Bosutinib (SKI-606) 化学構造
分子量: 530.45

高品質保証

カスタマーフィードバック(3)

MSDS

製品説明

  • Compare Src Inhibitors
    Src製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Bosutinib (SKI-606)のメカニズム

製品の説明

生物活性

製品説明 Bosutinib(SKI-606)はそれぞれ1.2nMと1nMのIC50値による新しい二重Sarcoma/アベルソン(Src/Abl)チロシン・キナーゼ阻害剤です。
ターゲット

Src

Abl

IC50

1.2 nM [1]

1 nM [2]

In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
NB7 MnnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwMEiyN|EhKM7:TR?= NIrCdWVUSU6JRWK=
SW756 NWXsdWtjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\zOIFKSzVyPUCuNVQxOjRiIN88US=> MWPTRW5ITVJ?
CTV-1 NWrGWmRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXYdINKSzVyPUCuNVY{QThiIN88US=> NGLBem1USU6JRWK=
HSC-4 NV60d|ZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwMUexOVghKM7:TR?= NFLOcYdUSU6JRWK=
LAMA-84 M3\FV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mof5TWM2OD1yLkK4OlY1KCEQvF2= Mm\qV2FPT0WU
KU812 NVG5U|FyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DOOWlEPTB;MD6zOFA3QCBizszN MWTTRW5ITVJ?
HCC1806 NEHtVYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fwUGlEPTB;MD6zOVIyPiBizszN MlnVV2FPT0WU
DOK NX3vZ5JyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXv0[lNHUUN3ME2wMlM4Pzh4IDFOwG0> NX\1N25mW0GQR1XS
NCI-H209 MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[xbHNMUUN3ME2wMlQxQDB6IDFOwG0> NH3CcldUSU6JRWK=
EoL-1-cell MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwNEG1O|YhKM7:TR?= MY\TRW5ITVJ?
H9 MkjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT0OoJKSzVyPUCuOFM1PjRiIN88US=> NUfjU5dMW0GQR1XS
EM-2 MkPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPTUJRPUUN3ME2wMlQ{QDliIN88US=> NV;sdZpwW0GQR1XS
NCI-H292 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwNESxNFghKM7:TR?= NXXJWI5wW0GQR1XS
697 MoDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfMenZzUUN3ME2wMlQ2PjN|IDFOwG0> MljWV2FPT0WU
BHT-101 NV;V[WdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\5TWM2OD1yLkS2OVkhKM7:TR?= NYfQVoRHW0GQR1XS
BE-13 MnjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwNEi1O|IhKM7:TR?= NYfjWYVvW0GQR1XS
RS4-11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7aN5ZCUUN3ME2wMlQ5PTh2IDFOwG0> MoHMV2FPT0WU
IGROV-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle1TWM2OD1yLkS4O|k4KCEQvF2= M{\JdXNCVkeHUh?=
KE-37 MnrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPoTWM2OD1yLkS5OVA6KCEQvF2= NYrVSFNzW0GQR1XS
BV-173 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTBwNUC3PVIhKM7:TR?= M4TSXnNCVkeHUh?=
MEG-01 M4LMSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwNUGyNVQhKM7:TR?= MWfTRW5ITVJ?
LB2241-RCC MmPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DkRWlEPTB;MD61N|cyQCBizszN M4\0NHNCVkeHUh?=
ACHN NVK4UpR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3riT2lEPTB;MD61OFA3QSBizszN MWnTRW5ITVJ?
CTB-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX76U4ZtUUN3ME2wMlU1QDJiIN88US=> MkPCV2FPT0WU
HT-1080 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\kUm9KSzVyPUCuOVU{PDliIN88US=> NF;tSYtUSU6JRWK=
CHL-1 NYTHcFdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTab5R3UUN3ME2wMlU2PDZ3IDFOwG0> MULTRW5ITVJ?
EW-3 NVTxbG1OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rJXGlEPTB;MD61OVk{PSBizszN MkHwV2FPT0WU
ES1 M1LxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon0TWM2OD1yLk[3OFk5KCEQvF2= NF7RNlVUSU6JRWK=
KASUMI-1 NI\4dZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwN{KzN{Ah|ryP NYjjTHBMW0GQR1XS
SW13 M2D4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfvc4FKSzVyPUCuO|M4QThiIN88US=> NFLJe2lUSU6JRWK=
A3-KAW MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XaZmlEPTB;MD63PVIxQCBizszN NYDzZ41OW0GQR1XS
LB771-HNC NHO4V2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[wenNKSzVyPUCuPFMyODRiIN88US=> NFn4SlVUSU6JRWK=
OC-314 M33MXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3z0W2lEPTB;MD64Olk3PSBizszN NUfnSIZlW0GQR1XS
MLMA MkO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwOUC2O|UhKM7:TR?= NFTMRo5USU6JRWK=
KARPAS-45 M{XYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXqTWM2OD1yLkmyOFY3KCEQvF2= NXT3ZmN7W0GQR1XS
CAL-27 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjQZW1yUUN3ME2wMlkzQTB4IDFOwG0> M3vPZnNCVkeHUh?=
SK-NEP-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;qNZZKSzVyPUCuPVczPDhiIN88US=> MWrTRW5ITVJ?
COR-L105 M4S4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzFRoVKSzVyPUGuNFA{QTRiIN88US=> NFrEN2dUSU6JRWK=
TI-73 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXJTWM2OD1zLkCxOlUhKM7:TR?= MUHTRW5ITVJ?
JVM-3 NH3LUoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTFwMEWwNVchKM7:TR?= NIXwUmtUSU6JRWK=
HAL-01 NGS0TmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT4TWM2OD1zLkC4PFEhKM7:TR?= MX7TRW5ITVJ?
QIMR-WIL NWjtfpV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjCZpVyUUN3ME2xMlA6ODV6IDFOwG0> MXjTRW5ITVJ?
HSC-3 NF3KUYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\ITWM2OD1zLkGxO|g{KCEQvF2= NHvnOItUSU6JRWK=
KY821 NHTDflJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm5[XlKSzVyPUGuNVM{PTFiIN88US=> M2e5XXNCVkeHUh?=
5637 MmrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TFUWlEPTB;MT6xN|gxOyBizszN M{K3ZnNCVkeHUh?=
CAL-33 MnPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPzTWM2OD1zLkG5N|AzKCEQvF2= MYDTRW5ITVJ?
ES4 M2i2XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm5V4o5UUN3ME2xMlIxPzliIN88US=> NXP2PHZRW0GQR1XS
BHY MmrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\oTWM2OD1zLkKyPFkzKCEQvF2= MXHTRW5ITVJ?
LB1047-RCC MmnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTFwMkO3PFUhKM7:TR?= M3\CXXNCVkeHUh?=
H4 M1P0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXRTWM2OD1zLkK0NlU2KCEQvF2= NFPhUZhUSU6JRWK=
RPMI-8866 NGLpWWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq4Z3dKSzVyPUGuNlYyODZiIN88US=> NHHITm9USU6JRWK=
HO-1-N-1 M1XONWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\oVWhKSzVyPUGuNlY{PjliIN88US=> NEHaeZBUSU6JRWK=
BB30-HNC NUDSSJFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnkWFlUUUN3ME2xMlI5PzF2IDFOwG0> MkG2V2FPT0WU
PC-14 M{Hle2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPKbnBKSzVyPUGuNlkzODViIN88US=> MV3TRW5ITVJ?
NUGC-3 NIT5S5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\5SphFUUN3ME2xMlI6OzV4IDFOwG0> NFjvZ2ZUSU6JRWK=
A4-Fuk NFzmPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPMeXBKSzVyPUGuN|A4ODRiIN88US=> Mme4V2FPT0WU
MHH-NB-11 M3PCd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITEdYpKSzVyPUGuN|E{QDNiIN88US=> M1XHc3NCVkeHUh?=
KOSC-2 NVHEVlB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHPdm5KSzVyPUGuN|E4PzViIN88US=> NFW5d|hUSU6JRWK=
A498 M{\jRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPocGtKUUN3ME2xMlQxOTF|IDFOwG0> MYrTRW5ITVJ?
KG-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DkbWlEPTB;MT60NVI4OyBizszN NEXZO2pUSU6JRWK=
DEL M2S1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXSTWM2OD1zLkSzOlU4KCEQvF2= NVrZOWs{W0GQR1XS
EW-16 NXPweFE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnqdnJqUUN3ME2xMlQ{QTd|IDFOwG0> NIDFfYRUSU6JRWK=
BPH-1 M2TiZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnYWGtrUUN3ME2xMlQ1QDB3IDFOwG0> Ml7kV2FPT0WU
JAR MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e5[mlEPTB;MT60PVM3KCEQvF2= M173[HNCVkeHUh?=
J-RT3-T3-5 MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTFwNUG3NlIhKM7:TR?= MVnTRW5ITVJ?
A375 M4nQcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTFwNUG3O|IhKM7:TR?= NYXzWpZxW0GQR1XS
SW954 MoDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVH0e2NFUUN3ME2xMlU2ODB5IDFOwG0> NUDxZpFrW0GQR1XS
Ca9-22 NGexRWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwNU[yOkAh|ryP M{HrXHNCVkeHUh?=
D-566MG MkLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PaPWlEPTB;MT61O|E2PSBizszN M3nCdnNCVkeHUh?=
SCC-15 NFj3UYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HkWWlEPTB;MT62NVgxPCBizszN M4rqb3NCVkeHUh?=
HD-MY-Z Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzFTWM2OD1zLk[zOVg1KCEQvF2= NVHMcmtLW0GQR1XS
HT-1376 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr6eFhKSzVyPUGuOlQ{PiBizszN MX\TRW5ITVJ?
CAL-54 NIfQUWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLJ[lNXUUN3ME2xMlY2PzB7IDFOwG0> M2LmcHNCVkeHUh?=
ONS-76 M2ryNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfFTG9KSzVyPUGuOlc2PTFiIN88US=> M3[0SnNCVkeHUh?=
EFO-27 M2HaN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlexTWM2OD1zLk[4PVIhKM7:TR?= MWjTRW5ITVJ?
769-P Mlf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPLTWM2OD1zLk[5OVk3KCEQvF2= NG[4NolUSU6JRWK=
MV-4-11 M2joU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrCXWc3UUN3ME2xMlY6QDV4IDFOwG0> M3PwcHNCVkeHUh?=
NKM-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPLT3hKSzVyPUGuO|E5ODJiIN88US=> NH3VS4FUSU6JRWK=
LOXIMVI Moi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rUemlEPTB;MT63OFU6QSBizszN MUTTRW5ITVJ?
KYSE-140 Mnq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rzb2lEPTB;MT63OVY2PSBizszN MkHzV2FPT0WU
ES5 NVTPbVQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzoSIJKSzVyPUGuPFY4PDdiIN88US=> NYrje3B2W0GQR1XS
BB65-RCC MoG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vyOGlEPTB;MT64PVg1QSBizszN MonWV2FPT0WU
HN M{HhR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHzcWJJUUN3ME2xMlg6QDd2IDFOwG0> Ml7OV2FPT0WU
A101D MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFwOUO2NlghKM7:TR?= NWG0bFFTW0GQR1XS
LoVo NVfoWoFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\2UVlZUUN3ME2xMlk4Pjd7IDFOwG0> NV\zfpA5W0GQR1XS
NCI-H526 MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzxepk3UUN3ME2xMlk6OzJ3IDFOwG0> MXnTRW5ITVJ?
NCI-H1693 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFwOUm4PFghKM7:TR?= NELmS49USU6JRWK=
OVCAR-4 NFTUVWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\UTWM2OD1{LkCwOFM2KCEQvF2= MXjTRW5ITVJ?
SK-HEP-1 M1nifWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHVPYpKSzVyPUKuNFA4PDViIN88US=> NWf6[YRjW0GQR1XS
C2BBe1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvwdJJJUUN3ME2yMlA{Ozd{IDFOwG0> NHrlc5ZUSU6JRWK=
MEL-JUSO NYXzPFk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTJwMES0OlQhKM7:TR?= MYXTRW5ITVJ?
MOLT-16 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjFOWxKSzVyPUKuNFcxPThiIN88US=> MlzHV2FPT0WU
NBsusSR NHnPNWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL2eINKSzVyPUKuNFk5QDliIN88US=> M3:3UXNCVkeHUh?=
TK10 NUT4VXJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJwMUO0OVghKM7:TR?= NHPObHlUSU6JRWK=
CAL-39 NWr1[Ih6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\USHJZUUN3ME2yMlE1PDhiIN88US=> NVO0OmhFW0GQR1XS
NCI-H2030 NEC4[VhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzBTWM2OD1{LkG4PVc{KCEQvF2= NGnOeHRUSU6JRWK=
HCT-116 NY\ybFBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTiNI1KSzVyPUKuNlI6QDRiIN88US=> Mn;jV2FPT0WU
HTC-C3 MkXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\STWM2OD1{LkK2PFI1KCEQvF2= NXL4T|h3W0GQR1XS
TYK-nu NUPFdnU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXGT3NKSzVyPUKuN|A6ODliIN88US=> M2ezfnNCVkeHUh?=
FADU NVjDd2hqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjLWJRyUUN3ME2yMlMzOjl4IDFOwG0> MlmzV2FPT0WU
A431 NX;5W2g{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzGTWM2OD1{LkO3NFI2KCEQvF2= Ml6yV2FPT0WU
TE-11 NHH1NlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T6bmlEPTB;Mj6zPFAyQSBizszN NV7qNIV5W0GQR1XS
CAL-12T M1n0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fRRmlEPTB;Mj60NFQyPyBizszN MXPTRW5ITVJ?
DB NXPtRWlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGD5OZRKSzVyPUKuOFI5PjliIN88US=> MmjvV2FPT0WU
L-363 NHvBRXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHvcmZmUUN3ME2yMlQ{PTB5IDFOwG0> M2XycnNCVkeHUh?=
MSTO-211H NYjBWmx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjzSVJKSzVyPUKuOlY{QTFiIN88US=> MXjTRW5ITVJ?
SK-UT-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj4TWM2OD1{LkexOFA3KCEQvF2= NWn2UINYW0GQR1XS
RPMI-8226 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJwN{OxOlQhKM7:TR?= NFTwcpRUSU6JRWK=
SF295 M1vmS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DoZ2lEPTB;Mj63OFMyKCEQvF2= M3nZ[nNCVkeHUh?=
OS-RC-2 NGPZV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PJ[mlEPTB;Mj63OlY4OyBizszN M1y2V3NCVkeHUh?=
SK-MEL-24 MoLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrmTWM2OD1{Lke4NlI1KCEQvF2= NVvvSoZRW0GQR1XS
COR-L23 NFTHU4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPkTWM2OD1{Lke5OFY1KCEQvF2= M3zVWHNCVkeHUh?=
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NCI-H1155 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTN7LkC0O|EhKM7:TR?= M4\YbHNCVkeHUh?=
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SW1116 NED4cXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\aN2wzUUN3ME20O{4xOTh{IDFOwG0> NY\VN3pIW0GQR1XS
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... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 A Phase I study to compare the Bosutinib clinical tablet and clinical capsule and to investigate food effect on Bosutinib commercial formulation in healthy subjects has been completed.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

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.

細胞アッセイ:

[2]

細胞株 Abl-MLV, Rat 2, KU812, K562, and MEG-01 cells
濃度 Dissolved in DMSO, final concentrations ~1 μM
反応時間 72 hours
実験の流れ

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.

動物実験:

[2]

動物モデル Nude female mice injected with K562 cells
製剤 Suspended in 0.5% methocel/0.4% Tween 80
投薬量 ~150 mg/kg/day
投与方法 Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Bosutinib (SKI-606) SDF
分子量 530.45
化学式

C26H29Cl2N5O3

CAS No. 380843-75-4
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (188.51 mM)
Ethanol 2 mg/mL (3.77 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 4-(2,4-dichloro-5-methoxyphenylamino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

文献中の引用 (14)

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.

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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