Bosutinib (SKI-606)

Licensed by Pfizer Catalog No.S1014

Bosutinib (SKI-606) Chemical Structure

Molecular Weight(MW): 530.45

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.

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4 Customer Reviews

  • A,IC50 of Bosutinib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. The effect of inhibitors is presented as the percentage of ANDV-induced permeability of inhibitor-treated monolayers 3 days postinfection and 30 min post-VEGF and FITC-dextran addition. B, VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for Fig. 1 at indicated times in the presence or absence of Bosutinib .

    J Virol 2011 85, 2296–2303. Bosutinib (SKI-606) purchased from Selleck.

    Both parental and HR cell lines were treated with bosutinib (0.01, 0.1, and 1 μmol/L) for 24 hours. Src-related signaling pathway molecules were then analyzed.

    Mol Cancer Ther, 2017. Bosutinib (SKI-606) purchased from Selleck.

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

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

    Rescue ofPKAand tyrosine phosphorylation by Ser/Thr phosphatase inhibitors. A and B, spermwere incubated in capacitating medium supplemented with SFK inhibitors and different concentrations of okadaic acid (OA) (A) or calyculin-A (B), before immunodetection of p-PKA substrates (clone 100G7E). C and D, PVDF membranes used in A and B were stripped as described and used for Western blot immunodetection with anti-PY antibodies (clone 4G10).

    Dr. Pablo E.Visconti from University of Massachusetts. Bosutinib (SKI-606) purchased from Selleck.

Purity & Quality Control

Choose Selective Src Inhibitors

Biological Activity

Description Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.
Targets
Abl [2]
(Cell-free assay)
Src [1]
(Cell-free assay)
1 nM 1.2 nM
In vitro

Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM. [1] Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation. [2] Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB7 NVO4[Vc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjMT3pKSzVyPUCuNFgzOzFiIN88US=> MoHIV2FPT0WU
SW756 M{nhbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmriTWM2OD1yLkG0NFI1KCEQvF2= NX:yO2R[W0GQR1XS
CTV-1 NGDpTZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17BcWlEPTB;MD6xOlM6QCBizszN MlHlV2FPT0WU
HSC-4 NXSxZmFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\RVJBLUUN3ME2wMlE4OTV6IDFOwG0> MX\TRW5ITVJ?
LAMA-84 M2LwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S1VGlEPTB;MD6yPFY3PCBizszN MkfHV2FPT0WU
KU812 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PSU2lEPTB;MD6zOFA3QCBizszN NF7vWnBUSU6JRWK=
HCC1806 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELtW5JKSzVyPUCuN|UzOTZiIN88US=> NIH5NIpUSU6JRWK=
DOK MoroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrPTWM2OD1yLkO3O|g3KCEQvF2= M3KxdXNCVkeHUh?=
NCI-H209 NEOwc|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm2em5KSzVyPUCuOFA5ODhiIN88US=> M2Sx[nNCVkeHUh?=
EoL-1-cell NIXVPIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXUUYZKSzVyPUCuOFE2PzZiIN88US=> M3\ENHNCVkeHUh?=
H9 M{HYOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW3dWxKSzVyPUCuOFM1PjRiIN88US=> MW\TRW5ITVJ?
EM-2 Ml3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HjZWlEPTB;MD60N|g6KCEQvF2= NEDvPHlUSU6JRWK=
NCI-H292 MnzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4j4Z2lEPTB;MD60OFExQCBizszN NXrmN3dlW0GQR1XS
697 MnrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD5[29mUUN3ME2wMlQ2PjN|IDFOwG0> M2ftU3NCVkeHUh?=
BHT-101 M4XD[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPtPYlKSzVyPUCuOFY2QSBizszN M3LtfnNCVkeHUh?=
BE-13 M3PBXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPzXndzUUN3ME2wMlQ5PTd{IDFOwG0> M1TYXHNCVkeHUh?=
RS4-11 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXj0WHN5UUN3ME2wMlQ5PTh2IDFOwG0> NIWwOZhUSU6JRWK=
IGROV-1 M3\i[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnjd|drUUN3ME2wMlQ5Pzl5IDFOwG0> Mkm2V2FPT0WU
KE-37 MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjKTWM2OD1yLkS5OVA6KCEQvF2= MYLTRW5ITVJ?
BV-173 M1zXOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vwUWlEPTB;MD61NFc6OiBizszN NYPGNoRNW0GQR1XS
MEG-01 NHvvcVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3OTWM2OD1yLkWxNlE1KCEQvF2= Mon4V2FPT0WU
LB2241-RCC M1jJdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrNO5RpUUN3ME2wMlU{PzF6IDFOwG0> MY\TRW5ITVJ?
ACHN M4XPbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPtTWM2OD1yLkW0NFY6KCEQvF2= NYr2bW9VW0GQR1XS
CTB-1 MnH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwNUS4NkAh|ryP MYfTRW5ITVJ?
HT-1080 Mnq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwNUWzOFkhKM7:TR?= NXTMe3B[W0GQR1XS
CHL-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwNUW0OlUhKM7:TR?= M4PJcnNCVkeHUh?=
EW-3 NXi1VoFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TSd2lEPTB;MD61OVk{PSBizszN M1Gyc3NCVkeHUh?=
ES1 Ml7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;KXGlEPTB;MD62O|Q6QCBizszN MnH6V2FPT0WU
KASUMI-1 MmW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PlfmlEPTB;MD63NlM{KCEQvF2= MXLTRW5ITVJ?
SW13 MlHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjKfIJNUUN3ME2wMlc{Pzl6IDFOwG0> NED0O4RUSU6JRWK=
A3-KAW NEHzfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwN{myNFghKM7:TR?= NUXvfnRwW0GQR1XS
LB771-HNC NV\BO5R{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfDTWM2OD1yLkizNVA1KCEQvF2= MmXYV2FPT0WU
OC-314 MnXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXwNIhKSzVyPUCuPFY6PjViIN88US=> NE\nUZZUSU6JRWK=
MLMA M1e0dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M371[WlEPTB;MD65NFY4PSBizszN M{HvSXNCVkeHUh?=
KARPAS-45 NYnCe5VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXJ[JZ1UUN3ME2wMlkzPDZ4IDFOwG0> NWX5clQ2W0GQR1XS
CAL-27 M2Gwc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2G4e2lEPTB;MD65NlkxPiBizszN NFvMb2lUSU6JRWK=
SK-NEP-1 MoPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\NTpVKSzVyPUCuPVczPDhiIN88US=> MWXTRW5ITVJ?
COR-L105 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfkTWM2OD1zLkCwN|k1KCEQvF2= NFTSbFJUSU6JRWK=
TI-73 NWflR4pJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTFwMEG2OUAh|ryP NVXh[HdbW0GQR1XS
JVM-3 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f2VGlEPTB;MT6wOVAyPyBizszN NHnS[mRUSU6JRWK=
HAL-01 NUDQeo5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\OZWlEPTB;MT6wPFgyKCEQvF2= NF;pSWJUSU6JRWK=
QIMR-WIL MoHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXLT4lJUUN3ME2xMlA6ODV6IDFOwG0> MXvTRW5ITVJ?
HSC-3 NUf6eW5MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXjWo9qUUN3ME2xMlEyPzh|IDFOwG0> NVXVdGZJW0GQR1XS
KY821 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFwMUOzOVEhKM7:TR?= NUfJbWZLW0GQR1XS
5637 NUPqUJVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjIeo1GUUN3ME2xMlE{QDB|IDFOwG0> NVGwVodJW0GQR1XS
CAL-33 NIDxPZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1Lub2lEPTB;MT6xPVMxOiBizszN M16wdXNCVkeHUh?=
ES4 M1vQU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYryZ4RPUUN3ME2xMlIxPzliIN88US=> NXjhNZl{W0GQR1XS
BHY MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTFwMkK4PVIhKM7:TR?= M17icnNCVkeHUh?=
LB1047-RCC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLLTWM2OD1zLkKzO|g2KCEQvF2= M3XkW3NCVkeHUh?=
H4 NHvoNWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrte3pGUUN3ME2xMlI1OjV3IDFOwG0> NF7yXGRUSU6JRWK=
RPMI-8866 NGn6fWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUflTHR1UUN3ME2xMlI3OTB4IDFOwG0> MmXJV2FPT0WU
HO-1-N-1 MlL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn65TWM2OD1zLkK2N|Y6KCEQvF2= NEnIXJJUSU6JRWK=
BB30-HNC NGDXV4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwMki3NVQhKM7:TR?= NInC[oVUSU6JRWK=
PC-14 M1TKdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fNWmlEPTB;MT6yPVIxPSBizszN MV;TRW5ITVJ?
NUGC-3 NG\qWZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfwTWM2OD1zLkK5N|U3KCEQvF2= M1:zdnNCVkeHUh?=
A4-Fuk NWP3XlV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIizd4VKSzVyPUGuN|A4ODRiIN88US=> NX;PPWJPW0GQR1XS
MHH-NB-11 NF\obVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTFwM{GzPFMhKM7:TR?= M1HsOHNCVkeHUh?=
KOSC-2 M3P6Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXySGJKSzVyPUGuN|E4PzViIN88US=> Mo\nV2FPT0WU
A498 MmLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHvXYVKSzVyPUGuOFAyOTNiIN88US=> MVnTRW5ITVJ?
KG-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvx[ldKSzVyPUGuOFEzPzNiIN88US=> NF[2SoFUSU6JRWK=
DEL NYTIUms3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\ZU2ZKSzVyPUGuOFM3PTdiIN88US=> NHPvbGRUSU6JRWK=
EW-16 NV36[XhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwNEO5O|MhKM7:TR?= NX;3b4NZW0GQR1XS
BPH-1 Mk\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf0NVNKSzVyPUGuOFQ5ODViIN88US=> M2rjdnNCVkeHUh?=
JAR MoPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHq1UGhKSzVyPUGuOFk{PiBizszN MV7TRW5ITVJ?
J-RT3-T3-5 MkfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFy5dFdKSzVyPUGuOVE4OjJiIN88US=> M17JPXNCVkeHUh?=
A375 NX\qNWpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXYZXNoUUN3ME2xMlUyPzd{IDFOwG0> NGPzUYxUSU6JRWK=
SW954 NGDWZoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX5VXNPUUN3ME2xMlU2ODB5IDFOwG0> Ml7KV2FPT0WU
Ca9-22 M33VXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fVdWlEPTB;MT61OlI3KCEQvF2= Mn;UV2FPT0WU
D-566MG M2TpUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUey[lRwUUN3ME2xMlU4OTV3IDFOwG0> M3zGO3NCVkeHUh?=
SCC-15 NInpSnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTFwNkG4NFQhKM7:TR?= NYrXNnd4W0GQR1XS
HD-MY-Z NIHOTZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrCdWRKSzVyPUGuOlM2QDRiIN88US=> NV[xRnFCW0GQR1XS
HT-1376 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe4cVBmUUN3ME2xMlY1OzZiIN88US=> M33ke3NCVkeHUh?=
CAL-54 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3NfZNKSzVyPUGuOlU4ODliIN88US=> MXnTRW5ITVJ?
ONS-76 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TlcWlEPTB;MT62O|U2OSBizszN M4Ll[XNCVkeHUh?=
EFO-27 MlfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvQTWM2OD1zLk[4PVIhKM7:TR?= NH:4bmVUSU6JRWK=
769-P Mn:xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDoOpQ3UUN3ME2xMlY6PTl4IDFOwG0> NY\QdZlnW0GQR1XS
MV-4-11 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[5VldKSzVyPUGuOlk5PTZiIN88US=> MYXTRW5ITVJ?
NKM-1 NUi0S2d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3WyemlEPTB;MT63NVgxOiBizszN NEiyfXdUSU6JRWK=
LOXIMVI NFnEZXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3m2SGlEPTB;MT63OFU6QSBizszN NVPBXlY2W0GQR1XS
KYSE-140 NVfDfWVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfhZ2ZKSzVyPUGuO|U3PTViIN88US=> MmP3V2FPT0WU
ES5 M3;EfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XzO2lEPTB;MT64Olc1PyBizszN MW\TRW5ITVJ?
BB65-RCC M4fhW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\2TnBWUUN3ME2xMlg6QDR7IDFOwG0> M3PlTHNCVkeHUh?=
HN NFHKbWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzpTWM2OD1zLki5PFc1KCEQvF2= MVfTRW5ITVJ?
A101D M1naSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFwOUO2NlghKM7:TR?= Mn7TV2FPT0WU
LoVo M3jqRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXX5WJBYUUN3ME2xMlk4Pjd7IDFOwG0> M{KyOXNCVkeHUh?=
NCI-H526 NVTCWXZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTFwOUmzNlUhKM7:TR?= NEnzWlZUSU6JRWK=
NCI-H1693 MknrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFwOUm4PFghKM7:TR?= MWrTRW5ITVJ?
OVCAR-4 NYLIPIpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXGbHhKSzVyPUKuNFA1OzViIN88US=> NWPmfnl{W0GQR1XS
SK-HEP-1 NYfnU|U{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDtU4ZjUUN3ME2yMlAxPzR3IDFOwG0> MofCV2FPT0WU
C2BBe1 M1nSUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j4dGlEPTB;Mj6wN|M4OiBizszN NWnwNXppW0GQR1XS
MEL-JUSO MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG3VpRKSzVyPUKuNFQ1PjRiIN88US=> MUPTRW5ITVJ?
MOLT-16 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\oSGlEPTB;Mj6wO|A2QCBizszN NHex[ZpUSU6JRWK=
NBsusSR M1;nVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHPTIdKSzVyPUKuNFk5QDliIN88US=> MVTTRW5ITVJ?
TK10 MlS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn5c2RrUUN3ME2yMlE{PDV6IDFOwG0> NX;kc2dVW0GQR1XS
CAL-39 M1HrUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjW[I5KSzVyPUKuNVQ1QCBizszN MWHTRW5ITVJ?
NCI-H2030 M3Tyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vBPGlEPTB;Mj6xPFk4OyBizszN M{e4cnNCVkeHUh?=
HCT-116 NELnO4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTifpJQUUN3ME2yMlIzQTh2IDFOwG0> NYnpdoNKW0GQR1XS
HTC-C3 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG0NplKSzVyPUKuNlY5OjRiIN88US=> MWnTRW5ITVJ?
TYK-nu NWTNSmZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDsTWM2OD1{LkOwPVA6KCEQvF2= Ml3wV2FPT0WU
FADU MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S2cGlEPTB;Mj6zNlI6PiBizszN MYrTRW5ITVJ?
A431 NX\GVWVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJwM{ewNlUhKM7:TR?= MUnTRW5ITVJ?
TE-11 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDXdGlXUUN3ME2yMlM5ODF7IDFOwG0> M2ToU3NCVkeHUh?=
CAL-12T MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHy0blZKSzVyPUKuOFA1OTdiIN88US=> MVLTRW5ITVJ?
DB NIH1UlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\RUJpKSzVyPUKuOFI5PjliIN88US=> MoX4V2FPT0WU
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MC116 NFfjT3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;5XlMxUUN3ME2zNE4xPzN|IDFOwG0> MoTpV2FPT0WU
NCI-H69 MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPDN4t{UUN3ME2zNE43ODl|IDFOwG0> M{ey[nNCVkeHUh?=
NB6 NHTvd|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnQe2I2UUN3ME2zNU4{PjJ7IDFOwG0> NYnafI1NW0GQR1XS
CAL-120 M4PVemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LE[2lEPTB;M{KuOFMyPyBizszN MmfWV2FPT0WU
U-87-MG MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjsTWM2OD1|Mz6wNlUyKCEQvF2= NVK2NWVnW0GQR1XS
NCI-H1304 NUHueZJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LQNGlEPTB;M{OuNFM2PCBizszN NU\wbWp[W0GQR1XS
YH-13 MkLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrSXmsyUUN3ME2zN{4zPTN3IDFOwG0> MYLTRW5ITVJ?
RMG-I MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTN|LkSyPFUhKM7:TR?= M1e5[HNCVkeHUh?=
LU-65 M3P1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFu4TG9KSzVyPUO0MlE1ODhiIN88US=> NWi5[G1FW0GQR1XS
GB-1 NIHH[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7vc5BlUUN3ME2zOU4xPzJ7IDFOwG0> NVe5VIdYW0GQR1XS
DU-4475 NUC4NHlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2noNmlEPTB;M{WuNVU2OyBizszN NEW5e4ZUSU6JRWK=
SBC-5 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTlfpNKSzVyPUO2MlU6ODJiIN88US=> M2TYPXNCVkeHUh?=
OE33 MnXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;aTWM2OD1|Nz63OVc4KCEQvF2= NFnaRoVUSU6JRWK=
C8166 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTN6LkWyOlchKM7:TR?= NYTUe|hCW0GQR1XS
COLO-684 M1vxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjsR3Y5UUN3ME2zPE44PDJ6IDFOwG0> MnXNV2FPT0WU
NCI-H1155 MnP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTN7LkC0O|EhKM7:TR?= MUHTRW5ITVJ?
ATN-1 M3vYTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1P6NWlEPTB;M{muO|c6OiBizszN NWPITldYW0GQR1XS
KARPAS-299 M3\tfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPHNVlwUUN3ME2zPU45OzliIN88US=> M3PrTHNCVkeHUh?=
KNS-81-FD NWezUnZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfLTWM2OD12MD6zOlA1KCEQvF2= MofmV2FPT0WU
NCI-H1563 NGnDO41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPBTWM2OD12MT61NFM6KCEQvF2= NGnUSpBUSU6JRWK=
NB14 M3;IfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPMWXJKSzVyPUSyMlczPjNiIN88US=> MoCwV2FPT0WU
COLO-800 M1faN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\zTWM2OD12Mj64OVE4KCEQvF2= M4nrNnNCVkeHUh?=
MS-1 M4HmVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITBdHlKSzVyPUSzMlA1QDNiIN88US=> NVXhR5FlW0GQR1XS
OVCAR-8 M3K5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjzdI5KSzVyPUSzMlY5ODliIN88US=> NWnpTWdQW0GQR1XS
SK-PN-DW MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYqzeplzUUN3ME20N{45Pzd4IDFOwG0> MWTTRW5ITVJ?
G-402 M1z1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;tNZdKSzVyPUSzMlkxODZiIN88US=> NX7FdWtoW0GQR1XS
NCI-H2291 NEO5VmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7KRphKSzVyPUS0MlgxOTdiIN88US=> MWjTRW5ITVJ?
PC-3 NGTaPHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTR3LkiwNlMhKM7:TR?= M{e1NHNCVkeHUh?=
NCI-H1581 M3jnOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfTR5JKSzVyPUS1Mlk5QDliIN88US=> MmTrV2FPT0WU
SW1116 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXTR5Z5UUN3ME20O{4xOTh{IDFOwG0> NVP2cY1lW0GQR1XS
ZR-75-30 M1S1W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELESItKSzVyPUS3MlAzOzliIN88US=> NUG5OllsW0GQR1XS
OCI-AML2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jkUGlEPTB;NEeuNFkyQCBizszN NXjOW404W0GQR1XS
MDA-MB-231 NGPKe3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIq1R2RKSzVyPUS3MlYzPDliIN88US=> MVrTRW5ITVJ?
ES3 NHOyN|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTDTWM2OD12OD6zOVI6KCEQvF2= NH62eoVUSU6JRWK=
NCI-H630 NETIfJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXj6XHhzUUN3ME20PU4yPzR{IDFOwG0> MkXZV2FPT0WU
OE19 NX\Vdox7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTR7LkK5NFIhKM7:TR?= NWDaVXdoW0GQR1XS
NCI-H1573 MnTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTR7Lk[4OlEhKM7:TR?= MkPIV2FPT0WU
EW-1 MkjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\2TWM2OD12OT65NFg1KCEQvF2= M2HPV3NCVkeHUh?=

... Click to View More Cell Line Experimental Data

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

Protocol

Kinase Assay:

[1]

+ Expand

The Src and Abl kinase assays:

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

[2]

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

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


    (Only for Reference)
Animal Research:

[2]

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.51 mM)
Ethanol 2 mg/mL (3.77 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/mL

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

Chemical Information

Molecular Weight 530.45
Formula

C26H29Cl2N5O3

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

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

Dilution Calculator

Dilution Calculator

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

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

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

  • C1
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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.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Can I give S1014 Bosutinib to mice by oral gavage? If so, how to dissolve the drug?

  • Answer:

    For oral gavage, S1014 Bosutinib can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID