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 M1;jbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXmTY9KSzVyPUCuNFgzOzFiIN88US=> NFXy[FZUSU6JRWK=
SW756 NV;i[WNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwMUSwNlQhKM7:TR?= NFPOdGVUSU6JRWK=
CTV-1 NWS5Z4NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfSTWM2OD1yLkG2N|k5KCEQvF2= NEDoeWxUSU6JRWK=
HSC-4 NX7LOIpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DVS2lEPTB;MD6xO|E2QCBizszN MXnTRW5ITVJ?
LAMA-84 Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfiTWM2OD1yLkK4OlY1KCEQvF2= MX;TRW5ITVJ?
KU812 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwM{SwOlghKM7:TR?= M{DPPXNCVkeHUh?=
HCC1806 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLmTWM2OD1yLkO1NlE3KCEQvF2= M17zR3NCVkeHUh?=
DOK NXX2fm9qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTVeJdKSzVyPUCuN|c4QDZiIN88US=> MmnTV2FPT0WU
NCI-H209 NGXaWpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwNEC4NFghKM7:TR?= NXzUT3BxW0GQR1XS
EoL-1-cell MljtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\qUIlKSzVyPUCuOFE2PzZiIN88US=> NHvCRXdUSU6JRWK=
H9 NFLPOYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIe3VGRKSzVyPUCuOFM1PjRiIN88US=> MV\TRW5ITVJ?
EM-2 MoTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;OfWlEPTB;MD60N|g6KCEQvF2= NYrIOmI3W0GQR1XS
NCI-H292 MonES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;Ud2VGUUN3ME2wMlQ1OTB6IDFOwG0> MUnTRW5ITVJ?
697 M2jxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwNEW2N|MhKM7:TR?= M2[3OHNCVkeHUh?=
BHT-101 NG\CdoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInrfJNKSzVyPUCuOFY2QSBizszN M2rrd3NCVkeHUh?=
BE-13 MorYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjsXlREUUN3ME2wMlQ5PTd{IDFOwG0> NVTLPIxKW0GQR1XS
RS4-11 NVTBRnZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:zUY1MUUN3ME2wMlQ5PTh2IDFOwG0> NVnqO4xLW0GQR1XS
IGROV-1 MnW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT6TWM2OD1yLkS4O|k4KCEQvF2= MY\TRW5ITVJ?
KE-37 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1O0e2lEPTB;MD60PVUxQSBizszN NHXHXoVUSU6JRWK=
BV-173 MnzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlq3TWM2OD1yLkWwO|kzKCEQvF2= MWTTRW5ITVJ?
MEG-01 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPVT3RqUUN3ME2wMlUyOjF2IDFOwG0> NUjuNIlIW0GQR1XS
LB2241-RCC MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojOTWM2OD1yLkWzO|E5KCEQvF2= NF62eZBUSU6JRWK=
ACHN MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwNUSwOlkhKM7:TR?= NYHSToxFW0GQR1XS
CTB-1 Ml\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\zWGlEPTB;MD61OFgzKCEQvF2= M3LP[nNCVkeHUh?=
HT-1080 NXnXbGdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHEfWlKSzVyPUCuOVU{PDliIN88US=> NGTGXVlUSU6JRWK=
CHL-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLOTWM2OD1yLkW1OFY2KCEQvF2= MoPpV2FPT0WU
EW-3 NWrBVYt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3WeFBKSzVyPUCuOVU6OzViIN88US=> NVLW[HVoW0GQR1XS
ES1 MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwNke0PVghKM7:TR?= M4\BbHNCVkeHUh?=
KASUMI-1 MoLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwN{KzN{Ah|ryP MVTTRW5ITVJ?
SW13 NHPJVpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwN{O3PVghKM7:TR?= NUnGcWY3W0GQR1XS
A3-KAW NELqSHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7GTWM2OD1yLke5NlA5KCEQvF2= M4DlN3NCVkeHUh?=
LB771-HNC M3zGS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYT5d41sUUN3ME2wMlg{OTB2IDFOwG0> M1zhT3NCVkeHUh?=
OC-314 Mn\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwOE[5OlUhKM7:TR?= MkSxV2FPT0WU
MLMA M1\aOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTpbJRKSzVyPUCuPVA3PzViIN88US=> MV7TRW5ITVJ?
KARPAS-45 NIH3UFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIKxcndKSzVyPUCuPVI1PjZiIN88US=> NIr5fpVUSU6JRWK=
CAL-27 MlHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwOUK5NFYhKM7:TR?= NFnEflNUSU6JRWK=
SK-NEP-1 NIHXdZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTBwOUeyOFghKM7:TR?= Mme4V2FPT0WU
COR-L105 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFwMECzPVQhKM7:TR?= MYPTRW5ITVJ?
TI-73 NV;3VppOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrPTVZ2UUN3ME2xMlAyPjViIN88US=> MVHTRW5ITVJ?
