Saracatinib (AZD0530)

製品コードS1006

Saracatinib (AZD0530)化学構造

分子量(MW):542.03

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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文献中の引用(35)

カスタマーフィードバック(8)

  • Saracatinib (AZD0530) administration alleviates provocative tumor formation conferred by LHBs exp ression. A and B, cell proliferation assay for Huh7 cells (A) and SK-Hep1 cells (B) after stable LHBs expression under treatment with saracatinib(1 μmol/L). *, P < 0.05.

    Cancer Res 2012 71, 7547-57. Saracatinib (AZD0530) purchased from Selleck.

    C and D, in vivo subcutaneous tumor growth curves (C) and tumor weight quantification of intersected subcutaneous tumor tissues (D) of Huh7 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n =18). *, P < 0.05. E and F,in vivo subcutaneous tumor growth curves (E) and tumor weight quantification of intersected subcutaneous tumor tissues (F) of SK-Hep1 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n = 18). *, P < 0.05.

    Cancer Res 2013 71, 7547-57. Saracatinib (AZD0530) purchased from Selleck.

  • cells treated for 1 hour with Src inhibitor AZD0530 (50 mmol/L), or the same volume of dimethyl sulfoxide, before TRAIL treatment (at concentrations described earlier) for 24 hours prior to alamar blue assay.

    Mol Cancer Res 2011 9, 249-258. Saracatinib (AZD0530) purchased from Selleck.

    MCF7 cells were plated in triplicate and treated with vehicle (VEH, DMSO) , AZD0530 (125 nM), AZD7762 (50 nM) or AZD7762 and AZD0530. Cells were isolated 48 h after exposure and subjected to the indicated various cell viability assays. Data for each assay is the mean of all data points from two studies(* p < 0.05 greater than CHK1 inhibitor value).

    Cancer Biol Ther 2011 12(3), 215-28. Saracatinib (AZD0530) purchased from Selleck.

  •  

    The TMZ-induced caveolin-1 modulation is Src-dependent in Hs683 GBM cells Western blot analyses of soluble caveolin-1 expression in Hs683 glioma cells treated with TMZ (100 μM) four times per week (day 1-4) for 7 h/d, the EGFR inhibitor (10 μM) (erlotinib; day 1), the Src inhibitor AZD0530 (10 μM) (day 1), and combination of the inhibitors and TMZ (+TMZ) compared with control untreated cells (Ct). Soluble caveolin-1 expression was measured on day 5.

    Transl Oncol 2011 4, 92-100. Saracatinib (AZD0530) purchased from Selleck.

    J Biomol Screen 2013 18, 54-66. Saracatinib (AZD0530) purchased from Selleck.

  • Example dose response curves of the PLK-1 inhibitor BI-2536. During the large dose response study for each reference compounds 8 dilutions were tested. Curves for IC50 determination for two independent experiments for the PLK1 inhibitor BI-2536 are displayed. This inhibitor is also used to achieve the LC values. IC50 has been determined with 7.48 +/- 0.09 log [M] and 6.75 +/- 0.21 log [M]. Correlating assay performance data are displayed in Suppl. Fig. 5. 

    J Biomol Screen 2013 18, 54-66. Saracatinib (AZD0530) purchased from Selleck.

    IP assay of tyrosine phosphorylation of VDR in the plasmamembrane. Primary human hepatocytes were treated with Veh, 1α, 25(OH)2-VD3 (50nM), LCA-acetate (10 μM), and/or the c-Src inhibitor AZD0530 (AZD) (5 μM) for 6 h.A rabbit anti-VDR antibody was used to immunoprecipitate VDR from cell membrane extracts (300 μg). A mouse anti-phospho-tyrosine was used to detect phosphotyrosines in VDR. A mouse anti-VDR was used to detect immunoprecipitated VDR. Ten % cell extract was set aside as input. Q-PCR assay of the effects of AZD on CYP7A1,CYP27A1, and CYP24A1 mRNA expression in primary human hepatocytes. Primary human hepatocytes were treated with Veh, 1α, 25(OH)2-VD3 (50 nM), LCA-acetate (10 μM), and/or AZD (5 μM) for 16 h. An $, *, or # indicates statistically significant difference, p < 0.05, AZD-treated versus vehicle control, 1α, 25(OH)2-VD3 or LCAacetate-treated versus vehicle control, or 1α, 25(OH)2-VD3 plus AZD or LCA-acetateplus AZD co-treated versus 1α, 25(OH)2-VD3 or LCA-acetate-treated. All the datarepresent one of three separate experiments using primary human hepatocytes from different liver donors (#HH1479, #HH1483, #HH1493, #HH1524, #HH1560, and#HH1567).

