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 NX;HbZVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwME[xOFMh|ryP M3Tu[XNCVkeHUh?=
LAMA-84 NXHURVFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXENFhKSzVyPUCuNVU6QSEQvF2= MlnTV2FPT0WU
MEG-01 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjQTWM2OD1yLkKzOlg5KM7:TR?= MknyV2FPT0WU
EM-2 NEnIfINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7VTWM2OD1yLkK2OUDPxE1? NFL6TnZUSU6JRWK=
TE-15 NX3SRZd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTKUWJKSzVyPUCuNlc1OTJizszN NInmVWpUSU6JRWK=
NCI-H1648 NI\WSmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LsRmlEPTB;MD6yPFEyPiEQvF2= NIDBOXNUSU6JRWK=
TE-12 M4fUc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLXTWM2OD1yLkOyOlgh|ryP NHnGeJRUSU6JRWK=
LB996-RCC M1vkeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPYeVhrUUN3ME2wMlQ1OTl4IN88US=> MmPPV2FPT0WU
K-562 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfXTWM2OD1yLkS0PVY4KM7:TR?= NFPNSo9USU6JRWK=
D-336MG NWfTdmVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\iOWlEPTB;MD61NFMxPCEQvF2= NYTmOoZ7W0GQR1XS
NOS-1 NVLsPIMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoniTWM2OD1yLk[wOVI6KM7:TR?= MVjTRW5ITVJ?
EW-24 Mki2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HZS2lEPTB;MD62NlY6OyEQvF2= NYr0To5zW0GQR1XS
BV-173 Mkf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFSxO5pKSzVyPUCuOlUzPDlizszN M4jj[HNCVkeHUh?=
NCCIT MoHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojMTWM2OD1yLkezNlE5KM7:TR?= M2jw[3NCVkeHUh?=
NCI-H1436 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHXO3p4UUN3ME2wMlc6ODR7IN88US=> M2DK[3NCVkeHUh?=
BB30-HNC NIDocGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\p[WlEPTB;MD64OlIxOyEQvF2= MUnTRW5ITVJ?
TE-8 NFGyb3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\TTWM2OD1yLki3Nlc2KM7:TR?= MYnTRW5ITVJ?
A704 NGnZV|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwOEmyNUDPxE1? M{fwTHNCVkeHUh?=
TK10 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jp[GlEPTB;MD65NFY3QSEQvF2= NEfxeGFUSU6JRWK=
KS-1 M{\Vcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFwMUm3O|kh|ryP MULTRW5ITVJ?
C2BBe1 M1flZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTSdnRDUUN3ME2xMlIxPTB5IN88US=> NIPkRoVUSU6JRWK=
RXF393 M4eyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vYNGlEPTB;MT6yOFM3KM7:TR?= NHXZXnZUSU6JRWK=
KGN NYrKW2hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\y[mlEPTB;MT6yO|Y5PyEQvF2= NGraVI1USU6JRWK=
NB69 NVy3c2JiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFwM{e0PVch|ryP NWnn[2s6W0GQR1XS
TE-11 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Oz[WlEPTB;MT60N|QyQCEQvF2= NIXySHNUSU6JRWK=
TE-1 MkfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\C[pFKSzVyPUGuOFQyODVizszN NHv2WFdUSU6JRWK=
ST486 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofqTWM2OD1zLkS1PFUzKM7:TR?= NYPwcoZVW0GQR1XS
HOP-62 NHu5U45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwNUCyOFYh|ryP MkP0V2FPT0WU
EW-16 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnz3TWM2OD1zLkW1NFg{KM7:TR?= NXLISIRRW0GQR1XS
LB1047-RCC M1nJPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M16x[GlEPTB;MT61OVQ2OyEQvF2= MVTTRW5ITVJ?
TE-10 MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHEdmt7UUN3ME2xMlY3OjV{IN88US=> MX;TRW5ITVJ?
RL95-2 M17hTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTITWM2OD1zLk[2PVAzKM7:TR?= NVXDO4pEW0GQR1XS
DOHH-2 NWL1OYYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln5TWM2OD1zLkexO|gzKM7:TR?= MUTTRW5ITVJ?
MFH-ino NU\vVY1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\1TWM2OD1zLke3PFch|ryP MkPZV2FPT0WU
GB-1 NF;3WolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTFwN{m4N|Mh|ryP M2q1dHNCVkeHUh?=
SK-N-DZ NFHOTZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2m4SWlEPTB;MT64OFY5QCEQvF2= NYPSWVR1W0GQR1XS
OS-RC-2 Mn3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTFwOEi1O|Qh|ryP NVfiWolNW0GQR1XS
SW982 NWjK[pdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTFwOUKwPVMh|ryP NHzFbHpUSU6JRWK=
