Saracatinib (AZD0530)

Catalog No.S1006

Saracatinib (AZD0530) Chemical Structure

Molecular Weight(MW): 542.03

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.

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In DMSO USD 91 In stock
USD 70 In stock
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Cited by 35 Publications

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  • 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.

    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.

  • 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.

Purity & Quality Control

Choose Selective Src Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.
Features The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
Targets
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

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 M3;Zdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTBwME[xOFMh|ryP MYLTRW5ITVJ?
LAMA-84 M{HRbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTBwMUW5PUDPxE1? NVS5V5pkW0GQR1XS
MEG-01 NF3kTHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnOyTWM2OD1yLkKzOlg5KM7:TR?= NYqxSo92W0GQR1XS
EM-2 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXCU41KSzVyPUCuNlY2KM7:TR?= NVHaZ2F5W0GQR1XS
TE-15 NVTYOWJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jEU2lEPTB;MD6yO|QyOiEQvF2= MVnTRW5ITVJ?
NCI-H1648 M2\vUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTBwMkixNVYh|ryP NGr2fplUSU6JRWK=
TE-12 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYixVG9GUUN3ME2wMlMzPjhizszN M4LDZXNCVkeHUh?=
LB996-RCC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTXTWM2OD1yLkS0NVk3KM7:TR?= MUDTRW5ITVJ?
K-562 M2LXTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUi4U3l7UUN3ME2wMlQ1QTZ5IN88US=> MmnEV2FPT0WU
D-336MG NF\4T5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmL2TWM2OD1yLkWwN|A1KM7:TR?= NVTwSZJ[W0GQR1XS
NOS-1 NHzPVGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnWb2ZKSzVyPUCuOlA2OjlizszN MVvTRW5ITVJ?
EW-24 MnjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwNkK2PVMh|ryP NHXNc2xUSU6JRWK=
BV-173 M3;rZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;zTopVUUN3ME2wMlY2OjR7IN88US=> NH\qNpVUSU6JRWK=
NCCIT MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\YNGlEPTB;MD63N|IyQCEQvF2= NX:wXWc4W0GQR1XS
NCI-H1436 Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjmTWM2OD1yLke5NFQ6KM7:TR?= MlGxV2FPT0WU
BB30-HNC NWnHRVFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7NN|FKSzVyPUCuPFYzODNizszN M2rwVXNCVkeHUh?=
TE-8 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPNTWM2OD1yLki3Nlc2KM7:TR?= NIK5emZUSU6JRWK=
A704 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;XfWlEPTB;MD64PVIyKM7:TR?= MVLTRW5ITVJ?
TK10 NUjFSHVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zCTWlEPTB;MD65NFY3QSEQvF2= NGX4UnVUSU6JRWK=
KS-1 M2TYV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTFwMUm3O|kh|ryP MX\TRW5ITVJ?
C2BBe1 NWD2W2RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTFwMkC1NFch|ryP MlXNV2FPT0WU
RXF393 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTFwMkSzOkDPxE1? MlyxV2FPT0WU
KGN MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTFwMke2PFch|ryP NFPDb2pUSU6JRWK=
NB69 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWf6NnhxUUN3ME2xMlM4PDl5IN88US=> M3HwXXNCVkeHUh?=
TE-11 Mn;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHMTWM2OD1zLkSzOFE5KM7:TR?= MmfKV2FPT0WU
TE-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInxbXNKSzVyPUGuOFQyODVizszN NYrtNnA6W0GQR1XS
ST486 NYTRWYhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFwNEW4OVIh|ryP NFHhVG9USU6JRWK=
HOP-62 MmHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL3OIxjUUN3ME2xMlUxOjR4IN88US=> MXTTRW5ITVJ?
EW-16 NWG4R2JGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkniTWM2OD1zLkW1NFg{KM7:TR?= NVzQdlRnW0GQR1XS
LB1047-RCC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTFwNUW0OVMh|ryP M4niRXNCVkeHUh?=
TE-10 NXSyd|Y{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm2[I1NUUN3ME2xMlY3OjV{IN88US=> NFfzUnFUSU6JRWK=
RL95-2 NYjMfY1bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7iTWM2OD1zLk[2PVAzKM7:TR?= MnS3V2FPT0WU
DOHH-2 MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXDcoxMUUN3ME2xMlcyPzh{IN88US=> M3P3O3NCVkeHUh?=
MFH-ino NGD0VmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTFwN{e4O{DPxE1? MmfQV2FPT0WU
GB-1 M33ReWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DtbWlEPTB;MT63PVg{OyEQvF2= NF\wZoRUSU6JRWK=
SK-N-DZ NFHTbVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLuTWM2OD1zLki0Olg5KM7:TR?= MkTvV2FPT0WU
OS-RC-2 NYTR[nV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jG[mlEPTB;MT64PFU4PCEQvF2= MonXV2FPT0WU
SW982 NY\hOYZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTFwOUKwPVMh|ryP MYDTRW5ITVJ?
KALS-1 NXjQZoNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn2TWM2OD1zLkm4O|IzKM7:TR?= NG\QUIlUSU6JRWK=
TGBC24TKB MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTJwMEW5OVgh|ryP NHTkfnlUSU6JRWK=
GI-1 M{DNbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVj0U2oxUUN3ME2yMlE3ODh2IN88US=> M1fvW3NCVkeHUh?=
SW962 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHDXG5GUUN3ME2yMlE4OTd6IN88US=> NF\FV3NUSU6JRWK=
SW872 MoPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TmcmlEPTB;Mj6xPFUxPyEQvF2= NGLWW3ZUSU6JRWK=
NCI-H747 M2rWbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHX0TmRKSzVyPUKuNlU4OTRizszN NGrHXIRUSU6JRWK=
MZ1-PC NGHFO3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLLRlM6UUN3ME2yMlI6OzV4IN88US=> M2PJUXNCVkeHUh?=
MSTO-211H M{K0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4C5T2lEPTB;Mj6zOVczOyEQvF2= MW\TRW5ITVJ?
BL-70 NVLYUW1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7WTWM2OD1{LkS3OFIzKM7:TR?= MoL4V2FPT0WU
SW954 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJwNUe0NFgh|ryP MknLV2FPT0WU
SNB75 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYX0UpFtUUN3ME2yMlY5PTl2IN88US=> MnPVV2FPT0WU
IST-SL2 MoPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfsU4U3UUN3ME2yMlczOzd7IN88US=> NXHFRZQzW0GQR1XS
GCIY NHLo[5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrWbVl3UUN3ME2yMlg4ODB3IN88US=> MmHGV2FPT0WU
KU812 M2S1Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHsZohwUUN3ME2zMlA2Ojl7IN88US=> NF70S5RUSU6JRWK=
LXF-289 NXPy[mQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnr4TWM2OD1|LkGyNVA6KM7:TR?= M{TZTnNCVkeHUh?=
ETK-1 MkjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\OUWlEPTB;Mz6yNFc3PyEQvF2= NUPmZoJ7W0GQR1XS
SF126 M4jxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTNwM{GxO|Qh|ryP MWfTRW5ITVJ?
LC-2-ad NGDkcG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHmWo5JUUN3ME2zMlU2PyEQvF2= NH7HXHVUSU6JRWK=
KNS-42 NYHFdphHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXySZNKSzVyPUOuOlUh|ryP M{jKSHNCVkeHUh?=
OVCAR-4 NITjTodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\jS3dKSzVyPUOuO|M1OzNizszN M2jPNHNCVkeHUh?=
PF-382 NYLhPFJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrkTWM2OD1|LkizOlk5KM7:TR?= MVzTRW5ITVJ?
SH-4 MmXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjZTWM2OD12LkK1NlU6KM7:TR?= MoiwV2FPT0WU
KM12 NIPuWFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{e2OGlEPTB;ND6zNlQyPiEQvF2= MYnTRW5ITVJ?
NB5 NF3kcYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13Bb2lEPTB;ND60NVg3PCEQvF2= MUHTRW5ITVJ?
KURAMOCHI MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nT[GlEPTB;ND62OVI2PiEQvF2= MU\TRW5ITVJ?
Becker M{TObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7t[VNKSzVyPUSuOlY1OTZizszN MoTSV2FPT0WU
MV-4-11 M4jrXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3JTmlFUUN3ME20MlgyOzR2IN88US=> M{OyTHNCVkeHUh?=
KINGS-1 NHTvdWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj6NWFjUUN3ME20MlgzOzd|IN88US=> NVPVOHo5W0GQR1XS
LS-123 M2nrUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTVwNEm2PFQh|ryP NGrVfohUSU6JRWK=
SF268 MmDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTVwNkGyOlIh|ryP NVXHbGx5W0GQR1XS
A388 NVK1UI5KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTVwNkO2Olch|ryP NUfzN4JFW0GQR1XS
NMC-G1 M4XHWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjLZnY3UUN3ME22MlAyQDFzIN88US=> NXXGbphkW0GQR1XS
CGTH-W-1 MlzmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHmNFBqUUN3ME22MlAzODd3IN88US=> NVH0fYV{W0GQR1XS
ES4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHq[pZCUUN3ME22MlU{ODd2IN88US=> M{\5WnNCVkeHUh?=
SR NHHqWY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTZwNUi4NFch|ryP Mlm0V2FPT0WU
BB49-HNC NUW2Z4tMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrsTWM2OD14LkezNlA3KM7:TR?= MVTTRW5ITVJ?
KLE Mnr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDKcohMUUN3ME22Mlc5Ozd5IN88US=> NXi4NGxmW0GQR1XS
HUTU-80 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTZwOUi0OlYh|ryP MVfTRW5ITVJ?
SNU-C2B M1;ke2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTdwOEK3N|ch|ryP MYHTRW5ITVJ?
BB65-RCC NYnmWohuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnpNVBpUUN3ME23Mlk1QTB2IN88US=> MknoV2FPT0WU
QIMR-WIL NH;oUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fzdGlEPTB;OD60NlgxQCEQvF2= MVfTRW5ITVJ?
GDM-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\yXo1KSzVyPUiuPVczQTJizszN MkP3V2FPT0WU
LC4-1 NInRW4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTlwMEC5NVEh|ryP MXPTRW5ITVJ?
MLMA NYKwZY83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorDTWM2OD17LkG1NFA3KM7:TR?= Mn;5V2FPT0WU
EoL-1-cell NYTTOYJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfOVWlKSzVyPUmuN|AyQTJizszN MYDTRW5ITVJ?
BOKU NUPXenpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTlwOU[0OlYh|ryP MWDTRW5ITVJ?
EVSA-T M2POSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[xTWM2OD1zMD62OVY5KM7:TR?= NFjndmxUSU6JRWK=
D-283MED NELQWWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTFyLkmxO|Yh|ryP NFi3ToRUSU6JRWK=
NB1 NUHNNHdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnlOYpXUUN3ME2xNU4xOjR{IN88US=> MkeyV2FPT0WU
RPMI-8402 NFHoS3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTFzLkG3PEDPxE1? M4XyR3NCVkeHUh?=
NCI-H1355 NYXjUpgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTFzLkG4NFYh|ryP MmLrV2FPT0WU
NB7 M4Ttemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PwTGlEPTB;MUGuN|I6PyEQvF2= NFPQcVFUSU6JRWK=
RPMI-6666 NIi3R|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTF{Lkm1Olch|ryP Moe2V2FPT0WU
697 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfuTWM2OD1zMz6yO|AyKM7:TR?= NYTxfmNbW0GQR1XS
CTB-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\kS5pKSzVyPUGzMlU6PDhizszN MoPVV2FPT0WU
VA-ES-BJ MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\wNWtKSzVyPUGzMlkzOzRizszN MkfjV2FPT0WU
BE-13 NGjPdVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M135bGlEPTB;MUSuN|kyPSEQvF2= NYrhemxwW0GQR1XS
SKM-1 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn0cGEyUUN3ME2xOE41PDl7IN88US=> NFTUXGRUSU6JRWK=
TE-6 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF2Lke1PVEh|ryP M4HzbnNCVkeHUh?=
LB771-HNC M1nUbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF2Lke4PVgh|ryP MmTsV2FPT0WU
ECC4 NI\odZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn62TWM2OD1zNz6wNlc4KM7:TR?= MYnTRW5ITVJ?
ES3 Mn\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2C2bWlEPTB;MUeuOFY2PSEQvF2= MVTTRW5ITVJ?
LB647-SCLC NXm0d|MyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTF5LkS5OFkh|ryP MYjTRW5ITVJ?
NB10 NGHUVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknITWM2OD1zOD61NlU3KM7:TR?= MXvTRW5ITVJ?
L-540 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF6LkixNFkh|ryP M3LaN3NCVkeHUh?=
NCI-H2126 M3;0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTF7LkWxJO69VQ>? M4HJWHNCVkeHUh?=
HH MlTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrMWXNKSzVyPUKwMlAxQTlizszN MVjTRW5ITVJ?
MPP-89 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTJ|LkKyPFkh|ryP NITnOIJUSU6JRWK=
IST-MEL1 MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HINmlEPTB;MkOuPFY2QCEQvF2= MWfTRW5ITVJ?
KP-N-YS MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mly0TWM2OD1{Mz65NlU2KM7:TR?= MXzTRW5ITVJ?
EC-GI-10 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTJ2LkW5PFkh|ryP M4nKdHNCVkeHUh?=
EKVX NXTheYJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTFOGI2UUN3ME2yOk4xOjB|IN88US=> Mn60V2FPT0WU
TGBC1TKB Ml\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHLcI1FUUN3ME2yOk41OzRizszN Mn\RV2FPT0WU
Daudi NXTMUmQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TJWGlEPTB;MkeuNFc4OyEQvF2= NH7jRVJUSU6JRWK=
ALL-PO NGHsV5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33Ve2lEPTB;MkeuNFgyKM7:TR?= MlLFV2FPT0WU
NB6 M1v2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHT5cXZKSzVyPUK3MlQ5QCEQvF2= M4HHZ3NCVkeHUh?=
ES6 NETj[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\kXY1KSzVyPUK3MlkyOjNizszN MWfTRW5ITVJ?
COLO-320-HSR M1PyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTJ6LkCzO|Mh|ryP M4Tnc3NCVkeHUh?=
K5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NET6cFRKSzVyPUK4MlEzQDdizszN MoPYV2FPT0WU
ES1 NWHtSW96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[zTWM2OD1{OD63O|c{KM7:TR?= NULpXm9kW0GQR1XS
LC-1F M2juWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTJ7LkezOFYh|ryP NEHsXGRUSU6JRWK=
SCLC-21H NYGwUXN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTNyLkezNVch|ryP MkjZV2FPT0WU
SK-PN-DW NFnsT2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrqTWM2OD1|Mj61OVk5KM7:TR?= Mkn0V2FPT0WU
D-247MG MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fDWmlEPTB;M{KuPVc4OyEQvF2= NYXJZ3VnW0GQR1XS
TE-5 M3;6dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW3TWM2OD1|Mz6wN|YzKM7:TR?= NYjsc4k2W0GQR1XS
MONO-MAC-6 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnke25KSzVyPUOzMlUxPDhizszN NEfxOGtUSU6JRWK=
LB2518-MEL NF7vfWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTN|Lke2OlYh|ryP MVvTRW5ITVJ?
LOXIMVI MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTN|Lke5Nlgh|ryP MUTTRW5ITVJ?
NCI-H209 NFvPNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe0VFNKSzVyPUO1MlE1PCEQvF2= MX3TRW5ITVJ?
A253 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHpTWM2OD1|NT63OFI6KM7:TR?= M1\P[XNCVkeHUh?=
HCC1599 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWwTWM2OD1|Nj63NFU{KM7:TR?= M3\EXHNCVkeHUh?=
EB-3 M1PQVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLwVZcyUUN3ME2zOk46PTF6IN88US=> MXrTRW5ITVJ?
GOTO M{LMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTSe5RKSzVyPUO3MlMzOjRizszN NUfJZoVpW0GQR1XS
SW684 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rFNWlEPTB;NEGuPFQ6PSEQvF2= NYPYeGVNW0GQR1XS
DEL MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTqTWM2OD12Mj6wOVIzKM7:TR?= MXvTRW5ITVJ?
HT-144 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTR{LkG2O|Yh|ryP M1v2UXNCVkeHUh?=
TE-9 M2HXb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnrVXhUUUN3ME20N{41PTl4IN88US=> MYDTRW5ITVJ?
KARPAS-45 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Ph[2lEPTB;NESuN|kzPSEQvF2= M4jiXnNCVkeHUh?=
HAL-01 NH32fnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfHWYZ[UUN3ME20OE42ODN2IN88US=> MV;TRW5ITVJ?
RCC10RGB NX63SVVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPkTWM2OD12ND63N|kzKM7:TR?= MoruV2FPT0WU
CP67-MEL NI\jeZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTR3Lk[yOFEh|ryP MV;TRW5ITVJ?
NB17 NGXD[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVm3dowzUUN3ME20OU43PjR|IN88US=> MkW0V2FPT0WU
SK-UT-1 NFvncpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWOwUnE5UUN3ME20OU46PDZ2IN88US=> NGO5SZZUSU6JRWK=
JiyoyeP-2003 M2LNT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXCWldlUUN3ME20Ok4xOTF7IN88US=> MWjTRW5ITVJ?
HCE-4 NFzjco5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfXTWM2OD12Nj61PVY5KM7:TR?= MXTTRW5ITVJ?
NCI-H720 MoPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jt[WlEPTB;NE[uO|Y5OiEQvF2= M2jlUHNCVkeHUh?=
KARPAS-422 NULSUZE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln6TWM2OD12Nz6wPFk2KM7:TR?= MkLqV2FPT0WU
Ramos-2G6-4C10 NWD3R2dWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf1TWM2OD12Nz6xOlIzKM7:TR?= MlLrV2FPT0WU
HCE-T M1;SdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrnS3VzUUN3ME20O{43QDJ6IN88US=> NFfkUWtUSU6JRWK=
PSN1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHK1UFlKSzVyPUS3Mlc5OTNizszN NVn5emhvW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[1]
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  • Cell lines: PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 and RWPE-1 cells
  • Concentrations: 62.5 nM - 16 mM
  • Incubation Time: 1, 3 and 5 days
  • Method: 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
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: CB17 mice are implanted with DU145 cells.
  • Formulation: Dissolved in 0.5% hydroxypropyl methylcellulose, 0.1% Tween 80
  • Dosages: 25 mg/kg
  • Administration: Orally administered daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL (64.57 mM) warming
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.

Chemical Information

Molecular Weight 542.03
Formula

C27H32ClN5O5

CAS No. 379231-04-6
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID