Bosutinib (SKI-606)

Licensed by Pfizer 製品コード:S1014

For research use only.

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.

Bosutinib (SKI-606)化学構造

CAS No. 380843-75-4

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 17100
JPY 13600
JPY 46800
JPY 118400

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(111)

製品安全説明書

Src阻害剤の選択性比較

相関Src製品

生物活性

製品説明 Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
ターゲット
S6 kinase [7] ERK [7] STAT3 [7] 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 M{nJRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFW0VGJKSzVyPUCuNFgzOzFiIN88US=> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
SW756 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVu1RYEzUUN3ME2wMlE1ODJ2IDFOwG0> MlnYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
CTV-1 NFHRVoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Li[WlEPTB;MD6xOlM6QCBizszN MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
HSC-4 Ml;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwMUexOVghKM7:TR?= NIO1Sos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
LAMA-84 NHO4d|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\BRVNPUUN3ME2wMlI5PjZ2IDFOwG0> NFW5W209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
KU812 M1zYVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj1W4U{UUN3ME2wMlM1ODZ6IDFOwG0> NV7Hfm1FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
HCC1806 M4rz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LsbWlEPTB;MD6zOVIyPiBizszN MoL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
DOK NEXpNFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFS5VYFKSzVyPUCuN|c4QDZiIN88US=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
NCI-H209 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;ERYJKSzVyPUCuOFA5ODhiIN88US=> MoryQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
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697 Mmf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwNEW2N|MhKM7:TR?= M1j1b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
BHT-101 NFXofIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwNE[1PUAh|ryP M3PmUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
BE-13 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D2fGlEPTB;MD60PFU4OiBizszN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
RS4-11 NWLhcJNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTBwNEi1PFQhKM7:TR?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
IGROV-1 M{njZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTDVmlKSzVyPUCuOFg4QTdiIN88US=> NHPQbVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
KE-37 NXfLcJVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXiNoNKSzVyPUCuOFk2ODliIN88US=> NFrMSWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
BV-173 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwNUC3PVIhKM7:TR?= NI\XeIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
MEG-01 NVnpNWJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7RTWM2OD1yLkWxNlE1KCEQvF2= M2XaXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
LB2241-RCC MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\nNHhoUUN3ME2wMlU{PzF6IDFOwG0> NXfmXI9SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
ACHN MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTBwNUSwOlkhKM7:TR?= MlXOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
CTB-1 MnvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwNUS4NkAh|ryP MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
HT-1080 M{nSN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PxfmlEPTB;MD61OVM1QSBizszN M13kdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
CHL-1 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTFeGE6UUN3ME2wMlU2PDZ3IDFOwG0> MlfIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
EW-3 MlH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnNVHNKSzVyPUCuOVU6OzViIN88US=> MnXXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
ES1 NUDEPFJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnTTWM2OD1yLk[3OFk5KCEQvF2= MkTLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
KASUMI-1 Mk\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTKV|VFUUN3ME2wMlczOzNiIN88US=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
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HeLa M3TjV2Z2dmO2aX;uJIF{e2G7 MnXWOE42KGi{cx?= MVjJcohq[mm2aX;uJI9nKEWkb3zheolzfXNiZ3z5Z49xem:2ZXnuM41ifHKreDDwdo91\WmwIG\QOFAh\W62comgbY4hcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC0MlUhcHK|IHLleIEudGGldHHtZZNmKHKncH;yeIVzKGG|c3H5MEBKSzVyIE2gN{45PSEQvF2u NV7DcVdnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2NlQ{QDdpPkK5OlI1Ozh5PD;hQi=>
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HepG2 MVTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MWC0PEBpenN? NIjGdXlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwJF0hOy57MTFOwG0v M3jiUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEi1O|E2Lz5zOES4OVcyPTxxYU6=
HT29 NUHQXI9USW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NYTwfm9MPDhiaILz MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWMkmgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJHRIUSB;IE[uOUDPxE1w MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR6NUexOUc,OTh2OEW3NVU9N2F-
HepG2 M2HLbWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NGe2WFQ1QCCqcoO= NUn4VG1XSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0PEBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiVFfJJF0hPy54NjFOwG0v NIr2XG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES4OVcyPSd-MUi0PFU4OTV:L3G+
Ba/F3 NGjkR4lE\WyuIHTlZZRpKGG|c3H5 NXjNW|lSUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigc4YhdXW{aX7lJGJiTjNiY3XscJMh\XiycnXzd4lv\yCQUF2vRWxMKEx{NU\UJI12fGGwdDDifUB1enmyYX6gZox2\SCneHPseZNqd25iYYPzZZk> NFfhXHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkm3NFQxOCd-MU[5O|A1ODB:L3G+
A673 NVjQT|ExeUiWUzDhd5NigQ>? NFLRNIxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= NEDEZoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
DAOY NEP5U2xyUFSVIHHzd4F6 NIDieW5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= NXTwTZA4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 MnfFdWhVWyCjc4PhfS=> MX\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD NWDWTpNqeUiWUzDhd5NigQ>? NVKxNlNDeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLEJINmdGy| MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NHTYWWFyUFSVIHHzd4F6 MYDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NX\5UI85RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NGHIepNyUFSVIHHzd4F6 MVzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
アッセイ
Methods Test Index PMID
Western blot p-Src / Src / p-c-Abl / c-Abl / p-S6 / S6 / p-ERK / ERK / p-STAT3 / STAT3 ; p-FAK / FAK / p-Pyk2 / p-p130Cas / p-AKT ; p-ABL / ABL 27903968 18483306 28199182
Immunofluorescence p-FAK / p-STAT3 / beta-catenin 18483306
Growth inhibition assay Cell viability ; IC50 24812339 27903968
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]

  • 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]

  • 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.

動物試験:

[2]

  • 動物モデル:Nude female mice injected with K562 cells
  • 投薬量:~150 mg/kg/day
  • 投与方法:Oral gavage

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。

10mg/mL

化学情報

分子量 530.45
化学式

C26H29Cl2N5O3

CAS No. 380843-75-4
Storage 3年 -20°C
2年 -80°C in solvent
Smiles CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04258943 Recruiting Drug: Bosutinib Philadelphia Chromosome Positive CML|Accelerated Phase Chronic Myelogenous Leukemia|Blastic Phase Chronic Myelogenous Leukemia|Chronic Phase Chronic Myelogenous Leukemia Children''s Oncology Group|Erasmus MC|Dutch Childhood Oncology Group|Innovative Therapies for Children with Cancer|Pfizer April 6 2020 Phase 1|Phase 2
NCT03023319 Completed Drug: Bosutinib|Drug: Pemetrexed Carcinoma Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer Nagla Abdel Karim|Augusta University December 10 2019 Phase 1
NCT05363488 Completed Drug: Bosutinib Myeloid Leukemia Pfizer May 16 2019 --
NCT03888222 Completed Drug: Placebo Oral Tablet|Drug: Bosutinib Oral Tablet Dementia With Lewy Bodies Georgetown University|Alzheimer''s Association April 23 2019 Phase 2
NCT03854903 Recruiting Drug: Palbociclib|Drug: Bosutinib|Drug: Fulvestrant Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer April 1 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
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お問い合わせ内容をご入力ください

よくある質問(FAQ)

質問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.

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