     

     

    2010 Dr. Shuxin Han of Kent State University. Saracatinib (AZD0530) purchased from Selleck.

製品安全説明書

Src阻害剤の選択性比較

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。
特性 The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
靶点
c-Src [2]
(Cell-free assay)
LCK [2]
(Cell-free assay)
c-YES [2]
(Cell-free assay)
EGFR (L861Q) [2]
(Cell-free assay)
Lyn [2]
(Cell-free assay)
2.7 nM <4 nM 4 nM 4 nM 5 nM
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CTV-1 NV\QXWN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M12yNWlEPTB;MD6wOlE1OyEQvF2= MorMV2FPT0WU
LAMA-84 MmjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwMUW5PUDPxE1? MU\TRW5ITVJ?
MEG-01 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:0bWlEPTB;MD6yN|Y5QCEQvF2= M{D6WnNCVkeHUh?=
EM-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnrXIVbUUN3ME2wMlI3PSEQvF2= NELXXHlUSU6JRWK=
TE-15 M134bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7HTWM2OD1yLkK3OFEzKM7:TR?= Mo\UV2FPT0WU
NCI-H1648 M37Ucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknSTWM2OD1yLkK4NVE3KM7:TR?= MVTTRW5ITVJ?
TE-12 Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3zeZlKSzVyPUCuN|I3QCEQvF2= NYjkeFZSW0GQR1XS
LB996-RCC NWfpXWF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzWT|JRUUN3ME2wMlQ1OTl4IN88US=> NI\t[2tUSU6JRWK=
K-562 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIroe4xKSzVyPUCuOFQ6PjdizszN NYHxSFNGW0GQR1XS
D-336MG NFXsW2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwNUCzNFQh|ryP NX3uPJl[W0GQR1XS
NOS-1 NWDKd21NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTP[lNIUUN3ME2wMlYxPTJ7IN88US=> M17USnNCVkeHUh?=
EW-24 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn1RYRKSzVyPUCuOlI3QTNizszN NEX6XmtUSU6JRWK=
BV-173 NHLFZVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f4XmlEPTB;MD62OVI1QSEQvF2= MYnTRW5ITVJ?
NCCIT M{jleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV20[2pYUUN3ME2wMlc{OjF6IN88US=> MVzTRW5ITVJ?
NCI-H1436 NWDCfZl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{ntNGlEPTB;MD63PVA1QSEQvF2= MWrTRW5ITVJ?
BB30-HNC NVjafnFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC0UWhiUUN3ME2wMlg3OjB|IN88US=> NILBN|JUSU6JRWK=
TE-8 NV\mOVFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rnO2lEPTB;MD64O|I4PSEQvF2= MnK5V2FPT0WU
A704 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXhTWM2OD1yLki5NlEh|ryP MUjTRW5ITVJ?
TK10 M2nzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv5TWM2OD1yLkmwOlY6KM7:TR?= MXrTRW5ITVJ?
KS-1 NWG0bZdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vDdWlEPTB;MT6xPVc4QSEQvF2= NE\qU4NUSU6JRWK=
C2BBe1 NFLz[FZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwMkC1NFch|ryP MkHGV2FPT0WU
RXF393 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTFwMkSzOkDPxE1? MV7TRW5ITVJ?
KGN MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH2WlJCUUN3ME2xMlI4Pjh5IN88US=> NVXQRlRRW0GQR1XS
NB69 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj6c3JKSzVyPUGuN|c1QTdizszN MYTTRW5ITVJ?
TE-11 M1TTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1raTWlEPTB;MT60N|QyQCEQvF2= M1nu[3NCVkeHUh?=
TE-1 NVfHVXI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVGzOJdWUUN3ME2xMlQ1OTB3IN88US=> NGDwc4RUSU6JRWK=
ST486 MlK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPRTWM2OD1zLkS1PFUzKM7:TR?= MU\TRW5ITVJ?
HOP-62 MorCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzmZ5hKSzVyPUGuOVAzPDZizszN M3TLUXNCVkeHUh?=
EW-16 Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL1TWM2OD1zLkW1NFg{KM7:TR?= Mn35V2FPT0WU
LB1047-RCC MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XXRWlEPTB;MT61OVQ2OyEQvF2= MUjTRW5ITVJ?
TE-10 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\PSnMyUUN3ME2xMlY3OjV{IN88US=> NEXDRXNUSU6JRWK=
RL95-2 M17nTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjHW4xKSzVyPUGuOlY6ODJizszN NUDRPZJVW0GQR1XS
DOHH-2 NGTOfYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3jRoxKSzVyPUGuO|E4QDJizszN MWrTRW5ITVJ?
MFH-ino M3j0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFwN{e4O{DPxE1? M2Oz[nNCVkeHUh?=
GB-1 MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TRdGlEPTB;MT63PVg{OyEQvF2= MXjTRW5ITVJ?
SK-N-DZ MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LpdGlEPTB;MT64OFY5QCEQvF2= MV;TRW5ITVJ?
OS-RC-2 NXTae3BGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3GTWM2OD1zLki4OVc1KM7:TR?= M13a[XNCVkeHUh?=
SW982 NWf6d4hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XHcGlEPTB;MT65NlA6OyEQvF2= NGfpfm5USU6JRWK=
KALS-1 NEG0bYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGi5foxKSzVyPUGuPVg4OjJizszN NWXucpVrW0GQR1XS
TGBC24TKB NEjmOI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSz[GxpUUN3ME2yMlA2QTV6IN88US=> NFHvTJpUSU6JRWK=
GI-1 M{\3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrSZZlHUUN3ME2yMlE3ODh2IN88US=> M1nwXHNCVkeHUh?=
SW962 NFfObXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjXVIpoUUN3ME2yMlE4OTd6IN88US=> MXTTRW5ITVJ?
SW872 NWL3T|ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJwMUi1NFch|ryP MX;TRW5ITVJ?
NCI-H747 NHzSSGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJwMkW3NVQh|ryP M3vpRnNCVkeHUh?=
MZ1-PC MnHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITKfIZKSzVyPUKuNlk{PTZizszN NIjNeJVUSU6JRWK=
MSTO-211H NHz0S3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJwM{W3NlMh|ryP NV6wZ|I3W0GQR1XS
BL-70 M3ixWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkToTWM2OD1{LkS3OFIzKM7:TR?= M4jybHNCVkeHUh?=
SW954 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTWTWM2OD1{LkW3OFA5KM7:TR?= M4TCN3NCVkeHUh?=
SNB75 NHTQUXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnjbZVKSzVyPUKuOlg2QTRizszN NH3qe2lUSU6JRWK=
IST-SL2 M2T4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X6NGlEPTB;Mj63NlM4QSEQvF2= NIHGSZJUSU6JRWK=
GCIY NESwbFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJwOEewNFUh|ryP NGHnfG9USU6JRWK=
KU812 Mon2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\TTWM2OD1|LkC1Nlk6KM7:TR?= NHzkUGRUSU6JRWK=
LXF-289 NH[1NnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DFRmlEPTB;Mz6xNlExQSEQvF2= M4ftSHNCVkeHUh?=
ETK-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDTO4d4UUN3ME2zMlIxPzZ5IN88US=> MoHsV2FPT0WU
SF126 NF7R[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vFZWlEPTB;Mz6zNVE4PCEQvF2= MXzTRW5ITVJ?
LC-2-ad MkTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkizTWM2OD1|LkW1O{DPxE1? NVrL[ZhbW0GQR1XS
KNS-42 Moj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFS5VZVKSzVyPUOuOlUh|ryP NWXpN3hiW0GQR1XS
OVCAR-4 NEm0fGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTNwN{O0N|Mh|ryP Mn\tV2FPT0WU
PF-382 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTNwOEO2PVgh|ryP MWXTRW5ITVJ?
SH-4 M3v5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnBUIhKSzVyPUSuNlUzPTlizszN NF\nWVZUSU6JRWK=
KM12 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTSTWM2OD12LkOyOFE3KM7:TR?= NGjlZVdUSU6JRWK=
NB5 M3viUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFz1UZRKSzVyPUSuOFE5PjRizszN M{fYW3NCVkeHUh?=
KURAMOCHI Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTRwNkWyOVYh|ryP M{DpO3NCVkeHUh?=
Becker NHLIV2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW1TWM2OD12Lk[2OFE3KM7:TR?= MYLTRW5ITVJ?
MV-4-11 NX7NN|dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{H6NmlEPTB;ND64NVM1PCEQvF2= NHyxWIRUSU6JRWK=
KINGS-1 M3TZWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LjUGlEPTB;ND64NlM4OyEQvF2= MkDkV2FPT0WU
LS-123 M3PnPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;ZOGlEPTB;NT60PVY5PCEQvF2= M4DaT3NCVkeHUh?=
SF268 NGG0NVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXX5[HV{UUN3ME21MlYyOjZ{IN88US=> MnzOV2FPT0WU
A388 M1\oUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTVwNkO2Olch|ryP NXvz[ZFzW0GQR1XS
NMC-G1 M2PWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHuTWM2OD14LkCxPFEyKM7:TR?= NIDFS4tUSU6JRWK=
CGTH-W-1 NFTqSY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnJN2ZKSzVyPU[uNFIxPzVizszN MWXTRW5ITVJ?
ES4 NF7rRZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTZwNUOwO|Qh|ryP MmDrV2FPT0WU
SR NYjkRWh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTZwNUi4NFch|ryP M3TaNnNCVkeHUh?=
BB49-HNC MkjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;RfFNKSzVyPU[uO|MzODZizszN M1f1bnNCVkeHUh?=
KLE NUP1[lhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jzeWlEPTB;Nj63PFM4PyEQvF2= M2fOTHNCVkeHUh?=
HUTU-80 MkfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLJTWM2OD14Lkm4OFY3KM7:TR?= MUDTRW5ITVJ?
SNU-C2B Mlv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPpPG1KSzVyPUeuPFI4OzdizszN MnHVV2FPT0WU
BB65-RCC NG\Jd2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPhfVhKSzVyPUeuPVQ6ODRizszN M4rPeHNCVkeHUh?=
QIMR-WIL MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT4NHJHUUN3ME24MlQzQDB6IN88US=> MmTtV2FPT0WU
GDM-1 MlHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPkU4hKSzVyPUiuPVczQTJizszN NWnrWFNOW0GQR1XS
LC4-1 NIPvN5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDQ[lFxUUN3ME25MlAxQTFzIN88US=> MYPTRW5ITVJ?
MLMA NGiySXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzybIZKSzVyPUmuNVUxODZizszN Mn:5V2FPT0WU
EoL-1-cell NVO4ZXoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmi5TWM2OD17LkOwNVkzKM7:TR?= NFTOOoxUSU6JRWK=
BOKU NUDyV5Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzV[XdvUUN3ME25Mlk3PDZ4IN88US=> NH7WWYRUSU6JRWK=
EVSA-T NV;1dHlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVyx[GFWUUN3ME2xNE43PTZ6IN88US=> MlTQV2FPT0WU
D-283MED M1LVOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHG1fnJKSzVyPUGwMlkyPzZizszN M3zDcXNCVkeHUh?=
NB1 NEHiTYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFzLkCyOFIh|ryP NVzRUIg1W0GQR1XS
RPMI-8402 M{i4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3GyfGlEPTB;MUGuNVc5KM7:TR?= NFL6SoZUSU6JRWK=
NCI-H1355 NUXMWoJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPGeGhKSzVyPUGxMlE5ODZizszN Mn3LV2FPT0WU
NB7 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTFzLkOyPVch|ryP MljFV2FPT0WU
RPMI-6666 NFPy[5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnezTWM2OD1zMj65OVY4KM7:TR?= M{\WNnNCVkeHUh?=
697 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LCOGlEPTB;MUOuNlcxOSEQvF2= NET0dWFUSU6JRWK=
CTB-1 NGLKWGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7DSo9KSzVyPUGzMlU6PDhizszN MlfZV2FPT0WU
VA-ES-BJ MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7RTWM2OD1zMz65NlM1KM7:TR?= MWnTRW5ITVJ?
BE-13 NXnJenkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3kV4ljUUN3ME2xOE4{QTF3IN88US=> MXHTRW5ITVJ?
SKM-1 MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rWfmlEPTB;MUSuOFQ6QSEQvF2= NXzyOpB4W0GQR1XS
TE-6 M2DSfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTaeHZSUUN3ME2xOE44PTlzIN88US=> MWPTRW5ITVJ?
LB771-HNC NIfsXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXmR5pKSzVyPUG0Mlc5QThizszN NHr3OVRUSU6JRWK=
ECC4 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHPVmlKSzVyPUG3MlAzPzdizszN MmPjV2FPT0WU
ES3 M4\2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTF5LkS2OVUh|ryP Mlf1V2FPT0WU
LB647-SCLC M4fsfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPsSZZKSzVyPUG3MlQ6PDlizszN M3fWWnNCVkeHUh?=
NB10 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrCV45KSzVyPUG4MlUzPTZizszN M1zWZXNCVkeHUh?=
L-540 NF3NbnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\E[|FFUUN3ME2xPE45OTB7IN88US=> MkPmV2FPT0WU
NCI-H2126 NWDCVmJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUizOZA6UUN3ME2xPU42OSEQvF2= Ml3TV2FPT0WU
HH MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJyLkCwPVkh|ryP MVfTRW5ITVJ?
MPP-89 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DtZWlEPTB;MkOuNlI5QSEQvF2= NXHaPY1CW0GQR1XS
IST-MEL1 MkC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvScI5lUUN3ME2yN{45PjV6IN88US=> NWLnSHByW0GQR1XS
KP-N-YS M4\yNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL1TWM2OD1{Mz65NlU2KM7:TR?= MWDTRW5ITVJ?
EC-GI-10 NInhPJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnQVJVKSzVyPUK0MlU6QDlizszN NFj5bIlUSU6JRWK=
EKVX Mk\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1W0bmlEPTB;Mk[uNFIxOyEQvF2= MkftV2FPT0WU
TGBC1TKB MmDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkf6TWM2OD1{Nj60N|Qh|ryP MYTTRW5ITVJ?
Daudi M3XofWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnXTWM2OD1{Nz6wO|c{KM7:TR?= MWfTRW5ITVJ?
ALL-PO M4Dh[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TUcmlEPTB;MkeuNFgyKM7:TR?= MmKxV2FPT0WU
NB6 NFrTcYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJ5LkS4PEDPxE1? MnXwV2FPT0WU
ES6 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJ5LkmxNlMh|ryP NUf6eo5kW0GQR1XS
COLO-320-HSR NF7SVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH2yV4dKSzVyPUK4MlA{PzNizszN M2TwbXNCVkeHUh?=
K5 M{j3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7UOW1KSzVyPUK4MlEzQDdizszN NUHvfIxwW0GQR1XS
ES1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XVVGlEPTB;MkiuO|c4OyEQvF2= MnS4V2FPT0WU
LC-1F Ml60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVr6XIVYUUN3ME2yPU44OzR4IN88US=> M1e5fXNCVkeHUh?=
SCLC-21H MoTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;LPWlEPTB;M{CuO|MyPyEQvF2= NHPYWFFUSU6JRWK=
SK-PN-DW NX\C[olCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN{LkW1PVgh|ryP NF:0XVhUSU6JRWK=
D-247MG MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoT6TWM2OD1|Mj65O|c{KM7:TR?= M3TTfXNCVkeHUh?=
TE-5 MmXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nsS2lEPTB;M{OuNFM3OiEQvF2= M2juenNCVkeHUh?=
MONO-MAC-6 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTN|LkWwOFgh|ryP MWnTRW5ITVJ?
LB2518-MEL MkfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\ue4k{UUN3ME2zN{44PjZ4IN88US=> MmLCV2FPT0WU
LOXIMVI NH7ZdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33nUGlEPTB;M{OuO|kzQCEQvF2= NXn3eGlHW0GQR1XS
NCI-H209 MkXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnHN3pJUUN3ME2zOU4yPDRizszN NF7KTZFUSU6JRWK=
A253 M{LUOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTN3Lke0Nlkh|ryP MU\TRW5ITVJ?
HCC1599 NH\6eY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTN4LkewOVMh|ryP MXLTRW5ITVJ?
EB-3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq5c3dtUUN3ME2zOk46PTF6IN88US=> M4nTTnNCVkeHUh?=
GOTO MlnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTN5LkOyNlQh|ryP MmrJV2FPT0WU
SW684 NGO0THNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XmXmlEPTB;NEGuPFQ6PSEQvF2= MnHYV2FPT0WU
DEL MlGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3qTWM2OD12Mj6wOVIzKM7:TR?= NFHJZ3FUSU6JRWK=
HT-144 MmnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\pO5NKSzVyPUSyMlE3PzZizszN MYjTRW5ITVJ?
TE-9 NXr4NZpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTR|LkS1PVYh|ryP MYDTRW5ITVJ?
KARPAS-45 NF\UfW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTMTWM2OD12ND6zPVI2KM7:TR?= NVHqWYxiW0GQR1XS
HAL-01 Ml:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjKW3FKSzVyPUS0MlUxOzRizszN MlzTV2FPT0WU
RCC10RGB MnL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTR2LkezPVIh|ryP M{XiWXNCVkeHUh?=
CP67-MEL NHnNbYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTR3Lk[yOFEh|ryP NGPvUG9USU6JRWK=
NB17 NXnodZJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTR3Lk[2OFMh|ryP MVnTRW5ITVJ?
SK-UT-1 NVPDVFNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVL0bpV4UUN3ME20OU46PDZ2IN88US=> M1ra[HNCVkeHUh?=
JiyoyeP-2003 NH\lT4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTR4LkCxNVkh|ryP M1zTbnNCVkeHUh?=
HCE-4 NXPHVoY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTR4LkW5Olgh|ryP M3XRSnNCVkeHUh?=
NCI-H720 NGDDO|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXPTmZKSzVyPUS2Mlc3QDJizszN MXjTRW5ITVJ?
KARPAS-422 MnnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfvfnY5UUN3ME20O{4xQDl3IN88US=> M{DXfHNCVkeHUh?=
Ramos-2G6-4C10 NVe0XFZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrZTWM2OD12Nz6xOlIzKM7:TR?= M1\YOnNCVkeHUh?=
HCE-T NVW0c5pqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz2TWM2OD12Nz62PFI5KM7:TR?= NV;ofmRCW0GQR1XS
PSN1 NVHGS21LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nIemlEPTB;NEeuO|gyOyEQvF2= MVrTRW5ITVJ?

... 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]

プロトコル(参考用のみ)

キナーゼアッセイ:[1]
+ 展開

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]
+ 展開
  • 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
    (参考用のみ)
動物実験:[1]
+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 35 mg/mL (64.57 mM) warming
Ethanol 31 mg/mL (57.19 mM)
Water <1 mg/mL
体内 2% DMSO+30% PEG 300+ddH2O 5mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 542.03
化学式

C27H32ClN5O5

CAS No. 379231-04-6
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02955186 Not yet recruiting Alcohol Drinking Yale University January 2017 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Womens Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2
NCT02732587 Active, not recruiting Alcohol Drinking Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) November 2015 Phase 1
NCT02167256 Active, not recruiting Alzheimers Disease Yale University|Alzheimers Therapeutic Research Institute December 2014 Phase 2
NCT02262026 Recruiting Alcoholism Yale University November 2014 Phase 1
NCT02116712 Completed Pulmonary Lymphangioleiomyomatosis Tony Eissa|University of Texas|University of Cincinnati|Baylor College of Medicine August 2014 Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    What is the half-life of Saracatinib?

  • 回答:

    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

Src信号経路図

Src Inhibitors with Unique Features

相関Src製品

Tags: Saracatinib (AZD0530)を買う | Saracatinib (AZD0530) ic50 | Saracatinib (AZD0530)供給者 | Saracatinib (AZD0530)を購入する | Saracatinib (AZD0530)費用 | Saracatinib (AZD0530)生産者 | オーダーSaracatinib (AZD0530) | Saracatinib (AZD0530)化学構造 | Saracatinib (AZD0530)分子量 | Saracatinib (AZD0530)代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID