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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JPY 13102.90 あり
JPY 10079.16 あり
JPY 24477.96 あり
JPY 96471.96 あり

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.
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 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV34SnZWUUN3ME2wMlA3OTR|IN88US=> MWXTRW5ITVJ?
LAMA-84 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP3TWM2OD1yLkG1PVkh|ryP M3zGeHNCVkeHUh?=
MEG-01 NVjYPIFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\FcWlEPTB;MD6yN|Y5QCEQvF2= NGLuWGNUSU6JRWK=
EM-2 M{mzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwMk[1JO69VQ>? MWnTRW5ITVJ?
TE-15 MnzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoH3TWM2OD1yLkK3OFEzKM7:TR?= NUPyUllsW0GQR1XS
NCI-H1648 NXP6cXFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHscZUyUUN3ME2wMlI5OTF4IN88US=> NHqxeJpUSU6JRWK=
TE-12 M17wOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TqTWlEPTB;MD6zNlY5KM7:TR?= Mnm3V2FPT0WU
LB996-RCC MkPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwNESxPVYh|ryP NVu5RWJsW0GQR1XS
K-562 NGDnZ|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLoTWM2OD1yLkS0PVY4KM7:TR?= MVzTRW5ITVJ?
D-336MG MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwNUCzNFQh|ryP NGX3VHpUSU6JRWK=
NOS-1 NX7NeohST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHCTWM2OD1yLk[wOVI6KM7:TR?= NETIXZdUSU6JRWK=
EW-24 NUD4fIZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrIc3UzUUN3ME2wMlYzPjl|IN88US=> NEjy[VlUSU6JRWK=
BV-173 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwNkWyOFkh|ryP MXrTRW5ITVJ?
NCCIT MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTBwN{OyNVgh|ryP Mn23V2FPT0WU
NCI-H1436 M3PGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkWyTWM2OD1yLke5NFQ6KM7:TR?= MkG1V2FPT0WU
BB30-HNC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorMTWM2OD1yLki2NlA{KM7:TR?= MkjmV2FPT0WU
TE-8 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\LZmlEPTB;MD64O|I4PSEQvF2= MnHMV2FPT0WU
A704 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwOEmyNUDPxE1? MkDJV2FPT0WU
TK10 NVTTWWJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmmyTWM2OD1yLkmwOlY6KM7:TR?= NFLVRllUSU6JRWK=
KS-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPDeZFKSzVyPUGuNVk4PzlizszN MlX6V2FPT0WU
C2BBe1 NG\Kd4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmD0TWM2OD1zLkKwOVA4KM7:TR?= M37ONHNCVkeHUh?=
RXF393 NYjsbIlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUex[nV2UUN3ME2xMlI1OzZizszN MX;TRW5ITVJ?
KGN MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\ZTWM2OD1zLkK3Olg4KM7:TR?= MVLTRW5ITVJ?
NB69 NUXieIJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojmTWM2OD1zLkO3OFk4KM7:TR?= NUXhNW82W0GQR1XS
TE-11 NVTUe|huT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPTOWtKSzVyPUGuOFM1OThizszN MnTqV2FPT0WU
TE-1 MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETXVI9KSzVyPUGuOFQyODVizszN MkHGV2FPT0WU
ST486 MoLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLLXIRKSzVyPUGuOFU5PTJizszN MmPuV2FPT0WU
HOP-62 Mnj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFwNUCyOFYh|ryP MnL1V2FPT0WU
EW-16 NUfEfGk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\mWYNnUUN3ME2xMlU2ODh|IN88US=> NHHRZodUSU6JRWK=
LB1047-RCC NX61ZWw{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3FTWM2OD1zLkW1OFU{KM7:TR?= MmTlV2FPT0WU
TE-10 M2XD[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfNTWM2OD1zLk[2NlUzKM7:TR?= MmXIV2FPT0WU
RL95-2 MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf5ZWNQUUN3ME2xMlY3QTB{IN88US=> NX7qZ206W0GQR1XS
DOHH-2 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPLTWM2OD1zLkexO|gzKM7:TR?= NFzOenlUSU6JRWK=
MFH-ino M1HWZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHv2SWlKSzVyPUGuO|c5PyEQvF2= M1zpVHNCVkeHUh?=
GB-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXmTWM2OD1zLke5PFM{KM7:TR?= M1qxUXNCVkeHUh?=
SK-N-DZ M1LkcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIn2fpBKSzVyPUGuPFQ3QDhizszN MUTTRW5ITVJ?
OS-RC-2 NXzzfZhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTFwOEi1O|Qh|ryP M3XwcHNCVkeHUh?=
SW982 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfPclkxUUN3ME2xMlkzODl|IN88US=> NHeyV25USU6JRWK=
KALS-1 MmnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTFwOUi3NlIh|ryP M4DHWXNCVkeHUh?=
TGBC24TKB NH;CPFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TiS2lEPTB;Mj6wOVk2QCEQvF2= NGHDOGxUSU6JRWK=
GI-1 NEPRV2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;1dmlEPTB;Mj6xOlA5PCEQvF2= MlnyV2FPT0WU
SW962 NUTmWmprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHv[llvUUN3ME2yMlE4OTd6IN88US=> M4LlVXNCVkeHUh?=
SW872 NGflVJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJwMUi1NFch|ryP MX\TRW5ITVJ?
NCI-H747 NUPpOmNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTJwMkW3NVQh|ryP MkPFV2FPT0WU
MZ1-PC MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTxTWM2OD1{LkK5N|U3KM7:TR?= NF\5bJBUSU6JRWK=
MSTO-211H NVSwRm14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3SwemlEPTB;Mj6zOVczOyEQvF2= MoKxV2FPT0WU
BL-70 NGnrdGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTnOo9ZUUN3ME2yMlQ4PDJ{IN88US=> NXv4SJRrW0GQR1XS
SW954 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjmbZZGUUN3ME2yMlU4PDB6IN88US=> NXnNSIQ{W0GQR1XS
SNB75 NXzlVlFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nrUWlEPTB;Mj62PFU6PCEQvF2= MXvTRW5ITVJ?
IST-SL2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnNPWJKSzVyPUKuO|I{PzlizszN M{PTV3NCVkeHUh?=
GCIY NW\NWWwxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PjbmlEPTB;Mj64O|AxPSEQvF2= MVPTRW5ITVJ?
KU812 Mn;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD4NFIzUUN3ME2zMlA2Ojl7IN88US=> MYDTRW5ITVJ?
LXF-289 M{XlcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzwTWM2OD1|LkGyNVA6KM7:TR?= M1frc3NCVkeHUh?=
ETK-1 NFnqSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmX3TWM2OD1|LkKwO|Y4KM7:TR?= NXjKN3NZW0GQR1XS
SF126 MkniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrTfXJwUUN3ME2zMlMyOTd2IN88US=> NYqzUGtrW0GQR1XS
LC-2-ad NITieFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XMfmlEPTB;Mz61OVch|ryP MmrlV2FPT0WU
KNS-42 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;1TWM2OD1|Lk[1JO69VQ>? NWDSdmhwW0GQR1XS
OVCAR-4 NVzXUIxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mny3TWM2OD1|LkezOFM{KM7:TR?= NWr0TnJkW0GQR1XS
PF-382 NVvxbXkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTNwOEO2PVgh|ryP NV3QWXlDW0GQR1XS
SH-4 NWr5NYo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7ibWtKSzVyPUSuNlUzPTlizszN NXW4S5k4W0GQR1XS
KM12 NX7sUVh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3uT21oUUN3ME20MlMzPDF4IN88US=> NF20cmVUSU6JRWK=
NB5 NGjLelhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTRwNEG4OlQh|ryP MkDjV2FPT0WU
KURAMOCHI MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLpTWM2OD12Lk[1NlU3KM7:TR?= NF\odItUSU6JRWK=
Becker NF7RbJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWryR4pvUUN3ME20MlY3PDF4IN88US=> NW\pN3pPW0GQR1XS
MV-4-11 NWfzNZVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfCeIFKSzVyPUSuPFE{PDRizszN NWnyc2E4W0GQR1XS
KINGS-1 NVfxU4hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13TOmlEPTB;ND64NlM4OyEQvF2= NIjSVXRUSU6JRWK=
LS-123 NWHzWXFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3K2d2lEPTB;NT60PVY5PCEQvF2= NIXiV4dUSU6JRWK=
SF268 NVXq[W5oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTVwNkGyOlIh|ryP NX71VJdDW0GQR1XS
A388 M1z6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTVwNkO2Olch|ryP NFnxVopUSU6JRWK=
NMC-G1 NEDVVZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTZwMEG4NVEh|ryP NYHvXm1bW0GQR1XS
CGTH-W-1 NUnoeoQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13oN2lEPTB;Nj6wNlA4PSEQvF2= Mn7CV2FPT0WU
ES4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M370[mlEPTB;Nj61N|A4PCEQvF2= MVHTRW5ITVJ?
SR M{TaTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDFTGkzUUN3ME22MlU5QDB5IN88US=> NFPC[HBUSU6JRWK=
BB49-HNC NIPyZmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4SzO2lEPTB;Nj63N|IxPiEQvF2= NX3JTnk1W0GQR1XS
KLE M1uyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XrNGlEPTB;Nj63PFM4PyEQvF2= NUH1U4hKW0GQR1XS
HUTU-80 NWG0bWVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\6cGlEPTB;Nj65PFQ3PiEQvF2= M4Txb3NCVkeHUh?=
SNU-C2B MmTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzmTWM2OD15LkiyO|M4KM7:TR?= M{npWXNCVkeHUh?=
BB65-RCC NULPTmJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTdwOUS5NFQh|ryP NIDQb3lUSU6JRWK=
QIMR-WIL MlfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m1TmlEPTB;OD60NlgxQCEQvF2= MXTTRW5ITVJ?
GDM-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnlcW1vUUN3ME24Mlk4Ojl{IN88US=> MlfKV2FPT0WU
LC4-1 NEOzb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTlwMEC5NVEh|ryP MYPTRW5ITVJ?
MLMA MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\1R2lEPTB;OT6xOVAxPiEQvF2= NFvZWIRUSU6JRWK=
EoL-1-cell M2K0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTlwM{CxPVIh|ryP NGPxRlVUSU6JRWK=
BOKU NYTObHFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\WTWM2OD17Lkm2OFY3KM7:TR?= NFjZVGdUSU6JRWK=
EVSA-T MomyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jmN2lEPTB;MUCuOlU3QCEQvF2= Mo\nV2FPT0WU
D-283MED NXjtSoJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrNTWM2OD1zMD65NVc3KM7:TR?= NGHDW|BUSU6JRWK=
NB1 NWrXN2hVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVGx[|ZEUUN3ME2xNU4xOjR{IN88US=> M1HkN3NCVkeHUh?=
RPMI-8402 NWrlPFM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYKzUmp[UUN3ME2xNU4yPzhizszN Ml7zV2FPT0WU
NCI-H1355 NGHBXmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrPTWM2OD1zMT6xPFA3KM7:TR?= MXXTRW5ITVJ?
NB7 MkDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTFzLkOyPVch|ryP Ml;kV2FPT0WU
RPMI-6666 NVe0fHNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\XeZJSUUN3ME2xNk46PTZ5IN88US=> MVrTRW5ITVJ?
697 NWXU[HRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTF|LkK3NFEh|ryP NETHXZVUSU6JRWK=
CTB-1 M2q3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPJTWM2OD1zMz61PVQ5KM7:TR?= NYXH[IFGW0GQR1XS
VA-ES-BJ MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTF|LkmyN|Qh|ryP MXfTRW5ITVJ?
BE-13 M4rGdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnhSnpEUUN3ME2xOE4{QTF3IN88US=> Mn3CV2FPT0WU
SKM-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGOzSGFKSzVyPUG0MlQ1QTlizszN MW\TRW5ITVJ?
TE-6 M1LEcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;FZ25HUUN3ME2xOE44PTlzIN88US=> MV\TRW5ITVJ?
LB771-HNC NV;m[mVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLsVoFvUUN3ME2xOE44QDl6IN88US=> Mnf6V2FPT0WU
ECC4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml6zTWM2OD1zNz6wNlc4KM7:TR?= MlnvV2FPT0WU
ES3 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHtOHNKSzVyPUG3MlQ3PTVizszN MW\TRW5ITVJ?
LB647-SCLC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnGR5VqUUN3ME2xO{41QTR7IN88US=> NV;hWWJ{W0GQR1XS
NB10 NWO3bFFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF6LkWyOVYh|ryP MVLTRW5ITVJ?
L-540 NVe3T4FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXjV4hKSzVyPUG4MlgyODlizszN MWLTRW5ITVJ?
NCI-H2126 NV7iVm5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXCTWM2OD1zOT61NUDPxE1? NXTNeIp7W0GQR1XS
HH NYP4dox{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P5VGlEPTB;MkCuNFA6QSEQvF2= M{\sbHNCVkeHUh?=
MPP-89 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\YTWM2OD1{Mz6yNlg6KM7:TR?= MkfvV2FPT0WU
IST-MEL1 NX7wTlN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTGNmxKSzVyPUKzMlg3PThizszN NWXZVGtYW0GQR1XS
KP-N-YS NXPlW3hET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDsS2l6UUN3ME2yN{46OjV3IN88US=> NFrJS2hUSU6JRWK=
EC-GI-10 M3j0dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[3cVlKSzVyPUK0MlU6QDlizszN M3P1VnNCVkeHUh?=
EKVX NXLV[VNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\zWZVsUUN3ME2yOk4xOjB|IN88US=> NXHZNVlSW0GQR1XS
TGBC1TKB NWC4fHRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTJ4LkSzOEDPxE1? MlPTV2FPT0WU
Daudi MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm1eINGUUN3ME2yO{4xPzd|IN88US=> M4raXHNCVkeHUh?=
ALL-PO M3njbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJ5LkC4NUDPxE1? MVXTRW5ITVJ?
NB6 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHLVlZGUUN3ME2yO{41QDhizszN MkfkV2FPT0WU
ES6 M3noUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTmfIZ7UUN3ME2yO{46OTJ|IN88US=> NXXxSWE4W0GQR1XS
COLO-320-HSR MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDwTWM2OD1{OD6wN|c{KM7:TR?= MkjuV2FPT0WU
K5 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;DTWM2OD1{OD6xNlg4KM7:TR?= NHzTd2tUSU6JRWK=
ES1 NFq0Z2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWL6OmxWUUN3ME2yPE44Pzd|IN88US=> MVjTRW5ITVJ?
LC-1F NEThTINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXpR5pKSzVyPUK5Mlc{PDZizszN NIizW4JUSU6JRWK=
SCLC-21H MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[5Z2E{UUN3ME2zNE44OzF5IN88US=> MYDTRW5ITVJ?
SK-PN-DW MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nXVWlEPTB;M{KuOVU6QCEQvF2= MWnTRW5ITVJ?
D-247MG MnXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTN{Lkm3O|Mh|ryP NILrcIxUSU6JRWK=
TE-5 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOxVJluUUN3ME2zN{4xOzZ{IN88US=> MWTTRW5ITVJ?
MONO-MAC-6 NV;zXHB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnXTVZKSzVyPUOzMlUxPDhizszN MkLQV2FPT0WU
LB2518-MEL M{jnfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fMUmlEPTB;M{OuO|Y3PiEQvF2= M2D0NXNCVkeHUh?=
LOXIMVI NVvXToZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHVTlhkUUN3ME2zN{44QTJ6IN88US=> NHXLUGtUSU6JRWK=
NCI-H209 NXX4UoRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTN3LkG0OEDPxE1? NFvkWHBUSU6JRWK=
A253 M374RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTN3Lke0Nlkh|ryP NEXDTGVUSU6JRWK=
HCC1599 NEXtO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DoN2lEPTB;M{[uO|A2OyEQvF2= NYLxUItOW0GQR1XS
EB-3 NITpZYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TuWmlEPTB;M{[uPVUyQCEQvF2= NW\RVpZuW0GQR1XS
GOTO MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnmeldTUUN3ME2zO{4{OjJ2IN88US=> M1XCRnNCVkeHUh?=
SW684 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTRzLki0PVUh|ryP M2e4W3NCVkeHUh?=
DEL MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HvZ2lEPTB;NEKuNFUzOiEQvF2= M4PPe3NCVkeHUh?=
HT-144 M{\jemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\PTWM2OD12Mj6xOlc3KM7:TR?= MX3TRW5ITVJ?
TE-9 MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr6[m5{UUN3ME20N{41PTl4IN88US=> MYfTRW5ITVJ?
KARPAS-45 M1ziZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX70T5J6UUN3ME20OE4{QTJ3IN88US=> MWfTRW5ITVJ?
HAL-01 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjOdVNKSzVyPUS0MlUxOzRizszN NGHsNpBUSU6JRWK=
RCC10RGB MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\tV4lIUUN3ME20OE44Ozl{IN88US=> MXzTRW5ITVJ?
CP67-MEL NIHhSm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PXfWlEPTB;NEWuOlI1OSEQvF2= NEi4RoRUSU6JRWK=
NB17 NFHGWFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTR3Lk[2OFMh|ryP NH3GeolUSU6JRWK=
SK-UT-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXGTWM2OD12NT65OFY1KM7:TR?= Mme5V2FPT0WU
JiyoyeP-2003 NUXkfmhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPaPYlUUUN3ME20Ok4xOTF7IN88US=> NXTuTWhTW0GQR1XS
HCE-4 NY\rfohyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnRe2prUUN3ME20Ok42QTZ6IN88US=> M3fubXNCVkeHUh?=
NCI-H720 M3rWb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTR4Lke2PFIh|ryP NFG0OlFUSU6JRWK=
KARPAS-422 MmftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmm2TWM2OD12Nz6wPFk2KM7:TR?= M1TXcnNCVkeHUh?=
Ramos-2G6-4C10 MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjHWXhKSzVyPUS3MlE3OjJizszN M4T5fXNCVkeHUh?=
HCE-T NHrOeZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzpVHVsUUN3ME20O{43QDJ6IN88US=> MVHTRW5ITVJ?
PSN1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXURXVKSzVyPUS3Mlc5OTNizszN NHrGN3VUSU6JRWK=

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
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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID