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
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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

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 NGXW[m5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4C2SmlEPTB;MD6wOlE1OyEQvF2= MkXXV2FPT0WU
LAMA-84 NFyxO4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPTVItKSzVyPUCuNVU6QSEQvF2= MXXTRW5ITVJ?
MEG-01 M2L4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn1OVlKSzVyPUCuNlM3QDhizszN M2LZXnNCVkeHUh?=
EM-2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwMk[1JO69VQ>? NFq3ZpJUSU6JRWK=
TE-15 NGnKNlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT0b5NFUUN3ME2wMlI4PDF{IN88US=> NGGxZXJUSU6JRWK=
NCI-H1648 NXXyUI1tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LTVWlEPTB;MD6yPFEyPiEQvF2= NVzaZYNEW0GQR1XS
TE-12 NFPESFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHuxVnJKSzVyPUCuN|I3QCEQvF2= MkHjV2FPT0WU
LB996-RCC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon5TWM2OD1yLkS0NVk3KM7:TR?= MnLDV2FPT0WU
K-562 NWHkWZV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfle|ZLUUN3ME2wMlQ1QTZ5IN88US=> M1rGdnNCVkeHUh?=
D-336MG MmOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwNUCzNFQh|ryP NGDSTplUSU6JRWK=
NOS-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTBwNkC1Nlkh|ryP NVjSOplXW0GQR1XS
EW-24 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7mToVKSzVyPUCuOlI3QTNizszN M3zFRXNCVkeHUh?=
BV-173 M3SyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrHTWM2OD1yLk[1NlQ6KM7:TR?= M17MO3NCVkeHUh?=
NCCIT M1jVcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLPUVhpUUN3ME2wMlc{OjF6IN88US=> M17tT3NCVkeHUh?=
NCI-H1436 NGHCOmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3HTWM2OD1yLke5NFQ6KM7:TR?= MY\TRW5ITVJ?
BB30-HNC M2e3W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi3ZWVKSzVyPUCuPFYzODNizszN MULTRW5ITVJ?
TE-8 MkHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjnRmxKSzVyPUCuPFczPzVizszN M1HWbHNCVkeHUh?=
A704 Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrzTWM2OD1yLki5NlEh|ryP NHrkZmhUSU6JRWK=
TK10 NWS4ZnR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvEXWhEUUN3ME2wMlkxPjZ7IN88US=> NUjwWmZyW0GQR1XS
KS-1 NFG1bldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGr0[5hKSzVyPUGuNVk4PzlizszN NFXDNnFUSU6JRWK=
C2BBe1 M3vt[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;E[FFjUUN3ME2xMlIxPTB5IN88US=> Mnv5V2FPT0WU
RXF393 NFPU[VBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\DPGlEPTB;MT6yOFM3KM7:TR?= NXLleotzW0GQR1XS
KGN NWXtSnRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\JW2lEPTB;MT6yO|Y5PyEQvF2= NIi0fIlUSU6JRWK=
NB69 NIjQN|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTFwM{e0PVch|ryP NWftUpBoW0GQR1XS
TE-11 Mk\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTFwNEO0NVgh|ryP NVrEPJpCW0GQR1XS
TE-1 NYfyeoFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1L1c2lEPTB;MT60OFExPSEQvF2= MlPUV2FPT0WU
ST486 NVzpWZZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFwNEW4OVIh|ryP NWDrOW5MW0GQR1XS
HOP-62 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTFwNUCyOFYh|ryP NUC5XHR{W0GQR1XS
EW-16 NYS4cIVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFwNUWwPFMh|ryP M{DyT3NCVkeHUh?=
LB1047-RCC NVe0[ItlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L3eGlEPTB;MT61OVQ2OyEQvF2= NEPnbY5USU6JRWK=
TE-10 NUHoVFlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTFwNk[yOVIh|ryP NVzxSI1NW0GQR1XS
RL95-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwNk[5NFIh|ryP NGexTmpUSU6JRWK=
DOHH-2 MmfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTFwN{G3PFIh|ryP M{K2Z3NCVkeHUh?=
MFH-ino M3GzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHYTWM2OD1zLke3PFch|ryP M{X0WnNCVkeHUh?=
GB-1 NX[5Z|J[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrNR4F4UUN3ME2xMlc6QDN|IN88US=> M4TSZ3NCVkeHUh?=
SK-N-DZ NVTyclVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTFwOES2PFgh|ryP NFfnSFNUSU6JRWK=
OS-RC-2 M{nFcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrrPIVlUUN3ME2xMlg5PTd2IN88US=> NVTj[GFnW0GQR1XS
SW982 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj6NlQyUUN3ME2xMlkzODl|IN88US=> NYrC[IRYW0GQR1XS
