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 NXvWRpptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvafHhOUUN3ME2wMlA5OjNzIDFOwG0> M1LoSHNCVkeHUh?=
SW756 MmfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPuTWM2OD1yLkG0NFI1KCEQvF2= M2DLcHNCVkeHUh?=
CTV-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHMV4g1UUN3ME2wMlE3Ozl6IDFOwG0> NYXvRZFCW0GQR1XS
HSC-4 MlfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHCSY5KSzVyPUCuNVcyPThiIN88US=> NHXySXZUSU6JRWK=
LAMA-84 NHu4UoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwMki2OlQhKM7:TR?= NHrrTGZUSU6JRWK=
KU812 MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rtdWlEPTB;MD6zOFA3QCBizszN Mn\YV2FPT0WU
HCC1806 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmW2TWM2OD1yLkO1NlE3KCEQvF2= MlLiV2FPT0WU
DOK MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjNc2JKSzVyPUCuN|c4QDZiIN88US=> MnW0V2FPT0WU
NCI-H209 NULnR2JsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLDTWM2OD1yLkSwPFA5KCEQvF2= M2HabXNCVkeHUh?=
EoL-1-cell M4nUOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPjTWM2OD1yLkSxOVc3KCEQvF2= Ml60V2FPT0WU
H9 NFLTd25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLqfFFXUUN3ME2wMlQ{PDZ2IDFOwG0> MnPwV2FPT0WU
EM-2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwNEO4PUAh|ryP NFTaW4JUSU6JRWK=
NCI-H292 NUm0SGFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnwbYVKSzVyPUCuOFQyODhiIN88US=> NIi0UHpUSU6JRWK=
697 NHGzSYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HafWlEPTB;MD60OVY{OyBizszN NHTjRnpUSU6JRWK=
BHT-101 Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TB[mlEPTB;MD60OlU6KCEQvF2= NHLy[GtUSU6JRWK=
BE-13 NXPOUWpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu0NGtKSzVyPUCuOFg2PzJiIN88US=> NEK2XnpUSU6JRWK=
RS4-11 NFXPZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHneGRKSzVyPUCuOFg2QDRiIN88US=> NYH3fIJmW0GQR1XS
IGROV-1 NVXEbXJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXixcWhbUUN3ME2wMlQ5Pzl5IDFOwG0> M1zzNHNCVkeHUh?=
KE-37 NV;4[4hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETv[YNKSzVyPUCuOFk2ODliIN88US=> NX3GeHBEW0GQR1XS
BV-173 NWrHVoNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwNUC3PVIhKM7:TR?= NGeyNlhUSU6JRWK=
MEG-01 NGi3bmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzpNZB4UUN3ME2wMlUyOjF2IDFOwG0> NHvwZXJUSU6JRWK=
LB2241-RCC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTBwNUO3NVghKM7:TR?= MmTBV2FPT0WU
ACHN M1T6e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPGTWM2OD1yLkW0NFY6KCEQvF2= Ml3FV2FPT0WU
CTB-1 NV\T[5U6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TSRWlEPTB;MD61OFgzKCEQvF2= NUm5[lZOW0GQR1XS
HT-1080 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTXdIpxUUN3ME2wMlU2OzR7IDFOwG0> MmK0V2FPT0WU
CHL-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\0XWFKSzVyPUCuOVU1PjViIN88US=> M4OyVHNCVkeHUh?=
EW-3 NV\LPWU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3RfmxUUUN3ME2wMlU2QTN3IDFOwG0> M3XmWXNCVkeHUh?=
ES1 NE\peVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTjSm5KSzVyPUCuOlc1QThiIN88US=> NHXlTYtUSU6JRWK=
KASUMI-1 MkD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfoTWM2OD1yLkeyN|MhKM7:TR?= M4nXTnNCVkeHUh?=
SW13 M1rOV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jORmlEPTB;MD63N|c6QCBizszN MorNV2FPT0WU
A3-KAW NH35c3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkm3TWM2OD1yLke5NlA5KCEQvF2= MWHTRW5ITVJ?
LB771-HNC NX25N4t5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTBwOEOxNFQhKM7:TR?= MknBV2FPT0WU
OC-314 M4KxSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwOE[5OlUhKM7:TR?= NIPBTlZUSU6JRWK=
MLMA NYTrfplKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfEcHRjUUN3ME2wMlkxPjd3IDFOwG0> MVLTRW5ITVJ?
KARPAS-45 NIHSPIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwOUK0OlYhKM7:TR?= MkXRV2FPT0WU
CAL-27 NWeySo46T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLle4lKSzVyPUCuPVI6ODZiIN88US=> NYG1WJZRW0GQR1XS
SK-NEP-1 MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFftcGZKSzVyPUCuPVczPDhiIN88US=> MYnTRW5ITVJ?
COR-L105 NGHGfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrYSJVKSzVyPUGuNFA{QTRiIN88US=> NHzLRnJUSU6JRWK=
TI-73 Mn;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGezSpRKSzVyPUGuNFE3PSBizszN MXfTRW5ITVJ?
JVM-3 M3m0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFwMEWwNVchKM7:TR?= NXzHVW5[W0GQR1XS
HAL-01 NIX1XoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTFwMEi4NUAh|ryP MmeyV2FPT0WU
QIMR-WIL NFrN[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrCTWM2OD1zLkC5NFU5KCEQvF2= M4TlNXNCVkeHUh?=
HSC-3 NV3SV245T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTFwMUG3PFMhKM7:TR?= NXHUdo9UW0GQR1XS
KY821 M3XHNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\EcmlEPTB;MT6xN|M2OSBizszN NEjR[WlUSU6JRWK=
5637 NWHGcHg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwMUO4NFMhKM7:TR?= M1z1UHNCVkeHUh?=
CAL-33 NHP5SVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm[5TWM2OD1zLkG5N|AzKCEQvF2= MV7TRW5ITVJ?
ES4 MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFwMkC3PUAh|ryP M4G3c3NCVkeHUh?=
BHY NWr4b2VGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfncYdmUUN3ME2xMlIzQDl{IDFOwG0> NXLqR2p[W0GQR1XS
LB1047-RCC MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rqemlEPTB;MT6yN|c5PSBizszN NEjGS5RUSU6JRWK=
H4 NGS0S4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;pXFFnUUN3ME2xMlI1OjV3IDFOwG0> NEe3NpFUSU6JRWK=
RPMI-8866 M1HmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvve5RSUUN3ME2xMlI3OTB4IDFOwG0> NVryb3poW0GQR1XS
HO-1-N-1 NFHnVINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHEdXJKSzVyPUGuNlY{PjliIN88US=> NGLKcFZUSU6JRWK=
BB30-HNC MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rW[GlEPTB;MT6yPFcyPCBizszN M1e3T3NCVkeHUh?=
PC-14 NHy3WHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrzZ2pKSzVyPUGuNlkzODViIN88US=> NYTwUGZyW0GQR1XS
NUGC-3 M3TyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzuO3BKSzVyPUGuNlk{PTZiIN88US=> M{fCSnNCVkeHUh?=
A4-Fuk NXftXGg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTFwM{C3NFQhKM7:TR?= NXH4NW16W0GQR1XS
MHH-NB-11 M1vNVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[3WmlEPTB;MT6zNVM5OyBizszN NXSyNpVzW0GQR1XS
KOSC-2 MlzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[5bWlEPTB;MT6zNVc4PSBizszN NE\rOZlUSU6JRWK=
A498 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Du[2lEPTB;MT60NFEyOyBizszN MkjjV2FPT0WU
KG-1 M3fsZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoCyTWM2OD1zLkSxNlc{KCEQvF2= MVPTRW5ITVJ?
DEL NXT2bGs5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jJWmlEPTB;MT60N|Y2PyBizszN MXXTRW5ITVJ?
EW-16 NGLW[4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zDR2lEPTB;MT60N|k4OyBizszN NFfkZVBUSU6JRWK=
BPH-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7nPVVKSzVyPUGuOFQ5ODViIN88US=> NFTGVW9USU6JRWK=
JAR MonDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXheG1sUUN3ME2xMlQ6OzZiIN88US=> MkLzV2FPT0WU
J-RT3-T3-5 M3e3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\QXFhKSzVyPUGuOVE4OjJiIN88US=> M2nHd3NCVkeHUh?=
A375 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v5[mlEPTB;MT61NVc4OiBizszN M335UXNCVkeHUh?=
SW954 NFnWXo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf6TWM2OD1zLkW1NFA4KCEQvF2= MnjzV2FPT0WU
Ca9-22 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFwNU[yOkAh|ryP MVPTRW5ITVJ?
D-566MG NIfiTopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3T0U2lEPTB;MT61O|E2PSBizszN MV;TRW5ITVJ?
SCC-15 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DobmlEPTB;MT62NVgxPCBizszN NFHTdZpUSU6JRWK=
HD-MY-Z Mmn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfpTWM2OD1zLk[zOVg1KCEQvF2= MmfmV2FPT0WU
HT-1376 M4\6R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\4cmlEPTB;MT62OFM3KCEQvF2= MULTRW5ITVJ?
CAL-54 M3vRNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFwNkW3NFkhKM7:TR?= NF;2dY9USU6JRWK=
ONS-76 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTFwNke1OVEhKM7:TR?= NGHJR4NUSU6JRWK=
EFO-27 NIHhUIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIP2dGhKSzVyPUGuOlg6OiBizszN NUGzZVhjW0GQR1XS
769-P NIrGXlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwNkm1PVYhKM7:TR?= MX\TRW5ITVJ?
MV-4-11 Mm[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTFwNkm4OVYhKM7:TR?= MnjxV2FPT0WU
NKM-1 M{PkPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTFwN{G4NFIhKM7:TR?= M2Xqc3NCVkeHUh?=
LOXIMVI M37BS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPjcmlKSzVyPUGuO|Q2QTliIN88US=> MXnTRW5ITVJ?
KYSE-140 M{DicGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDGeJdKSzVyPUGuO|U3PTViIN88US=> NXzLXI9qW0GQR1XS
ES5 NED6W4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;2bnZKSzVyPUGuPFY4PDdiIN88US=> NEW1XlNUSU6JRWK=
BB65-RCC MlnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlO0TWM2OD1zLki5PFQ6KCEQvF2= MoHjV2FPT0WU
HN MmjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vzV2lEPTB;MT64PVg4PCBizszN NF;iW45USU6JRWK=
A101D MlXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwOUO2NlghKM7:TR?= MULTRW5ITVJ?
LoVo M4f6ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTFwOUe2O|khKM7:TR?= NWPuV3oyW0GQR1XS
NCI-H526 NEPmWnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFwOUmzNlUhKM7:TR?= M2XQWXNCVkeHUh?=
NCI-H1693 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi5fVdKSzVyPUGuPVk5QDhiIN88US=> MYfTRW5ITVJ?
OVCAR-4 MnXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTJwMEC0N|UhKM7:TR?= NICwXFhUSU6JRWK=
SK-HEP-1 M3vuNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnI[ZBCUUN3ME2yMlAxPzR3IDFOwG0> MnjIV2FPT0WU
C2BBe1 NYf5[IlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rPcWlEPTB;Mj6wN|M4OiBizszN MkjDV2FPT0WU
MEL-JUSO MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XuVWlEPTB;Mj6wOFQ3PCBizszN NFfUR5lUSU6JRWK=
MOLT-16 MkD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJwMEewOVghKM7:TR?= MWXTRW5ITVJ?
NBsusSR NWizeZpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LwbGlEPTB;Mj6wPVg5QSBizszN M4DO[XNCVkeHUh?=
TK10 NVy3[Wg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\aTWM2OD1{LkGzOFU5KCEQvF2= NI\DU4ZUSU6JRWK=
CAL-39 Ml\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHmy[VJKSzVyPUKuNVQ1QCBizszN NXK3c2V[W0GQR1XS
NCI-H2030 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LBSmlEPTB;Mj6xPFk4OyBizszN M{faZnNCVkeHUh?=
HCT-116 NFvIfXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z1b2lEPTB;Mj6yNlk5PCBizszN MWHTRW5ITVJ?
HTC-C3 NYfqc2s5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTJwMk[4NlQhKM7:TR?= NWHUNJV5W0GQR1XS
TYK-nu NH7Je4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n6fmlEPTB;Mj6zNFkxQSBizszN MXzTRW5ITVJ?
FADU M1PvT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37xbmlEPTB;Mj6zNlI6PiBizszN M4XwTHNCVkeHUh?=
A431 NFjZR41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHsW|JlUUN3ME2yMlM4ODJ3IDFOwG0> M4HEeXNCVkeHUh?=
TE-11 M4HlUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnpO|lJUUN3ME2yMlM5ODF7IDFOwG0> NUjk[GpsW0GQR1XS
CAL-12T Mlv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HtU2lEPTB;Mj60NFQyPyBizszN M1K2SnNCVkeHUh?=
DB NHrwW4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\MVmlEPTB;Mj60Nlg3QSBizszN MUnTRW5ITVJ?
L-363 NH7iOpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjzZVdKSzVyPUKuOFM2ODdiIN88US=> NXLpeYdOW0GQR1XS
MSTO-211H M2LPRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3zNWpKSzVyPUKuOlY{QTFiIN88US=> MYnTRW5ITVJ?
SK-UT-1 NYTJWmF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTJwN{G0NFYhKM7:TR?= MnHNV2FPT0WU
RPMI-8226 NGXDZ|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvTTWM2OD1{LkezNVY1KCEQvF2= MVjTRW5ITVJ?
SF295 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFS2enlKSzVyPUKuO|Q{OSBizszN MmfYV2FPT0WU
OS-RC-2 NWTVTIY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHS4UYdKSzVyPUKuO|Y3PzNiIN88US=> MlnJV2FPT0WU
SK-MEL-24 M4HhOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJwN{iyNlQhKM7:TR?= MXXTRW5ITVJ?
COR-L23 MoHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrFTWM2OD1{Lke5OFY1KCEQvF2= NF62fppUSU6JRWK=
MHH-PREB-1 M4\scmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\td2lKSzVyPUKuPFAyPjFiIN88US=> NWf5bmpwW0GQR1XS
SK-N-DZ MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj6TWM2OD1{LkixOlM5KCEQvF2= NXy3ZmpxW0GQR1XS
OMC-1 NWnUWlZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDITWM2OD1{Lki1NFA{KCEQvF2= M2DCVnNCVkeHUh?=
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GB-1 NXfh[G1ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTN3LkC3NlkhKM7:TR?= NWLxc2ROW0GQR1XS
DU-4475 NFLYfHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnHR5NKSzVyPUO1MlE2PTNiIN88US=> NVLES4ViW0GQR1XS
SBC-5 M1fzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrJ[nNKSzVyPUO2MlU6ODJiIN88US=> MWXTRW5ITVJ?
OE33 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\pZmlEPTB;M{euO|U4PyBizszN MVXTRW5ITVJ?
C8166 M2DDeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXEXGpKSzVyPUO4MlUzPjdiIN88US=> MX;TRW5ITVJ?
COLO-684 M{exTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrVe49KSzVyPUO4Mlc1OjhiIN88US=> NETYSYFUSU6JRWK=
NCI-H1155 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrjbY8{UUN3ME2zPU4xPDdzIDFOwG0> MYDTRW5ITVJ?
ATN-1 M4HofWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PBVGlEPTB;M{muO|c6OiBizszN M3zHcnNCVkeHUh?=
KARPAS-299 NHHKenJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37tSmlEPTB;M{muPFM6KCEQvF2= NI\oUIFUSU6JRWK=
KNS-81-FD NWC2WWRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFmycFZKSzVyPUSwMlM3ODRiIN88US=> Ml\wV2FPT0WU
NCI-H1563 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTRzLkWwN|khKM7:TR?= MXfTRW5ITVJ?
NB14 NITPWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjNTWM2OD12Mj63NlY{KCEQvF2= NXnPdmZVW0GQR1XS
COLO-800 NGOwSolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;IZolKSzVyPUSyMlg2OTdiIN88US=> NU\6e3l4W0GQR1XS
MS-1 M3vpPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTR|LkC0PFMhKM7:TR?= NWHpT2dYW0GQR1XS
OVCAR-8 NVTMOW9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDaWItFUUN3ME20N{43QDB7IDFOwG0> M1q4e3NCVkeHUh?=
SK-PN-DW NYCwVllFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTRWmRKSzVyPUSzMlg4PzZiIN88US=> NF3I[mxUSU6JRWK=
G-402 MkLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPJSZhKSzVyPUSzMlkxODZiIN88US=> MnvSV2FPT0WU
NCI-H2291 NUXxR|NJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnqOIRKSzVyPUS0MlgxOTdiIN88US=> MnrnV2FPT0WU
PC-3 NYDEOIhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vF[2lEPTB;NEWuPFAzOyBizszN Mkj6V2FPT0WU
NCI-H1581 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL5TWM2OD12NT65PFg6KCEQvF2= NH:5S3NUSU6JRWK=
SW1116 NXnJeGxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnTTWM2OD12Nz6wNVgzKCEQvF2= NUDlZ5B1W0GQR1XS
ZR-75-30 NH6xT5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf4NXA4UUN3ME20O{4xOjN7IDFOwG0> MmO1V2FPT0WU
OCI-AML2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37RNGlEPTB;NEeuNFkyQCBizszN NYS3S2NHW0GQR1XS
MDA-MB-231 MnXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTR5Lk[yOFkhKM7:TR?= MlHzV2FPT0WU
ES3 M1:yS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS2TWM2OD12OD6zOVI6KCEQvF2= MkG4V2FPT0WU
NCI-H630 MlTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTR7LkG3OFIhKM7:TR?= MmXHV2FPT0WU
OE19 M{HoVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTR7LkK5NFIhKM7:TR?= MY\TRW5ITVJ?
NCI-H1573 NX;O[GVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LjeWlEPTB;NEmuOlg3OSBizszN Moj5V2FPT0WU
EW-1 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HQPGlEPTB;NEmuPVA5PCBizszN MVjTRW5ITVJ?

... 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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