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)は一種の新たな二重Src/Abl阻害剤で、無細胞試験でIC50値が1.2 nMと1 nM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 MkDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;HfHRKSzVyPUCuNFgzOzFiIN88US=> MUTTRW5ITVJ?
SW756 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnLTWM2OD1yLkG0NFI1KCEQvF2= NIm2eXVUSU6JRWK=
CTV-1 NXvxW2hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXuyVIIyUUN3ME2wMlE3Ozl6IDFOwG0> MXXTRW5ITVJ?
HSC-4 NFHFR4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwMUexOVghKM7:TR?= NIm4NYVUSU6JRWK=
LAMA-84 NXH1SmpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7pN41qUUN3ME2wMlI5PjZ2IDFOwG0> NUPIO5VTW0GQR1XS
KU812 M1;KO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S3fWlEPTB;MD6zOFA3QCBizszN NEnvdZNUSU6JRWK=
HCC1806 NXWzPYVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofJTWM2OD1yLkO1NlE3KCEQvF2= NWjzUotwW0GQR1XS
DOK MonzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILveXBKSzVyPUCuN|c4QDZiIN88US=> NUT1NGFlW0GQR1XS
NCI-H209 NVHuTWNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojlTWM2OD1yLkSwPFA5KCEQvF2= NYCz[YY1W0GQR1XS
EoL-1-cell MlznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7rbIczUUN3ME2wMlQyPTd4IDFOwG0> MmDMV2FPT0WU
H9 NXTDV2JlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofsTWM2OD1yLkSzOFY1KCEQvF2= MnTsV2FPT0WU
EM-2 MnH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\CTWM2OD1yLkSzPFkhKM7:TR?= M{XXUXNCVkeHUh?=
NCI-H292 NGDJ[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwNESxNFghKM7:TR?= MnXBV2FPT0WU
697 NGqyclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDJTWM2OD1yLkS1OlM{KCEQvF2= NIr1dmtUSU6JRWK=
BHT-101 M4HHfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7YWlE{UUN3ME2wMlQ3PTliIN88US=> MkDtV2FPT0WU
BE-13 MonLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwNEi1O|IhKM7:TR?= MUDTRW5ITVJ?
RS4-11 M3XLc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfRXG5yUUN3ME2wMlQ5PTh2IDFOwG0> MYnTRW5ITVJ?
IGROV-1 NWToNHB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17KS2lEPTB;MD60PFc6PyBizszN NVL0clVrW0GQR1XS
KE-37 Moq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYi3WWxHUUN3ME2wMlQ6PTB7IDFOwG0> M{DYcXNCVkeHUh?=
BV-173 NEPIXGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwNUC3PVIhKM7:TR?= MYPTRW5ITVJ?
MEG-01 MmXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYn4OIpuUUN3ME2wMlUyOjF2IDFOwG0> NWfTfpp7W0GQR1XS
LB2241-RCC Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonnTWM2OD1yLkWzO|E5KCEQvF2= MnfmV2FPT0WU
ACHN M3nU[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e4TmlEPTB;MD61OFA3QSBizszN NFThUldUSU6JRWK=
CTB-1 NEfPVJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEWyeYVKSzVyPUCuOVQ5OiBizszN NUHLSldpW0GQR1XS
HT-1080 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWP0UplsUUN3ME2wMlU2OzR7IDFOwG0> M2fFOnNCVkeHUh?=
CHL-1 M1ri[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTQTWM2OD1yLkW1OFY2KCEQvF2= M2ezdHNCVkeHUh?=
EW-3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\BfHpKSzVyPUCuOVU6OzViIN88US=> MnL0V2FPT0WU
ES1 M4ThSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPQ[5gzUUN3ME2wMlY4PDl6IDFOwG0> MkPVV2FPT0WU
KASUMI-1 MoHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnqN3FIUUN3ME2wMlczOzNiIN88US=> MYfTRW5ITVJ?
SW13 Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fZWmlEPTB;MD63N|c6QCBizszN MnqxV2FPT0WU
A3-KAW NH2xdYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PMN2lEPTB;MD63PVIxQCBizszN NXznOpNRW0GQR1XS
LB771-HNC NHnVfXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTrTWM2OD1yLkizNVA1KCEQvF2= MVHTRW5ITVJ?
OC-314 NGnlWXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HLOWlEPTB;MD64Olk3PSBizszN Mm\jV2FPT0WU
MLMA MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHhdXBKSzVyPUCuPVA3PzViIN88US=> NGjmUGZUSU6JRWK=
KARPAS-45 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD0cpZ7UUN3ME2wMlkzPDZ4IDFOwG0> M32xOHNCVkeHUh?=
CAL-27 M3jw[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwOUK5NFYhKM7:TR?= MWDTRW5ITVJ?
SK-NEP-1 M1Xpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLTNXNKSzVyPUCuPVczPDhiIN88US=> MW\TRW5ITVJ?
COR-L105 NIe1VVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\ETWM2OD1zLkCwN|k1KCEQvF2= M4K4UXNCVkeHUh?=
TI-73 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HPRWlEPTB;MT6wNVY2KCEQvF2= NXrFZ|hpW0GQR1XS
JVM-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGq3bY9KSzVyPUGuNFUxOTdiIN88US=> M1m1V3NCVkeHUh?=
HAL-01 M1fMTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M173O2lEPTB;MT6wPFgyKCEQvF2= NUHmcY1JW0GQR1XS
QIMR-WIL M1\hXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PyRWlEPTB;MT6wPVA2QCBizszN MkHlV2FPT0WU
HSC-3 NFS1TYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjLOYNNUUN3ME2xMlEyPzh|IDFOwG0> MkTSV2FPT0WU
KY821 NEHl[5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7PTWM2OD1zLkGzN|UyKCEQvF2= MnXmV2FPT0WU
5637 NUn0[2J6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7uTWM2OD1zLkGzPFA{KCEQvF2= MV3TRW5ITVJ?
CAL-33 Moq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnkS4JiUUN3ME2xMlE6OzB{IDFOwG0> NXXLb|k4W0GQR1XS
ES4 NHvQemhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPJWG5KSzVyPUGuNlA4QSBizszN M2HMfXNCVkeHUh?=
BHY NUC1O4ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Sy[2lEPTB;MT6yNlg6OiBizszN M1zPZXNCVkeHUh?=
LB1047-RCC NGToOGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXTcWg4UUN3ME2xMlI{Pzh3IDFOwG0> MorMV2FPT0WU
H4 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFwMkSyOVUhKM7:TR?= Mmj3V2FPT0WU
RPMI-8866 NYfqdIdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwMk[xNFYhKM7:TR?= MVjTRW5ITVJ?
HO-1-N-1 NV7DNG1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XNPWlEPTB;MT6yOlM3QSBizszN Mnf5V2FPT0WU
BB30-HNC NFz0TGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPDTWM2OD1zLkK4O|E1KCEQvF2= NYTTXJp{W0GQR1XS
PC-14 Ml3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rsN2lEPTB;MT6yPVIxPSBizszN M1nEUHNCVkeHUh?=
NUGC-3 M3TqeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT1UY9KSzVyPUGuNlk{PTZiIN88US=> Moj1V2FPT0WU
A4-Fuk MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfUTIpKSzVyPUGuN|A4ODRiIN88US=> M{D6TXNCVkeHUh?=
MHH-NB-11 NYHYeHlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFwM{GzPFMhKM7:TR?= NF;4c3dUSU6JRWK=
KOSC-2 NF2wRnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFwM{G3O|UhKM7:TR?= MoDTV2FPT0WU
A498 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rWdmlEPTB;MT60NFEyOyBizszN NIjmVWhUSU6JRWK=
KG-1 NVX6UpFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnrTWU6UUN3ME2xMlQyOjd|IDFOwG0> MUXTRW5ITVJ?
DEL MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVq3XVlvUUN3ME2xMlQ{PjV5IDFOwG0> NULTXGlUW0GQR1XS
EW-16 Mo\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3X2V2lEPTB;MT60N|k4OyBizszN MYTTRW5ITVJ?
BPH-1 NUjiT5FqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTLS|ZmUUN3ME2xMlQ1QDB3IDFOwG0> NX60VIJbW0GQR1XS
JAR MnfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkG5TWM2OD1zLkS5N|YhKM7:TR?= MkGzV2FPT0WU
J-RT3-T3-5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrRTWM2OD1zLkWxO|IzKCEQvF2= MkLSV2FPT0WU
A375 M2jPUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn5eINoUUN3ME2xMlUyPzd{IDFOwG0> NHXybXBUSU6JRWK=
SW954 Mor6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml65TWM2OD1zLkW1NFA4KCEQvF2= MoTTV2FPT0WU
Ca9-22 MlHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjw[3pKSzVyPUGuOVYzPiBizszN NGPqUohUSU6JRWK=
D-566MG NIO0ZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTFwNUexOVUhKM7:TR?= MlL4V2FPT0WU
SCC-15 NGjqWXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW5PJlUUUN3ME2xMlYyQDB2IDFOwG0> M{HlcnNCVkeHUh?=
HD-MY-Z M3HYV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfFelFKSzVyPUGuOlM2QDRiIN88US=> M4TSOHNCVkeHUh?=
HT-1376 NGLiWmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFwNkSzOkAh|ryP NX\OZ45ZW0GQR1XS
CAL-54 M2LmVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjIRm1FUUN3ME2xMlY2PzB7IDFOwG0> MlPtV2FPT0WU
ONS-76 NH7PUXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTFwNke1OVEhKM7:TR?= NUnMZ5BoW0GQR1XS
EFO-27 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PsN2lEPTB;MT62PFkzKCEQvF2= NU\MXnZpW0GQR1XS
769-P NEn5ToRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFwNkm1PVYhKM7:TR?= M13kXnNCVkeHUh?=
MV-4-11 M3fzNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwNkm4OVYhKM7:TR?= NHjKUJJUSU6JRWK=
NKM-1 M1fpUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7UTWM2OD1zLkexPFAzKCEQvF2= NHjUfFhUSU6JRWK=
LOXIMVI M4LlbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD6cllKSzVyPUGuO|Q2QTliIN88US=> M1zoVnNCVkeHUh?=
KYSE-140 NWDVbYgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TwbWlEPTB;MT63OVY2PSBizszN NUD1fYpTW0GQR1XS
ES5 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFwOE[3OFchKM7:TR?= M{n4R3NCVkeHUh?=
BB65-RCC NHfzOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fNemlEPTB;MT64PVg1QSBizszN MWrTRW5ITVJ?
HN MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36wUmlEPTB;MT64PVg4PCBizszN NVXsZlZOW0GQR1XS
A101D M1rVR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrKS|hKSzVyPUGuPVM3OjhiIN88US=> NGqweWxUSU6JRWK=
LoVo MlrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rSVGlEPTB;MT65O|Y4QSBizszN NFz4XVdUSU6JRWK=
NCI-H526 NXrpUYh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1:0WWlEPTB;MT65PVMzPSBizszN NIrXXWlUSU6JRWK=
NCI-H1693 NUPmOZdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFwOUm4PFghKM7:TR?= MmXsV2FPT0WU
OVCAR-4 M2WxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXQTWM2OD1{LkCwOFM2KCEQvF2= NG\2ephUSU6JRWK=
SK-HEP-1 NIHCVVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[xTlZNUUN3ME2yMlAxPzR3IDFOwG0> M360XnNCVkeHUh?=
C2BBe1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj1TWM2OD1{LkCzN|czKCEQvF2= M1z5OHNCVkeHUh?=
MEL-JUSO M4LDdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3QSHdKSzVyPUKuNFQ1PjRiIN88US=> NV[2XI5JW0GQR1XS
MOLT-16 NX61T2I5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz0RWZKSzVyPUKuNFcxPThiIN88US=> MoDqV2FPT0WU
NBsusSR NEPmbplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXj6eVdZUUN3ME2yMlA6QDh7IDFOwG0> NI\OZ5ZUSU6JRWK=
TK10 NHnXbJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH3TWM2OD1{LkGzOFU5KCEQvF2= MkHPV2FPT0WU
CAL-39 M4Lmc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJwMUS0PEAh|ryP NXTGc3k{W0GQR1XS
NCI-H2030 NUDVXXNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfOfopKSzVyPUKuNVg6PzNiIN88US=> M1vrWXNCVkeHUh?=
HCT-116 MmHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y3UmlEPTB;Mj6yNlk5PCBizszN MYHTRW5ITVJ?
HTC-C3 NIjVc45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHMNo9XUUN3ME2yMlI3QDJ2IDFOwG0> NH\jUJBUSU6JRWK=
TYK-nu NUj1U5ppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjwNXRKSzVyPUKuN|A6ODliIN88US=> MXHTRW5ITVJ?
FADU M3zpOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTJwM{KyPVYhKM7:TR?= NHvPdYxUSU6JRWK=
A431 NXGzTG5qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHQPYdqUUN3ME2yMlM4ODJ3IDFOwG0> NEXnRYNUSU6JRWK=
TE-11 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H3UGlEPTB;Mj6zPFAyQSBizszN MVrTRW5ITVJ?
CAL-12T MkTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:yTWM2OD1{LkSwOFE4KCEQvF2= M1zQVHNCVkeHUh?=
DB MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:yW4RKSzVyPUKuOFI5PjliIN88US=> NGrwUm1USU6JRWK=
L-363 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTJZ2ZIUUN3ME2yMlQ{PTB5IDFOwG0> MVPTRW5ITVJ?
MSTO-211H MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnkTWM2OD1{Lk[2N|kyKCEQvF2= NEPNWHJUSU6JRWK=
SK-UT-1 MnrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTLWWRKSzVyPUKuO|E1ODZiIN88US=> MUnTRW5ITVJ?
RPMI-8226 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvEN|RZUUN3ME2yMlc{OTZ2IDFOwG0> M12w[HNCVkeHUh?=
SF295 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFOxNYhKSzVyPUKuO|Q{OSBizszN M1rTPXNCVkeHUh?=
OS-RC-2 M3Sxd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJwN{[2O|MhKM7:TR?= NWHadXI1W0GQR1XS
SK-MEL-24 MnLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m2TGlEPTB;Mj63PFIzPCBizszN NW\yR|RTW0GQR1XS
COR-L23 NEHVT2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPo[2NKSzVyPUKuO|k1PjRiIN88US=> NF3tOnZUSU6JRWK=
MHH-PREB-1 NGOxOpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJwOECxOlEhKM7:TR?= M1PoV3NCVkeHUh?=
SK-N-DZ MmrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2K1OmlEPTB;Mj64NVY{QCBizszN M33scXNCVkeHUh?=
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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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