Bosutinib (SKI-606)

Licensed by Pfizer 製品コードS1014

Bosutinib (SKI-606)化学構造

分子量(MW):530.45

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。

サイズ 価格(税別) 在庫  
JPY 15106.00 あり
JPY 11620.00 あり
JPY 44820.00 あり

カスタマーフィードバック(4)

  • 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.

製品安全説明書

Src阻害剤の選択性比較

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
Abl [2]
(Cell-free assay)
Src [1]
(Cell-free assay)
1 nM 1.2 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB7 M2HTZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;TOmlEPTB;MD6wPFI{OSBizszN MXLTRW5ITVJ?
SW756 MnPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fWNGlEPTB;MD6xOFAzPCBizszN MUTTRW5ITVJ?
CTV-1 M2PNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTBwMU[zPVghKM7:TR?= MUDTRW5ITVJ?
HSC-4 NH7ieJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ixPWlEPTB;MD6xO|E2QCBizszN NVX0XWZWW0GQR1XS
LAMA-84 NGTTUZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELMclNKSzVyPUCuNlg3PjRiIN88US=> MVPTRW5ITVJ?
KU812 M4fCc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHCblFKSzVyPUCuN|QxPjhiIN88US=> MYHTRW5ITVJ?
HCC1806 NYXvXJpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HlfGlEPTB;MD6zOVIyPiBizszN NE\ZSWtUSU6JRWK=
DOK MmSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljzTWM2OD1yLkO3O|g3KCEQvF2= NETCSVNUSU6JRWK=
NCI-H209 MnHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwNEC4NFghKM7:TR?= NYTWcVBsW0GQR1XS
EoL-1-cell MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILrWJRKSzVyPUCuOFE2PzZiIN88US=> MkPyV2FPT0WU
H9 NHTSVFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnXN5ZnUUN3ME2wMlQ{PDZ2IDFOwG0> NFXrUmNUSU6JRWK=
EM-2 NH20dVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwNEO4PUAh|ryP MXHTRW5ITVJ?
NCI-H292 M2rUOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwNESxNFghKM7:TR?= NYrZ[|MxW0GQR1XS
697 M3fHRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi2[WJKSzVyPUCuOFU3OzNiIN88US=> MWrTRW5ITVJ?
BHT-101 NGe5c2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fKS2lEPTB;MD60OlU6KCEQvF2= MYTTRW5ITVJ?
BE-13 NYC1fIZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;j[pRNUUN3ME2wMlQ5PTd{IDFOwG0> MXHTRW5ITVJ?
RS4-11 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWzTWM2OD1yLkS4OVg1KCEQvF2= NVX3[nlLW0GQR1XS
IGROV-1 NXXxcGJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwNEi3PVchKM7:TR?= MVnTRW5ITVJ?
KE-37 MmXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwNEm1NFkhKM7:TR?= MVvTRW5ITVJ?
BV-173 NIjkbWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPHTWM2OD1yLkWwO|kzKCEQvF2= M2D4V3NCVkeHUh?=
MEG-01 M1n4VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInzb2JKSzVyPUCuOVEzOTRiIN88US=> MVTTRW5ITVJ?
LB2241-RCC MlLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\LVWlEPTB;MD61N|cyQCBizszN NFjQcHdUSU6JRWK=
ACHN NUCzbGs1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTBwNUSwOlkhKM7:TR?= NWHyW4lkW0GQR1XS
CTB-1 M3K5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjwS3lKSzVyPUCuOVQ5OiBizszN MVLTRW5ITVJ?
HT-1080 NYm3c49DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXTTWM2OD1yLkW1N|Q6KCEQvF2= M3u2[nNCVkeHUh?=
CHL-1 NX;kUZlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPjTHFKSzVyPUCuOVU1PjViIN88US=> MY\TRW5ITVJ?
EW-3 NG[wZVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M321bWlEPTB;MD61OVk{PSBizszN MorqV2FPT0WU
ES1 M3XKUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwNke0PVghKM7:TR?= MlTGV2FPT0WU
KASUMI-1 MmjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjmOYVKSzVyPUCuO|I{OyBizszN NYLnSY5YW0GQR1XS
SW13 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3mxdGlEPTB;MD63N|c6QCBizszN NUj3XXlmW0GQR1XS
A3-KAW M4fnNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwN{myNFghKM7:TR?= NWnMVGZ[W0GQR1XS
LB771-HNC M2HEZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzXTWM2OD1yLkizNVA1KCEQvF2= MmrYV2FPT0WU
OC-314 NHH5bnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4W1TWlEPTB;MD64Olk3PSBizszN MVjTRW5ITVJ?
MLMA NVrMUVE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfpTWM2OD1yLkmwOlc2KCEQvF2= Mlq3V2FPT0WU
KARPAS-45 NXnabIVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoriTWM2OD1yLkmyOFY3KCEQvF2= NWrPdYhwW0GQR1XS
CAL-27 NXT2WVFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXWZWFKSzVyPUCuPVI6ODZiIN88US=> MVrTRW5ITVJ?
SK-NEP-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjRdoxuUUN3ME2wMlk4OjR6IDFOwG0> NEOwc2dUSU6JRWK=
COR-L105 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfEWHVkUUN3ME2xMlAxOzl2IDFOwG0> NED3XoVUSU6JRWK=
TI-73 M1\5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf3[YhKSzVyPUGuNFE3PSBizszN M3LKfHNCVkeHUh?=
JVM-3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTFwMEWwNVchKM7:TR?= NXTlXo9kW0GQR1XS
HAL-01 MkjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q2PWlEPTB;MT6wPFgyKCEQvF2= MWPTRW5ITVJ?
QIMR-WIL MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjqTIhGUUN3ME2xMlA6ODV6IDFOwG0> MoPGV2FPT0WU
HSC-3 MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTFwMUG3PFMhKM7:TR?= NHT5WWxUSU6JRWK=
KY821 M1PoPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTFwMUOzOVEhKM7:TR?= NFX4eWNUSU6JRWK=
5637 NXrs[VFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjaU5ZYUUN3ME2xMlE{QDB|IDFOwG0> NUPyTFJMW0GQR1XS
CAL-33 NYXQNVVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlntTWM2OD1zLkG5N|AzKCEQvF2= M{Oxe3NCVkeHUh?=
ES4 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[xd5d5UUN3ME2xMlIxPzliIN88US=> M4TUc3NCVkeHUh?=
BHY NFniTHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFwMkK4PVIhKM7:TR?= Mn;JV2FPT0WU
LB1047-RCC MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTMTWM2OD1zLkKzO|g2KCEQvF2= NEPD[|NUSU6JRWK=
H4 M1XkcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWftfnN[UUN3ME2xMlI1OjV3IDFOwG0> M3LjSnNCVkeHUh?=
RPMI-8866 MlnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXKzNlFiUUN3ME2xMlI3OTB4IDFOwG0> MU\TRW5ITVJ?
HO-1-N-1 NYnDVJhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrlVoI{UUN3ME2xMlI3OzZ7IDFOwG0> Mk[1V2FPT0WU
BB30-HNC NVXq[HF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\NXWlEPTB;MT6yPFcyPCBizszN NXjyZ3pyW0GQR1XS
PC-14 MkWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH2TWM2OD1zLkK5NlA2KCEQvF2= MkfLV2FPT0WU
NUGC-3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFwMkmzOVYhKM7:TR?= MlLjV2FPT0WU
A4-Fuk Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjhO4xKSzVyPUGuN|A4ODRiIN88US=> MUfTRW5ITVJ?
MHH-NB-11 NUXzdIpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TCfGlEPTB;MT6zNVM5OyBizszN NIXBN41USU6JRWK=
KOSC-2 MmPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnqyTWM2OD1zLkOxO|c2KCEQvF2= MlznV2FPT0WU
A498 NUfaSGxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmO2TWM2OD1zLkSwNVE{KCEQvF2= NYq5SIlSW0GQR1XS
KG-1 NUHZOIdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO3N4RMUUN3ME2xMlQyOjd|IDFOwG0> Mmr5V2FPT0WU
DEL MoDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFP1e49KSzVyPUGuOFM3PTdiIN88US=> NHLXOoxUSU6JRWK=
EW-16 NH7nSpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTFwNEO5O|MhKM7:TR?= NF;QNGFUSU6JRWK=
BPH-1 Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfOZ4xKSzVyPUGuOFQ5ODViIN88US=> MnrZV2FPT0WU
JAR NWfOclVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[4TWM2OD1zLkS5N|YhKM7:TR?= NIPJOYVUSU6JRWK=
J-RT3-T3-5 MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zUT2lEPTB;MT61NVczOiBizszN NEjJd2NUSU6JRWK=
A375 M{\VVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrqTWM2OD1zLkWxO|czKCEQvF2= NXjK[XZbW0GQR1XS
SW954 Mki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2S5O2lEPTB;MT61OVAxPyBizszN NHPwdohUSU6JRWK=
Ca9-22 NH63SmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\U[FJKSzVyPUGuOVYzPiBizszN M1rSZnNCVkeHUh?=
D-566MG Mnf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTFwNUexOVUhKM7:TR?= Mo\MV2FPT0WU
SCC-15 NIPPZ4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPGOnhKSzVyPUGuOlE5ODRiIN88US=> Mn\0V2FPT0WU
HD-MY-Z MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHRcVdKSzVyPUGuOlM2QDRiIN88US=> NWn0NIZqW0GQR1XS
HT-1376 MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTFwNkSzOkAh|ryP MoXwV2FPT0WU
CAL-54 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmiwTWM2OD1zLk[1O|A6KCEQvF2= NUT2XG1xW0GQR1XS
ONS-76 M4rt[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIe5TmtKSzVyPUGuOlc2PTFiIN88US=> NETZOYJUSU6JRWK=
EFO-27 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTFwNki5NkAh|ryP NFL0fGtUSU6JRWK=
769-P M1y3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XQV2lEPTB;MT62PVU6PiBizszN MXzTRW5ITVJ?
MV-4-11 M1m1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfjU3V[UUN3ME2xMlY6QDV4IDFOwG0> MkTSV2FPT0WU
NKM-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTFwN{G4NFIhKM7:TR?= MWnTRW5ITVJ?
LOXIMVI MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTFwN{S1PVkhKM7:TR?= NXizT3R2W0GQR1XS
KYSE-140 NVLoXWFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHiTWM2OD1zLke1OlU2KCEQvF2= NHjO[IdUSU6JRWK=
ES5 MonIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTFwOE[3OFchKM7:TR?= M2DsbnNCVkeHUh?=
BB65-RCC NYXVT41lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzSelJKSzVyPUGuPFk5PDliIN88US=> NWHxfJFlW0GQR1XS
HN NGj6Zo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DSTmlEPTB;MT64PVg4PCBizszN MU\TRW5ITVJ?
A101D NXKwfGduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTFwOUO2NlghKM7:TR?= NHzrSJRUSU6JRWK=
LoVo M3PnPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LFXmlEPTB;MT65O|Y4QSBizszN NIjBUXpUSU6JRWK=
NCI-H526 M4jYe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHy[WVKSzVyPUGuPVk{OjViIN88US=> NFr5b3FUSU6JRWK=
NCI-H1693 NYGxbHhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn1TWM2OD1zLkm5PFg5KCEQvF2= NIPJbHRUSU6JRWK=
OVCAR-4 MmnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXO4ZW9IUUN3ME2yMlAxPDN3IDFOwG0> NX;HWoRVW0GQR1XS
SK-HEP-1 NVzxSWoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly3TWM2OD1{LkCwO|Q2KCEQvF2= M3vJfnNCVkeHUh?=
C2BBe1 NY\ESVZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M16z[2lEPTB;Mj6wN|M4OiBizszN NUHUfWk{W0GQR1XS
MEL-JUSO NE\YWHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\0TWM2OD1{LkC0OFY1KCEQvF2= NFHkb21USU6JRWK=
MOLT-16 MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HnSGlEPTB;Mj6wO|A2QCBizszN NV7MNnpLW0GQR1XS
NBsusSR NWTRPWZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DGW2lEPTB;Mj6wPVg5QSBizszN MYrTRW5ITVJ?
TK10 NX\PdnRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XISmlEPTB;Mj6xN|Q2QCBizszN MWHTRW5ITVJ?
CAL-39 M{C0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TLNmlEPTB;Mj6xOFQ5KCEQvF2= M3L4SnNCVkeHUh?=
NCI-H2030 MkXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJwMUi5O|MhKM7:TR?= MV;TRW5ITVJ?
HCT-116 MmPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn5R5pVUUN3ME2yMlIzQTh2IDFOwG0> M2T2XnNCVkeHUh?=
HTC-C3 NWi5UGZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33UWmlEPTB;Mj6yOlgzPCBizszN M{TGfHNCVkeHUh?=
TYK-nu M1Tnc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLVTZBKSzVyPUKuN|A6ODliIN88US=> NEmyOIhUSU6JRWK=
FADU NVThSVV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j3ZmlEPTB;Mj6zNlI6PiBizszN M2TRRnNCVkeHUh?=
A431 MmrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HETWlEPTB;Mj6zO|AzPSBizszN M4[xTXNCVkeHUh?=
TE-11 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYm5XmdQUUN3ME2yMlM5ODF7IDFOwG0> M2fXN3NCVkeHUh?=
CAL-12T MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlq2TWM2OD1{LkSwOFE4KCEQvF2= MWPTRW5ITVJ?
DB Mlf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rkPGlEPTB;Mj60Nlg3QSBizszN Mm\jV2FPT0WU
L-363 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTJwNEO1NFchKM7:TR?= MWrTRW5ITVJ?
MSTO-211H M2\wT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXDPHNKSzVyPUKuOlY{QTFiIN88US=> MUHTRW5ITVJ?
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MC116 NV;re3hqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvCd3dKSzVyPUOwMlA4OzNiIN88US=> MWHTRW5ITVJ?
NCI-H69 M3H3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFm1dpFKSzVyPUOwMlYxQTNiIN88US=> NGLE[HJUSU6JRWK=
NB6 NGrXW5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTNzLkO2NlkhKM7:TR?= NILIN|lUSU6JRWK=
CAL-120 NF7SeXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTN{LkSzNVchKM7:TR?= MV3TRW5ITVJ?
U-87-MG NFG3OJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvUTWM2OD1|Mz6wNlUyKCEQvF2= NUTLOHRHW0GQR1XS
NCI-H1304 M3zJT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX3bmhKSzVyPUOzMlA{PTRiIN88US=> NHTxbGxUSU6JRWK=
YH-13 NEfUfpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTN|LkK1N|UhKM7:TR?= NVzjWlllW0GQR1XS
RMG-I M{nESGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfZd3ljUUN3ME2zN{41Ojh3IDFOwG0> MmLBV2FPT0WU
LU-65 NHjSenFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTke4NbUUN3ME2zOE4yPDB6IDFOwG0> MUjTRW5ITVJ?
GB-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3OcphKSzVyPUO1MlA4OjliIN88US=> MkfpV2FPT0WU
DU-4475 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4n5SGlEPTB;M{WuNVU2OyBizszN Ml\3V2FPT0WU
SBC-5 Moe1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zkOGlEPTB;M{[uOVkxOiBizszN NWPIRnhoW0GQR1XS
OE33 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTN5Lke1O|chKM7:TR?= NFf0UZRUSU6JRWK=
C8166 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjWZ3dIUUN3ME2zPE42OjZ5IDFOwG0> NInO[WhUSU6JRWK=
COLO-684 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLiTWM2OD1|OD63OFI5KCEQvF2= M4\zfnNCVkeHUh?=
NCI-H1155 M3fkSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTN7LkC0O|EhKM7:TR?= MkTDV2FPT0WU
ATN-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIflbmhKSzVyPUO5Mlc4QTJiIN88US=> M3SwRnNCVkeHUh?=
KARPAS-299 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfPTWM2OD1|OT64N|khKM7:TR?= NV\UcmJyW0GQR1XS
KNS-81-FD NXL5XZpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFm1Rm9KSzVyPUSwMlM3ODRiIN88US=> NEG1RopUSU6JRWK=
NCI-H1563 M3K1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTRzLkWwN|khKM7:TR?= M2XyWXNCVkeHUh?=
NB14 M4jKSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HpfWlEPTB;NEKuO|I3OyBizszN Mm\5V2FPT0WU
COLO-800 NHrjR3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTR{Lki1NVchKM7:TR?= NXznbYkxW0GQR1XS
MS-1 MkjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTVTWM2OD12Mz6wOFg{KCEQvF2= NHK5[nBUSU6JRWK=
OVCAR-8 NV;JTVBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknGTWM2OD12Mz62PFA6KCEQvF2= M{XmT3NCVkeHUh?=
SK-PN-DW NV\qZVdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;NUndxUUN3ME20N{45Pzd4IDFOwG0> MUPTRW5ITVJ?
G-402 Ml3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTSV|REUUN3ME20N{46ODB4IDFOwG0> MlLtV2FPT0WU
NCI-H2291 NIfXZ4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTR2LkiwNVchKM7:TR?= NETSTXBUSU6JRWK=
PC-3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTR3LkiwNlMhKM7:TR?= NGLKfJhUSU6JRWK=
NCI-H1581 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j2bmlEPTB;NEWuPVg5QSBizszN MoX5V2FPT0WU
SW1116 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTR5LkCxPFIhKM7:TR?= M2nZeXNCVkeHUh?=
ZR-75-30 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonLTWM2OD12Nz6wNlM6KCEQvF2= MXHTRW5ITVJ?
OCI-AML2 NIDndZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjETWM2OD12Nz6wPVE5KCEQvF2= NIq0ZYJUSU6JRWK=
MDA-MB-231 M2DCNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\pOWpKSzVyPUS3MlYzPDliIN88US=> NXnq[5RPW0GQR1XS
ES3 MkjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTR6LkO1NlkhKM7:TR?= NX71[Ik{W0GQR1XS
NCI-H630 NGHlNopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX1d5Z3UUN3ME20PU4yPzR{IDFOwG0> NHi0UZBUSU6JRWK=
OE19 MmLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:0UFRKSzVyPUS5MlI6ODJiIN88US=> NYnrdJJNW0GQR1XS
NCI-H1573 NUL3Znc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzKTWM2OD12OT62PFYyKCEQvF2= NW\BXpJSW0GQR1XS
EW-1 NH3kXo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnYS2ZiUUN3ME20PU46ODh2IDFOwG0> NUfyUZk4W0GQR1XS

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[2]

+ 展開
  • 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.


    (参考用のみ)
動物試験:

[2]

+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (188.51 mM)
Ethanol 2 mg/mL (3.77 mM)
Water Insoluble
体内 順序で溶剤を入れること:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 530.45
化学式

C26H29Cl2N5O3

CAS No. 380843-75-4
保管
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    Can I give S1014 Bosutinib to mice by oral gavage? If so, how to dissolve the drug?

  • 回答:

    For oral gavage, S1014 Bosutinib can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension.

Src信号経路図

Src Inhibitors with Unique Features

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Tags: Bosutinib (SKI-606)を買う | Bosutinib (SKI-606) ic50 | Bosutinib (SKI-606)供給者 | Bosutinib (SKI-606)を購入する | Bosutinib (SKI-606)費用 | Bosutinib (SKI-606)生産者 | オーダーBosutinib (SKI-606) | Bosutinib (SKI-606)化学構造 | Bosutinib (SKI-606)分子量 | Bosutinib (SKI-606)代理店
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