KALS-1 NFTlUGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfMe4pGUUN3ME2xMlk5PzJ{IN88US=> NHnY[XZUSU6JRWK=
TGBC24TKB M1TuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvFTWM2OD1{LkC1PVU5KM7:TR?= MlHyV2FPT0WU
GI-1 MmHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTJwMU[wPFQh|ryP NG\2UYhUSU6JRWK=
SW962 M37vRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3j4OmlEPTB;Mj6xO|E4QCEQvF2= NX3iN25rW0GQR1XS
SW872 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHK3PZFKSzVyPUKuNVg2ODdizszN NFjFPGJUSU6JRWK=
NCI-H747 MlW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NECyXoRKSzVyPUKuNlU4OTRizszN NFjWTXRUSU6JRWK=
MZ1-PC MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7STWM2OD1{LkK5N|U3KM7:TR?= NXrO[W97W0GQR1XS
MSTO-211H M4LXUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX1TWM2OD1{LkO1O|I{KM7:TR?= MULTRW5ITVJ?
BL-70 NIn2TJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i2eGlEPTB;Mj60O|QzOiEQvF2= MX3TRW5ITVJ?
SW954 NIrFUnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LtXGlEPTB;Mj61O|QxQCEQvF2= MnTlV2FPT0WU
SNB75 NVPWSGNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTifY5FUUN3ME2yMlY5PTl2IN88US=> NInXboJUSU6JRWK=
IST-SL2 M3LvNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L1bmlEPTB;Mj63NlM4QSEQvF2= NXzVdXBmW0GQR1XS
GCIY MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\pUGlEPTB;Mj64O|AxPSEQvF2= NYntXIpwW0GQR1XS
KU812 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTNwMEWyPVkh|ryP M1Pz[nNCVkeHUh?=
LXF-289 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4D0UWlEPTB;Mz6xNlExQSEQvF2= MVnTRW5ITVJ?
ETK-1 NUnQXphnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;ONJpKSzVyPUOuNlA4PjdizszN MnTYV2FPT0WU
SF126 NXjuPGlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fjfGlEPTB;Mz6zNVE4PCEQvF2= NH\HWVhUSU6JRWK=
LC-2-ad MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHYTWM2OD1|LkW1O{DPxE1? NUDtXZB1W0GQR1XS
KNS-42 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XiRmlEPTB;Mz62OUDPxE1? MYfTRW5ITVJ?
OVCAR-4 M{nXcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTNwN{O0N|Mh|ryP NGiyTJdUSU6JRWK=
PF-382 NUTQUYQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfWfmxKSzVyPUOuPFM3QThizszN MXjTRW5ITVJ?
SH-4 MmDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXCSlJ5UUN3ME20MlI2OjV7IN88US=> M1\Rc3NCVkeHUh?=
KM12 M{\Zb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTRwM{K0NVYh|ryP Mlu0V2FPT0WU
NB5 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHKzXppKSzVyPUSuOFE5PjRizszN NXm0[Il6W0GQR1XS
KURAMOCHI MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPyTWM2OD12Lk[1NlU3KM7:TR?= Mnm0V2FPT0WU
Becker NVnUVWRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T1[mlEPTB;ND62OlQyPiEQvF2= M1OzTXNCVkeHUh?=
MV-4-11 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTRwOEGzOFQh|ryP NEHue2NUSU6JRWK=
KINGS-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LrZmlEPTB;ND64NlM4OyEQvF2= NEWwfY9USU6JRWK=
LS-123 MkC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;GNIhKSzVyPUWuOFk3QDRizszN NHHGUHdUSU6JRWK=
SF268 NF3VZZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PGXGlEPTB;NT62NVI3OiEQvF2= M3faTXNCVkeHUh?=
A388 NFLXSm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjlR45FUUN3ME21MlY{PjZ5IN88US=> MVjTRW5ITVJ?
NMC-G1 M2rMWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;nOWlEPTB;Nj6wNVgyOSEQvF2= Mk\oV2FPT0WU
CGTH-W-1 NV7Ud281T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPL[HRXUUN3ME22MlAzODd3IN88US=> NWSyfIdRW0GQR1XS
ES4 MnTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7UTWM2OD14LkWzNFc1KM7:TR?= NH[1b|lUSU6JRWK=
SR MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PLbGlEPTB;Nj61PFgxPyEQvF2= NH7QNpdUSU6JRWK=
BB49-HNC MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLlTWM2OD14LkezNlA3KM7:TR?= NEPrOWpUSU6JRWK=
KLE NHfkeYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrzbppzUUN3ME22Mlc5Ozd5IN88US=> MnW0V2FPT0WU
HUTU-80 M376Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXBWVRKSzVyPU[uPVg1PjZizszN MnnNV2FPT0WU
SNU-C2B NFT5bWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrDNHJKSzVyPUeuPFI4OzdizszN MkHQV2FPT0WU
BB65-RCC M4TPcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37hPWlEPTB;Nz65OFkxPCEQvF2= MXfTRW5ITVJ?
