE19 M{f4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfwTWM2OD12OT6yPVAzKCEQvF2= NFXvfGVUSU6JRWK=
NCI-H1573 M2ny[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTR7Lk[4OlEhKM7:TR?= NU\t[5N3W0GQR1XS
EW-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrFdFl7UUN3ME20PU46ODh2IDFOwG0> MlPnV2FPT0WU

... 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 )

  • 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

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