Bosutinib (SKI-606) 化学構造
分子量: 530.45

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Quality Control & 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 MoXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwMEiyN|EhKM7:TR?= NW\4[5RqW0GQR1XS
SW756 NFPpNpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXwb3BKSzVyPUCuNVQxOjRiIN88US=> NIjlSJZUSU6JRWK=
CTV-1 M3rOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHYTWM2OD1yLkG2N|k5KCEQvF2= M172XHNCVkeHUh?=
HSC-4 M2PNemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwMUexOVghKM7:TR?= MnTMV2FPT0WU
LAMA-84 M2rV[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Lo[GlEPTB;MD6yPFY3PCBizszN NXLqdYxkW0GQR1XS
KU812 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnjWpFKSzVyPUCuN|QxPjhiIN88US=> M2rkV3NCVkeHUh?=
HCC1806 MoPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjLUYpjUUN3ME2wMlM2OjF4IDFOwG0> Mk\EV2FPT0WU
DOK M2LLVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXHTWM2OD1yLkO3O|g3KCEQvF2= MWfTRW5ITVJ?
NCI-H209 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwNEC4NFghKM7:TR?= MlXOV2FPT0WU
EoL-1-cell MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwNEG1O|YhKM7:TR?= Mn7KV2FPT0WU
H9 Mmm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\zUpNGUUN3ME2wMlQ{PDZ2IDFOwG0> MV;TRW5ITVJ?
EM-2 NF\jZXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwNEO4PUAh|ryP MmP5V2FPT0WU
NCI-H292 NFrKUnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XwSWlEPTB;MD60OFExQCBizszN MmLrV2FPT0WU
697 NYnnV|ZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfDfmxKSzVyPUCuOFU3OzNiIN88US=> MnHpV2FPT0WU
BHT-101 Mn\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnOTWM2OD1yLkS2OVkhKM7:TR?= MkLwV2FPT0WU
BE-13 M{HYU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHkRmh6UUN3ME2wMlQ5PTd{IDFOwG0> MkCwV2FPT0WU
RS4-11 NX3xUZdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwNEi1PFQhKM7:TR?= MWXTRW5ITVJ?
IGROV-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwNEi3PVchKM7:TR?= MVnTRW5ITVJ?
KE-37 NYPIcnQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfncpU2UUN3ME2wMlQ6PTB7IDFOwG0> MmPkV2FPT0WU
BV-173 M1HRZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mni0TWM2OD1yLkWwO|kzKCEQvF2= M1n4U3NCVkeHUh?=
MEG-01 MnPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwNUGyNVQhKM7:TR?= NY\WeZI2W0GQR1XS
LB2241-RCC NH2x[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XMVWlEPTB;MD61N|cyQCBizszN M3LJO3NCVkeHUh?=
ACHN MmDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwNUSwOlkhKM7:TR?= NWjaWlNUW0GQR1XS
CTB-1 M{nQZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmH2TWM2OD1yLkW0PFIhKM7:TR?= Ml[2V2FPT0WU
HT-1080 Ml\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPaWGNKSzVyPUCuOVU{PDliIN88US=> NX3XelRqW0GQR1XS
CHL-1 NW\iS|RXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HFS2lEPTB;MD61OVQ3PSBizszN M{fGZnNCVkeHUh?=
EW-3 NUDFPXptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrGOlNxUUN3ME2wMlU2QTN3IDFOwG0> MVPTRW5ITVJ?
ES1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwNke0PVghKM7:TR?= MkXhV2FPT0WU
KASUMI-1 MoHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rVNmlEPTB;MD63NlM{KCEQvF2= NFL6RWFUSU6JRWK=
SW13 MoL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\1TWM2OD1yLkezO|k5KCEQvF2= NXfOVIlDW0GQR1XS
A3-KAW MkHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPn[IJWUUN3ME2wMlc6OjB6IDFOwG0> NFm1TJJUSU6JRWK=
LB771-HNC M2S1OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoP4TWM2OD1yLkizNVA1KCEQvF2= NWCxWGs3W0GQR1XS
OC-314 MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwOE[5OlUhKM7:TR?= M{naOXNCVkeHUh?=
MLMA M1qzOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LEVWlEPTB;MD65NFY4PSBizszN NF3sXVdUSU6JRWK=
KARPAS-45 M3n3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrYW45KSzVyPUCuPVI1PjZiIN88US=> NH33fYtUSU6JRWK=
CAL-27 NFfmXWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvITWM2OD1yLkmyPVA3KCEQvF2= NIDXfFBUSU6JRWK=
SK-NEP-1 NELqTFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwOUeyOFghKM7:TR?= NFjpWYJUSU6JRWK=
COR-L105 NUTUXVM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLsTWM2OD1zLkCwN|k1KCEQvF2= NW\QOm9uW0GQR1XS
TI-73 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoK1TWM2OD1zLkCxOlUhKM7:TR?= MV;TRW5ITVJ?
JVM-3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGG4eJVKSzVyPUGuNFUxOTdiIN88US=> M3jXNXNCVkeHUh?=
HAL-01 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LRUGlEPTB;MT6wPFgyKCEQvF2= NHfKbW9USU6JRWK=
QIMR-WIL MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7Edmk3UUN3ME2xMlA6ODV6IDFOwG0> MY\TRW5ITVJ?
HSC-3 MofrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwMUG3PFMhKM7:TR?= NEHiPJRUSU6JRWK=
KY821 NYHydVU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PaXWlEPTB;MT6xN|M2OSBizszN NYT3dnh7W0GQR1XS
5637 NHKwUotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi1TWM2OD1zLkGzPFA{KCEQvF2= NFi5d49USU6JRWK=
CAL-33 NX[0PWNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDQTWM2OD1zLkG5N|AzKCEQvF2= MXzTRW5ITVJ?
ES4 NUjs[JByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTLO25KSzVyPUGuNlA4QSBizszN NYLHPWwyW0GQR1XS
BHY NULZTGZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3mdnBoUUN3ME2xMlIzQDl{IDFOwG0> NHTXcnNUSU6JRWK=
LB1047-RCC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPFTWM2OD1zLkKzO|g2KCEQvF2= NGfoUFNUSU6JRWK=
H4 M1fBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTTVGJRUUN3ME2xMlI1OjV3IDFOwG0> M2q5VnNCVkeHUh?=
RPMI-8866 M2rucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTFwMk[xNFYhKM7:TR?= M3zEXHNCVkeHUh?=
HO-1-N-1 NVe0dZVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jUZmlEPTB;MT6yOlM3QSBizszN NHL4RVNUSU6JRWK=
BB30-HNC M1\SWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DuUmlEPTB;MT6yPFcyPCBizszN MlrEV2FPT0WU
PC-14 NEPPRYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nBSWlEPTB;MT6yPVIxPSBizszN Ml\NV2FPT0WU
NUGC-3 M2HUbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzYdXI4UUN3ME2xMlI6OzV4IDFOwG0> Mnn6V2FPT0WU
A4-Fuk MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LqbWlEPTB;MT6zNFcxPCBizszN M37ZRnNCVkeHUh?=
MHH-NB-11 NH3sWFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml2yTWM2OD1zLkOxN|g{KCEQvF2= MWPTRW5ITVJ?
KOSC-2 MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37pdGlEPTB;MT6zNVc4PSBizszN M{DRZ3NCVkeHUh?=
A498 NXXjWHlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfqbph3UUN3ME2xMlQxOTF|IDFOwG0> NFiwN|lUSU6JRWK=
KG-1 NYnpSmU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvpTWM2OD1zLkSxNlc{KCEQvF2= M2\WNnNCVkeHUh?=
DEL MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37HVWlEPTB;MT60N|Y2PyBizszN NEDRZ2VUSU6JRWK=
EW-16 NXm2R5lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPJfolKSzVyPUGuOFM6PzNiIN88US=> M1\YbXNCVkeHUh?=
BPH-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f6NWlEPTB;MT60OFgxPSBizszN M3zpdXNCVkeHUh?=
JAR Mn;vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonrTWM2OD1zLkS5N|YhKM7:TR?= NFfEdWNUSU6JRWK=
J-RT3-T3-5 M4X2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIribW5KSzVyPUGuOVE4OjJiIN88US=> Mn7wV2FPT0WU
A375 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTFwNUG3O|IhKM7:TR?= NILL[5FUSU6JRWK=
SW954 NEXLPIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHW3UnZKSzVyPUGuOVUxODdiIN88US=> NXLCcY9RW0GQR1XS
Ca9-22 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTFwNU[yOkAh|ryP MmXoV2FPT0WU
D-566MG NXHrUYJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrvTWM2OD1zLkW3NVU2KCEQvF2= MUjTRW5ITVJ?
SCC-15 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwNkG4NFQhKM7:TR?= MoHGV2FPT0WU
HD-MY-Z NYXUNXNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XCPGlEPTB;MT62N|U5PCBizszN NXTPU|FqW0GQR1XS
HT-1376 Mlf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWyfXdYUUN3ME2xMlY1OzZiIN88US=> M2\UNHNCVkeHUh?=
CAL-54 NXPWOoc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn4XpdKSzVyPUGuOlU4ODliIN88US=> NVfN[FVXW0GQR1XS
ONS-76 MkHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrQV|ZKSzVyPUGuOlc2PTFiIN88US=> NUfxRlZQW0GQR1XS
EFO-27 M4jIfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFwNki5NkAh|ryP NIGxTmpUSU6JRWK=
769-P MkLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXyXohKSzVyPUGuOlk2QTZiIN88US=> NGTXNotUSU6JRWK=
MV-4-11 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwNkm4OVYhKM7:TR?= M3\HSnNCVkeHUh?=
NKM-1 M4\MTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jlbWlEPTB;MT63NVgxOiBizszN MXrTRW5ITVJ?
LOXIMVI NUDXWoJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPte|ZKSzVyPUGuO|Q2QTliIN88US=> MY\TRW5ITVJ?
KYSE-140 NGrQZ4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFwN{W2OVUhKM7:TR?= NV3xVWU1W0GQR1XS
ES5 MoPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\xTWM2OD1zLki2O|Q4KCEQvF2= NWTuRXQ2W0GQR1XS
BB65-RCC M3zqNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe4O5ZMUUN3ME2xMlg6QDR7IDFOwG0> NX6yZ5Z3W0GQR1XS
HN MmnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrFRnVYUUN3ME2xMlg6QDd2IDFOwG0> MlTqV2FPT0WU
A101D Ml7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[yTWM2OD1zLkmzOlI5KCEQvF2= MWrTRW5ITVJ?
LoVo Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFwOUe2O|khKM7:TR?= M{PPb3NCVkeHUh?=
NCI-H526 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETDfnlKSzVyPUGuPVk{OjViIN88US=> NXqxTnIyW0GQR1XS
NCI-H1693 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELKTHNKSzVyPUGuPVk5QDhiIN88US=> MoDFV2FPT0WU
OVCAR-4 MmfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7uTWM2OD1{LkCwOFM2KCEQvF2= MnrRV2FPT0WU
SK-HEP-1 M1OyOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVG4bYJSUUN3ME2yMlAxPzR3IDFOwG0> MXHTRW5ITVJ?