JVM-3 NXvZUIlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TwW2lEPTB;MT6wOVAyPyBizszN MojOV2FPT0WU
HAL-01 NWPEPFZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTFwMEi4NUAh|ryP NG\LeVBUSU6JRWK=
QIMR-WIL M2\SfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4[wTGlEPTB;MT6wPVA2QCBizszN MYfTRW5ITVJ?
HSC-3 M{niZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTFwMUG3PFMhKM7:TR?= MXnTRW5ITVJ?
KY821 NVPycZJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwMUOzOVEhKM7:TR?= MmXZV2FPT0WU
5637 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoryTWM2OD1zLkGzPFA{KCEQvF2= MVzTRW5ITVJ?
CAL-33 MmTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3qUG9GUUN3ME2xMlE6OzB{IDFOwG0> NYLZN3Y2W0GQR1XS
ES4 NID1foVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFwMkC3PUAh|ryP MnzhV2FPT0WU
BHY NITTbG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojTTWM2OD1zLkKyPFkzKCEQvF2= M1XRdHNCVkeHUh?=
LB1047-RCC M2Cxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPsclZSUUN3ME2xMlI{Pzh3IDFOwG0> Mo[xV2FPT0WU
H4 Mn:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGOxR2NKSzVyPUGuNlQzPTViIN88US=> NVvmfo56W0GQR1XS
RPMI-8866 Ml7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv5TWM2OD1zLkK2NVA3KCEQvF2= Mmr5V2FPT0WU
HO-1-N-1 NF7ueZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrhTWM2OD1zLkK2N|Y6KCEQvF2= Ml3wV2FPT0WU
BB30-HNC MlX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWCxWpNoUUN3ME2xMlI5PzF2IDFOwG0> M3rSbXNCVkeHUh?=
PC-14 NFvl[HNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPr[5JKSzVyPUGuNlkzODViIN88US=> MXvTRW5ITVJ?
NUGC-3 M2rlVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7pZppKSzVyPUGuNlk{PTZiIN88US=> NUjGWohYW0GQR1XS
A4-Fuk Ml7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;FXnlRUUN3ME2xMlMxPzB2IDFOwG0> MkfqV2FPT0WU
MHH-NB-11 NIGwb3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjLTWM2OD1zLkOxN|g{KCEQvF2= NIjpfGxUSU6JRWK=
KOSC-2 M{m5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVriWXNYUUN3ME2xMlMyPzd3IDFOwG0> M4DIUHNCVkeHUh?=
A498 NUnhV4Z3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;rVmlKSzVyPUGuOFAyOTNiIN88US=> M1XaeXNCVkeHUh?=
KG-1 NHq3RoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWT4NHg4UUN3ME2xMlQyOjd|IDFOwG0> MljJV2FPT0WU
DEL M{PhXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDvTWM2OD1zLkSzOlU4KCEQvF2= NUKyeoc4W0GQR1XS
EW-16 M3nqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfVe4JYUUN3ME2xMlQ{QTd|IDFOwG0> M1rpWnNCVkeHUh?=
BPH-1 M2LiNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwNES4NFUhKM7:TR?= NXvzfnBUW0GQR1XS
JAR M2PRS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFi5fFdKSzVyPUGuOFk{PiBizszN MlnsV2FPT0WU
J-RT3-T3-5 NWnzVJU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTFwNUG3NlIhKM7:TR?= NHfUOpRUSU6JRWK=
A375 NXzY[oE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[wUmJKSzVyPUGuOVE4PzJiIN88US=> MmKyV2FPT0WU
SW954 NIOwWFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUCzXFk4UUN3ME2xMlU2ODB5IDFOwG0> M4jpTnNCVkeHUh?=
Ca9-22 MmTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4WwR2lEPTB;MT61OlI3KCEQvF2= MYDTRW5ITVJ?
D-566MG NIT6NZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHm5bJdKSzVyPUGuOVcyPTViIN88US=> NIjzUlNUSU6JRWK=
SCC-15 NHz6PVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\MWGlEPTB;MT62NVgxPCBizszN NWnoeXBqW0GQR1XS
HD-MY-Z NXzqTYZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDUTWM2OD1zLk[zOVg1KCEQvF2= MUXTRW5ITVJ?
HT-1376 Mn\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjJTWM2OD1zLk[0N|YhKM7:TR?= MmXwV2FPT0WU
CAL-54 MoTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\QVXNIUUN3ME2xMlY2PzB7IDFOwG0> M3TPR3NCVkeHUh?=
ONS-76 M4T4WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWniN2RSUUN3ME2xMlY4PTVzIDFOwG0> NVf4WYxCW0GQR1XS
EFO-27 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7qTWM2OD1zLk[4PVIhKM7:TR?= MnLGV2FPT0WU
769-P NEPkfGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3KzPWlEPTB;MT62PVU6PiBizszN MVnTRW5ITVJ?