KALS-1 M2HIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTFwOUi3NlIh|ryP MXPTRW5ITVJ?
TGBC24TKB MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTJwMEW5OVgh|ryP M1HQS3NCVkeHUh?=
GI-1 M3K2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rHNGlEPTB;Mj6xOlA5PCEQvF2= NIPwXpFUSU6JRWK=
SW962 MoDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJwMUexO|gh|ryP MV7TRW5ITVJ?
SW872 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJwMUi1NFch|ryP M4TQVnNCVkeHUh?=
NCI-H747 NVv4XFN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJwMkW3NVQh|ryP NXPNfWdRW0GQR1XS
MZ1-PC NVLqWGI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFm4WJhKSzVyPUKuNlk{PTZizszN MVTTRW5ITVJ?
MSTO-211H MkDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1W0SWlEPTB;Mj6zOVczOyEQvF2= M3jYeHNCVkeHUh?=
BL-70 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTLOotKSzVyPUKuOFc1OjJizszN NWroXVIzW0GQR1XS
SW954 NYm3PJBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUP6ZWYyUUN3ME2yMlU4PDB6IN88US=> M{G5XXNCVkeHUh?=
SNB75 NYLKWVZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP6TWM2OD1{Lk[4OVk1KM7:TR?= M{nhNHNCVkeHUh?=
IST-SL2 NHXTdoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILOdXpKSzVyPUKuO|I{PzlizszN NWLIS|htW0GQR1XS
GCIY MkH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHOW402UUN3ME2yMlg4ODB3IN88US=> MVrTRW5ITVJ?
KU812 NX7FR4hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vZZ2lEPTB;Mz6wOVI6QSEQvF2= MoLZV2FPT0WU
LXF-289 NHrsXVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTNwMUKxNFkh|ryP MkO1V2FPT0WU
ETK-1 NVLXZlh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DJfWlEPTB;Mz6yNFc3PyEQvF2= NILoN3RUSU6JRWK=
SF126 MoSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3vdIJKSzVyPUOuN|EyPzRizszN NXjGW2toW0GQR1XS
LC-2-ad M372dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLmc|VqUUN3ME2zMlU2PyEQvF2= M{Xue3NCVkeHUh?=
KNS-42 NFnM[2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fKeGlEPTB;Mz62OUDPxE1? M4PuS3NCVkeHUh?=
OVCAR-4 NYDpT5h[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\4TWM2OD1|LkezOFM{KM7:TR?= NUT4c4hXW0GQR1XS
PF-382 NE\nUo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTNwOEO2PVgh|ryP M4PvO3NCVkeHUh?=
SH-4 M4C4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK3TWM2OD12LkK1NlU6KM7:TR?= MX7TRW5ITVJ?
KM12 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrMV5lKSzVyPUSuN|I1OTZizszN MmnlV2FPT0WU
NB5 MnXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTRwNEG4OlQh|ryP NUfwbIlyW0GQR1XS
KURAMOCHI NWjRRZdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTRwNkWyOVYh|ryP NEj2RXBUSU6JRWK=
Becker Mn;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK1TWM2OD12Lk[2OFE3KM7:TR?= MWDTRW5ITVJ?
MV-4-11 NUjiS|RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;qVWlEPTB;ND64NVM1PCEQvF2= M1;XRnNCVkeHUh?=
KINGS-1 Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7SVFVKSzVyPUSuPFI{PzNizszN NHrrdm1USU6JRWK=
LS-123 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2G3ZWlEPTB;NT60PVY5PCEQvF2= MmC1V2FPT0WU
SF268 NUS0[JN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvIc5J[UUN3ME21MlYyOjZ{IN88US=> M1qweXNCVkeHUh?=
A388 MkHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTVwNkO2Olch|ryP M4DCNHNCVkeHUh?=
NMC-G1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rtOGlEPTB;Nj6wNVgyOSEQvF2= M3PVOHNCVkeHUh?=
CGTH-W-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTZwMEKwO|Uh|ryP MofPV2FPT0WU
ES4 NFiwZmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVz3S|ZWUUN3ME22MlU{ODd2IN88US=> NVO1O|BHW0GQR1XS
SR M2\LVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTVbWN1UUN3ME22MlU5QDB5IN88US=> M4DEU3NCVkeHUh?=
BB49-HNC MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{myUmlEPTB;Nj63N|IxPiEQvF2= NH74OJZUSU6JRWK=
KLE NFy1OHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PuO2lEPTB;Nj63PFM4PyEQvF2= NEe3ZZFUSU6JRWK=
HUTU-80 NGnVVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\lZWlEPTB;Nj65PFQ3PiEQvF2= NGjuUWdUSU6JRWK=
SNU-C2B NHLTRoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\CTWM2OD15LkiyO|M4KM7:TR?= NFOyS3BUSU6JRWK=
BB65-RCC MmTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTdwOUS5NFQh|ryP MXPTRW5ITVJ?
QIMR-WIL M1LsUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:1SmlEPTB;OD60NlgxQCEQvF2= MVvTRW5ITVJ?
GDM-1 Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRThwOUeyPVIh|ryP NGL6cZZUSU6JRWK=
LC4-1 NXrZe2xoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPFVmU1UUN3ME25MlAxQTFzIN88US=> Ml:yV2FPT0WU
MLMA NXL0VoQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\2OGlEPTB;OT6xOVAxPiEQvF2= M2LZN3NCVkeHUh?=
EoL-1-cell M3vtfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4KzNGlEPTB;OT6zNFE6OiEQvF2= NEjnOoRUSU6JRWK=
BOKU NXe2e2h6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvNb49KSzVyPUmuPVY1PjZizszN MYXTRW5ITVJ?
EVSA-T M2TGNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTYdndKSzVyPUGwMlY2PjhizszN NWfLSFZZW0GQR1XS
D-283MED M2W5Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDKbphEUUN3ME2xNE46OTd4IN88US=> NWDofFkzW0GQR1XS
NB1 NHe0[I9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK4cY52UUN3ME2xNU4xOjR{IN88US=> NHKzc4lUSU6JRWK=
RPMI-8402 NHH2VHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojpTWM2OD1zMT6xO|gh|ryP M4SxXXNCVkeHUh?=
NCI-H1355 MnLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfSNlNKSzVyPUGxMlE5ODZizszN NFfESJpUSU6JRWK=
NB7 NFXKPWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTFzLkOyPVch|ryP MnXvV2FPT0WU
RPMI-6666 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\oTWM2OD1zMj65OVY4KM7:TR?= MnntV2FPT0WU
697 NFHycmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITYdGtKSzVyPUGzMlI4ODFizszN M2TlUHNCVkeHUh?=
CTB-1 NEDBfJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DUSmlEPTB;MUOuOVk1QCEQvF2= NWHMS5FFW0GQR1XS
VA-ES-BJ M3Tmd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LXe2lEPTB;MUOuPVI{PCEQvF2= Mn;aV2FPT0WU
BE-13 NYjaVZVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;welZKSzVyPUG0MlM6OTVizszN NHLoNVJUSU6JRWK=
SKM-1 M4jIb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PYe2lEPTB;MUSuOFQ6QSEQvF2= M2TJb3NCVkeHUh?=
TE-6 M2nDbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnZfoRJUUN3ME2xOE44PTlzIN88US=> NV\rTmJkW0GQR1XS
LB771-HNC MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTNdmNEUUN3ME2xOE44QDl6IN88US=> M3\aSHNCVkeHUh?=
ECC4 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGS3[HhKSzVyPUG3MlAzPzdizszN NILGdYJUSU6JRWK=
ES3 MlzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTF5LkS2OVUh|ryP NE\EcndUSU6JRWK=
LB647-SCLC MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;5b4lKUUN3ME2xO{41QTR7IN88US=> MnmxV2FPT0WU
NB10 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF6LkWyOVYh|ryP NFi4WplUSU6JRWK=
L-540 MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDPTGdYUUN3ME2xPE45OTB7IN88US=> MmG4V2FPT0WU
NCI-H2126 MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPLbmtPUUN3ME2xPU42OSEQvF2= MkDnV2FPT0WU
HH NF70[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJyLkCwPVkh|ryP M{\Ub3NCVkeHUh?=
MPP-89 NEXqO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLDOppWUUN3ME2yN{4zOjh7IN88US=> MlzVV2FPT0WU
IST-MEL1 M1vFNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLE[|BKSzVyPUKzMlg3PThizszN MkDJV2FPT0WU
KP-N-YS MlryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rKfGlEPTB;MkOuPVI2PSEQvF2= MkS3V2FPT0WU
EC-GI-10 M3K4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLVTWM2OD1{ND61PVg6KM7:TR?= M{jWUnNCVkeHUh?=
EKVX NGjzNlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWT4RXRZUUN3ME2yOk4xOjB|IN88US=> NIjqU4pUSU6JRWK=
TGBC1TKB MmLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXObIhKSzVyPUK2MlQ{PCEQvF2= M1vmVXNCVkeHUh?=
Daudi M1v1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJ5LkC3O|Mh|ryP MlGyV2FPT0WU
ALL-PO MmLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLNTWM2OD1{Nz6wPFEh|ryP NWTzfnpJW0GQR1XS
NB6 NVv1S4l6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjTe|JLUUN3ME2yO{41QDhizszN NFrFZ|RUSU6JRWK=
ES6 MkXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XFe2lEPTB;MkeuPVEzOyEQvF2= NFK4Z|dUSU6JRWK=
COLO-320-HSR MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fqXWlEPTB;MkiuNFM4OyEQvF2= M3\uOHNCVkeHUh?=
K5 NEnmN3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnFOIhGUUN3ME2yPE4yOjh5IN88US=> NHLBcYhUSU6JRWK=
ES1 M2DCWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJ6Lke3O|Mh|ryP M{X0O3NCVkeHUh?=
LC-1F M2TpVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTCfHRKSzVyPUK5Mlc{PDZizszN MnG5V2FPT0WU
SCLC-21H MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zPW2lEPTB;M{CuO|MyPyEQvF2= M2q4UXNCVkeHUh?=
SK-PN-DW M{jSZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rYcmlEPTB;M{KuOVU6QCEQvF2= NXnBOVl6W0GQR1XS
D-247MG NVvDWW5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nUcmlEPTB;M{KuPVc4OyEQvF2= NY\QWVZWW0GQR1XS
TE-5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XjR2lEPTB;M{OuNFM3OiEQvF2= NYnjT4JMW0GQR1XS
MONO-MAC-6 MmPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfDTWM2OD1|Mz61NFQ5KM7:TR?= M{HHSnNCVkeHUh?=
LB2518-MEL Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33rPGlEPTB;M{OuO|Y3PiEQvF2= MW\TRW5ITVJ?
LOXIMVI NWGySW5QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHlTWM2OD1|Mz63PVI5KM7:TR?= M4L3V3NCVkeHUh?=
NCI-H209 M1njZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[yXFhKSzVyPUO1MlE1PCEQvF2= NG[1PHFUSU6JRWK=
A253 NVzvZodbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvFTWM2OD1|NT63OFI6KM7:TR?= NIKwXJNUSU6JRWK=
HCC1599 M4TYfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j2TGlEPTB;M{[uO|A2OyEQvF2= NXi0XFlxW0GQR1XS
EB-3 MnnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;hTWM2OD1|Nj65OVE5KM7:TR?= NEGyW5NUSU6JRWK=
GOTO MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrOTWM2OD1|Nz6zNlI1KM7:TR?= MUXTRW5ITVJ?
SW684 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S4WWlEPTB;NEGuPFQ6PSEQvF2= M3;VTnNCVkeHUh?=
DEL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTFTWM2OD12Mj6wOVIzKM7:TR?= M1TvR3NCVkeHUh?=
HT-144 M1nuTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M373fGlEPTB;NEKuNVY4PiEQvF2= NVyzO2wxW0GQR1XS
TE-9 M1jmfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TqTmlEPTB;NEOuOFU6PiEQvF2= Ml7DV2FPT0WU
KARPAS-45 MmTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3DTWM2OD12ND6zPVI2KM7:TR?= NH\IZ5pUSU6JRWK=
HAL-01 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTR2LkWwN|Qh|ryP NELrboVUSU6JRWK=
RCC10RGB NGe0cplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrnV5RKSzVyPUS0Mlc{QTJizszN MnjUV2FPT0WU
CP67-MEL NGTBcHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLhOY95UUN3ME20OU43OjRzIN88US=> MWnTRW5ITVJ?
NB17 M2jlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzZb5ZvUUN3ME20OU43PjR|IN88US=> NGn3RnJUSU6JRWK=
SK-UT-1 M3yySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DZcGlEPTB;NEWuPVQ3PCEQvF2= M3faSHNCVkeHUh?=
JiyoyeP-2003 Mki4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPXRlNIUUN3ME20Ok4xOTF7IN88US=> NVzvR4pkW0GQR1XS
HCE-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTR4LkW5Olgh|ryP MY\TRW5ITVJ?
NCI-H720 NInDcGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTR4Lke2PFIh|ryP M4nDdXNCVkeHUh?=
KARPAS-422 MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfPTWM2OD12Nz6wPFk2KM7:TR?= MX3TRW5ITVJ?
Ramos-2G6-4C10 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTR5LkG2NlIh|ryP MWfTRW5ITVJ?
HCE-T M4nNW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M133NmlEPTB;NEeuOlgzQCEQvF2= Mki5V2FPT0WU
PSN1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYq5WmtPUUN3ME20O{44QDF|IN88US=> NWPqNmZvW0GQR1XS

... 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 to the product individually and in order:
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
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
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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    Molecular Weight

*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
    V1
    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

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

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

  • * Indicates a Required Field

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

Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID