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 NYDWNnN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFG1UW9KSzVyPUCuNFgzOzFiIN88US=> M4PpOXNCVkeHUh?=
SW756 Mle3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXsN29wUUN3ME2wMlE1ODJ2IDFOwG0> M1zycXNCVkeHUh?=
CTV-1 NHqwXVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwMU[zPVghKM7:TR?= NVf6ZlN1W0GQR1XS
HSC-4 M3PsRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnWXppKSzVyPUCuNVcyPThiIN88US=> NX\KTIJSW0GQR1XS
LAMA-84 MmrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PRfmlEPTB;MD6yPFY3PCBizszN M1jZNnNCVkeHUh?=
KU812 NVLsNFNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\QcWlEPTB;MD6zOFA3QCBizszN MkHIV2FPT0WU
HCC1806 NIXGT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\s[WlEPTB;MD6zOVIyPiBizszN NE\w[VhUSU6JRWK=
DOK MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvTVFFKSzVyPUCuN|c4QDZiIN88US=> MmfrV2FPT0WU
NCI-H209 NX\oNVM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\XTWM2OD1yLkSwPFA5KCEQvF2= NVvpe3BuW0GQR1XS
EoL-1-cell MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzDXGpKSzVyPUCuOFE2PzZiIN88US=> M4rIbnNCVkeHUh?=
H9 M4\mSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;VWmlEPTB;MD60N|Q3PCBizszN NULBVFhuW0GQR1XS
EM-2 MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWzNlFKSzVyPUCuOFM5QSBizszN NGLDT5dUSU6JRWK=
NCI-H292 M1PCW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTOemtTUUN3ME2wMlQ1OTB6IDFOwG0> MVvTRW5ITVJ?
697 NWjQOGdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNEW2N|MhKM7:TR?= NEDCSXZUSU6JRWK=
BHT-101 NUWyV4U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LDVGlEPTB;MD60OlU6KCEQvF2= MVTTRW5ITVJ?
BE-13 M2nQcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTBwNEi1O|IhKM7:TR?= NGHXTohUSU6JRWK=
RS4-11 MlfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfRNVlKSzVyPUCuOFg2QDRiIN88US=> NETmeXpUSU6JRWK=
IGROV-1 NILuS3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwNEi3PVchKM7:TR?= NWT5c5FGW0GQR1XS
KE-37 MnTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fPd2lEPTB;MD60PVUxQSBizszN MUnTRW5ITVJ?
BV-173 M3f0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nKSGlEPTB;MD61NFc6OiBizszN MkTpV2FPT0WU
MEG-01 Mn7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjsTWM2OD1yLkWxNlE1KCEQvF2= NXLmfo5uW0GQR1XS
LB2241-RCC NVfPPWU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLjfWhZUUN3ME2wMlU{PzF6IDFOwG0> NH\0bohUSU6JRWK=
ACHN NF;PPYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTBwNUSwOlkhKM7:TR?= NH\hdWlUSU6JRWK=
CTB-1 MoG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwNUS4NkAh|ryP NEPPZoRUSU6JRWK=
HT-1080 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjCTWM2OD1yLkW1N|Q6KCEQvF2= NF\RT|JUSU6JRWK=
CHL-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwNUW0OlUhKM7:TR?= M3joSHNCVkeHUh?=
EW-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILlbHFKSzVyPUCuOVU6OzViIN88US=> NITy[5BUSU6JRWK=
ES1 MmfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LlNWlEPTB;MD62O|Q6QCBizszN NV;BVnZSW0GQR1XS
KASUMI-1 MojwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe2TWM2OD1yLkeyN|MhKM7:TR?= MlXyV2FPT0WU
SW13 NGLo[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfTTWM2OD1yLkezO|k5KCEQvF2= NWXHclNUW0GQR1XS
A3-KAW NVjOfHpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DHUGlEPTB;MD63PVIxQCBizszN MkXSV2FPT0WU
LB771-HNC NVfxS5dlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTTZ2ZKSzVyPUCuPFMyODRiIN88US=> M{m2bXNCVkeHUh?=
OC-314 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv5fYFKSzVyPUCuPFY6PjViIN88US=> MYDTRW5ITVJ?
MLMA MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTBwOUC2O|UhKM7:TR?= M4nkcXNCVkeHUh?=
KARPAS-45 NIrsRXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwOUK0OlYhKM7:TR?= NInjVGpUSU6JRWK=
CAL-27 NVPGfJRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fX[2lEPTB;MD65NlkxPiBizszN MlHwV2FPT0WU
SK-NEP-1 NUHzU4xET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrWeZg4UUN3ME2wMlk4OjR6IDFOwG0> MoDNV2FPT0WU
COR-L105 NIPrTJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HafWlEPTB;MT6wNFM6PCBizszN NYK3PZJFW0GQR1XS
TI-73 MmDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjmNWlmUUN3ME2xMlAyPjViIN88US=> NFX2N4NUSU6JRWK=
JVM-3 NHnGXoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwMEWwNVchKM7:TR?= NWHOeZhjW0GQR1XS
HAL-01 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUiyfIljUUN3ME2xMlA5QDFiIN88US=> M3XrRnNCVkeHUh?=
QIMR-WIL MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnqTWM2OD1zLkC5NFU5KCEQvF2= NIPKZmlUSU6JRWK=
HSC-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwMUG3PFMhKM7:TR?= NHXlSHRUSU6JRWK=
KY821 M{\tN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfJbYFHUUN3ME2xMlE{OzVzIDFOwG0> MmjTV2FPT0WU
5637 MlXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:1XWVxUUN3ME2xMlE{QDB|IDFOwG0> MUfTRW5ITVJ?
CAL-33 NWnEdFZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[wTWM2OD1zLkG5N|AzKCEQvF2= NGLjSJRUSU6JRWK=
ES4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrkTWM2OD1zLkKwO|khKM7:TR?= NWL3eHlVW0GQR1XS
BHY M3fqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTFwMkK4PVIhKM7:TR?= MYHTRW5ITVJ?
LB1047-RCC Mn\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[5TWM2OD1zLkKzO|g2KCEQvF2= MneyV2FPT0WU
H4 MmXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTFwMkSyOVUhKM7:TR?= MUHTRW5ITVJ?
RPMI-8866 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjueIZ5UUN3ME2xMlI3OTB4IDFOwG0> NGr3VmpUSU6JRWK=
HO-1-N-1 NVfhO4d6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;CR41FUUN3ME2xMlI3OzZ7IDFOwG0> NEPjco1USU6JRWK=
BB30-HNC MnrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfoTWM2OD1zLkK4O|E1KCEQvF2= MnHLV2FPT0WU
PC-14 MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\1eGdEUUN3ME2xMlI6OjB3IDFOwG0> NVfFT2NmW0GQR1XS
NUGC-3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnDTWM2OD1zLkK5N|U3KCEQvF2= NFPZc3hUSU6JRWK=
A4-Fuk NHPrV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTXTWM2OD1zLkOwO|A1KCEQvF2= MkSxV2FPT0WU
MHH-NB-11 M{D3Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[5TFhPUUN3ME2xMlMyOzh|IDFOwG0> MlnuV2FPT0WU
KOSC-2 NFvlUY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HoTGlEPTB;MT6zNVc4PSBizszN NWPQ[JJHW0GQR1XS
A498 M{\KcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXQTnAyUUN3ME2xMlQxOTF|IDFOwG0> M1fNRXNCVkeHUh?=
KG-1 NED6S25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLRS3pEUUN3ME2xMlQyOjd|IDFOwG0> Mo[5V2FPT0WU
DEL MljPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzKTWM2OD1zLkSzOlU4KCEQvF2= M2W5XHNCVkeHUh?=
EW-16 NYKxOpl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:4WZRKSzVyPUGuOFM6PzNiIN88US=> MluxV2FPT0WU
BPH-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTFwNES4NFUhKM7:TR?= NEjB[mpUSU6JRWK=
JAR NUX4VmxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\JbFBKSzVyPUGuOFk{PiBizszN NEG1NVlUSU6JRWK=
J-RT3-T3-5 Mlv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f5W2lEPTB;MT61NVczOiBizszN NEPuNndUSU6JRWK=
A375 NEDWc45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTxTWM2OD1zLkWxO|czKCEQvF2= M3P2O3NCVkeHUh?=
SW954 MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7oTWM2OD1zLkW1NFA4KCEQvF2= NEez[ZVUSU6JRWK=
Ca9-22 M{nFU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnH0TWM2OD1zLkW2NlYhKM7:TR?= M3Ww[XNCVkeHUh?=
D-566MG M4K0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\uXGlEPTB;MT61O|E2PSBizszN M1LmS3NCVkeHUh?=
SCC-15 M3HIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnqdlMyUUN3ME2xMlYyQDB2IDFOwG0> NUfET3Z1W0GQR1XS
HD-MY-Z Mn3aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPodIZKSzVyPUGuOlM2QDRiIN88US=> MXnTRW5ITVJ?
HT-1376 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TG[mlEPTB;MT62OFM3KCEQvF2= M4\5ZXNCVkeHUh?=
CAL-54 NUn0SmplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTFwNkW3NFkhKM7:TR?= MmqzV2FPT0WU
ONS-76 Mn\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP4TWM2OD1zLk[3OVUyKCEQvF2= NGXDeVFUSU6JRWK=
EFO-27 M2TGTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFwNki5NkAh|ryP MlfzV2FPT0WU
769-P NHXWXoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwNkm1PVYhKM7:TR?= MknnV2FPT0WU
MV-4-11 M2fYeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjj[mlEUUN3ME2xMlY6QDV4IDFOwG0> MVHTRW5ITVJ?
NKM-1 NYHWXHpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDXXmdwUUN3ME2xMlcyQDB{IDFOwG0> MnLBV2FPT0WU
LOXIMVI MlLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fkZmlEPTB;MT63OFU6QSBizszN NGDKTmJUSU6JRWK=
KYSE-140 NF;iO2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP0fG1tUUN3ME2xMlc2PjV3IDFOwG0> NU\HcJhrW0GQR1XS
ES5 NHe3OWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTFwOE[3OFchKM7:TR?= MlPmV2FPT0WU
BB65-RCC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\rUWlEPTB;MT64PVg1QSBizszN MYTTRW5ITVJ?
HN NIXjVFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfDOIlFUUN3ME2xMlg6QDd2IDFOwG0> Mo\PV2FPT0WU
A101D M{DQXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHFc3pKSzVyPUGuPVM3OjhiIN88US=> M3PvfXNCVkeHUh?=
LoVo MlzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTlO4lGUUN3ME2xMlk4Pjd7IDFOwG0> NIHOSHBUSU6JRWK=
NCI-H526 M2fEVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7WTWM2OD1zLkm5N|I2KCEQvF2= M{\4PXNCVkeHUh?=
NCI-H1693 M3zGdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS3XGFsUUN3ME2xMlk6QDh6IDFOwG0> Mlz5V2FPT0WU
OVCAR-4 NVPFUGJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrqS3FIUUN3ME2yMlAxPDN3IDFOwG0> NWLjbVlkW0GQR1XS
SK-HEP-1 NXnUb5VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTJwMEC3OFUhKM7:TR?= MUTTRW5ITVJ?
C2BBe1 NYfQR3o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYL6S2dtUUN3ME2yMlA{Ozd{IDFOwG0> M{nHbHNCVkeHUh?=
MEL-JUSO NUfDTXVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln4TWM2OD1{LkC0OFY1KCEQvF2= MYPTRW5ITVJ?
MOLT-16 NXKxTlYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrSZoR5UUN3ME2yMlA4ODV6IDFOwG0> M2\Sc3NCVkeHUh?=
NBsusSR M2LVW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS4TWM2OD1{LkC5PFg6KCEQvF2= MYDTRW5ITVJ?
TK10 NYH3WJM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP6TWM2OD1{LkGzOFU5KCEQvF2= NF3VXldUSU6JRWK=
CAL-39 M37hOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHwWHVjUUN3ME2yMlE1PDhiIN88US=> M4HIdHNCVkeHUh?=
NCI-H2030 MmDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4roRmlEPTB;Mj6xPFk4OyBizszN Mm\ZV2FPT0WU
HCT-116 NW\VWJJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXtTWM2OD1{LkKyPVg1KCEQvF2= NHfvS41USU6JRWK=
HTC-C3 MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy0bVg6UUN3ME2yMlI3QDJ2IDFOwG0> Mo\vV2FPT0WU
TYK-nu NEjqSZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;KXmlEPTB;Mj6zNFkxQSBizszN MlHVV2FPT0WU
FADU NXnUOVM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;WOZZKSzVyPUKuN|IzQTZiIN88US=> M{THOnNCVkeHUh?=
A431 Mn3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzqNndKSzVyPUKuN|cxOjViIN88US=> MUfTRW5ITVJ?
TE-11 M{W4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPadoh4UUN3ME2yMlM5ODF7IDFOwG0> NUXLW284W0GQR1XS
CAL-12T NHHYbGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\aV2lEPTB;Mj60NFQyPyBizszN MlmxV2FPT0WU
DB M3uwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnuNphtUUN3ME2yMlQzQDZ7IDFOwG0> MknNV2FPT0WU
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NCI-H69 M2\oXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPuTWM2OD1|MD62NFk{KCEQvF2= NILJZW5USU6JRWK=
NB6 NVLrc49QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[1TWM2OD1|MT6zOlI6KCEQvF2= NFzZbo5USU6JRWK=
CAL-120 NIrvUZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPCfY9zUUN3ME2zNk41OzF5IDFOwG0> MlPEV2FPT0WU
U-87-MG NUjJeW0yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q0cGlEPTB;M{OuNFI2OSBizszN MV;TRW5ITVJ?
NCI-H1304 MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXRWHQ3UUN3ME2zN{4xOzV2IDFOwG0> M1zSSnNCVkeHUh?=
YH-13 NYmzbHVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLBSmlKSzVyPUOzMlI2OzViIN88US=> M1j4OHNCVkeHUh?=
RMG-I NFXmbo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPaTWM2OD1|Mz60Nlg2KCEQvF2= NHH1d5NUSU6JRWK=
LU-65 NHvUbpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PwSWlEPTB;M{SuNVQxQCBizszN Mn3DV2FPT0WU
GB-1 NYHYcoV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzPZoRKSzVyPUO1MlA4OjliIN88US=> MoHDV2FPT0WU
DU-4475 NF;nb2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLjTWM2OD1|NT6xOVU{KCEQvF2= NF2ybXlUSU6JRWK=
SBC-5 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrhUHBKSzVyPUO2MlU6ODJiIN88US=> M2nCU3NCVkeHUh?=
OE33 NGr3dXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPzc2ZyUUN3ME2zO{44PTd5IDFOwG0> MoLuV2FPT0WU
C8166 NXfwWZJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rvVGlEPTB;M{iuOVI3PyBizszN NHXrN3lUSU6JRWK=
COLO-684 NITuVlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjTTWM2OD1|OD63OFI5KCEQvF2= M4TVVnNCVkeHUh?=
NCI-H1155 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLidnA{UUN3ME2zPU4xPDdzIDFOwG0> M1\LeXNCVkeHUh?=
ATN-1 NXPvR|BDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrmRmZKSzVyPUO5Mlc4QTJiIN88US=> NXXUPVdWW0GQR1XS
KARPAS-299 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTN7LkizPUAh|ryP Ml3LV2FPT0WU
KNS-81-FD MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHaeVlKSzVyPUSwMlM3ODRiIN88US=> M4D0bHNCVkeHUh?=
NCI-H1563 Mn;WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXrR5BOUUN3ME20NU42ODN7IDFOwG0> Mkm5V2FPT0WU
NB14 M2XCPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\1ZmRvUUN3ME20Nk44OjZ|IDFOwG0> NE\YNnhUSU6JRWK=
COLO-800 M1LXbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr1TWM2OD12Mj64OVE4KCEQvF2= MnvsV2FPT0WU
MS-1 MnzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTWRphKSzVyPUSzMlA1QDNiIN88US=> MVnTRW5ITVJ?
OVCAR-8 M3vYb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDRdW9KSzVyPUSzMlY5ODliIN88US=> MUnTRW5ITVJ?
SK-PN-DW MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XFd2lEPTB;NEOuPFc4PiBizszN NX;We|NlW0GQR1XS
G-402 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fLOmlEPTB;NEOuPVAxPiBizszN MmnXV2FPT0WU
NCI-H2291 M{T5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnMTWM2OD12ND64NFE4KCEQvF2= MoHhV2FPT0WU
PC-3 NGCw[pBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\iU2lEPTB;NEWuPFAzOyBizszN Mo\sV2FPT0WU
NCI-H1581 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P3UWlEPTB;NEWuPVg5QSBizszN MX;TRW5ITVJ?
SW1116 NVfNSIoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDUdVRKSzVyPUS3MlAyQDJiIN88US=> M{WzRXNCVkeHUh?=
ZR-75-30 MmfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXUcoNSUUN3ME20O{4xOjN7IDFOwG0> MVLTRW5ITVJ?
OCI-AML2 MkH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTR5LkC5NVghKM7:TR?= Ml3yV2FPT0WU
MDA-MB-231 MnnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzJTWM2OD12Nz62NlQ6KCEQvF2= M2TFe3NCVkeHUh?=
ES3 M{HiWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlixTWM2OD12OD6zOVI6KCEQvF2= MVzTRW5ITVJ?
NCI-H630 NXTGPJlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;kTWM2OD12OT6xO|QzKCEQvF2= MmTrV2FPT0WU
OE19 NE\qOFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfSTWM2OD12OT6yPVAzKCEQvF2= MmThV2FPT0WU
NCI-H1573 MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHuwU3hKSzVyPUS5MlY5PjFiIN88US=> M{PXPXNCVkeHUh?=
EW-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7QZ|NKSzVyPUS5MlkxQDRiIN88US=> NUTSfXQ5W0GQR1XS

... 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
+ 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
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  • 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
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  • 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)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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
NCT02810990 Not yet recruiting Chronic Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto September 2016 Phase 2
NCT02782403 Not yet recruiting Leukemia M.D. Anderson Cancer Center|Pfizer August 2016 Phase 1|Phase 2
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
NCT02638467 Recruiting Leukemia|Myelogenous|Chronic|BCR-ABL Positive University of Milano Bicocca|IRCCS San Raffaele November 2015 Phase 2
NCT02546375 Active, not recruiting Chronic Myeloid Leukaemia Pfizer|pH Associates July 2015 --
NCT02501330 Active, not recruiting Chronic Myelogenous Leukemia Pfizer July 2015 --

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.

Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID