Saracatinib (AZD0530) 化学構造
分子量: 542.03

高品質保証

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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
  • Saracatinib (AZD0530)のメカニズム

製品の説明

生物活性

製品説明 Saracatinib(AZD0530)は、c-SrcのためのSrc阻害剤で、IC50 が2.7 nMです。
ターゲット c-Src v-Abl
IC50 2.7 nM 30 nM [1]
In vitro試験 Saracatinib also potently inhibits other Src tyrosine kinase family members including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck with IC50 from 4-10 nM. Saracatinib sensitively inhibits Src Y530F NIH 3T3 with IC50 of 80 nM. Saracatinib significantly impairs the invasion of HT1080 cells through a 3-dimensional collagen matrix and completely inhibits EGF-induced cell scattering in NBT-II bladder cancer cells. [1] Saracatinib potent inhibits Src activation in DU145 and PC3 cells, which through inhibition of Y419 phosphorylation. Saracatinib inhibits the growth of prostate cancer including PC3, DU145, CWR22Rv1 and LNCaP, while Saracatinib shows low activity in LAPC-4, PZ-HPV7 and RWPE-1 cells. Saracatinib induces cell cycle arrest at G1/S but not caspase 3 cleavages. Saracatinib also significantly inhibits DU145 and PC3 migration in the Boyden chamber. [2] Saracatinib gives a potent and sustained blockage of AKT and enhances the sensitivity to irradiation in A549 and Calu-6 cells. [3] Saracatinib inhibits osteoclast in activity, resorption and formation. Saracatinib also reversibly prevents osteoclast precursor migration. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
CTV-1 MnXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHYTWM2OD1yLkC2NVQ{KM7:TR?= MlewV2FPT0WU
LAMA-84 NX63Zol3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4n3U2lEPTB;MD6xOVk6KM7:TR?= NW\HT5JSW0GQR1XS
MEG-01 NHuyNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUH5NXZMUUN3ME2wMlI{Pjh6IN88US=> NIfKcXZUSU6JRWK=
EM-2 Ml3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFX2WW1KSzVyPUCuNlY2KM7:TR?= NXX0U3F6W0GQR1XS
TE-15 MkH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v1bGlEPTB;MD6yO|QyOiEQvF2= NGD0SpdUSU6JRWK=
NCI-H1648 MofhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnToTWM2OD1yLkK4NVE3KM7:TR?= NXfxVFBUW0GQR1XS
TE-12 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHWTWM2OD1yLkOyOlgh|ryP MVvTRW5ITVJ?
LB996-RCC MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHpOYlYUUN3ME2wMlQ1OTl4IN88US=> M1Tp[XNCVkeHUh?=
K-562 NXztSlFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PKWWlEPTB;MD60OFk3PyEQvF2= MnLxV2FPT0WU
D-336MG M{T0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;BXGlEPTB;MD61NFMxPCEQvF2= NUHRRZREW0GQR1XS
NOS-1 M{\0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrCc2hKSzVyPUCuOlA2OjlizszN M2i3UHNCVkeHUh?=
EW-24 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2K4[2lEPTB;MD62NlY6OyEQvF2= MVzTRW5ITVJ?
BV-173 Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rkWmlEPTB;MD62OVI1QSEQvF2= MnfUV2FPT0WU
NCCIT MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwN{OyNVgh|ryP MWrTRW5ITVJ?
NCI-H1436 MnjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGw[W5SUUN3ME2wMlc6ODR7IN88US=> NVLrb41bW0GQR1XS
BB30-HNC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnK3TWM2OD1yLki2NlA{KM7:TR?= NFzvXGVUSU6JRWK=
TE-8 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLITWM2OD1yLki3Nlc2KM7:TR?= MVzTRW5ITVJ?
A704 M2\u[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH2TGdKSzVyPUCuPFkzOSEQvF2= NHrMN2tUSU6JRWK=
TK10 NETQUVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnCTWM2OD1yLkmwOlY6KM7:TR?= NF24cJdUSU6JRWK=
KS-1 NFfCOG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Kz[mlEPTB;MT6xPVc4QSEQvF2= NHjWVnVUSU6JRWK=
C2BBe1 NIKxV2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwMkC1NFch|ryP NEfFVJFUSU6JRWK=
RXF393 NGjDXmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3npbGlEPTB;MT6yOFM3KM7:TR?= MnryV2FPT0WU
KGN MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHlfo1KSzVyPUGuNlc3QDdizszN MmXnV2FPT0WU
NB69 Mn[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPpT4JIUUN3ME2xMlM4PDl5IN88US=> M{HUU3NCVkeHUh?=
TE-11 NIfWfnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTFwNEO0NVgh|ryP NIXkeZRUSU6JRWK=
TE-1 NILEXXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlqwTWM2OD1zLkS0NVA2KM7:TR?= Mm\oV2FPT0WU
ST486 MofuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTyTWM2OD1zLkS1PFUzKM7:TR?= MoPGV2FPT0WU
HOP-62 MmfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXIRodqUUN3ME2xMlUxOjR4IN88US=> NFfkblhUSU6JRWK=
EW-16 MkjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwNUWwPFMh|ryP NED5VHlUSU6JRWK=
LB1047-RCC NX64TnpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHUU5NKSzVyPUGuOVU1PTNizszN M13sOHNCVkeHUh?=
TE-10 MnTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u3NGlEPTB;MT62OlI2OiEQvF2= NUTSSVBRW0GQR1XS
RL95-2 M{TOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFwNk[5NFIh|ryP M4O0WXNCVkeHUh?=
DOHH-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTFwN{G3PFIh|ryP NIriepdUSU6JRWK=
MFH-ino MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwN{e4O{DPxE1? NXnQdodHW0GQR1XS
GB-1 M3XKU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXTbWtKSzVyPUGuO|k5OzNizszN MWrTRW5ITVJ?
SK-N-DZ MlvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFwOES2PFgh|ryP MV\TRW5ITVJ?
OS-RC-2 NIO5OHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDDTpV4UUN3ME2xMlg5PTd2IN88US=> NWHwOI5yW0GQR1XS
SW982 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjtTWM2OD1zLkmyNFk{KM7:TR?= NHzrRnpUSU6JRWK=
KALS-1 NI\GR4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzybZlKSzVyPUGuPVg4OjJizszN MXnTRW5ITVJ?
TGBC24TKB NIi1eZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnnRm9bUUN3ME2yMlA2QTV6IN88US=> MkfYV2FPT0WU
GI-1 MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTJwMU[wPFQh|ryP NXn1c|BPW0GQR1XS
SW962 NFKwXopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7EUYxKSzVyPUKuNVcyPzhizszN NUG3bo1vW0GQR1XS
SW872 M1XOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvUTWM2OD1{LkG4OVA4KM7:TR?= NWPZTIptW0GQR1XS
NCI-H747 MnzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HBfmlEPTB;Mj6yOVcyPCEQvF2= NGr4[pBUSU6JRWK=
MZ1-PC Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DvTmlEPTB;Mj6yPVM2PiEQvF2= NEjZb|JUSU6JRWK=
MSTO-211H Mmq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXENZloUUN3ME2yMlM2PzJ|IN88US=> M3fUR3NCVkeHUh?=
BL-70 M2TCSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDkTWM2OD1{LkS3OFIzKM7:TR?= NH2wTnlUSU6JRWK=
SW954 NVOw[XI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXnVGFKSzVyPUKuOVc1ODhizszN MVjTRW5ITVJ?
SNB75 Ml73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvu[GFDUUN3ME2yMlY5PTl2IN88US=> MX7TRW5ITVJ?
IST-SL2 MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfHNopKSzVyPUKuO|I{PzlizszN MWLTRW5ITVJ?
GCIY NH\CSYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHkWIxzUUN3ME2yMlg4ODB3IN88US=> NUHLWGpEW0GQR1XS
KU812 NEO1b4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3O3RmlEPTB;Mz6wOVI6QSEQvF2= NFL4UmVUSU6JRWK=
LXF-289 NU\wV4RKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[4W49VUUN3ME2zMlEzOTB7IN88US=> NIHy[41USU6JRWK=
ETK-1 Mn75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\GOmc{UUN3ME2zMlIxPzZ5IN88US=> MYXTRW5ITVJ?
SF126 Mor4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPlTWM2OD1|LkOxNVc1KM7:TR?= MonOV2FPT0WU
LC-2-ad MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf3TWM2OD1|LkW1O{DPxE1? NIPOfmlUSU6JRWK=
KNS-42 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nKXGlEPTB;Mz62OUDPxE1? NWjE[2FNW0GQR1XS
OVCAR-4 NX7ZXmhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7PXWRqUUN3ME2zMlc{PDN|IN88US=> NGPBNXlUSU6JRWK=
PF-382 NHrpXlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jvUGlEPTB;Mz64N|Y6QCEQvF2= M4DXOnNCVkeHUh?=
SH-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG5TWM2OD12LkK1NlU6KM7:TR?= MULTRW5ITVJ?
KM12 M4rMdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XS[2lEPTB;ND6zNlQyPiEQvF2= NVj3UZNKW0GQR1XS
NB5 M4D6U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXtTWM2OD12LkSxPFY1KM7:TR?= MlO1V2FPT0WU
KURAMOCHI NUO5S3VNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TLOGlEPTB;ND62OVI2PiEQvF2= NIHjVJRUSU6JRWK=
Becker NGTVZXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XkOWlEPTB;ND62OlQyPiEQvF2= M3LPZ3NCVkeHUh?=
MV-4-11 NF7zXG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfMTWM2OD12LkixN|Q1KM7:TR?= MlPrV2FPT0WU
KINGS-1 NYr3[XplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLETWM2OD12LkiyN|c{KM7:TR?= M1nKbXNCVkeHUh?=
LS-123 NYDTeVNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDzTWM2OD13LkS5Olg1KM7:TR?= M{\0e3NCVkeHUh?=
SF268 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\hcmNKSzVyPUWuOlEzPjJizszN NXf4XoxoW0GQR1XS
A388 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn6V5drUUN3ME21MlY{PjZ5IN88US=> NYTKPVZYW0GQR1XS
NMC-G1 MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M321dmlEPTB;Nj6wNVgyOSEQvF2= MkSwV2FPT0WU
CGTH-W-1 M32wSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPoTWM2OD14LkCyNFc2KM7:TR?= NHS4XolUSU6JRWK=
ES4 NFv5ZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLOPVBWUUN3ME22MlU{ODd2IN88US=> NHvubGNUSU6JRWK=
SR NY\6VpVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;yWmxrUUN3ME22MlU5QDB5IN88US=> MVTTRW5ITVJ?
BB49-HNC M2HDbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\nSoJMUUN3ME22Mlc{OjB4IN88US=> Mnf4V2FPT0WU
KLE NFW5dpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PNV2lEPTB;Nj63PFM4PyEQvF2= MVXTRW5ITVJ?
HUTU-80 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTZwOUi0OlYh|ryP NULlV3B7W0GQR1XS
SNU-C2B NWrFZZh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTdwOEK3N|ch|ryP MmO1V2FPT0WU
BB65-RCC NHrJRWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDrTWM2OD15Lkm0PVA1KM7:TR?= NV74R2pZW0GQR1XS
QIMR-WIL NVXqNlNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRThwNEK4NFgh|ryP M3TISXNCVkeHUh?=
GDM-1 M1foSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRThwOUeyPVIh|ryP NUfPVW9wW0GQR1XS
LC4-1 NVHG[Gl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTlwMEC5NVEh|ryP M1e1eHNCVkeHUh?=
MLMA NXfDN45nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrJXnlXUUN3ME25MlE2ODB4IN88US=> NE\URYlUSU6JRWK=
EoL-1-cell MnvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T5[2lEPTB;OT6zNFE6OiEQvF2= MX7TRW5ITVJ?
BOKU NViwUYszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYO1RpVyUUN3ME25Mlk3PDZ4IN88US=> MmSxV2FPT0WU
EVSA-T MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfydmhKSzVyPUGwMlY2PjhizszN NIHCRmpUSU6JRWK=
D-283MED MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTFyLkmxO|Yh|ryP Mn3pV2FPT0WU
NB1 NWi5Z3N{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\lbYtWUUN3ME2xNU4xOjR{IN88US=> MlnkV2FPT0WU
RPMI-8402 MkXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTFzLkG3PEDPxE1? NWjMW216W0GQR1XS
NCI-H1355 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEC0WXFKSzVyPUGxMlE5ODZizszN NWD0dm8zW0GQR1XS
NB7 M3nLbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzoTWM2OD1zMT6zNlk4KM7:TR?= M2PNb3NCVkeHUh?=
RPMI-6666 Mn\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTF{Lkm1Olch|ryP M2G2UXNCVkeHUh?=
697 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF|LkK3NFEh|ryP MoHzV2FPT0WU
CTB-1 NXjneIh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHoTWM2OD1zMz61PVQ5KM7:TR?= NVPFdpc6W0GQR1XS
VA-ES-BJ NEXET2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF|LkmyN|Qh|ryP MXrTRW5ITVJ?
BE-13 NHe2Z2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\UTWM2OD1zND6zPVE2KM7:TR?= NFnGdnJUSU6JRWK=
SKM-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkCzTWM2OD1zND60OFk6KM7:TR?= Ml7qV2FPT0WU
TE-6 MlriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Pt[mlEPTB;MUSuO|U6OSEQvF2= Mk\tV2FPT0WU
LB771-HNC NUPBR49wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG1TWM2OD1zND63PFk5KM7:TR?= NY\NOHN{W0GQR1XS
ECC4 M1TIfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTF5LkCyO|ch|ryP NFH2c4ZUSU6JRWK=
ES3 NGXlc25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTtbWhrUUN3ME2xO{41PjV3IN88US=> M1;KbHNCVkeHUh?=
LB647-SCLC MkXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fMVGlEPTB;MUeuOFk1QSEQvF2= MXXTRW5ITVJ?
NB10 NX3DXJNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzPNHhiUUN3ME2xPE42OjV4IN88US=> NGT3UnpUSU6JRWK=
L-540 M3XXRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXRTWM2OD1zOD64NVA6KM7:TR?= Mom3V2FPT0WU
NCI-H2126 M2fqTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;4T3lGUUN3ME2xPU42OSEQvF2= MVnTRW5ITVJ?
HH MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfJNm1KSzVyPUKwMlAxQTlizszN M4jwcnNCVkeHUh?=
MPP-89 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXmU2hKSzVyPUKzMlIzQDlizszN MXTTRW5ITVJ?
IST-MEL1 NIXNfHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnBTWM2OD1{Mz64OlU5KM7:TR?= NEXqWHRUSU6JRWK=
KP-N-YS NUnYZmdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\TOVNrUUN3ME2yN{46OjV3IN88US=> M1PBbXNCVkeHUh?=
EC-GI-10 NVnvepE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3u0ZmlEPTB;MkSuOVk5QSEQvF2= M1n4c3NCVkeHUh?=
EKVX M1\DUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ4LkCyNFMh|ryP NHLXSmRUSU6JRWK=
TGBC1TKB NXHrfGU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTJ4LkSzOEDPxE1? NIHtVZhUSU6JRWK=
Daudi NHzVVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTJ5LkC3O|Mh|ryP MUXTRW5ITVJ?
ALL-PO M3rRfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJ5LkC4NUDPxE1? Mo\WV2FPT0WU
NB6 NGm4eJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fOSGlEPTB;MkeuOFg5KM7:TR?= NH3l[HhUSU6JRWK=
ES6 MmHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHxTWM2OD1{Nz65NVI{KM7:TR?= M3TBe3NCVkeHUh?=
COLO-320-HSR MoPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LyS2lEPTB;MkiuNFM4OyEQvF2= NGTqO3BUSU6JRWK=
K5 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4OyfmlEPTB;MkiuNVI5PyEQvF2= NFfIO2FUSU6JRWK=
ES1 M37uR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTJ6Lke3O|Mh|ryP M3rFNHNCVkeHUh?=
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SCLC-21H NFLsWYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XI[WlEPTB;M{CuO|MyPyEQvF2= M4LLbnNCVkeHUh?=
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NCI-H209 MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTN3LkG0OEDPxE1? NWrYbGtpW0GQR1XS
A253 NWTDSVRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DBO2lEPTB;M{WuO|QzQSEQvF2= Ml;QV2FPT0WU
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EB-3 MlPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHCTWM2OD1|Nj65OVE5KM7:TR?= MXvTRW5ITVJ?
GOTO Mk\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\r[GlEPTB;M{euN|IzPCEQvF2= MkL1V2FPT0WU
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... Click to View More Cell Line Experimental Data

In vivo試験 Saracatinib shows great tumor growth inhibition in Src3T3 allografts and a moderate growth delay in Calu-6, MDA-MB-231, AsPc-1 and BT474C xenografts. [1] Saracatinib shows great antitumor activity in orthotopic DU145 xenograft mice at a dose of 25mg/kg (orally administered, daily). [2]
臨床試験 Saracatinib is currently in Phase II clinical trial in recurrent osteosarcoma localized to the lung.
特集 The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Kinase Assay IC50 of tyrosine kinase activity is measured by an enzyme-linked immunosorbent assay (ELISA) with recombinant catalytic domains of a panel of receptor and non-receptor tyrosine kinases (in some cases only part of the catalytic domain is used). Saracatinib dose ranges from 0.001-10 mM. Specificity assays against a panel of serine/threonine kinases are performed using a filter capture assay with 32P. Briefly, multidrop 384 plates containing 0.5 μL Saracatinib or controls (DMSO) alone or pH 3.0 buffer controls) are incubated with 15 μL of enzyme plus peptide/protein substrate for 5 min before the reaction is initiated by the addition of 10 μL of 20 mM Mg-ATP. For all enzymes the final concentration is approximated to the Michaelis constant (Km). Assays are carried out for 30min at room temperature before termination by the addition of 5 μL orthophosphoric acid. After mixing, the well contents are harvested onto a P81 Unifilter plate, using orthophosphoric acid as the wash buffer. Then IC50 is calculated.

細胞アッセイ: [1]

細胞株 PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 and RWPE-1 cells
濃度 62.5 nM - 16 mM
反応時間 1, 3 and 5 days
実験の流れ Cells are seeded at a density of 2× 103 in 96-well plates and incubated overnight. Then Saracatinib (62.5 nM-16 mM) is added to the cells. After 1, 3 and 5 days, culture medium is removed followed by addition of 0.2 mL DMSO per well and continuous shaking of plates at 200 rotations per minute for 15min. Then IC50 is measured by MTT metho

動物実験: [1]

動物モデル CB17 mice are implanted with DU145 cells.
製剤 Dissolved in 0.5% hydroxypropyl methylcellulose, 0.1% Tween 80
投薬量 25 mg/kg
投与方法 Orally administered daily

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 Saracatinib (AZD0530) SDF
分子量 542.03
化学式

C27H32ClN5O5

CAS No. 379231-04-6
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 35 mg/mL warming (64.57 mM)
エタノール 31 mg/mL (57.19 mM)
<1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose+0.2% Tween 80 30 mg/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 N-(5-chlorobenzo[d][1,3]dioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine

文献中の引用 (35)

Frequently Asked Questions

  • Question 1
    What is the half-life of Saracatinib?

    Answer: Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

技術サポート&よくある質問(FAQ)

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