MV-4-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPZcotZUUN3ME2xMlY6QDV4IDFOwG0> M3XiSHNCVkeHUh?=
NKM-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW0TZoyUUN3ME2xMlcyQDB{IDFOwG0> MlTCV2FPT0WU
LOXIMVI NYL0R3JuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTQTWM2OD1zLke0OVk6KCEQvF2= NUeyd5Z2W0GQR1XS
KYSE-140 Mn\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;jTWM2OD1zLke1OlU2KCEQvF2= NEDk[ldUSU6JRWK=
ES5 NXvLTotNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTVUolVUUN3ME2xMlg3PzR5IDFOwG0> NUHibGFZW0GQR1XS
BB65-RCC NH7FfXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrpR3RKSzVyPUGuPFk5PDliIN88US=> NUTuVZBVW0GQR1XS
HN M2X4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17KNmlEPTB;MT64PVg4PCBizszN MYDTRW5ITVJ?
A101D MonLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml2wTWM2OD1zLkmzOlI5KCEQvF2= MXHTRW5ITVJ?
LoVo M{i0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwOUe2O|khKM7:TR?= MlO0V2FPT0WU
NCI-H526 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2ryVGlEPTB;MT65PVMzPSBizszN NVr0VXBSW0GQR1XS
NCI-H1693 M33aXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULxR|BKUUN3ME2xMlk6QDh6IDFOwG0> NXXmdmVnW0GQR1XS
OVCAR-4 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjlTWM2OD1{LkCwOFM2KCEQvF2= M{DDXnNCVkeHUh?=
SK-HEP-1 M1;kcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;3bIU1UUN3ME2yMlAxPzR3IDFOwG0> Ml;1V2FPT0WU
C2BBe1 NYPiO2RPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTJwMEOzO|IhKM7:TR?= MVPTRW5ITVJ?
MEL-JUSO NILHZWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rC[2lEPTB;Mj6wOFQ3PCBizszN M135cHNCVkeHUh?=
MOLT-16 NELZS|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\2flJ7UUN3ME2yMlA4ODV6IDFOwG0> MXjTRW5ITVJ?
NBsusSR MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[zTWM2OD1{LkC5PFg6KCEQvF2= M1qyWnNCVkeHUh?=
TK10 NHzZNYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDuTWM2OD1{LkGzOFU5KCEQvF2= M4HQZ3NCVkeHUh?=
CAL-39 MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTvTJpKSzVyPUKuNVQ1QCBizszN M3uxW3NCVkeHUh?=
NCI-H2030 M4TFVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MormTWM2OD1{LkG4PVc{KCEQvF2= MYLTRW5ITVJ?
HCT-116 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj0RY1KSzVyPUKuNlI6QDRiIN88US=> NVq5e|QxW0GQR1XS
HTC-C3 NYXmO2VqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPHT49KSzVyPUKuNlY5OjRiIN88US=> NFSy[oNUSU6JRWK=
TYK-nu MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXwTWM2OD1{LkOwPVA6KCEQvF2= MWHTRW5ITVJ?
FADU M{LURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:0emwzUUN3ME2yMlMzOjl4IDFOwG0> MXjTRW5ITVJ?
A431 MnPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTJwM{ewNlUhKM7:TR?= MYPTRW5ITVJ?
TE-11 M1XqWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXzdodoUUN3ME2yMlM5ODF7IDFOwG0> Mm\rV2FPT0WU
CAL-12T M2[4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;ifIo2UUN3ME2yMlQxPDF5IDFOwG0> Mn;iV2FPT0WU
DB M3Tx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHroR45KSzVyPUKuOFI5PjliIN88US=> MXHTRW5ITVJ?
L-363 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rUbWlEPTB;Mj60N|UxPyBizszN Mn7LV2FPT0WU
MSTO-211H NIPMeZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLFTWM2OD1{Lk[2N|kyKCEQvF2= M1\lSnNCVkeHUh?=
SK-UT-1 NH\HSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXOzW2c2UUN3ME2yMlcyPDB4IDFOwG0> MYXTRW5ITVJ?
RPMI-8226 NFjkfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3a[4FKSzVyPUKuO|MyPjRiIN88US=> M3XScnNCVkeHUh?=
SF295 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHToUXpKSzVyPUKuO|Q{OSBizszN NYTyW|FtW0GQR1XS
OS-RC-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;sfFNYUUN3ME2yMlc3Pjd|IDFOwG0> MVnTRW5ITVJ?
SK-MEL-24 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPwUI9yUUN3ME2yMlc5OjJ2IDFOwG0> NH[xc5JUSU6JRWK=
COR-L23 MlP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLBU5h[UUN3ME2yMlc6PDZ2IDFOwG0> M1vzVHNCVkeHUh?=
MHH-PREB-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfhR4VKSzVyPUKuPFAyPjFiIN88US=> NXXJcpNYW0GQR1XS
SK-N-DZ MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LvSGlEPTB;Mj64NVY{QCBizszN NV[4cXE2W0GQR1XS
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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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