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 NVPpVGp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwMEiyN|EhKM7:TR?= MoW2V2FPT0WU
SW756 MmnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzCTWM2OD1yLkG0NFI1KCEQvF2= M{fMOHNCVkeHUh?=
CTV-1 M4focGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL6N2tKSzVyPUCuNVY{QThiIN88US=> NXPjO3NRW0GQR1XS
HSC-4 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fISGlEPTB;MD6xO|E2QCBizszN MUfTRW5ITVJ?
LAMA-84 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLCV2xKSzVyPUCuNlg3PjRiIN88US=> NILhVXZUSU6JRWK=
KU812 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWyTWM2OD1yLkO0NFY5KCEQvF2= MYjTRW5ITVJ?
HCC1806 NEfGRXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn6zTWM2OD1yLkO1NlE3KCEQvF2= MVPTRW5ITVJ?
DOK M13LVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwM{e3PFYhKM7:TR?= NIHsNo1USU6JRWK=
NCI-H209 M4TqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorMTWM2OD1yLkSwPFA5KCEQvF2= MlrzV2FPT0WU
EoL-1-cell NUPme4JPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwNEG1O|YhKM7:TR?= NWKyZVNCW0GQR1XS
H9 Mn7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXnT4dJUUN3ME2wMlQ{PDZ2IDFOwG0> NFrPSnpUSU6JRWK=
EM-2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfzTWM2OD1yLkSzPFkhKM7:TR?= NGfid5NUSU6JRWK=
NCI-H292 M3X0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHRTWM2OD1yLkS0NVA5KCEQvF2= NF;OTWRUSU6JRWK=
697 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\YWGlEPTB;MD60OVY{OyBizszN MWPTRW5ITVJ?
BHT-101 M2m5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf0TWM2OD1yLkS2OVkhKM7:TR?= MlHLV2FPT0WU
BE-13 NVvDNFlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3iwSWlEPTB;MD60PFU4OiBizszN Mn;OV2FPT0WU
RS4-11 MkTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jSXWlEPTB;MD60PFU5PCBizszN MnmxV2FPT0WU
IGROV-1 NIfOd|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HFcmlEPTB;MD60PFc6PyBizszN MVXTRW5ITVJ?
KE-37 MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki4TWM2OD1yLkS5OVA6KCEQvF2= MnPUV2FPT0WU
BV-173 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;SUVJKSzVyPUCuOVA4QTJiIN88US=> NXXtcIlVW0GQR1XS
MEG-01 NXXGNphqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHqemo{UUN3ME2wMlUyOjF2IDFOwG0> MYLTRW5ITVJ?
LB2241-RCC NEn6PIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzIbJNKSzVyPUCuOVM4OThiIN88US=> NHuybHRUSU6JRWK=
ACHN NYjKNlRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELpS3pKSzVyPUCuOVQxPjliIN88US=> MYjTRW5ITVJ?
CTB-1 NGjCVYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\mTWM2OD1yLkW0PFIhKM7:TR?= NFrXRWlUSU6JRWK=
HT-1080 NUS2OlhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fFVWlEPTB;MD61OVM1QSBizszN NXOwXHFJW0GQR1XS
CHL-1 M3;pNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfUdZY5UUN3ME2wMlU2PDZ3IDFOwG0> NGXJ[mlUSU6JRWK=
EW-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXCTWM2OD1yLkW1PVM2KCEQvF2= MnfTV2FPT0WU
ES1 NUToeYhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwNke0PVghKM7:TR?= MXzTRW5ITVJ?
KASUMI-1 NXftUINbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPGTWM2OD1yLkeyN|MhKM7:TR?= MVnTRW5ITVJ?
SW13 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwN{O3PVghKM7:TR?= M1TqTnNCVkeHUh?=
A3-KAW MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDHTXJKSzVyPUCuO|kzODhiIN88US=> MnG1V2FPT0WU
LB771-HNC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\U[IlKSzVyPUCuPFMyODRiIN88US=> NEHKcGVUSU6JRWK=
OC-314 NILKfYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLpSZBKSzVyPUCuPFY6PjViIN88US=> NV\uTm5FW0GQR1XS
MLMA NUTKVXZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnTTWM2OD1yLkmwOlc2KCEQvF2= NWG4b2tXW0GQR1XS
KARPAS-45 NFrXRmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwOUK0OlYhKM7:TR?= MkLlV2FPT0WU
CAL-27 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwOUK5NFYhKM7:TR?= Mkm5V2FPT0WU
SK-NEP-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwOUeyOFghKM7:TR?= NWP3UoFbW0GQR1XS
COR-L105 MlznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFwMECzPVQhKM7:TR?= NFHEUI9USU6JRWK=
TI-73 MmfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HOdWlEPTB;MT6wNVY2KCEQvF2= Mny3V2FPT0WU
JVM-3 NETUXXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;1RWlEPTB;MT6wOVAyPyBizszN MnvJV2FPT0WU
HAL-01 NGjYTlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPifoRKSzVyPUGuNFg5OSBizszN MoHtV2FPT0WU
QIMR-WIL NEL5SYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHQ[I5sUUN3ME2xMlA6ODV6IDFOwG0> M{fW[HNCVkeHUh?=
HSC-3 M{i5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDSWoVKSzVyPUGuNVE4QDNiIN88US=> MWrTRW5ITVJ?
KY821 MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFwMUOzOVEhKM7:TR?= M{H0cnNCVkeHUh?=
5637 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTFwMUO4NFMhKM7:TR?= MljjV2FPT0WU
CAL-33 M2\qb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTFwMUmzNFIhKM7:TR?= MkO4V2FPT0WU
ES4 NULHNVYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7KeYpCUUN3ME2xMlIxPzliIN88US=> MUjTRW5ITVJ?
BHY MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDZTYRuUUN3ME2xMlIzQDl{IDFOwG0> M1rWXXNCVkeHUh?=
LB1047-RCC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWr3TJBJUUN3ME2xMlI{Pzh3IDFOwG0> NXLaUIJiW0GQR1XS
H4 NV;4PI8{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjyTWM2OD1zLkK0NlU2KCEQvF2= M{TUNnNCVkeHUh?=
RPMI-8866 Mor4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXrfo5NUUN3ME2xMlI3OTB4IDFOwG0> NI[zZVFUSU6JRWK=
HO-1-N-1 M2L2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrJTWM2OD1zLkK2N|Y6KCEQvF2= MYjTRW5ITVJ?
BB30-HNC MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTFwMki3NVQhKM7:TR?= NHT0[FZUSU6JRWK=
PC-14 NEPtV4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnnTWM2OD1zLkK5NlA2KCEQvF2= NFfpem5USU6JRWK=
NUGC-3 MoTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXDSYxKUUN3ME2xMlI6OzV4IDFOwG0> MYjTRW5ITVJ?
A4-Fuk M1zKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7VTGFmUUN3ME2xMlMxPzB2IDFOwG0> NIrsdnFUSU6JRWK=
MHH-NB-11 NVrmSYV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTFwM{GzPFMhKM7:TR?= MlHwV2FPT0WU
KOSC-2 M4\FR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LpfmlEPTB;MT6zNVc4PSBizszN M4LJSnNCVkeHUh?=
A498 Mk\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofUTWM2OD1zLkSwNVE{KCEQvF2= MlPPV2FPT0WU
KG-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvaR494UUN3ME2xMlQyOjd|IDFOwG0> Mn;NV2FPT0WU
DEL NGjNfXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXxdIdKUUN3ME2xMlQ{PjV5IDFOwG0> MUnTRW5ITVJ?
EW-16 MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1myOGlEPTB;MT60N|k4OyBizszN NV:5cJZKW0GQR1XS
BPH-1 NWXiWG1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TmNmlEPTB;MT60OFgxPSBizszN M4PuVXNCVkeHUh?=
JAR M3\MWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XR[mlEPTB;MT60PVM3KCEQvF2= M{j2NXNCVkeHUh?=
J-RT3-T3-5 NXPyW4FlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHIXHFKSzVyPUGuOVE4OjJiIN88US=> MonFV2FPT0WU
A375 MmPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLF[YJkUUN3ME2xMlUyPzd{IDFOwG0> NEXLVphUSU6JRWK=
SW954 M{Ppd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3UPWlKSzVyPUGuOVUxODdiIN88US=> MWDTRW5ITVJ?
Ca9-22 NVzJWm9MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn4OFJxUUN3ME2xMlU3OjZiIN88US=> NX\6SHBuW0GQR1XS
D-566MG MmDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFwNUexOVUhKM7:TR?= MnXzV2FPT0WU
SCC-15 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFwNkG4NFQhKM7:TR?= NIq4b|lUSU6JRWK=
HD-MY-Z Mn;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTFwNkO1PFQhKM7:TR?= MXnTRW5ITVJ?
HT-1376 NFSyT2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTOW2xLUUN3ME2xMlY1OzZiIN88US=> M3u0RnNCVkeHUh?=
CAL-54 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXsTWM2OD1zLk[1O|A6KCEQvF2= NHXRS3NUSU6JRWK=
ONS-76 NHTaW4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXDV|BKSzVyPUGuOlc2PTFiIN88US=> NYTDbWpGW0GQR1XS
EFO-27 NFvvcoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHu0UIdKSzVyPUGuOlg6OiBizszN MULTRW5ITVJ?
769-P NXfMWIFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PKZ2lEPTB;MT62PVU6PiBizszN NH70UFhUSU6JRWK=
MV-4-11 NHHiTnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTVTndEUUN3ME2xMlY6QDV4IDFOwG0> NFTm[4VUSU6JRWK=
NKM-1 NW\IbXp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzieVVKSzVyPUGuO|E5ODJiIN88US=> NI\VfpJUSU6JRWK=
LOXIMVI NWfhdGZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnRdXdVUUN3ME2xMlc1PTl7IDFOwG0> NILUeVBUSU6JRWK=
KYSE-140 MmjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LqTmlEPTB;MT63OVY2PSBizszN NV3GdW1wW0GQR1XS
ES5 MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYG3e2VFUUN3ME2xMlg3PzR5IDFOwG0> MX3TRW5ITVJ?
BB65-RCC NIPM[3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFwOEm4OFkhKM7:TR?= NWjsNlh4W0GQR1XS
HN MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFwOEm4O|QhKM7:TR?= MVLTRW5ITVJ?
A101D MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE[3OIZKSzVyPUGuPVM3OjhiIN88US=> NGnYWWVUSU6JRWK=
LoVo MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DXOGlEPTB;MT65O|Y4QSBizszN NFfTW3RUSU6JRWK=
NCI-H526 NYOxdFdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLjTWM2OD1zLkm5N|I2KCEQvF2= NEjBPItUSU6JRWK=
NCI-H1693 MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPzSZBwUUN3ME2xMlk6QDh6IDFOwG0> NX3nUpp2W0GQR1XS
OVCAR-4 NHfCUJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJwMEC0N|UhKM7:TR?= MXvTRW5ITVJ?
SK-HEP-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3ITWM2OD1{LkCwO|Q2KCEQvF2= M2LqVXNCVkeHUh?=
C2BBe1 NUTWeHRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHlRWZmUUN3ME2yMlA{Ozd{IDFOwG0> MmrlV2FPT0WU
MEL-JUSO MoL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzSdGpKSzVyPUKuNFQ1PjRiIN88US=> NFvVSpZUSU6JRWK=
MOLT-16 M2HNfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrRWGhKSzVyPUKuNFcxPThiIN88US=> NITie3ZUSU6JRWK=
NBsusSR M1L3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HZOmlEPTB;Mj6wPVg5QSBizszN MXLTRW5ITVJ?
TK10 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXDdWZKSzVyPUKuNVM1PThiIN88US=> MWPTRW5ITVJ?
CAL-39 M2jqN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTJwMUS0PEAh|ryP MYDTRW5ITVJ?
NCI-H2030 NX;JZol7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HoR2lEPTB;Mj6xPFk4OyBizszN MXvTRW5ITVJ?
HCT-116 MmLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq5cIluUUN3ME2yMlIzQTh2IDFOwG0> Ml7VV2FPT0WU
HTC-C3 NGm4d2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPMTWM2OD1{LkK2PFI1KCEQvF2= M4frOHNCVkeHUh?=
TYK-nu NGTtelVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTj[lVNUUN3ME2yMlMxQTB7IDFOwG0> MWnTRW5ITVJ?
FADU NIHPNIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjYNFhkUUN3ME2yMlMzOjl4IDFOwG0> NX7Bcnd1W0GQR1XS
A431 MkjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTQTWM2OD1{LkO3NFI2KCEQvF2= NYDDWncyW0GQR1XS
TE-11 NYP5UVNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfSTWM2OD1{LkO4NFE6KCEQvF2= M4PWPXNCVkeHUh?=
CAL-12T M{DvWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjjUVdQUUN3ME2yMlQxPDF5IDFOwG0> MmHuV2FPT0WU
DB M13IR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnizTWM2OD1{LkSyPFY6KCEQvF2= NGfmOphUSU6JRWK=
L-363 NVzLWWdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzMOJNKSzVyPUKuOFM2ODdiIN88US=> NES0PGhUSU6JRWK=
MSTO-211H NGLCVXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nzc2lEPTB;Mj62OlM6OSBizszN M2L3W3NCVkeHUh?=
SK-UT-1 NHjOdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnH[nRyUUN3ME2yMlcyPDB4IDFOwG0> M1rSRnNCVkeHUh?=
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NCI-H69 NUTzcVdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LVd2lEPTB;M{CuOlA6OyBizszN MX;TRW5ITVJ?
NB6 M4[3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTNzLkO2NlkhKM7:TR?= MnzrV2FPT0WU
CAL-120 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjRdpFKSzVyPUOyMlQ{OTdiIN88US=> MVjTRW5ITVJ?
U-87-MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTN|LkCyOVEhKM7:TR?= MU\TRW5ITVJ?
NCI-H1304 NWH0VYd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnufG9KSzVyPUOzMlA{PTRiIN88US=> NE\3c4NUSU6JRWK=
YH-13 NX7xOYhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnu2TWM2OD1|Mz6yOVM2KCEQvF2= NHHmXJdUSU6JRWK=
RMG-I M{fYUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTN|LkSyPFUhKM7:TR?= M{XBUnNCVkeHUh?=
LU-65 M2K2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTN2LkG0NFghKM7:TR?= M2THTHNCVkeHUh?=
GB-1 M4judmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3WWolKSzVyPUO1MlA4OjliIN88US=> Mo\oV2FPT0WU
DU-4475 NYfx[4tZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTN3LkG1OVMhKM7:TR?= NE\KUHhUSU6JRWK=
SBC-5 NHz2[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPWO4h{UUN3ME2zOk42QTB{IDFOwG0> MXPTRW5ITVJ?
OE33 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTN5Lke1O|chKM7:TR?= MYHTRW5ITVJ?
C8166 MnLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnm[|FKSzVyPUO4MlUzPjdiIN88US=> NYDsRXdHW0GQR1XS
COLO-684 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkO3TWM2OD1|OD63OFI5KCEQvF2= NX3V[WtJW0GQR1XS
NCI-H1155 NXq5bIZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrPZWVzUUN3ME2zPU4xPDdzIDFOwG0> Mk\GV2FPT0WU
ATN-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHMVGJKSzVyPUO5Mlc4QTJiIN88US=> M1jpcXNCVkeHUh?=
KARPAS-299 NFvQSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zobWlEPTB;M{muPFM6KCEQvF2= Mn\pV2FPT0WU
KNS-81-FD NGLwWYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTJTWM2OD12MD6zOlA1KCEQvF2= Mn25V2FPT0WU
NCI-H1563 M2fuTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XUcWlEPTB;NEGuOVA{QSBizszN NHuxdm1USU6JRWK=
NB14 Mo\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTR{LkeyOlMhKM7:TR?= M{D5VXNCVkeHUh?=
COLO-800 NEP5VVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTR{Lki1NVchKM7:TR?= MlzTV2FPT0WU
MS-1 M122bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PGbGlEPTB;NEOuNFQ5OyBizszN M1HtT3NCVkeHUh?=
OVCAR-8 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTR|Lk[4NFkhKM7:TR?= MmHJV2FPT0WU
SK-PN-DW NEnQVpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\XTWM2OD12Mz64O|c3KCEQvF2= M1PKSXNCVkeHUh?=
G-402 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HUUGlEPTB;NEOuPVAxPiBizszN NHqyRmRUSU6JRWK=
NCI-H2291 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLjdm5DUUN3ME20OE45ODF5IDFOwG0> MmDIV2FPT0WU
PC-3 MlTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\4TWM2OD12NT64NFI{KCEQvF2= NWi0NIh6W0GQR1XS
NCI-H1581 M2LnNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nodWlEPTB;NEWuPVg5QSBizszN NFzyVG1USU6JRWK=
SW1116 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHaTWM2OD12Nz6wNVgzKCEQvF2= NUnBNWVTW0GQR1XS
ZR-75-30 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7KTWM2OD12Nz6wNlM6KCEQvF2= MYLTRW5ITVJ?
OCI-AML2 MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfm[JZKSzVyPUS3MlA6OThiIN88US=> NFXGWoxUSU6JRWK=
MDA-MB-231 MmfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HzTmlEPTB;NEeuOlI1QSBizszN NWnMbGx5W0GQR1XS
ES3 NXvKNVg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHpWZZbUUN3ME20PE4{PTJ7IDFOwG0> NXW3PZpPW0GQR1XS
NCI-H630 NFjSTZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTR7LkG3OFIhKM7:TR?= M2XlW3NCVkeHUh?=
OE19 MknJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTBR4NKSzVyPUS5MlI6ODJiIN88US=> NFnn[ZhUSU6JRWK=
NCI-H1573 NYHFdIdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;T[XdyUUN3ME20PU43QDZzIDFOwG0> MoHBV2FPT0WU
EW-1 NHfNTWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nuemlEPTB;NEmuPVA5PCBizszN MoTIV2FPT0WU

... 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 slightly soluble or 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
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
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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