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 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwME[xOFMh|ryP NGPFdXZUSU6JRWK=
LAMA-84 M{Dw[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFftNmxKSzVyPUCuNVU6QSEQvF2= NVvmeJJKW0GQR1XS
MEG-01 M2rRZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\LO4JKSzVyPUCuNlM3QDhizszN NIW2S2tUSU6JRWK=
EM-2 NYrwU5h6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[yVXJFUUN3ME2wMlI3PSEQvF2= MXHTRW5ITVJ?
TE-15 NXvRenhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnuTWM2OD1yLkK3OFEzKM7:TR?= MY\TRW5ITVJ?
NCI-H1648 M{TNfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHu3UnlKSzVyPUCuNlgyOTZizszN MVTTRW5ITVJ?
TE-12 NXv6e25bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTBwM{K2PEDPxE1? NX3JWHFYW0GQR1XS
LB996-RCC MnHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlixTWM2OD1yLkS0NVk3KM7:TR?= MnjZV2FPT0WU
K-562 NF;lNVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIm5clJKSzVyPUCuOFQ6PjdizszN NXnNfVR5W0GQR1XS
D-336MG NFnGT4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjFOpNYUUN3ME2wMlUxOzB2IN88US=> M3nLUHNCVkeHUh?=
NOS-1 M{fQ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj1SmZKSzVyPUCuOlA2OjlizszN NXr6VZFSW0GQR1XS
EW-24 M1Kz[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDtTWM2OD1yLk[yOlk{KM7:TR?= MnuzV2FPT0WU
BV-173 Ml3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwNkWyOFkh|ryP M3L0ZnNCVkeHUh?=
NCCIT NHPTb5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\sfGlEPTB;MD63N|IyQCEQvF2= NXHPbnAyW0GQR1XS
NCI-H1436 NUiyOZdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvFcZJKSzVyPUCuO|kxPDlizszN NX;rbHJOW0GQR1XS
BB30-HNC MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHL1eI9KSzVyPUCuPFYzODNizszN NX;SUmQ5W0GQR1XS
TE-8 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwOEeyO|Uh|ryP MVnTRW5ITVJ?
A704 NX[zbm1vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTBwOEmyNUDPxE1? NFrI[4RUSU6JRWK=
TK10 NYmye|lST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknOTWM2OD1yLkmwOlY6KM7:TR?= NVTFSndOW0GQR1XS
KS-1 MkfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;COWlEPTB;MT6xPVc4QSEQvF2= NH\WbWRUSU6JRWK=
C2BBe1 NWnYW|RrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwMkC1NFch|ryP NEHtc2xUSU6JRWK=
RXF393 M1u2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETzd4JKSzVyPUGuNlQ{PiEQvF2= NIP3TZNUSU6JRWK=
KGN M1PaNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHBTWM2OD1zLkK3Olg4KM7:TR?= MYLTRW5ITVJ?
NB69 MlfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[1TWM2OD1zLkO3OFk4KM7:TR?= M1r2NXNCVkeHUh?=
TE-11 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwNEO0NVgh|ryP M3q3c3NCVkeHUh?=
TE-1 NIft[HlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTFwNESxNFUh|ryP NXXlfndEW0GQR1XS
ST486 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\OdGlEPTB;MT60OVg2OiEQvF2= MX3TRW5ITVJ?
HOP-62 NW\4eYt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHi2W3NKSzVyPUGuOVAzPDZizszN M4\GZXNCVkeHUh?=
EW-16 NXTtT3F2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFwNUWwPFMh|ryP M3PKRXNCVkeHUh?=
LB1047-RCC M1L2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFwNUW0OVMh|ryP M1ezUHNCVkeHUh?=
TE-10 MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\yZ2lEPTB;MT62OlI2OiEQvF2= M3jCcnNCVkeHUh?=
RL95-2 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jvfWlEPTB;MT62OlkxOiEQvF2= MUTTRW5ITVJ?
DOHH-2 MlLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTFwN{G3PFIh|ryP NVXvSmM1W0GQR1XS
MFH-ino Mm\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG1RpFKSzVyPUGuO|c5PyEQvF2= MWPTRW5ITVJ?
GB-1 NHn3WmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXvVolSUUN3ME2xMlc6QDN|IN88US=> NITnPG1USU6JRWK=
SK-N-DZ NYPS[VVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXrOm0{UUN3ME2xMlg1Pjh6IN88US=> NXPBOHNkW0GQR1XS
OS-RC-2 NH71fm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\1TWM2OD1zLki4OVc1KM7:TR?= MlLBV2FPT0WU
SW982 NFHieYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{i0R2lEPTB;MT65NlA6OyEQvF2= M4ixSXNCVkeHUh?=
KALS-1 NV\rToNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFwOUi3NlIh|ryP MYPTRW5ITVJ?
TGBC24TKB NXWxTlk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWmxWWJ5UUN3ME2yMlA2QTV6IN88US=> Mk\WV2FPT0WU
GI-1 M3fuXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4mzV2lEPTB;Mj6xOlA5PCEQvF2= MYjTRW5ITVJ?
SW962 NXTxXoI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1m4fGlEPTB;Mj6xO|E4QCEQvF2= MnrRV2FPT0WU
SW872 M3zTVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjSTWM2OD1{LkG4OVA4KM7:TR?= Ml34V2FPT0WU
NCI-H747 NYfKUFRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fYS2lEPTB;Mj6yOVcyPCEQvF2= NHXMZmVUSU6JRWK=
MZ1-PC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjNTWM2OD1{LkK5N|U3KM7:TR?= Mlj5V2FPT0WU
MSTO-211H MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTx[lBvUUN3ME2yMlM2PzJ|IN88US=> NXPnPVFRW0GQR1XS
BL-70 M37MXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rqO2lEPTB;Mj60O|QzOiEQvF2= M3riV3NCVkeHUh?=
SW954 M4jTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3u4XGlEPTB;Mj61O|QxQCEQvF2= MkD0V2FPT0WU
SNB75 NFHGTpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnwRZlKSzVyPUKuOlg2QTRizszN NInL[ppUSU6JRWK=
IST-SL2 M3H3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTRTWM2OD1{LkeyN|c6KM7:TR?= MUHTRW5ITVJ?
GCIY NVLaS2pvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LSRmlEPTB;Mj64O|AxPSEQvF2= NGnPNHZUSU6JRWK=
KU812 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLueZhKSzVyPUOuNFUzQTlizszN NHLYfIVUSU6JRWK=
LXF-289 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D1VWlEPTB;Mz6xNlExQSEQvF2= Mnz6V2FPT0WU
ETK-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXT4To5FUUN3ME2zMlIxPzZ5IN88US=> M1r4U3NCVkeHUh?=
SF126 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnjfGdKSzVyPUOuN|EyPzRizszN M4PYNXNCVkeHUh?=
LC-2-ad NXj1eopDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzib|dKSzVyPUOuOVU4KM7:TR?= MnnsV2FPT0WU
KNS-42 NIjQNY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTNwNkWg{txO MXPTRW5ITVJ?
OVCAR-4 NHG3ZnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33XW2lEPTB;Mz63N|Q{OyEQvF2= NYXqc4NoW0GQR1XS
PF-382 NI\hS3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3yzNmlEPTB;Mz64N|Y6QCEQvF2= M3PjdXNCVkeHUh?=
SH-4 MlPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PoNWlEPTB;ND6yOVI2QSEQvF2= MnLaV2FPT0WU
KM12 NUDJbJZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPZ[FlKSzVyPUSuN|I1OTZizszN M{LkTXNCVkeHUh?=
NB5 MmfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTRwNEG4OlQh|ryP NF;zTWRUSU6JRWK=
KURAMOCHI M1;VNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTUTWM2OD12Lk[1NlU3KM7:TR?= NVG1[GY{W0GQR1XS
Becker M1vjRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnexTWM2OD12Lk[2OFE3KM7:TR?= NYL2PHNGW0GQR1XS
MV-4-11 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;iTWM2OD12LkixN|Q1KM7:TR?= NUfaXmRiW0GQR1XS
KINGS-1 M{GxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XqeWlEPTB;ND64NlM4OyEQvF2= MWrTRW5ITVJ?
LS-123 NVX3NYx5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;1WJlKSzVyPUWuOFk3QDRizszN NIC4UJBUSU6JRWK=
SF268 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTVwNkGyOlIh|ryP NEKxZnRUSU6JRWK=
A388 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\vVGRKSzVyPUWuOlM3PjdizszN NGG1TVVUSU6JRWK=
NMC-G1 MoPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K5OGlEPTB;Nj6wNVgyOSEQvF2= M33OZ3NCVkeHUh?=
CGTH-W-1 MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PBemlEPTB;Nj6wNlA4PSEQvF2= M{[zWnNCVkeHUh?=
ES4 NXflNFh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXDe3lwUUN3ME22MlU{ODd2IN88US=> M1znZ3NCVkeHUh?=
SR M2X3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTZwNUi4NFch|ryP M{S2NXNCVkeHUh?=
BB49-HNC MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTZwN{OyNFYh|ryP Mme5V2FPT0WU
KLE NYTRe5pST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\PTWM2OD14Lke4N|c4KM7:TR?= M1rMVHNCVkeHUh?=
HUTU-80 M17USWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvzeYoyUUN3ME22Mlk5PDZ4IN88US=> MXPTRW5ITVJ?
SNU-C2B MnSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGi3UVlKSzVyPUeuPFI4OzdizszN M1\kV3NCVkeHUh?=
BB65-RCC NXn2VXNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTdwOUS5NFQh|ryP M1foOXNCVkeHUh?=
QIMR-WIL MlTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGW3UVdKSzVyPUiuOFI5ODhizszN MUjTRW5ITVJ?
GDM-1 MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3OxZmlEPTB;OD65O|I6OiEQvF2= MnzqV2FPT0WU
LC4-1 MkDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPITWxkUUN3ME25MlAxQTFzIN88US=> MUDTRW5ITVJ?
MLMA NXnaUHh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTlwMUWwNFYh|ryP M2\HSnNCVkeHUh?=
EoL-1-cell MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTKTWM2OD17LkOwNVkzKM7:TR?= NIDZR3JUSU6JRWK=
BOKU MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTpTWM2OD17Lkm2OFY3KM7:TR?= NETvPYhUSU6JRWK=
EVSA-T MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHO0V5lKSzVyPUGwMlY2PjhizszN NEDJPVJUSU6JRWK=
D-283MED M{Lmdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\h[GlEPTB;MUCuPVE4PiEQvF2= MkX0V2FPT0WU
NB1 NHfLdnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPOcXRsUUN3ME2xNU4xOjR{IN88US=> NETh[YJUSU6JRWK=
RPMI-8402 NYL5VWY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHiTWM2OD1zMT6xO|gh|ryP MmfOV2FPT0WU
NCI-H1355 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TPR2lEPTB;MUGuNVgxPiEQvF2= NELycIlUSU6JRWK=
NB7 M3:1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnTbZVDUUN3ME2xNU4{Ojl5IN88US=> NWLy[mlKW0GQR1XS
RPMI-6666 M1LGZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7CTWM2OD1zMj65OVY4KM7:TR?= MVPTRW5ITVJ?
697 NX[wNoV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi1O2k1UUN3ME2xN{4zPzBzIN88US=> NFLkdGFUSU6JRWK=
CTB-1 NH7jNZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTF|LkW5OFgh|ryP NHHINXBUSU6JRWK=
VA-ES-BJ NIrHNHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTF|LkmyN|Qh|ryP M1LjbnNCVkeHUh?=
BE-13 NXvmSXh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVi3[nlIUUN3ME2xOE4{QTF3IN88US=> NWCxdFdVW0GQR1XS
SKM-1 NH7XUGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGe1ZpRKSzVyPUG0MlQ1QTlizszN NIHYWVBUSU6JRWK=
TE-6 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTF2Lke1PVEh|ryP M2PVcnNCVkeHUh?=
LB771-HNC NFfWeFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;FNmdKSzVyPUG0Mlc5QThizszN MkPSV2FPT0WU
ECC4 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTF5LkCyO|ch|ryP MnPoV2FPT0WU
ES3 NWjEfVlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjacI9DUUN3ME2xO{41PjV3IN88US=> NFPacZFUSU6JRWK=
LB647-SCLC MlTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\pTWM2OD1zNz60PVQ6KM7:TR?= NI\S[WhUSU6JRWK=
NB10 M3vSdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;ITWM2OD1zOD61NlU3KM7:TR?= NEL3VIZUSU6JRWK=
L-540 NWP5fYJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi2TJlKSzVyPUG4MlgyODlizszN MlvxV2FPT0WU
NCI-H2126 NXu3SplbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Lkc2lEPTB;MUmuOVEh|ryP NIjkO5BUSU6JRWK=
HH Mn7wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHMVnhwUUN3ME2yNE4xODl7IN88US=> NH;uWIZUSU6JRWK=
MPP-89 NEnTUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfxOVJKSzVyPUKzMlIzQDlizszN MWHTRW5ITVJ?
IST-MEL1 MlvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJ|Lki2OVgh|ryP NVrObnE{W0GQR1XS
KP-N-YS MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTJ|LkmyOVUh|ryP MWnTRW5ITVJ?
EC-GI-10 M{nJSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmH1TWM2OD1{ND61PVg6KM7:TR?= MknsV2FPT0WU
EKVX MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjjWIVKSzVyPUK2MlAzODNizszN NFHnVolUSU6JRWK=
TGBC1TKB NFy4fpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ4LkSzOEDPxE1? M1zXXnNCVkeHUh?=
Daudi MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXjTWM2OD1{Nz6wO|c{KM7:TR?= M4K3T3NCVkeHUh?=
ALL-PO M4LIXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYT4TWZ3UUN3ME2yO{4xQDFizszN NYLENYtNW0GQR1XS
NB6 NFzwUoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjZUpNEUUN3ME2yO{41QDhizszN Mnj5V2FPT0WU
ES6 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPwN4ZKSzVyPUK3MlkyOjNizszN NITWO5FUSU6JRWK=
COLO-320-HSR M1fYS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HTSmlEPTB;MkiuNFM4OyEQvF2= M37DW3NCVkeHUh?=
K5 NH;6O4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{KxSmlEPTB;MkiuNVI5PyEQvF2= NF:xPWpUSU6JRWK=
ES1 NH;iU2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DWfGlEPTB;MkiuO|c4OyEQvF2= MYPTRW5ITVJ?
LC-1F Mn\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJ7LkezOFYh|ryP MoDLV2FPT0WU
SCLC-21H NIniZmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnrc5lKSzVyPUOwMlc{OTdizszN NIiyW5pUSU6JRWK=
SK-PN-DW NX3SfHE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rSemlEPTB;M{KuOVU6QCEQvF2= MmrBV2FPT0WU
D-247MG Mm\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLPWHFTUUN3ME2zNk46Pzd|IN88US=> NHWwc|NUSU6JRWK=
TE-5 M4XlUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTN|LkCzOlIh|ryP MXXTRW5ITVJ?
MONO-MAC-6 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTN|LkWwOFgh|ryP NEnHUG1USU6JRWK=
LB2518-MEL NWT6XlVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTN|Lke2OlYh|ryP NY\3VFhUW0GQR1XS
LOXIMVI NUH6eWQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkOyTWM2OD1|Mz63PVI5KM7:TR?= NUnZbm9{W0GQR1XS
NCI-H209 NGC1RmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLETWM2OD1|NT6xOFQh|ryP M{TzS3NCVkeHUh?=
A253 M37NXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnhcHJFUUN3ME2zOU44PDJ7IN88US=> MYTTRW5ITVJ?
HCC1599 Ml\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTN4LkewOVMh|ryP MknWV2FPT0WU
EB-3 NXmxWmlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rqXGlEPTB;M{[uPVUyQCEQvF2= Mn7kV2FPT0WU
GOTO NInweoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rZWGlEPTB;M{euN|IzPCEQvF2= Mom2V2FPT0WU
SW684 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTRzLki0PVUh|ryP NFjp[3ZUSU6JRWK=
DEL NFvjbYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTR{LkC1NlIh|ryP NVPmb5dNW0GQR1XS
HT-144 M4TydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTR{LkG2O|Yh|ryP Mo\2V2FPT0WU
TE-9 MlXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXUbnNKSzVyPUSzMlQ2QTZizszN NXXUe5MzW0GQR1XS
KARPAS-45 NVz2WXBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULGfot[UUN3ME20OE4{QTJ3IN88US=> NV7VWnFlW0GQR1XS
HAL-01 NIfpVlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:0VXNKSzVyPUS0MlUxOzRizszN MljHV2FPT0WU
RCC10RGB M1nCV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnjUXdKSzVyPUS0Mlc{QTJizszN NETVOYNUSU6JRWK=
CP67-MEL M36wOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK4ZZFJUUN3ME20OU43OjRzIN88US=> M{HkZ3NCVkeHUh?=
NB17 NXrGTpdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL2TWM2OD12NT62OlQ{KM7:TR?= MVrTRW5ITVJ?
SK-UT-1 MkHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTR3Lkm0OlQh|ryP MnrBV2FPT0WU
JiyoyeP-2003 NX3vfHN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfDWZdKSzVyPUS2MlAyOTlizszN MYnTRW5ITVJ?
HCE-4 NFLTfJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D2[mlEPTB;NE[uOVk3QCEQvF2= M1\xbnNCVkeHUh?=
NCI-H720 MmPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfETWM2OD12Nj63OlgzKM7:TR?= NXfiVoRiW0GQR1XS
KARPAS-422 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\Y[2Q{UUN3ME20O{4xQDl3IN88US=> NGLRVFdUSU6JRWK=
Ramos-2G6-4C10 MkK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\wcmlEPTB;NEeuNVYzOiEQvF2= NIDMZ45USU6JRWK=
HCE-T MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHKwRXZKSzVyPUS3MlY5OjhizszN MlzPV2FPT0WU
PSN1 NITldpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjwc3hKSzVyPUS3Mlc5OTNizszN MWnTRW5ITVJ?

... 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

カスタマーフィードバック (8)


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Rating
Source Cancer Res, 2012, 71, 7547-57. Saracatinib (AZD0530) purchased from Selleck
Method Cell proliferation assay
Cell Lines Huh7 cells/SK-Hep1 cells
Concentrations 1 μmol/L
Incubation Time
Results Results of cell proliferation assay showed that saracatinib treatment could significantly atten-uate promotive hepatoma cellular proliferation conferred by stable LHBs expression in Huh7 and SK-Hep1 cells (Fig. A and B).

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Rating
Source Cancer Res, 2013, 71, 7547-57. Saracatinib (AZD0530) purchased from Selleck
Method Tumor xenograft experiments
Cell Lines tumor xenografted nude mice
Concentrations 25 mg/kg
Incubation Time 4 weeks
Results tumor xenograft experiments in nude mice showed that orally saracatinib administration could also alleviate instigative tumor formation induced by stable LHBs expression in Huh7 and SK-Hep1 cells .

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Rating
Source Mol Cancer Res, 2011, 9, 249-258. Saracatinib (AZD0530) purchased from Selleck
Method Cell Viability Assay
Cell Lines MDA-MB-231/1205Lu cells
Concentrations 50 uM
Incubation Time 1 h
Results To verify this observation, we used a second Src inhibitor, AZD0530, which also caused cell rounding (data not shown) and TRAIL sensitization.

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Rating
Source Cancer Biol Ther, 2011, 12(3), 215-28. Saracatinib (AZD0530) purchased from Selleck
Method Cell viability assays
Cell Lines embryonic fibroblasts
Concentrations 125 nM
Incubation Time 48 h
Results In transformed embryonic fibroblasts genetically deleted for toxic BH3 domain proteins BAX and BAK, but not deleted for BID, the combination of a SRC inhibitor (AZD0530; PP2; dasatinib) with a CHK1 inhibitor (UCN-01, AZD7762) was unable to cause cell killing.

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Rating
Source Transl Oncol, 2011, 4, 92-100. Saracatinib (AZD0530) purchased from Selleck
Method Western Blot
Cell Lines Hs683 cells
Concentrations 10 μM
Incubation Time 4 d
Results Figure 4 shows that AZD0530 prevented TMZ-induced soluble caveolin-1 expression but did not change basal levels of soluble caveolin-1 in Hs683 GBM cells. In contrast, erlotinib increased soluble caveolin-1 expression to a similar degree as TMZ in these Hs683 GBM cells.

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Rating
Source J Biomol Screen, 2013, 18, 54-66. Saracatinib (AZD0530) purchased from Selleck
Method 3D Tumor Growth Assay
Cell Lines PC-3M cells
Concentrations 0-10 uM
Incubation Time 7 d
Results Reduction of colony size was observed for a number of established anticancer drugs, and IC 50 values for those reference compounds were determined based on the average area size of the cluster. IC 50 values were determined in two independent experiments and were quite reproducible.

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Rating
Source J Biomol Screen, 2013, 18, 54-66. Saracatinib (AZD0530) purchased from Selleck
Method 3D Tumor Growth Assay
Cell Lines PC-3M cells
Concentrations 0-10uM
Incubation Time 7 day
Results Reduction of colony size was observed for a number of established anticancer drugs, and IC 50 values for those reference compounds were determined based on the average area size of the cluster. IC 50 values were determined in two independent experiments and were quite reproducible.

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Rating
Source 2010, Dr. Shuxin Han of Kent State University. Saracatinib (AZD0530) purchased from Selleck
Method IP assay, Q-PCR assay
Cell Lines Primary human hepatocytes
Concentrations 5 μM
Incubation Time 6 h
Results

文献中の引用 (34)

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