QIMR-WIL NX\TTmtvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfmTWM2OD16LkSyPFA5KM7:TR?= NW\2bndJW0GQR1XS
GDM-1 M{\1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRThwOUeyPVIh|ryP NHrIZ49USU6JRWK=
LC4-1 M{i2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTlwMEC5NVEh|ryP NHzRRWtUSU6JRWK=
MLMA MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSxNY96UUN3ME25MlE2ODB4IN88US=> MnzFV2FPT0WU
EoL-1-cell M4TIdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjoTWM2OD17LkOwNVkzKM7:TR?= MX7TRW5ITVJ?
BOKU M2DLemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTlwOU[0OlYh|ryP MYfTRW5ITVJ?
EVSA-T MnLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnXSWdKSzVyPUGwMlY2PjhizszN MXTTRW5ITVJ?
D-283MED MnrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFyLkmxO|Yh|ryP MVLTRW5ITVJ?
NB1 NUjRTZJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH5TWM2OD1zMT6wNlQzKM7:TR?= M3\XWXNCVkeHUh?=
RPMI-8402 M2jQSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLTTWM2OD1zMT6xO|gh|ryP NV3jbo03W0GQR1XS
NCI-H1355 M1vBeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXKx[odRUUN3ME2xNU4yQDB4IN88US=> M4GzN3NCVkeHUh?=
NB7 NGH6[HZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfDTWM2OD1zMT6zNlk4KM7:TR?= MmDyV2FPT0WU
RPMI-6666 MmH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIOyWFZKSzVyPUGyMlk2PjdizszN NXzYc3VqW0GQR1XS
697 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvoTWM2OD1zMz6yO|AyKM7:TR?= Mo\KV2FPT0WU
CTB-1 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nROGlEPTB;MUOuOVk1QCEQvF2= MXjTRW5ITVJ?
VA-ES-BJ NVzHWZJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Xw[2lEPTB;MUOuPVI{PCEQvF2= M2OxfnNCVkeHUh?=
BE-13 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7oTWM2OD1zND6zPVE2KM7:TR?= NHfCbFBUSU6JRWK=
SKM-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PwVmlEPTB;MUSuOFQ6QSEQvF2= NWLndJpoW0GQR1XS
TE-6 NIXWVGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTF2Lke1PVEh|ryP NUH2UVd4W0GQR1XS
LB771-HNC MofYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1W0PWlEPTB;MUSuO|g6QCEQvF2= NYXINlNzW0GQR1XS
ECC4 NHrCN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:2TWM2OD1zNz6wNlc4KM7:TR?= NUfQOVJIW0GQR1XS
ES3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\TfGlXUUN3ME2xO{41PjV3IN88US=> NGTESmdUSU6JRWK=
LB647-SCLC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvmTWM2OD1zNz60PVQ6KM7:TR?= MoLNV2FPT0WU
NB10 MmK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFroPWpKSzVyPUG4MlUzPTZizszN NH;QNWVUSU6JRWK=
L-540 M{TRcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nTVWlEPTB;MUiuPFExQSEQvF2= NWr3VlFkW0GQR1XS
NCI-H2126 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTF7LkWxJO69VQ>? MXPTRW5ITVJ?
HH MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoS2TWM2OD1{MD6wNFk6KM7:TR?= NHnZdJVUSU6JRWK=
MPP-89 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vBU2lEPTB;MkOuNlI5QSEQvF2= MkS0V2FPT0WU
IST-MEL1 NWGybphVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlr0TWM2OD1{Mz64OlU5KM7:TR?= NGnNdXlUSU6JRWK=
KP-N-YS M1TvOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Tve2lEPTB;MkOuPVI2PSEQvF2= M{PiSXNCVkeHUh?=
EC-GI-10 NGnw[m1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPqTW1KSzVyPUK0MlU6QDlizszN MXLTRW5ITVJ?
EKVX M1\NU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\sdZBKUUN3ME2yOk4xOjB|IN88US=> NILXZ3ZUSU6JRWK=
TGBC1TKB M1v3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13BfWlEPTB;Mk[uOFM1KM7:TR?= M1fsPHNCVkeHUh?=
Daudi NEPLWXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXrRo1KSzVyPUK3MlA4PzNizszN M4PQfnNCVkeHUh?=
ALL-PO NH\mRpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJ5LkC4NUDPxE1? NHWwZZdUSU6JRWK=
NB6 NITnR|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnNW3dKSzVyPUK3MlQ5QCEQvF2= M4nrNnNCVkeHUh?=
ES6 NEm3c5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M330UGlEPTB;MkeuPVEzOyEQvF2= Ml;CV2FPT0WU
COLO-320-HSR NFL4XI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nobWlEPTB;MkiuNFM4OyEQvF2= M2fINHNCVkeHUh?=
K5 NVzNbnRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7NTWM2OD1{OD6xNlg4KM7:TR?= NI\WWmNUSU6JRWK=
ES1 NV\yR2c5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWiyb5p3UUN3ME2yPE44Pzd|IN88US=> MV\TRW5ITVJ?
LC-1F M2HKeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnVcVdiUUN3ME2yPU44OzR4IN88US=> NFnDPJZUSU6JRWK=
SCLC-21H NVrZNXlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHQeJZKSzVyPUOwMlc{OTdizszN NYH2SmM6W0GQR1XS
SK-PN-DW MoL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjQTWM2OD1|Mj61OVk5KM7:TR?= Ml7BV2FPT0WU
D-247MG NHW5TZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjtTWM2OD1|Mj65O|c{KM7:TR?= MULTRW5ITVJ?
TE-5 NIfjcFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN|LkCzOlIh|ryP NFK1fVZUSU6JRWK=
MONO-MAC-6 M4j0O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTN|LkWwOFgh|ryP M2DrbXNCVkeHUh?=
LB2518-MEL MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTlTWM2OD1|Mz63OlY3KM7:TR?= MlfrV2FPT0WU
LOXIMVI M1zRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTN|Lke5Nlgh|ryP MkTvV2FPT0WU
NCI-H209 MoiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLLRpVJUUN3ME2zOU4yPDRizszN M3HlXnNCVkeHUh?=
A253 NF\HfndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe2VZQ1UUN3ME2zOU44PDJ7IN88US=> NXToSpFvW0GQR1XS
HCC1599 NUi1ZZdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrDdG9KSzVyPUO2MlcxPTNizszN MYfTRW5ITVJ?
EB-3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonwTWM2OD1|Nj65OVE5KM7:TR?= NYKyflFvW0GQR1XS
GOTO NHvzVmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u0RWlEPTB;M{euN|IzPCEQvF2= NWjhbpZKW0GQR1XS
SW684 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzPTWM2OD12MT64OFk2KM7:TR?= NWf4Wmt4W0GQR1XS
DEL NY\FOGRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH1cGNKSzVyPUSyMlA2OjJizszN NXG5NmFvW0GQR1XS
HT-144 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7EWpdKSzVyPUSyMlE3PzZizszN NX7yfW4{W0GQR1XS
TE-9 MlLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTR|LkS1PVYh|ryP NYXyd2RUW0GQR1XS
KARPAS-45 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGX2SJBKSzVyPUS0MlM6OjVizszN M1XTWnNCVkeHUh?=
HAL-01 NHvSOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rqVGlEPTB;NESuOVA{PCEQvF2= NWL3OlNSW0GQR1XS
RCC10RGB M2XjZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPNTWM2OD12ND63N|kzKM7:TR?= Mo\YV2FPT0WU
CP67-MEL NY\aS4hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR3Lk[yOFEh|ryP NX24[5VFW0GQR1XS
NB17 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle1TWM2OD12NT62OlQ{KM7:TR?= Mn;uV2FPT0WU
SK-UT-1 MljqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\PTWM2OD12NT65OFY1KM7:TR?= Mo\yV2FPT0WU
JiyoyeP-2003 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmmyTWM2OD12Nj6wNVE6KM7:TR?= MYDTRW5ITVJ?
HCE-4 NIfhe2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3EWIdJUUN3ME20Ok42QTZ6IN88US=> MYPTRW5ITVJ?
NCI-H720 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjzTWM2OD12Nj63OlgzKM7:TR?= NXH3SJhtW0GQR1XS
KARPAS-422 NV20NG1lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjITWM2OD12Nz6wPFk2KM7:TR?= Mo\oV2FPT0WU
Ramos-2G6-4C10 M33h[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDXN2NEUUN3ME20O{4yPjJ{IN88US=> M3nYTHNCVkeHUh?=
HCE-T NF;6elhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPGTWM2OD12Nz62PFI5KM7:TR?= MV3TRW5ITVJ?
PSN1 NYnhPIdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTR5Lke4NVMh|ryP MmW2V2FPT0WU

... 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]
+ Expand
  • 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 warmed (64.57 mM)
Ethanol 31 mg/mL (57.19 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 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)

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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 )

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    C2
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* 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

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
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    C4=C3/X C4: LOG(C4):
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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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    What is the half-life of Saracatinib?

  • Answer:

    Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID