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, 16(6):1145-1154. Bosutinib (SKI-606) purchased from Selleck.

  • SFK inhibitors abrogate tyrosine phosphorylation associated with sperm capacitation. Mouse sperm were incubated in the absence or in the presence of SKI606 for 60 min in capacitating (cap, with HCO3) or non-capacitating media (NC, without HCO3). Western blot analyses were performed withanti-pY antibodies.

    J Biol Chem 2010 285, 7977–7985. Bosutinib (SKI-606) purchased from Selleck.

    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 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD2TWM2OD1yLkC4NlMyKCEQvF2= MmPVV2FPT0WU
SW756 M4H1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwMUSwNlQhKM7:TR?= MnjZV2FPT0WU
CTV-1 NVrlcok4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEizSFNKSzVyPUCuNVY{QThiIN88US=> MWrTRW5ITVJ?
HSC-4 MkXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[3bGZDUUN3ME2wMlE4OTV6IDFOwG0> MX;TRW5ITVJ?
LAMA-84 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWWyWWd3UUN3ME2wMlI5PjZ2IDFOwG0> MXHTRW5ITVJ?
KU812 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXhXYQ1UUN3ME2wMlM1ODZ6IDFOwG0> MVPTRW5ITVJ?
HCC1806 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;vSlJKSzVyPUCuN|UzOTZiIN88US=> MXLTRW5ITVJ?
DOK MoHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;T[5YzUUN3ME2wMlM4Pzh4IDFOwG0> MW\TRW5ITVJ?
NCI-H209 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTBwNEC4NFghKM7:TR?= M1rx[nNCVkeHUh?=
EoL-1-cell NYm2bXVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfsTWM2OD1yLkSxOVc3KCEQvF2= M3exRnNCVkeHUh?=
H9 M{PLeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTBwNEO0OlQhKM7:TR?= MnTnV2FPT0WU
EM-2 NGHwUFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D1SmlEPTB;MD60N|g6KCEQvF2= M4DDb3NCVkeHUh?=
NCI-H292 MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nrNGlEPTB;MD60OFExQCBizszN Moq4V2FPT0WU
697 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjqTWM2OD1yLkS1OlM{KCEQvF2= MVXTRW5ITVJ?
BHT-101 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHDZVhKSzVyPUCuOFY2QSBizszN MlzUV2FPT0WU
BE-13 M{P5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\0XGlEPTB;MD60PFU4OiBizszN NHrW[otUSU6JRWK=
RS4-11 NVjyVmlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwNEi1PFQhKM7:TR?= MWrTRW5ITVJ?
IGROV-1 NGPh[4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi1TWM2OD1yLkS4O|k4KCEQvF2= M{XjfnNCVkeHUh?=
KE-37 NX;6WoVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnNTWM2OD1yLkS5OVA6KCEQvF2= MUDTRW5ITVJ?
BV-173 NWPseXozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfUbmdVUUN3ME2wMlUxPzl{IDFOwG0> MoT3V2FPT0WU
MEG-01 NYDMPW95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PWT2lEPTB;MD61NVIyPCBizszN M3TOenNCVkeHUh?=
LB2241-RCC NEDNU4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnmPFBKSzVyPUCuOVM4OThiIN88US=> NXTvPWFDW0GQR1XS
ACHN MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwNUSwOlkhKM7:TR?= NFvtWWtUSU6JRWK=
CTB-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInLWnFKSzVyPUCuOVQ5OiBizszN M2LEd3NCVkeHUh?=
HT-1080 NVfIeppDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXJZYRKSzVyPUCuOVU{PDliIN88US=> MmC2V2FPT0WU
CHL-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M32xZmlEPTB;MD61OVQ3PSBizszN M3zrNXNCVkeHUh?=
EW-3 NG\h[ZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\yemlEPTB;MD61OVk{PSBizszN NXjte|dvW0GQR1XS
ES1 M1XIN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX0TI5KSzVyPUCuOlc1QThiIN88US=> MorXV2FPT0WU
KASUMI-1 MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwN{KzN{Ah|ryP MXPTRW5ITVJ?
SW13 NX:xc3cxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoG2TWM2OD1yLkezO|k5KCEQvF2= MljFV2FPT0WU
A3-KAW NILzVHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTBwN{myNFghKM7:TR?= M1LwZXNCVkeHUh?=
LB771-HNC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfWZ25SUUN3ME2wMlg{OTB2IDFOwG0> MV7TRW5ITVJ?
OC-314 M3HVe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHRZXJKSzVyPUCuPFY6PjViIN88US=> M{KzXHNCVkeHUh?=
MLMA Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHsTWxKSzVyPUCuPVA3PzViIN88US=> M2TBZXNCVkeHUh?=
KARPAS-45 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwOUK0OlYhKM7:TR?= MYfTRW5ITVJ?
CAL-27 NV7hSIt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzQTWM2OD1yLkmyPVA3KCEQvF2= NFq5c4lUSU6JRWK=
SK-NEP-1 M3j4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\rZWlEPTB;MD65O|I1QCBizszN NU\QSHRsW0GQR1XS
COR-L105 NUe0R|BwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfRe2ZKSzVyPUGuNFA{QTRiIN88US=> NY[zW5B7W0GQR1XS
TI-73 NHfTbZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDHbFBKSzVyPUGuNFE3PSBizszN Mk\mV2FPT0WU
JVM-3 NWjkeVV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfDZXlRUUN3ME2xMlA2ODF5IDFOwG0> MnjVV2FPT0WU
HAL-01 M4LRS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjBVpRKSzVyPUGuNFg5OSBizszN NWi2OVIyW0GQR1XS
QIMR-WIL NV7ZNIdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknsTWM2OD1zLkC5NFU5KCEQvF2= MmjSV2FPT0WU
HSC-3 NGXxZ5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXldo9XUUN3ME2xMlEyPzh|IDFOwG0> NY\tNpd4W0GQR1XS
KY821 M2W3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2joZWlEPTB;MT6xN|M2OSBizszN NWTEVotsW0GQR1XS
5637 NI\OXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnObGQzUUN3ME2xMlE{QDB|IDFOwG0> NVHBR5luW0GQR1XS
CAL-33 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTFwMUmzNFIhKM7:TR?= M{D3VXNCVkeHUh?=
ES4 M3y1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILzSZRKSzVyPUGuNlA4QSBizszN NYfnVFljW0GQR1XS
BHY MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XIfWlEPTB;MT6yNlg6OiBizszN M3fzRXNCVkeHUh?=
LB1047-RCC NIW4b29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTFwMkO3PFUhKM7:TR?= MYfTRW5ITVJ?
H4 NEL5RnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFwMkSyOVUhKM7:TR?= MnrtV2FPT0WU
RPMI-8866 NXnzR3hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTFwMk[xNFYhKM7:TR?= NXzndploW0GQR1XS
HO-1-N-1 NHu2VppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37xcWlEPTB;MT6yOlM3QSBizszN M4TycHNCVkeHUh?=
BB30-HNC MlTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDjRlAxUUN3ME2xMlI5PzF2IDFOwG0> NYDIZVM1W0GQR1XS
PC-14 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjNV4c2UUN3ME2xMlI6OjB3IDFOwG0> NXTm[2JoW0GQR1XS
NUGC-3 NHLUeWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\oWGlEPTB;MT6yPVM2PiBizszN NH:0dJlUSU6JRWK=
A4-Fuk NGrQNI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXUToxmUUN3ME2xMlMxPzB2IDFOwG0> M1XZVnNCVkeHUh?=
MHH-NB-11 MnPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDiXVlvUUN3ME2xMlMyOzh|IDFOwG0> MYDTRW5ITVJ?
KOSC-2 NEjpNXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFwM{G3O|UhKM7:TR?= Mn;wV2FPT0WU
A498 NEi0fFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlftTWM2OD1zLkSwNVE{KCEQvF2= NVKwTphWW0GQR1XS
KG-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TxV2lEPTB;MT60NVI4OyBizszN MkLMV2FPT0WU
DEL MlLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nBdmlEPTB;MT60N|Y2PyBizszN M1LIU3NCVkeHUh?=
EW-16 MoDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIS3TFRKSzVyPUGuOFM6PzNiIN88US=> MonGV2FPT0WU
BPH-1 M4fKcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmn3TWM2OD1zLkS0PFA2KCEQvF2= MkmzV2FPT0WU
JAR M3r0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTFwNEmzOkAh|ryP NEnCWVdUSU6JRWK=
J-RT3-T3-5 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\uOmlEPTB;MT61NVczOiBizszN Mn;JV2FPT0WU
A375 NV;yVnVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnadFVuUUN3ME2xMlUyPzd{IDFOwG0> NEHrb|RUSU6JRWK=
SW954 NXXRSm1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHwXHZKSzVyPUGuOVUxODdiIN88US=> M37jR3NCVkeHUh?=
Ca9-22 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFwNU[yOkAh|ryP MVvTRW5ITVJ?
D-566MG MlruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17kWWlEPTB;MT61O|E2PSBizszN M2jtPXNCVkeHUh?=
SCC-15 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTFwNkG4NFQhKM7:TR?= MU\TRW5ITVJ?
HD-MY-Z NIPoblNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PsTGlEPTB;MT62N|U5PCBizszN MUjTRW5ITVJ?
HT-1376 M{DScmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTHN4lKSzVyPUGuOlQ{PiBizszN NHGwcVlUSU6JRWK=
CAL-54 NXvRNIpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG3TWM2OD1zLk[1O|A6KCEQvF2= NVPrcFBxW0GQR1XS
ONS-76 M3O5V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf2VYlKSzVyPUGuOlc2PTFiIN88US=> MlHkV2FPT0WU
EFO-27 NEXHO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{L1U2lEPTB;MT62PFkzKCEQvF2= M1PwT3NCVkeHUh?=
769-P NVXoUm86T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3KzWmlEPTB;MT62PVU6PiBizszN NFmxNmlUSU6JRWK=
MV-4-11 MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHuWWhmUUN3ME2xMlY6QDV4IDFOwG0> MoDUV2FPT0WU
NKM-1 NELqRnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzMSlZKSzVyPUGuO|E5ODJiIN88US=> NX3EcG9HW0GQR1XS
LOXIMVI NWHl[pY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rvXGlEPTB;MT63OFU6QSBizszN NFrVcZRUSU6JRWK=
KYSE-140 MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT0bmRYUUN3ME2xMlc2PjV3IDFOwG0> M4PTfnNCVkeHUh?=
ES5 NXjOUFQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLyTWM2OD1zLki2O|Q4KCEQvF2= Ml7oV2FPT0WU
BB65-RCC NV;oUFVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTkR2lKSzVyPUGuPFk5PDliIN88US=> NIHZfJRUSU6JRWK=
HN MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fhNWlEPTB;MT64PVg4PCBizszN NXjCe5lxW0GQR1XS
A101D M{fRXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HLN2lEPTB;MT65N|YzQCBizszN M3rme3NCVkeHUh?=
LoVo MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3vfY1KSzVyPUGuPVc3PzliIN88US=> NUiydHBzW0GQR1XS
NCI-H526 NWT6[3h4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTFwOUmzNlUhKM7:TR?= MXjTRW5ITVJ?
NCI-H1693 M{XnRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3y5PWlEPTB;MT65PVg5QCBizszN NXSxe41sW0GQR1XS
OVCAR-4 NWnIWIt5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzmPZVKSzVyPUKuNFA1OzViIN88US=> Mk\KV2FPT0WU
SK-HEP-1 M4SyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLCTWM2OD1{LkCwO|Q2KCEQvF2= MWnTRW5ITVJ?
C2BBe1 NYH1Xo9PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3xV3JuUUN3ME2yMlA{Ozd{IDFOwG0> MWfTRW5ITVJ?
MEL-JUSO MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXGTWM2OD1{LkC0OFY1KCEQvF2= MXHTRW5ITVJ?
MOLT-16 M3HIOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jQe2lEPTB;Mj6wO|A2QCBizszN NFzveJNUSU6JRWK=
NBsusSR NF;GRotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTJwMEm4PFkhKM7:TR?= MlXMV2FPT0WU
TK10 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfpTWM2OD1{LkGzOFU5KCEQvF2= MUHTRW5ITVJ?
CAL-39 NX3keJdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\NcpZKSzVyPUKuNVQ1QCBizszN M13mWHNCVkeHUh?=
NCI-H2030 MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPRbZFKSzVyPUKuNVg6PzNiIN88US=> M1nUOXNCVkeHUh?=
HCT-116 NWnYXZRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:3UHhmUUN3ME2yMlIzQTh2IDFOwG0> MVrTRW5ITVJ?
HTC-C3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\NTWM2OD1{LkK2PFI1KCEQvF2= NY\6UXZ[W0GQR1XS
TYK-nu MkDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37ycGlEPTB;Mj6zNFkxQSBizszN NGjLUJVUSU6JRWK=
FADU NEnqdWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGK5RlZKSzVyPUKuN|IzQTZiIN88US=> NYrmWFZTW0GQR1XS
A431 NIraUohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnRTWM2OD1{LkO3NFI2KCEQvF2= MonEV2FPT0WU
TE-11 NVjMPIZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zZb2lEPTB;Mj6zPFAyQSBizszN MYfTRW5ITVJ?
CAL-12T M2LpZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmK3TWM2OD1{LkSwOFE4KCEQvF2= MoDXV2FPT0WU
DB NEjLeHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf5TWM2OD1{LkSyPFY6KCEQvF2= MnnlV2FPT0WU
L-363 NUj0e45pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LJSWlEPTB;Mj60N|UxPyBizszN NWLXeFdUW0GQR1XS
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NCI-H69 NUXzPXN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTNyLk[wPVMhKM7:TR?= MoT5V2FPT0WU
NB6 M2LPc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTPTWM2OD1|MT6zOlI6KCEQvF2= MYLTRW5ITVJ?
CAL-120 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP5NFZKSzVyPUOyMlQ{OTdiIN88US=> MmjYV2FPT0WU
U-87-MG MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXIeoR4UUN3ME2zN{4xOjVzIDFOwG0> NUDXT4NXW0GQR1XS
NCI-H1304 M{jVdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTN|LkCzOVQhKM7:TR?= MmCxV2FPT0WU
YH-13 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTkTWM2OD1|Mz6yOVM2KCEQvF2= M1nxPHNCVkeHUh?=
RMG-I NGLyOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF76S21KSzVyPUOzMlQzQDViIN88US=> M{XJTHNCVkeHUh?=
LU-65 M2fQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTN2LkG0NFghKM7:TR?= NGPsOnZUSU6JRWK=
GB-1 NFPW[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV64TXJjUUN3ME2zOU4xPzJ7IDFOwG0> MorjV2FPT0WU
DU-4475 NU\KfGZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LQOWlEPTB;M{WuNVU2OyBizszN M{HSNHNCVkeHUh?=
SBC-5 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL6cpRQUUN3ME2zOk42QTB{IDFOwG0> MVnTRW5ITVJ?
OE33 NGDH[2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPsO5hKSzVyPUO3Mlc2PzdiIN88US=> MoLWV2FPT0WU
C8166 M2POZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT2TWM2OD1|OD61NlY4KCEQvF2= NIL0VnVUSU6JRWK=
COLO-684 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\JTWM2OD1|OD63OFI5KCEQvF2= NHfVTGFUSU6JRWK=
NCI-H1155 MonQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTN7LkC0O|EhKM7:TR?= M1W1fnNCVkeHUh?=
ATN-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTN7Lke3PVIhKM7:TR?= NFjlUldUSU6JRWK=
KARPAS-299 NHjnNW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\4U2lEPTB;M{muPFM6KCEQvF2= NGr5TJZUSU6JRWK=
KNS-81-FD M2nvfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTRyLkO2NFQhKM7:TR?= MXrTRW5ITVJ?
NCI-H1563 NUXpTW1OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33CVGlEPTB;NEGuOVA{QSBizszN NFrTeYFUSU6JRWK=
NB14 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj5U3VKSzVyPUSyMlczPjNiIN88US=> M2K1enNCVkeHUh?=
COLO-800 NHi5OWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTR{Lki1NVchKM7:TR?= MoTWV2FPT0WU
MS-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rDWWlEPTB;NEOuNFQ5OyBizszN M32xO3NCVkeHUh?=
OVCAR-8 NHnxTm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTDWZVKSzVyPUSzMlY5ODliIN88US=> MYjTRW5ITVJ?
SK-PN-DW M1Tj[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTR|Lki3O|YhKM7:TR?= M2DVbXNCVkeHUh?=
G-402 NXnVWlZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fGS2lEPTB;NEOuPVAxPiBizszN NXzWb4N[W0GQR1XS
NCI-H2291 NHT5bZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfVZ4hKSzVyPUS0MlgxOTdiIN88US=> MXHTRW5ITVJ?
PC-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;nTGVDUUN3ME20OU45ODJ|IDFOwG0> NGnJWIdUSU6JRWK=
NCI-H1581 M3vKcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTR3Lkm4PFkhKM7:TR?= NUjnXVVUW0GQR1XS
SW1116 MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP0S2lKSzVyPUS3MlAyQDJiIN88US=> MWnTRW5ITVJ?
ZR-75-30 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LHOWlEPTB;NEeuNFI{QSBizszN M3zxenNCVkeHUh?=
OCI-AML2 M{ixXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXCTWM2OD12Nz6wPVE5KCEQvF2= NWDRSldjW0GQR1XS
MDA-MB-231 MnjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX32eWNHUUN3ME20O{43OjR7IDFOwG0> NEmzTHpUSU6JRWK=
ES3 NUe2bZM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHiTnNKSzVyPUS4MlM2OjliIN88US=> M{nLb3NCVkeHUh?=
NCI-H630 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULxcG5UUUN3ME20PU4yPzR{IDFOwG0> MWXTRW5ITVJ?
OE19 NHzNfW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jRcGlEPTB;NEmuNlkxOiBizszN NVLSS3llW0GQR1XS
NCI-H1573 NHvQb|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLKTWM2OD12OT62PFYyKCEQvF2= NFPVXIJUSU6JRWK=
EW-1 M2TQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP0TWM2OD12OT65NFg1KCEQvF2= NWnHTIVqW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively. [1] Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity. [2] As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts. [4]

Protocol

Kinase Assay:

[1]

+ Expand

The Src and Abl kinase assays:

The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution.
Cell Research:

[2]

+ Expand
  • Cell lines: Abl-MLV, Rat 2, KU812, K562, and MEG-01 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~1 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are exposed to various concentrations of Bosutinib for 72 hours. Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts is measured in 96-well ultra-low binding plates treated with Sigmacote to block residual cell attachment. Cell proliferation is measured with MTS or Cell-Glo. For the determination of cell cycle or cell death, cells are prepared for FACS analysis in the CycleTest Plus DNA reagent kit and analyzed on a fluorescence-activated cell sorter flow cytometer.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: Nude female mice injected with K562 cells
  • Formulation: Suspended in 0.5% methocel/0.4% Tween 80
  • Dosages: ~150 mg/kg/day
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.51 mM)
Ethanol 2 mg/mL (3.77 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 530.45
Formula

C26H29Cl2N5O3

CAS No. 380843-75-4
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • 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):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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.

Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID