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 M2\jdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrZUI5HUUN3ME2wMlA5OjNzIDFOwG0> MVnTRW5ITVJ?
SW756 M1u4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwMUSwNlQhKM7:TR?= NX\FcnJrW0GQR1XS
CTV-1 NXnmUmtKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnmRZRZUUN3ME2wMlE3Ozl6IDFOwG0> MUTTRW5ITVJ?
HSC-4 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELEXXlKSzVyPUCuNVcyPThiIN88US=> MV3TRW5ITVJ?
LAMA-84 NFnnUI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rSS2lEPTB;MD6yPFY3PCBizszN NWfYeGVHW0GQR1XS
KU812 NFnMZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3m4OmlEPTB;MD6zOFA3QCBizszN NE\zWYlUSU6JRWK=
HCC1806 Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXm1RZpFUUN3ME2wMlM2OjF4IDFOwG0> MkS3V2FPT0WU
DOK NGTlW4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjq[3N[UUN3ME2wMlM4Pzh4IDFOwG0> M1;FRnNCVkeHUh?=
NCI-H209 NVXSRpc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk[2TWM2OD1yLkSwPFA5KCEQvF2= M1LqVHNCVkeHUh?=
EoL-1-cell NEPKTmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rDbWlEPTB;MD60NVU4PiBizszN NUTlVGM5W0GQR1XS
H9 NIDNUIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\U[29TUUN3ME2wMlQ{PDZ2IDFOwG0> NFLqc2JUSU6JRWK=
EM-2 M2f2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInPSmdKSzVyPUCuOFM5QSBizszN NFv5bI5USU6JRWK=
NCI-H292 MkD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHRTWM2OD1yLkS0NVA5KCEQvF2= M{\GWnNCVkeHUh?=
697 MlTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTBwNEW2N|MhKM7:TR?= M3HGUHNCVkeHUh?=
BHT-101 Mk[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4q0[WlEPTB;MD60OlU6KCEQvF2= NFvrbGRUSU6JRWK=
BE-13 Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwNEi1O|IhKM7:TR?= MX7TRW5ITVJ?
RS4-11 M3i2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPmTWM2OD1yLkS4OVg1KCEQvF2= MojmV2FPT0WU
IGROV-1 NUHvTog2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LpdGlEPTB;MD60PFc6PyBizszN NIjlXJBUSU6JRWK=
KE-37 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HjWGlEPTB;MD60PVUxQSBizszN M4\z[XNCVkeHUh?=
BV-173 M{HHdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml61TWM2OD1yLkWwO|kzKCEQvF2= MUDTRW5ITVJ?
MEG-01 MnXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV:ybJRYUUN3ME2wMlUyOjF2IDFOwG0> NFnVV4tUSU6JRWK=
LB2241-RCC NFuwPFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXLfoY3UUN3ME2wMlU{PzF6IDFOwG0> NUXoSWdnW0GQR1XS
ACHN MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnT5TWM2OD1yLkW0NFY6KCEQvF2= M3\WVXNCVkeHUh?=
CTB-1 NYXLPW5DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTBwNUS4NkAh|ryP NV\JOXBLW0GQR1XS
HT-1080 NFe0T3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4KzfGlEPTB;MD61OVM1QSBizszN NEC3cYNUSU6JRWK=
CHL-1 NXvhVGYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjPTWM2OD1yLkW1OFY2KCEQvF2= NYq5fmFIW0GQR1XS
EW-3 M{LJUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETpTIFKSzVyPUCuOVU6OzViIN88US=> MULTRW5ITVJ?
ES1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nseWlEPTB;MD62O|Q6QCBizszN NYS5dXpPW0GQR1XS
KASUMI-1 MlrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr0e21VUUN3ME2wMlczOzNiIN88US=> NIXBTFBUSU6JRWK=
SW13 MmPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHZV2szUUN3ME2wMlc{Pzl6IDFOwG0> NF\RcWZUSU6JRWK=
A3-KAW Mn3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXwXW9wUUN3ME2wMlc6OjB6IDFOwG0> M4nPVHNCVkeHUh?=
LB771-HNC NIjqfI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYmxPFB7UUN3ME2wMlg{OTB2IDFOwG0> Mlv1V2FPT0WU
OC-314 NGLZXVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moj0TWM2OD1yLki2PVY2KCEQvF2= NHy4ZZZUSU6JRWK=
MLMA NETCPXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTBwOUC2O|UhKM7:TR?= MWTTRW5ITVJ?
KARPAS-45 NWDCO4w2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HkbWlEPTB;MD65NlQ3PiBizszN NGDwbXhUSU6JRWK=
CAL-27 MmXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn[5TWM2OD1yLkmyPVA3KCEQvF2= NID2c25USU6JRWK=
SK-NEP-1 NGKxTINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwOUeyOFghKM7:TR?= NIPEc21USU6JRWK=
COR-L105 M3HN[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTFwMECzPVQhKM7:TR?= MXnTRW5ITVJ?
TI-73 M2LsUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTFwMEG2OUAh|ryP M1OwS3NCVkeHUh?=
JVM-3 M13yVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDRbmFKSzVyPUGuNFUxOTdiIN88US=> NFvUcGtUSU6JRWK=
HAL-01 NFrD[GRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnNTWM2OD1zLkC4PFEhKM7:TR?= NFXmd4xUSU6JRWK=
QIMR-WIL NXPvUnNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PrSGlEPTB;MT6wPVA2QCBizszN MVTTRW5ITVJ?
HSC-3 M2jCeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzEfoxsUUN3ME2xMlEyPzh|IDFOwG0> M3f3SnNCVkeHUh?=
KY821 NEmwOHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXqycnBGUUN3ME2xMlE{OzVzIDFOwG0> NHfqXHdUSU6JRWK=
5637 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PvNGlEPTB;MT6xN|gxOyBizszN M4qwUHNCVkeHUh?=
CAL-33 MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTFwMUmzNFIhKM7:TR?= MnXUV2FPT0WU
ES4 NUnBcpdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDvTWM2OD1zLkKwO|khKM7:TR?= NX7LcoNOW0GQR1XS
BHY NWjnZpNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnqwTWM2OD1zLkKyPFkzKCEQvF2= M2nvOXNCVkeHUh?=
LB1047-RCC NH\6SYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFwMkO3PFUhKM7:TR?= MV7TRW5ITVJ?
H4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zzb2lEPTB;MT6yOFI2PSBizszN NInSNohUSU6JRWK=
RPMI-8866 NVTWcmpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFwMk[xNFYhKM7:TR?= M{XM[HNCVkeHUh?=
HO-1-N-1 M2jLOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwMk[zOlkhKM7:TR?= M1LlZXNCVkeHUh?=
BB30-HNC Ml3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojHTWM2OD1zLkK4O|E1KCEQvF2= MkTPV2FPT0WU
PC-14 MkjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTFwMkmyNFUhKM7:TR?= M2TpXHNCVkeHUh?=
NUGC-3 MoCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTFwMkmzOVYhKM7:TR?= NYXwSoh2W0GQR1XS
A4-Fuk NELoV3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFwM{C3NFQhKM7:TR?= NVSze4NwW0GQR1XS
MHH-NB-11 NHX5WoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFwM{GzPFMhKM7:TR?= MX7TRW5ITVJ?
KOSC-2 M3;TZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\qVGlEPTB;MT6zNVc4PSBizszN NVHUNZlyW0GQR1XS
A498 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHW1XY5KSzVyPUGuOFAyOTNiIN88US=> NH7ENVJUSU6JRWK=
KG-1 Mn25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTFwNEGyO|MhKM7:TR?= MmP5V2FPT0WU
DEL NYrRXYo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwNEO2OVchKM7:TR?= MmXaV2FPT0WU
EW-16 NVLOTINXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nPVWlEPTB;MT60N|k4OyBizszN MnS1V2FPT0WU
BPH-1 NXHGfZh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIThe5dKSzVyPUGuOFQ5ODViIN88US=> Mn7BV2FPT0WU
JAR MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\K[nhKSzVyPUGuOFk{PiBizszN MU\TRW5ITVJ?
J-RT3-T3-5 NHfSV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHzTlNKSzVyPUGuOVE4OjJiIN88US=> MlLrV2FPT0WU
A375 NITEeWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PhN2lEPTB;MT61NVc4OiBizszN NH\oc3FUSU6JRWK=
SW954 NHmzfZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTFwNUWwNFchKM7:TR?= NUDz[GhUW0GQR1XS
Ca9-22 M{PQUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfsXnNJUUN3ME2xMlU3OjZiIN88US=> M3niVHNCVkeHUh?=
D-566MG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDSTpE2UUN3ME2xMlU4OTV3IDFOwG0> MlTuV2FPT0WU
SCC-15 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\lR4ZpUUN3ME2xMlYyQDB2IDFOwG0> MYrTRW5ITVJ?
HD-MY-Z MkTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjyTWM2OD1zLk[zOVg1KCEQvF2= MnO3V2FPT0WU
HT-1376 M2rzeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7hZ2ZtUUN3ME2xMlY1OzZiIN88US=> M2TVbnNCVkeHUh?=
CAL-54 NUDtVppMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojwTWM2OD1zLk[1O|A6KCEQvF2= NUjqeY5ZW0GQR1XS
ONS-76 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HsSWlEPTB;MT62O|U2OSBizszN NUfPNZFNW0GQR1XS
EFO-27 NFi0PXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTFwNki5NkAh|ryP M3PHOXNCVkeHUh?=
769-P M1;6W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPwcYtTUUN3ME2xMlY6PTl4IDFOwG0> MljQV2FPT0WU
MV-4-11 M{\tR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojNTWM2OD1zLk[5PFU3KCEQvF2= MVTTRW5ITVJ?
NKM-1 NVP1TmpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;nTWM2OD1zLkexPFAzKCEQvF2= MoPZV2FPT0WU
LOXIMVI MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwN{S1PVkhKM7:TR?= NVPHcm9zW0GQR1XS
KYSE-140 NGfHZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D2e2lEPTB;MT63OVY2PSBizszN MlzWV2FPT0WU
ES5 M3;UcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTFwOE[3OFchKM7:TR?= NFv5RZNUSU6JRWK=
BB65-RCC MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:0cmlEPTB;MT64PVg1QSBizszN M{\tT3NCVkeHUh?=
HN NXPrVlhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknSTWM2OD1zLki5PFc1KCEQvF2= M4TK[nNCVkeHUh?=
A101D M1rGfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnTR5NKSzVyPUGuPVM3OjhiIN88US=> MnvDV2FPT0WU
LoVo M3mwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELieW5KSzVyPUGuPVc3PzliIN88US=> NHrDSW5USU6JRWK=
NCI-H526 NGTzOGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjXcHZKSzVyPUGuPVk{OjViIN88US=> NUOyeHo{W0GQR1XS
NCI-H1693 NHrTXnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofuTWM2OD1zLkm5PFg5KCEQvF2= MknmV2FPT0WU
OVCAR-4 M3vTT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXWz[WpwUUN3ME2yMlAxPDN3IDFOwG0> MXHTRW5ITVJ?
SK-HEP-1 NGHqVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\NeWFKSzVyPUKuNFA4PDViIN88US=> MoHyV2FPT0WU
C2BBe1 NYPv[205T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTJwMEOzO|IhKM7:TR?= M13DVnNCVkeHUh?=
MEL-JUSO NFTGdHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPuTWM2OD1{LkC0OFY1KCEQvF2= MUPTRW5ITVJ?
MOLT-16 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTJwMEewOVghKM7:TR?= NFjQcVBUSU6JRWK=
NBsusSR NFS4SFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LDV2lEPTB;Mj6wPVg5QSBizszN NXrF[W5iW0GQR1XS
TK10 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLQTWM2OD1{LkGzOFU5KCEQvF2= NVq0ZYJPW0GQR1XS
CAL-39 NX:1[ZBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLU[2Z{UUN3ME2yMlE1PDhiIN88US=> MkXNV2FPT0WU
NCI-H2030 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPiUFIxUUN3ME2yMlE5QTd|IDFOwG0> NXv2d2hHW0GQR1XS
HCT-116 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJwMkK5PFQhKM7:TR?= M33ve3NCVkeHUh?=
HTC-C3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJwMk[4NlQhKM7:TR?= NF3zWGhUSU6JRWK=
TYK-nu M1;n[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHZUHhKSzVyPUKuN|A6ODliIN88US=> M2nnVHNCVkeHUh?=
FADU MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHoXWtKSzVyPUKuN|IzQTZiIN88US=> M4\JWXNCVkeHUh?=
A431 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TLO2lEPTB;Mj6zO|AzPSBizszN MmfEV2FPT0WU
TE-11 MkfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJwM{iwNVkhKM7:TR?= MVHTRW5ITVJ?
CAL-12T NYf3SlNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTvS25SUUN3ME2yMlQxPDF5IDFOwG0> MY\TRW5ITVJ?
DB MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\0Wo5KSzVyPUKuOFI5PjliIN88US=> MWfTRW5ITVJ?
L-363 Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWeycpROUUN3ME2yMlQ{PTB5IDFOwG0> NEDsR2xUSU6JRWK=
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MC116 MmDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\iTWM2OD1|MD6wO|M{KCEQvF2= NH3kWYRUSU6JRWK=
NCI-H69 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTNyLk[wPVMhKM7:TR?= MUDTRW5ITVJ?
NB6 MkHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPkTWM2OD1|MT6zOlI6KCEQvF2= MlS0V2FPT0WU
CAL-120 M3fSOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES4O4tKSzVyPUOyMlQ{OTdiIN88US=> NVezRVVsW0GQR1XS
U-87-MG MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf0fXdKSzVyPUOzMlAzPTFiIN88US=> Mly1V2FPT0WU
NCI-H1304 MoLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe5dJlKSzVyPUOzMlA{PTRiIN88US=> MlXJV2FPT0WU
YH-13 NHv2V5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;1SpY1UUN3ME2zN{4zPTN3IDFOwG0> M2XnV3NCVkeHUh?=
RMG-I NFPlTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfUTWM2OD1|Mz60Nlg2KCEQvF2= MoLTV2FPT0WU
LU-65 NYSxcWNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TzOWlEPTB;M{SuNVQxQCBizszN NHj5NYZUSU6JRWK=
GB-1 M{nyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDYU3gzUUN3ME2zOU4xPzJ7IDFOwG0> NXvXPXVoW0GQR1XS
DU-4475 NE[4WXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTJcnB1UUN3ME2zOU4yPTV|IDFOwG0> M1HhenNCVkeHUh?=
SBC-5 NGi0flFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTN4LkW5NFIhKM7:TR?= MYLTRW5ITVJ?
OE33 M3jNNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTN5Lke1O|chKM7:TR?= MVvTRW5ITVJ?
C8166 M2TuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX3TWM2OD1|OD61NlY4KCEQvF2= NV;DU4U2W0GQR1XS
COLO-684 NEHXPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLVOJJTUUN3ME2zPE44PDJ6IDFOwG0> NUHCPGY4W0GQR1XS
NCI-H1155 NHvnfGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nEb2lEPTB;M{muNFQ4OSBizszN MWTTRW5ITVJ?
ATN-1 MonkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfURW1KSzVyPUO5Mlc4QTJiIN88US=> MmHvV2FPT0WU
KARPAS-299 M3;HNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4S3[WlEPTB;M{muPFM6KCEQvF2= MoqwV2FPT0WU
KNS-81-FD MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTRyLkO2NFQhKM7:TR?= M3vOPHNCVkeHUh?=
NCI-H1563 NWmxfIdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFyyWWhKSzVyPUSxMlUxOzliIN88US=> Ml;sV2FPT0WU
NB14 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXyzeIk1UUN3ME20Nk44OjZ|IDFOwG0> MoXiV2FPT0WU
COLO-800 MnLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTR{Lki1NVchKM7:TR?= M1yyenNCVkeHUh?=
MS-1 NWK5SWVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXIRnhKSzVyPUSzMlA1QDNiIN88US=> NVXsOVV{W0GQR1XS
OVCAR-8 M2DMcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTR|Lk[4NFkhKM7:TR?= NWLnV5NYW0GQR1XS
SK-PN-DW NGPQd3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NET4bG5KSzVyPUSzMlg4PzZiIN88US=> M17FRXNCVkeHUh?=
G-402 MlPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVuz[pVxUUN3ME20N{46ODB4IDFOwG0> MWjTRW5ITVJ?
NCI-H2291 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;yNHRjUUN3ME20OE45ODF5IDFOwG0> M2XRW3NCVkeHUh?=
PC-3 MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjHbW9KSzVyPUS1MlgxOjNiIN88US=> M1fQSHNCVkeHUh?=
NCI-H1581 NILldoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO1TWM2OD12NT65PFg6KCEQvF2= M4D4e3NCVkeHUh?=
SW1116 MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPWTWM2OD12Nz6wNVgzKCEQvF2= NH;EcZlUSU6JRWK=
ZR-75-30 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfQTWM2OD12Nz6wNlM6KCEQvF2= NWi3[|ExW0GQR1XS
OCI-AML2 M{\tNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrtVlNKSzVyPUS3MlA6OThiIN88US=> NHryVYRUSU6JRWK=
MDA-MB-231 NGLifmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTR5Lk[yOFkhKM7:TR?= MlnNV2FPT0WU
ES3 NWDn[VNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Xrd2lEPTB;NEiuN|UzQSBizszN MXHTRW5ITVJ?
NCI-H630 MlrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HTR2lEPTB;NEmuNVc1OiBizszN NWK1cXh6W0GQR1XS
OE19 M1XpU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTQfVJKSzVyPUS5MlI6ODJiIN88US=> M3eweHNCVkeHUh?=
NCI-H1573 MlHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy0TlZmUUN3ME20PU43QDZzIDFOwG0> NIrvbnhUSU6JRWK=
EW-1 NF3NcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f6RWlEPTB;NEmuPVA5PCBizszN NYnWOpptW0GQR1XS

... 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
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