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。

サイズ 価格(税別)  
JPY 15106.00
JPY 11620.00
JPY 28220.00
JPY 111220.00

文献中の使用例(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.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CTV-1 NF3GcZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX3PFd2UUN3ME2wMlA3OTR|IN88US=> MVPTRW5ITVJ?
LAMA-84 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIf4bHlKSzVyPUCuNVU6QSEQvF2= MVjTRW5ITVJ?
MEG-01 NVXWeWszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwMkO2PFgh|ryP MYPTRW5ITVJ?
EM-2 NH7j[4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjOfHpKSzVyPUCuNlY2KM7:TR?= MlTkV2FPT0WU
TE-15 M{XaUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwMke0NVIh|ryP MUnTRW5ITVJ?
NCI-H1648 MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwMkixNVYh|ryP M3nVPHNCVkeHUh?=
TE-12 M1ezdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInie45KSzVyPUCuN|I3QCEQvF2= M{fLUXNCVkeHUh?=
LB996-RCC NH\CbZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H6bmlEPTB;MD60OFE6PiEQvF2= NVXvZpN{W0GQR1XS
K-562 MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHSWIdmUUN3ME2wMlQ1QTZ5IN88US=> NG\BSIpUSU6JRWK=
D-336MG MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DOXmlEPTB;MD61NFMxPCEQvF2= NWf3VmpqW0GQR1XS
NOS-1 NHnvZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\sUWlEPTB;MD62NFUzQSEQvF2= NFHFUYJUSU6JRWK=
EW-24 MlzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknITWM2OD1yLk[yOlk{KM7:TR?= MVrTRW5ITVJ?
BV-173 NUC4O3dDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1yze2lEPTB;MD62OVI1QSEQvF2= M3O3VXNCVkeHUh?=
NCCIT NWPzVoZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTaPHJ6UUN3ME2wMlc{OjF6IN88US=> NFm1bGNUSU6JRWK=
NCI-H1436 NXnlNFl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXmbnJKSzVyPUCuO|kxPDlizszN MUXTRW5ITVJ?
BB30-HNC MlPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnziTWM2OD1yLki2NlA{KM7:TR?= Mm\JV2FPT0WU
TE-8 NUDTW2ZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwOEeyO|Uh|ryP MnfNV2FPT0WU
A704 MkjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwOEmyNUDPxE1? NXvmelJoW0GQR1XS
TK10 MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrSTWM2OD1yLkmwOlY6KM7:TR?= NIrZXnpUSU6JRWK=
KS-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X2PGlEPTB;MT6xPVc4QSEQvF2= NUD1VmpCW0GQR1XS
C2BBe1 NHHwTW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTFwMkC1NFch|ryP MmjBV2FPT0WU
RXF393 NV;Ee3FWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXISGZKSzVyPUGuNlQ{PiEQvF2= MoLWV2FPT0WU
KGN NFWwS4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTFwMke2PFch|ryP Mm\FV2FPT0WU
NB69 M{Lrd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfWZVJKSzVyPUGuN|c1QTdizszN MWnTRW5ITVJ?
TE-11 NEm5e5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mny2TWM2OD1zLkSzOFE5KM7:TR?= M4rhOnNCVkeHUh?=
TE-1 NXOxXFk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHZZ45KSzVyPUGuOFQyODVizszN M1fqWXNCVkeHUh?=
ST486 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[xU2lEPTB;MT60OVg2OiEQvF2= MX3TRW5ITVJ?
HOP-62 Mne1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPQTWM2OD1zLkWwNlQ3KM7:TR?= M3\5c3NCVkeHUh?=
EW-16 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPwU3VQUUN3ME2xMlU2ODh|IN88US=> NF3KO|lUSU6JRWK=
LB1047-RCC NV3kXHZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj0TWM2OD1zLkW1OFU{KM7:TR?= NX;XenZsW0GQR1XS
TE-10 Ml\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTFwNk[yOVIh|ryP MoXUV2FPT0WU
RL95-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLlTlFKSzVyPUGuOlY6ODJizszN MX\TRW5ITVJ?
DOHH-2 NF7ZdGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmO4TWM2OD1zLkexO|gzKM7:TR?= MkO5V2FPT0WU
MFH-ino M3Lkb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnNdXN7UUN3ME2xMlc4QDdizszN M2jpOHNCVkeHUh?=
GB-1 NILlT5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUi3T|ZUUUN3ME2xMlc6QDN|IN88US=> NWjIVFRmW0GQR1XS
SK-N-DZ Ml;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofVTWM2OD1zLki0Olg5KM7:TR?= MlPLV2FPT0WU
OS-RC-2 M1fH[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;oco01UUN3ME2xMlg5PTd2IN88US=> NXPoOph[W0GQR1XS
SW982 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDFRlUyUUN3ME2xMlkzODl|IN88US=> M4m0VXNCVkeHUh?=
KALS-1 MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTFwOUi3NlIh|ryP NX7LdnY5W0GQR1XS
TGBC24TKB NWPkb4FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkG3TWM2OD1{LkC1PVU5KM7:TR?= MlzWV2FPT0WU
GI-1 MkPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTJwMU[wPFQh|ryP NIKy[nhUSU6JRWK=
SW962 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XtNGlEPTB;Mj6xO|E4QCEQvF2= NILER2dUSU6JRWK=
SW872 M4rKNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnn0TWM2OD1{LkG4OVA4KM7:TR?= M2ixXHNCVkeHUh?=
NCI-H747 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWzTWM2OD1{LkK1O|E1KM7:TR?= MVLTRW5ITVJ?
MZ1-PC NFr6[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;yelZKSzVyPUKuNlk{PTZizszN MYDTRW5ITVJ?
MSTO-211H M2XiSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj3O5U3UUN3ME2yMlM2PzJ|IN88US=> MmfzV2FPT0WU
BL-70 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnIOZpKSzVyPUKuOFc1OjJizszN NWXCd4N7W0GQR1XS
SW954 MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHexV2pKSzVyPUKuOVc1ODhizszN MnXBV2FPT0WU
SNB75 M1HDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjRNndKSzVyPUKuOlg2QTRizszN MVPTRW5ITVJ?
IST-SL2 M4jBfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DPWWlEPTB;Mj63NlM4QSEQvF2= M3;yWHNCVkeHUh?=
GCIY MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13GWGlEPTB;Mj64O|AxPSEQvF2= M2LGbHNCVkeHUh?=
KU812 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW0VIZKSzVyPUOuNFUzQTlizszN NHP3UYZUSU6JRWK=
LXF-289 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLjdVdtUUN3ME2zMlEzOTB7IN88US=> MnHnV2FPT0WU
ETK-1 MkTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrwTWM2OD1|LkKwO|Y4KM7:TR?= M4L0PHNCVkeHUh?=
SF126 M2XyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlX6TWM2OD1|LkOxNVc1KM7:TR?= NVjSN3RsW0GQR1XS
LC-2-ad NXi2RYxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTNwNUW3JO69VQ>? NIPaeWdUSU6JRWK=
KNS-42 NGTP[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTNwNkWg{txO MYHTRW5ITVJ?
OVCAR-4 NYPuOWdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPhTWM2OD1|LkezOFM{KM7:TR?= NFi4cmZUSU6JRWK=
PF-382 NUX1SZdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorITWM2OD1|LkizOlk5KM7:TR?= NG\yXZlUSU6JRWK=
SH-4 NIrxfVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknDTWM2OD12LkK1NlU6KM7:TR?= NYHJdIdWW0GQR1XS
KM12 NXvBUYtJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDOTWM2OD12LkOyOFE3KM7:TR?= Mk\oV2FPT0WU
NB5 MlrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTRwNEG4OlQh|ryP NFLHUGtUSU6JRWK=
KURAMOCHI NYPTbZJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHGTWM2OD12Lk[1NlU3KM7:TR?= NFj6bXBUSU6JRWK=
Becker M4juN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLyW4d2UUN3ME20MlY3PDF4IN88US=> NWDseGZvW0GQR1XS
MV-4-11 M4rQWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17HW2lEPTB;ND64NVM1PCEQvF2= NUX5S4c4W0GQR1XS
KINGS-1 NHntc49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjtOolbUUN3ME20MlgzOzd|IN88US=> MnO3V2FPT0WU
LS-123 NFvUe2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LVOmlEPTB;NT60PVY5PCEQvF2= MVvTRW5ITVJ?
SF268 NWj5OmRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTVwNkGyOlIh|ryP MVXTRW5ITVJ?
A388 Mlm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknNTWM2OD13Lk[zOlY4KM7:TR?= MXLTRW5ITVJ?
NMC-G1 M37ZVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjqVpZKSzVyPU[uNFE5OTFizszN NGfUZYZUSU6JRWK=
CGTH-W-1 M1fuOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rk[WlEPTB;Nj6wNlA4PSEQvF2= MYfTRW5ITVJ?
ES4 NY\RXGdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LYR2lEPTB;Nj61N|A4PCEQvF2= M{X6PXNCVkeHUh?=
SR M3PCPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHqW3ZiUUN3ME22MlU5QDB5IN88US=> MnnXV2FPT0WU
BB49-HNC NUCxOnE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTZwN{OyNFYh|ryP MVfTRW5ITVJ?
KLE MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrhNFN5UUN3ME22Mlc5Ozd5IN88US=> NFzNPWpUSU6JRWK=
HUTU-80 M3rpNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTZwOUi0OlYh|ryP NGDjWpNUSU6JRWK=
SNU-C2B MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HQN2lEPTB;Nz64Nlc{PyEQvF2= M4\xXnNCVkeHUh?=
BB65-RCC MoXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTwTWM2OD15Lkm0PVA1KM7:TR?= M1PiZnNCVkeHUh?=
QIMR-WIL NVuwOJJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRThwNEK4NFgh|ryP NH;jToJUSU6JRWK=
GDM-1 M{LXV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3jTWM2OD16Lkm3NlkzKM7:TR?= MlfHV2FPT0WU
LC4-1 NIH6SHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\YVoNKSzVyPUmuNFA6OTFizszN NI\tPGhUSU6JRWK=
MLMA MkXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;uTWM2OD17LkG1NFA3KM7:TR?= MkTmV2FPT0WU
EoL-1-cell M4fheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTEOmJKSzVyPUmuN|AyQTJizszN MmfaV2FPT0WU
BOKU NFLhdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfCWmZKSzVyPUmuPVY1PjZizszN NYX1S5lWW0GQR1XS
EVSA-T MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTFyLk[1Olgh|ryP MoiwV2FPT0WU
D-283MED NV;hSHhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFyLkmxO|Yh|ryP MXPTRW5ITVJ?
NB1 NEnQeI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTFzLkCyOFIh|ryP NHrwVoVUSU6JRWK=
RPMI-8402 NXjPbXRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3nRoxQUUN3ME2xNU4yPzhizszN MVfTRW5ITVJ?
NCI-H1355 M{L3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFixfWdKSzVyPUGxMlE5ODZizszN NETsXWdUSU6JRWK=
NB7 Ml\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnaVIpsUUN3ME2xNU4{Ojl5IN88US=> MULTRW5ITVJ?
RPMI-6666 M4X6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvkR3JFUUN3ME2xNk46PTZ5IN88US=> MXTTRW5ITVJ?
697 M4nzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\xbnVKSzVyPUGzMlI4ODFizszN NX;4bop1W0GQR1XS
CTB-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz5Wml{UUN3ME2xN{42QTR6IN88US=> MV3TRW5ITVJ?
VA-ES-BJ NYrPcIR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2faWmlEPTB;MUOuPVI{PCEQvF2= NE\2[mVUSU6JRWK=
BE-13 M1j5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF2LkO5NVUh|ryP MknoV2FPT0WU
SKM-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvnTWM2OD1zND60OFk6KM7:TR?= Mn;kV2FPT0WU
TE-6 Mk\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHOZXhKSzVyPUG0Mlc2QTFizszN MYPTRW5ITVJ?
LB771-HNC NWniZm1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjyTWM2OD1zND63PFk5KM7:TR?= MVXTRW5ITVJ?
ECC4 NVjGNJk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7EZ454UUN3ME2xO{4xOjd5IN88US=> MWnTRW5ITVJ?
ES3 MkPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;MRpBVUUN3ME2xO{41PjV3IN88US=> MUXTRW5ITVJ?
LB647-SCLC MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTF5LkS5OFkh|ryP NHzVOJRUSU6JRWK=
NB10 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzFXoIxUUN3ME2xPE42OjV4IN88US=> M1O1[HNCVkeHUh?=
L-540 NV3RO2ExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LGbmlEPTB;MUiuPFExQSEQvF2= NXr5Tm5IW0GQR1XS
NCI-H2126 Mk[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWC3XVBKUUN3ME2xPU42OSEQvF2= NXXaSGJSW0GQR1XS
HH M{TnV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJyLkCwPVkh|ryP M4S1b3NCVkeHUh?=
MPP-89 M120SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJ|LkKyPFkh|ryP M2fabnNCVkeHUh?=
IST-MEL1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVK0OXE4UUN3ME2yN{45PjV6IN88US=> NUfJZXlyW0GQR1XS
KP-N-YS MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3ZeXBKSzVyPUKzMlkzPTVizszN MVHTRW5ITVJ?
EC-GI-10 NV3LOJY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PUOGlEPTB;MkSuOVk5QSEQvF2= NF7YV29USU6JRWK=
EKVX NVPadpVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnMUm1KSzVyPUK2MlAzODNizszN NWPyc4l5W0GQR1XS
TGBC1TKB M1njb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL5WnBKSzVyPUK2MlQ{PCEQvF2= NYPHN3lRW0GQR1XS
Daudi M4rEOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJ5LkC3O|Mh|ryP Mni1V2FPT0WU
ALL-PO MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPZb2VKSzVyPUK3MlA5OSEQvF2= MVTTRW5ITVJ?
NB6 M4rBbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJ5LkS4PEDPxE1? NXHSWI5yW0GQR1XS
ES6 NITLU2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nDTmlEPTB;MkeuPVEzOyEQvF2= NYHFXoNwW0GQR1XS
COLO-320-HSR NWXPXFFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLyWZUxUUN3ME2yPE4xOzd|IN88US=> MmHEV2FPT0WU
K5 M1nIS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\vPIFCUUN3ME2yPE4yOjh5IN88US=> NFvjbmVUSU6JRWK=
ES1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJ6Lke3O|Mh|ryP MYfTRW5ITVJ?
LC-1F M2W3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLFTWM2OD1{OT63N|Q3KM7:TR?= MkHiV2FPT0WU
SCLC-21H MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mly4TWM2OD1|MD63N|E4KM7:TR?= NWTZfG9JW0GQR1XS
SK-PN-DW MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnId5ZKSzVyPUOyMlU2QThizszN M1;NVHNCVkeHUh?=
D-247MG NUXDW4FLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml71TWM2OD1|Mj65O|c{KM7:TR?= NIDQOodUSU6JRWK=
TE-5 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrxTWM2OD1|Mz6wN|YzKM7:TR?= NIXteolUSU6JRWK=
MONO-MAC-6 NUnyfVQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWxSVBlUUN3ME2zN{42ODR6IN88US=> M1jCenNCVkeHUh?=
LB2518-MEL MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIS5O4pKSzVyPUOzMlc3PjZizszN M1z5R3NCVkeHUh?=
LOXIMVI M17TNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXoXnhKSzVyPUOzMlc6OjhizszN NY\kSHNrW0GQR1XS
NCI-H209 NFPQe21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LzNmlEPTB;M{WuNVQ1KM7:TR?= MYXTRW5ITVJ?
A253 NITKXoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K1T2lEPTB;M{WuO|QzQSEQvF2= M2TL[HNCVkeHUh?=
HCC1599 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTN4LkewOVMh|ryP M2G3e3NCVkeHUh?=
EB-3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XwOGlEPTB;M{[uPVUyQCEQvF2= M1WwdnNCVkeHUh?=
GOTO M3;jfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHkVldRUUN3ME2zO{4{OjJ2IN88US=> M{m5dXNCVkeHUh?=
SW684 MnnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjOWoFKSzVyPUSxMlg1QTVizszN MWrTRW5ITVJ?
DEL NF;jeHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:5TWM2OD12Mj6wOVIzKM7:TR?= NEXOfVJUSU6JRWK=
HT-144 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\ZRpNxUUN3ME20Nk4yPjd4IN88US=> MUDTRW5ITVJ?
TE-9 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf1UFRKSzVyPUSzMlQ2QTZizszN MlHvV2FPT0WU
KARPAS-45 NInsNW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTR2LkO5NlUh|ryP M1jvU3NCVkeHUh?=
HAL-01 MlXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXCNm5KSzVyPUS0MlUxOzRizszN NEH0d|FUSU6JRWK=
RCC10RGB MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3q5dGlEPTB;NESuO|M6OiEQvF2= NFvqN|BUSU6JRWK=
CP67-MEL NYny[5R1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;rOmlEPTB;NEWuOlI1OSEQvF2= MlHsV2FPT0WU
NB17 NHvFNXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVSxO|MyUUN3ME20OU43PjR|IN88US=> M2faS3NCVkeHUh?=
SK-UT-1 NF\oV|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH30eJJKSzVyPUS1Mlk1PjRizszN NXeyPJZyW0GQR1XS
JiyoyeP-2003 NIrIb5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHSyWWxKSzVyPUS2MlAyOTlizszN MX3TRW5ITVJ?
HCE-4 NH3TU49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\KNolqUUN3ME20Ok42QTZ6IN88US=> NFft[nhUSU6JRWK=
NCI-H720 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTR4Lke2PFIh|ryP MojLV2FPT0WU
KARPAS-422 NVfIUGZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXYRotKSzVyPUS3MlA5QTVizszN NInBTJlUSU6JRWK=
Ramos-2G6-4C10 NWLNbWNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPvXoNKSzVyPUS3MlE3OjJizszN NUnQb5k6W0GQR1XS
HCE-T NYrvOHBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq5TWM2OD12Nz62PFI5KM7:TR?= NWG3VoFiW0GQR1XS
PSN1 NVHXVIUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nz[2lEPTB;NEeuO|gyOyEQvF2= MYjTRW5ITVJ?

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[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.
細胞試験: [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)
動物試験:[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 Insoluble
体内 順序で溶剤を入れること:
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 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
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

Related Antibodies

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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID