Saracatinib (AZD0530)

Saracatinib (AZD0530)は一種の有効なSrc阻害剤で、無細胞試験でIC50値が2.7 nMです。Saracatinib (AZD0530)はc-Yes、Fyn、Lyn、Blk、FgrとLckにも活性をしていますが、AblとEGFR (L858RとL861Q)に作用する活性が低いです。臨床2/3期。

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Saracatinib (AZD0530) 化学構造
分子量: 542.03

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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)は一種の有効なSrc阻害剤で、無細胞試験でIC50値が2.7 nMです。Saracatinib (AZD0530)はc-Yes、Fyn、Lyn、Blk、FgrとLckにも活性をしていますが、AblとEGFR (L858RとL861Q)に作用する活性が低いです。臨床2/3期。
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 NVLBNXhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnaS|hKSzVyPUCuNFYyPDNizszN MYnTRW5ITVJ?
LAMA-84 NGPBcJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDBTWtKSzVyPUCuNVU6QSEQvF2= Mn\IV2FPT0WU
MEG-01 Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PLZWlEPTB;MD6yN|Y5QCEQvF2= MVvTRW5ITVJ?
EM-2 NF\KVVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFX4flFKSzVyPUCuNlY2KM7:TR?= NFjCcIdUSU6JRWK=
TE-15 M1zhTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDaTWM2OD1yLkK3OFEzKM7:TR?= NHL1d4dUSU6JRWK=
NCI-H1648 NFTsfoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzGW4RKSzVyPUCuNlgyOTZizszN MVzTRW5ITVJ?
TE-12 M{LNN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PIS2lEPTB;MD6zNlY5KM7:TR?= NEDxdZVUSU6JRWK=
LB996-RCC NIjQeVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwNESxPVYh|ryP MlrqV2FPT0WU
K-562 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DUOmlEPTB;MD60OFk3PyEQvF2= MY\TRW5ITVJ?
D-336MG NFPsfIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwNUCzNFQh|ryP M37RNnNCVkeHUh?=
NOS-1 M1vOSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\venM{UUN3ME2wMlYxPTJ7IN88US=> NHLpbGZUSU6JRWK=
EW-24 NI[2OmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHhTHJKSzVyPUCuOlI3QTNizszN MXjTRW5ITVJ?
BV-173 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL0TWM2OD1yLk[1NlQ6KM7:TR?= NXfScYZuW0GQR1XS
NCCIT Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwN{OyNVgh|ryP NHjtWllUSU6JRWK=
NCI-H1436 MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoSwTWM2OD1yLke5NFQ6KM7:TR?= NVXhb3JkW0GQR1XS
BB30-HNC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwOE[yNFMh|ryP NXzJdVVKW0GQR1XS
TE-8 NFvZ[XZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwOEeyO|Uh|ryP NH;BelVUSU6JRWK=
A704 M1PDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFi5WnNKSzVyPUCuPFkzOSEQvF2= MUHTRW5ITVJ?
TK10 M4jCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVH5[JQxUUN3ME2wMlkxPjZ7IN88US=> NHKxXGNUSU6JRWK=
KS-1 M{X4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXrPHUzUUN3ME2xMlE6Pzd7IN88US=> NUX3eGJjW0GQR1XS
C2BBe1 M{HoZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXBSWVKSzVyPUGuNlA2ODdizszN MVPTRW5ITVJ?
RXF393 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXyc4hKSzVyPUGuNlQ{PiEQvF2= MkfMV2FPT0WU
KGN NFfC[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkiwTWM2OD1zLkK3Olg4KM7:TR?= MXfTRW5ITVJ?
NB69 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHNe25KSzVyPUGuN|c1QTdizszN M{\OOnNCVkeHUh?=
TE-11 M2DHZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFwNEO0NVgh|ryP MlTCV2FPT0WU
TE-1 M1vCWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTFwNESxNFUh|ryP M{Ti[nNCVkeHUh?=
ST486 M1LXTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTFwNEW4OVIh|ryP NI[xdHhUSU6JRWK=
HOP-62 Mk\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnkOVBVUUN3ME2xMlUxOjR4IN88US=> NYj0Z2VyW0GQR1XS
EW-16 NILBVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTFwNUWwPFMh|ryP NIXNd4lUSU6JRWK=
LB1047-RCC NEXOPGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwNUW0OVMh|ryP MVnTRW5ITVJ?
TE-10 MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjRenhKSzVyPUGuOlYzPTJizszN MnLpV2FPT0WU
RL95-2 M3z5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\i[WlEPTB;MT62OlkxOiEQvF2= MlLoV2FPT0WU
DOHH-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTIZmRpUUN3ME2xMlcyPzh{IN88US=> M4XBPXNCVkeHUh?=
MFH-ino MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETqZVBKSzVyPUGuO|c5PyEQvF2= MUjTRW5ITVJ?
GB-1 NF\RcHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\jZYZjUUN3ME2xMlc6QDN|IN88US=> NFHwd2lUSU6JRWK=
SK-N-DZ Ml\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTFwOES2PFgh|ryP M1S3[HNCVkeHUh?=
OS-RC-2 MmS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYW3cXdTUUN3ME2xMlg5PTd2IN88US=> NHfWeZBUSU6JRWK=
SW982 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHW[WZKSzVyPUGuPVIxQTNizszN M3i3ZXNCVkeHUh?=
KALS-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrXZ3hKSzVyPUGuPVg4OjJizszN NWD4SWF3W0GQR1XS
TGBC24TKB NX:xS5V2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvSTWM2OD1{LkC1PVU5KM7:TR?= M3PYR3NCVkeHUh?=
GI-1 M3HWfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DpTGlEPTB;Mj6xOlA5PCEQvF2= M4Xh[HNCVkeHUh?=
SW962 NYfZcVBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPmS4ZzUUN3ME2yMlE4OTd6IN88US=> NILlUYNUSU6JRWK=
SW872 NIfhfHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHWxdHhKSzVyPUKuNVg2ODdizszN Ml\rV2FPT0WU
NCI-H747 M3PEOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTJwMkW3NVQh|ryP MXLTRW5ITVJ?
MZ1-PC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJwMkmzOVYh|ryP MUjTRW5ITVJ?
MSTO-211H NFLneG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEmy[o1KSzVyPUKuN|U4OjNizszN NG\GOIhUSU6JRWK=
BL-70 Mn;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\QVmlEPTB;Mj60O|QzOiEQvF2= MnHTV2FPT0WU
SW954 M1jDdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHNWGp1UUN3ME2yMlU4PDB6IN88US=> Ml\jV2FPT0WU
SNB75 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDnPZJKSzVyPUKuOlg2QTRizszN M3\jT3NCVkeHUh?=
IST-SL2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj6OY1KSzVyPUKuO|I{PzlizszN MXLTRW5ITVJ?
GCIY NFrDdm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjyTWM2OD1{Lki3NFA2KM7:TR?= M4rRRXNCVkeHUh?=
KU812 NIHKfZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHQOZRKSzVyPUOuNFUzQTlizszN M2HQZnNCVkeHUh?=
LXF-289 NEDqNo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIr3RZRKSzVyPUOuNVIyODlizszN M{j0Z3NCVkeHUh?=
ETK-1 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\2c|hKSzVyPUOuNlA4PjdizszN NIPGS2VUSU6JRWK=
SF126 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTNwM{GxO|Qh|ryP M13peHNCVkeHUh?=
LC-2-ad NGCwSIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUW4e4lJUUN3ME2zMlU2PyEQvF2= NY\2bIg6W0GQR1XS
KNS-42 NVH2RWw2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HPOWlEPTB;Mz62OUDPxE1? NF74TWhUSU6JRWK=
OVCAR-4 MkLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnMdoxTUUN3ME2zMlc{PDN|IN88US=> MlmxV2FPT0WU
PF-382 NES1WoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTNwOEO2PVgh|ryP MUnTRW5ITVJ?
SH-4 NIiwfIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTRwMkWyOVkh|ryP M3LlTXNCVkeHUh?=
KM12 NInCfZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXO0OHU{UUN3ME20MlMzPDF4IN88US=> MnjiV2FPT0WU
NB5 M2HL[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTRwNEG4OlQh|ryP MXLTRW5ITVJ?
KURAMOCHI NGnzd5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTRwNkWyOVYh|ryP MmHvV2FPT0WU
Becker M2Pw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTRwNk[0NVYh|ryP M2KwW3NCVkeHUh?=
MV-4-11 M4ryNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2eyemlEPTB;ND64NVM1PCEQvF2= NX7mdGFwW0GQR1XS
KINGS-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXn4NVBwUUN3ME20MlgzOzd|IN88US=> MmfFV2FPT0WU
LS-123 NEXYSWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom3TWM2OD13LkS5Olg1KM7:TR?= M{PPOXNCVkeHUh?=
SF268 M2PSOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[zWGlEPTB;NT62NVI3OiEQvF2= NYP2TVk6W0GQR1XS
A388 M1PJb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjtTWM2OD13Lk[zOlY4KM7:TR?= M4e4V3NCVkeHUh?=
NMC-G1 M3u5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPOO3VjUUN3ME22MlAyQDFzIN88US=> NI\tWJhUSU6JRWK=
CGTH-W-1 M1rlbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzxSIlKSzVyPU[uNFIxPzVizszN MoLzV2FPT0WU
ES4 M3fP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTZwNUOwO|Qh|ryP MVHTRW5ITVJ?
SR NUmyZ45VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvhTWM2OD14LkW4PFA4KM7:TR?= Mme1V2FPT0WU
BB49-HNC MlfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX24N3ZJUUN3ME22Mlc{OjB4IN88US=> M1zwbHNCVkeHUh?=
KLE MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rhWmlEPTB;Nj63PFM4PyEQvF2= NH2xVmFUSU6JRWK=
HUTU-80 M{DoOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HVXWlEPTB;Nj65PFQ3PiEQvF2= MV;TRW5ITVJ?
SNU-C2B NWHufmN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHXTWM2OD15LkiyO|M4KM7:TR?= Mny4V2FPT0WU
BB65-RCC M3nuSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHydXlXUUN3ME23Mlk1QTB2IN88US=> NWfUSpRXW0GQR1XS
QIMR-WIL NELDW5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXtSoVKSzVyPUiuOFI5ODhizszN M2DVR3NCVkeHUh?=
GDM-1 MmriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInUOWZKSzVyPUiuPVczQTJizszN M3nsSXNCVkeHUh?=
LC4-1 MmrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTlwMEC5NVEh|ryP MlrGV2FPT0WU
MLMA MlvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTlwMUWwNFYh|ryP M2XicHNCVkeHUh?=
EoL-1-cell NFTlXWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7MTWM2OD17LkOwNVkzKM7:TR?= M2LpXHNCVkeHUh?=
BOKU MlPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXpTWM2OD17Lkm2OFY3KM7:TR?= NX22fHZ3W0GQR1XS
EVSA-T MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fxfWlEPTB;MUCuOlU3QCEQvF2= NHSy[lBUSU6JRWK=
D-283MED NY\RRXNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HoNWlEPTB;MUCuPVE4PiEQvF2= MWXTRW5ITVJ?
NB1 M3XDSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFzLkCyOFIh|ryP MX3TRW5ITVJ?
RPMI-8402 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXixNpdiUUN3ME2xNU4yPzhizszN M2\TeXNCVkeHUh?=
NCI-H1355 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGmzRVNKSzVyPUGxMlE5ODZizszN M2TKR3NCVkeHUh?=
NB7 Mmr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFzLkOyPVch|ryP NVyyOnBKW0GQR1XS
RPMI-6666 NUjofIRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT0TWM2OD1zMj65OVY4KM7:TR?= M1fQWXNCVkeHUh?=
697 M{S5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zWPGlEPTB;MUOuNlcxOSEQvF2= M1TjTnNCVkeHUh?=
CTB-1 M4PQVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF|LkW5OFgh|ryP Mmj1V2FPT0WU
VA-ES-BJ M{\4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;1N2lEPTB;MUOuPVI{PCEQvF2= NVTvWlhLW0GQR1XS
BE-13 NGrZRotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF2LkO5NVUh|ryP Mmi1V2FPT0WU
SKM-1 Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;pTWM2OD1zND60OFk6KM7:TR?= NVvXcXF3W0GQR1XS
TE-6 NITFVIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTF2Lke1PVEh|ryP M4m4b3NCVkeHUh?=
LB771-HNC NIrpZ4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NISzUVJKSzVyPUG0Mlc5QThizszN MXfTRW5ITVJ?
ECC4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr2RnJ3UUN3ME2xO{4xOjd5IN88US=> MonBV2FPT0WU
ES3 NHe3R4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofwTWM2OD1zNz60OlU2KM7:TR?= MnXCV2FPT0WU
LB647-SCLC MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGX2WXBKSzVyPUG3MlQ6PDlizszN NVi1[lNDW0GQR1XS
NB10 M2XocGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHOXnRKSzVyPUG4MlUzPTZizszN M3z4[3NCVkeHUh?=
L-540 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLMTWM2OD1zOD64NVA6KM7:TR?= NX[zV4FtW0GQR1XS
NCI-H2126 NYrTXJluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTF7LkWxJO69VQ>? NWfpclU3W0GQR1XS
HH NF3KSmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjHXnZbUUN3ME2yNE4xODl7IN88US=> MorQV2FPT0WU
MPP-89 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTJ|LkKyPFkh|ryP MYjTRW5ITVJ?
IST-MEL1 M1PtNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvteIl7UUN3ME2yN{45PjV6IN88US=> MlTjV2FPT0WU
KP-N-YS NUjEV3dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHacYhtUUN3ME2yN{46OjV3IN88US=> NIXRU4RUSU6JRWK=
EC-GI-10 NXTSZVhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFywZnBKSzVyPUK0MlU6QDlizszN MWfTRW5ITVJ?
EKVX M2HMeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYH1UVF6UUN3ME2yOk4xOjB|IN88US=> M4HWWXNCVkeHUh?=
TGBC1TKB MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDZVoVmUUN3ME2yOk41OzRizszN MWfTRW5ITVJ?
Daudi MkDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD0TWM2OD1{Nz6wO|c{KM7:TR?= M2jMfXNCVkeHUh?=
ALL-PO MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELNSZdKSzVyPUK3MlA5OSEQvF2= MnjLV2FPT0WU
NB6 NUS0dWFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTJ5LkS4PEDPxE1? NVXZVIR7W0GQR1XS
ES6 NYPn[mlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3iTWM2OD1{Nz65NVI{KM7:TR?= MnzFV2FPT0WU
COLO-320-HSR MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u5T2lEPTB;MkiuNFM4OyEQvF2= NHXVXVZUSU6JRWK=
K5 M33IWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO0N|dJUUN3ME2yPE4yOjh5IN88US=> MlnoV2FPT0WU
ES1 NGHENIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\z[oNKSzVyPUK4Mlc4PzNizszN M1XZbHNCVkeHUh?=
LC-1F NX;Qem1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjwS5J2UUN3ME2yPU44OzR4IN88US=> MVPTRW5ITVJ?
SCLC-21H Mm\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTNyLkezNVch|ryP M3ToVHNCVkeHUh?=
SK-PN-DW NIjDPIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS2TWM2OD1|Mj61OVk5KM7:TR?= M3nJXHNCVkeHUh?=
D-247MG M2Xhemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe4SJJxUUN3ME2zNk46Pzd|IN88US=> MX7TRW5ITVJ?
TE-5 NYT6PJNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjKNFBoUUN3ME2zN{4xOzZ{IN88US=> M4P0[XNCVkeHUh?=
MONO-MAC-6 Mny5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T3VmlEPTB;M{OuOVA1QCEQvF2= M4X5NXNCVkeHUh?=
LB2518-MEL NFP2[olIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrKR|JKSzVyPUOzMlc3PjZizszN M4GxU3NCVkeHUh?=
LOXIMVI NV3sc4N5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTN|Lke5Nlgh|ryP MVfTRW5ITVJ?
NCI-H209 M{LYb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn5RodKSzVyPUO1MlE1PCEQvF2= MWnTRW5ITVJ?
A253 NVPhZ4R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPHTWM2OD1|NT63OFI6KM7:TR?= MX;TRW5ITVJ?
HCC1599 NH[1SFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXDOYY1UUN3ME2zOk44ODV|IN88US=> MUnTRW5ITVJ?
EB-3 NH\UbZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDpNFRKSzVyPUO2Mlk2OThizszN NIX5cZZUSU6JRWK=
GOTO M1LVWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2ey[mlEPTB;M{euN|IzPCEQvF2= NULxNY5GW0GQR1XS
SW684 NH\xdlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TWPGlEPTB;NEGuPFQ6PSEQvF2= NUTCNXMyW0GQR1XS
DEL M4O1S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTR{LkC1NlIh|ryP NUXaXWxIW0GQR1XS
HT-144 NFvXNGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPzfIw6UUN3ME20Nk4yPjd4IN88US=> M4ezWnNCVkeHUh?=
TE-9 NUHGSW41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXBTWM2OD12Mz60OVk3KM7:TR?= MnLYV2FPT0WU
KARPAS-45 NF;he2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHoTWM2OD12ND6zPVI2KM7:TR?= MUHTRW5ITVJ?
HAL-01 NEm3VmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTR2LkWwN|Qh|ryP MXfTRW5ITVJ?
RCC10RGB MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWWyTGhJUUN3ME20OE44Ozl{IN88US=> NV24O2JiW0GQR1XS
CP67-MEL NIT3T3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLnXpVNUUN3ME20OU43OjRzIN88US=> MXTTRW5ITVJ?
NB17 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFiwWWZKSzVyPUS1MlY3PDNizszN MUHTRW5ITVJ?
SK-UT-1 NYXoWGRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTR3Lkm0OlQh|ryP MljkV2FPT0WU
JiyoyeP-2003 NHLwSnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTR4LkCxNVkh|ryP NHv2SGxUSU6JRWK=
HCE-4 NHHGRVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXHTWM2OD12Nj61PVY5KM7:TR?= Ml\zV2FPT0WU
NCI-H720 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;jSpBqUUN3ME20Ok44Pjh{IN88US=> NEPEVJNUSU6JRWK=
KARPAS-422 NXHDdlh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEi5XoJKSzVyPUS3MlA5QTVizszN MWHTRW5ITVJ?
Ramos-2G6-4C10 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXxXYZ{UUN3ME20O{4yPjJ{IN88US=> M17TTXNCVkeHUh?=
HCE-T MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPMTWM2OD12Nz62PFI5KM7:TR?= Mor3V2FPT0WU
PSN1 M1rnSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnaTWM2OD12Nz63PFE{KM7:TR?= MnSzV2FPT0WU

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 35 mg/mL warming (64.57 mM)
Ethanol 31 mg/mL (57.19 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/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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