C2BBe1 M3vCVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTVTWM2OD1{LkCzN|czKCEQvF2= M1jHbXNCVkeHUh?=
MEL-JUSO NFTTOW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHPTnQ5UUN3ME2yMlA1PDZ2IDFOwG0> M4jEO3NCVkeHUh?=
MOLT-16 NVjBcphPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jEV2lEPTB;Mj6wO|A2QCBizszN MlyyV2FPT0WU
NBsusSR MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13h[WlEPTB;Mj6wPVg5QSBizszN NG\3OpVUSU6JRWK=
TK10 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVezW5NkUUN3ME2yMlE{PDV6IDFOwG0> MVHTRW5ITVJ?
CAL-39 NVPrWY91T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jkbWlEPTB;Mj6xOFQ5KCEQvF2= MUTTRW5ITVJ?
NCI-H2030 MknwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJwMUi5O|MhKM7:TR?= M2rp[HNCVkeHUh?=
HCT-116 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlziTWM2OD1{LkKyPVg1KCEQvF2= MnT4V2FPT0WU
HTC-C3 M1GyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jET2lEPTB;Mj6yOlgzPCBizszN MUTTRW5ITVJ?
TYK-nu MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTJwM{C5NFkhKM7:TR?= M3;m[nNCVkeHUh?=
FADU NELOVllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPIVnhUUUN3ME2yMlMzOjl4IDFOwG0> MVPTRW5ITVJ?
A431 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzGTGxKSzVyPUKuN|cxOjViIN88US=> MX;TRW5ITVJ?
TE-11 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvifINKSzVyPUKuN|gxOTliIN88US=> NXzm[IZ2W0GQR1XS
CAL-12T Mn\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HpbGlEPTB;Mj60NFQyPyBizszN MWHTRW5ITVJ?
DB MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknoTWM2OD1{LkSyPFY6KCEQvF2= M2PXdXNCVkeHUh?=
L-363 NESzVnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU[2U5FyUUN3ME2yMlQ{PTB5IDFOwG0> M3m1THNCVkeHUh?=
MSTO-211H MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTMXoJZUUN3ME2yMlY3OzlzIDFOwG0> NYfDd|NZW0GQR1XS
SK-UT-1 NGDkbHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D0RWlEPTB;Mj63NVQxPiBizszN NVPacolJW0GQR1XS
RPMI-8226 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13LZmlEPTB;Mj63N|E3PCBizszN NV\jRVhQW0GQR1XS
SF295 NF3oR5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXrTWM2OD1{Lke0N|EhKM7:TR?= NVXiVZdwW0GQR1XS
OS-RC-2 NVHtVnJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTJwN{[2O|MhKM7:TR?= M1XrOnNCVkeHUh?=
SK-MEL-24 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvaeWlKSzVyPUKuO|gzOjRiIN88US=> NYPFeFZYW0GQR1XS
COR-L23 NWS1ZottT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWX1WJpIUUN3ME2yMlc6PDZ2IDFOwG0> MXjTRW5ITVJ?
MHH-PREB-1 NXnXfnNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjnS4xKSzVyPUKuPFAyPjFiIN88US=> NVrjfoxsW0GQR1XS
SK-N-DZ NV3Te49wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTnTWM2OD1{LkixOlM5KCEQvF2= NIGxOZJUSU6JRWK=
OMC-1 MnPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJwOEWwNFMhKM7:TR?= MV\TRW5ITVJ?
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NCI-H69 NV;nR2xXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTNyLk[wPVMhKM7:TR?= NX3wOYhoW0GQR1XS
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CAL-120 NG\HZoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzmUZFKSzVyPUOyMlQ{OTdiIN88US=> M3nRRXNCVkeHUh?=
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NCI-H1304 NH[5dIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTN|LkCzOVQhKM7:TR?= MnXJV2FPT0WU
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RMG-I Mn3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mme4TWM2OD1|Mz60Nlg2KCEQvF2= Mnf5V2FPT0WU
LU-65 MljUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPR[ZRKSzVyPUO0MlE1ODhiIN88US=> NVHVeYV4W0GQR1XS
GB-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoX5TWM2OD1|NT6wO|I6KCEQvF2= NF7TfYxUSU6JRWK=
DU-4475 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\CTWM2OD1|NT6xOVU{KCEQvF2= M4LmZnNCVkeHUh?=
SBC-5 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHrfHRKSzVyPUO2MlU6ODJiIN88US=> NW\tW4l5W0GQR1XS
OE33 NEfYWndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDzTWM2OD1|Nz63OVc4KCEQvF2= M2fYdHNCVkeHUh?=
C8166 MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4mwTGlEPTB;M{iuOVI3PyBizszN MYnTRW5ITVJ?
COLO-684 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHLN5FKSzVyPUO4Mlc1OjhiIN88US=> MkX2V2FPT0WU
NCI-H1155 NGTBWnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3VTWM2OD1|OT6wOFcyKCEQvF2= NXLhRmhUW0GQR1XS
ATN-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\Ib5g2UUN3ME2zPU44Pzl{IDFOwG0> MUPTRW5ITVJ?
KARPAS-299 M1e3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDXepBKSzVyPUO5Mlg{QSBizszN NYfzU2Q3W0GQR1XS
KNS-81-FD NW\qR|dyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorRTWM2OD12MD6zOlA1KCEQvF2= MVPTRW5ITVJ?
NCI-H1563 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW2OJRKSzVyPUSxMlUxOzliIN88US=> NHLIZpJUSU6JRWK=
NB14 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PiS2lEPTB;NEKuO|I3OyBizszN MUjTRW5ITVJ?
COLO-800 NH7SOoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTR{Lki1NVchKM7:TR?= NFLiUFRUSU6JRWK=
MS-1 NIDkS5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH6zTHJKSzVyPUSzMlA1QDNiIN88US=> NXTyWVhTW0GQR1XS
OVCAR-8 MonzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvOTWM2OD12Mz62PFA6KCEQvF2= M{LScHNCVkeHUh?=
SK-PN-DW NHG4N2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmi1TWM2OD12Mz64O|c3KCEQvF2= M3nI[3NCVkeHUh?=
G-402 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTR|LkmwNFYhKM7:TR?= MUfTRW5ITVJ?
NCI-H2291 NE[wemtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\OTWM2OD12ND64NFE4KCEQvF2= M{PINnNCVkeHUh?=
PC-3 MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLVZ4JKSzVyPUS1MlgxOjNiIN88US=> NHywUWlUSU6JRWK=
NCI-H1581 Mn;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTR[ItKSzVyPUS1Mlk5QDliIN88US=> NHe0NXdUSU6JRWK=
SW1116 NYn4OYdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWKzcIxzUUN3ME20O{4xOTh{IDFOwG0> NW\MfJdqW0GQR1XS
ZR-75-30 M2OyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfjXY1tUUN3ME20O{4xOjN7IDFOwG0> NX;M[IZMW0GQR1XS
OCI-AML2 NFu1NGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjRTY9jUUN3ME20O{4xQTF6IDFOwG0> MoT2V2FPT0WU
MDA-MB-231 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;SZpNlUUN3ME20O{43OjR7IDFOwG0> NUfBWlYyW0GQR1XS
ES3 M2D3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHjPXVKSzVyPUS4MlM2OjliIN88US=> MXzTRW5ITVJ?
NCI-H630 NVXSVIN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fCU2lEPTB;NEmuNVc1OiBizszN MXfTRW5ITVJ?
OE19 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEe4bpdKSzVyPUS5MlI6ODJiIN88US=> Ml7nV2FPT0WU
NCI-H1573 M4fLUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWe1b2d2UUN3ME20PU43QDZzIDFOwG0> Mo\nV2FPT0WU
EW-1 NXu4O|JTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTR7LkmwPFQhKM7:TR?= NIG5b4hUSU6JRWK=

... 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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (188.51 mM)
エタノール 2 mg/mL (3.77 mM)
<1 mg/mL (<1 mM)
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)

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