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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Cited by 39 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.

  • Dose response studies. HT29-BSRwt cells cultured on 48-well plates were treated with increasing concentrations of saracatinib for 2h. The changes in normalized bioluminescence activity (Fluc/Gluc) were plotted as fold induction over vehicle-treated values. Western blotting analysis with phospho-tyrosine, phospho-Src, and total Src-specific antibodies was performed to confirm the inhibition of Src activity.

    Theranostics, 2016, 6(4):594-609. 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 MnPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoK1TWM2OD1yLkC2NVQ{KM7:TR?= NHHKO4JUSU6JRWK=
LAMA-84 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonBTWM2OD1yLkG1PVkh|ryP NH21PJlUSU6JRWK=
MEG-01 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTBwMkO2PFgh|ryP M3XpV3NCVkeHUh?=
EM-2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj6fFlKSzVyPUCuNlY2KM7:TR?= M{\TdXNCVkeHUh?=
TE-15 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHQTWM2OD1yLkK3OFEzKM7:TR?= MkT2V2FPT0WU
NCI-H1648 M4rxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDDTWM2OD1yLkK4NVE3KM7:TR?= MXvTRW5ITVJ?
TE-12 Ml7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzGTWM2OD1yLkOyOlgh|ryP NGHFO5dUSU6JRWK=
LB996-RCC NVXQfodvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnENWIxUUN3ME2wMlQ1OTl4IN88US=> MVHTRW5ITVJ?
K-562 MlL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUT0R4lRUUN3ME2wMlQ1QTZ5IN88US=> MVzTRW5ITVJ?
D-336MG MlP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3L4e2lEPTB;MD61NFMxPCEQvF2= MWLTRW5ITVJ?
NOS-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLNTWM2OD1yLk[wOVI6KM7:TR?= NF\Q[GRUSU6JRWK=
EW-24 NXLFXWV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwNkK2PVMh|ryP NWjydIU6W0GQR1XS
BV-173 NYDteoZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvXW3VxUUN3ME2wMlY2OjR7IN88US=> M{LhXnNCVkeHUh?=
NCCIT MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLKXW5UUUN3ME2wMlc{OjF6IN88US=> NEXVZmlUSU6JRWK=
NCI-H1436 NVjsbWFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[5TWM2OD1yLke5NFQ6KM7:TR?= Mn\6V2FPT0WU
BB30-HNC NUHPUHl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwOE[yNFMh|ryP NWHQ[lZEW0GQR1XS
TE-8 NHj3[2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTWTWM2OD1yLki3Nlc2KM7:TR?= NGrVR|hUSU6JRWK=
A704 NYn0[mV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\LdJpHUUN3ME2wMlg6OjFizszN NF\hZ2lUSU6JRWK=
TK10 NF7Fd3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwOUC2Olkh|ryP NFr4XmRUSU6JRWK=
KS-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\PTWM2OD1zLkG5O|c6KM7:TR?= MYrTRW5ITVJ?
C2BBe1 M2\OSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XKZmlEPTB;MT6yNFUxPyEQvF2= MWPTRW5ITVJ?
RXF393 MoCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DvTmlEPTB;MT6yOFM3KM7:TR?= MVTTRW5ITVJ?
KGN MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfuT417UUN3ME2xMlI4Pjh5IN88US=> M{TJSXNCVkeHUh?=
NB69 Mn7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoraTWM2OD1zLkO3OFk4KM7:TR?= MYTTRW5ITVJ?
TE-11 NI[3RpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfIT2RLUUN3ME2xMlQ{PDF6IN88US=> M{GwO3NCVkeHUh?=
TE-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTFwNESxNFUh|ryP MonkV2FPT0WU
ST486 NIHXRVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTFwNEW4OVIh|ryP MlHwV2FPT0WU
HOP-62 NW\l[oozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz6WY44UUN3ME2xMlUxOjR4IN88US=> MVTTRW5ITVJ?
EW-16 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\SPGlEPTB;MT61OVA5OyEQvF2= NEDUXZlUSU6JRWK=
LB1047-RCC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rIZmlEPTB;MT61OVQ2OyEQvF2= MmPkV2FPT0WU
TE-10 M1nleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLTNmgyUUN3ME2xMlY3OjV{IN88US=> M2jJN3NCVkeHUh?=
RL95-2 Ml7YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlW0TWM2OD1zLk[2PVAzKM7:TR?= NHr1epBUSU6JRWK=
DOHH-2 M2jEWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfrNYFKSzVyPUGuO|E4QDJizszN NHr0OpRUSU6JRWK=
MFH-ino NH;uXYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGC4Z5pKSzVyPUGuO|c5PyEQvF2= M4HRbXNCVkeHUh?=
GB-1 MkWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFwN{m4N|Mh|ryP NFjRVYdUSU6JRWK=
SK-N-DZ MonHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3EVYdKSzVyPUGuPFQ3QDhizszN M2PpPHNCVkeHUh?=
OS-RC-2 NX;Xc2c5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjPN|hKSzVyPUGuPFg2PzRizszN NFfEe5FUSU6JRWK=
SW982 NVjMXnl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HXZ2lEPTB;MT65NlA6OyEQvF2= MUXTRW5ITVJ?
KALS-1 Ml\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHseI9VUUN3ME2xMlk5PzJ{IN88US=> NXrFUHo6W0GQR1XS
TGBC24TKB MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJwMEW5OVgh|ryP MnzqV2FPT0WU
GI-1 NUC5NVR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHv4WZJKSzVyPUKuNVYxQDRizszN NW\PbmJnW0GQR1XS
SW962 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJwMUexO|gh|ryP NFjkbmlUSU6JRWK=
SW872 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlG0TWM2OD1{LkG4OVA4KM7:TR?= NXznW|RlW0GQR1XS
NCI-H747 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXTTWM2OD1{LkK1O|E1KM7:TR?= NGPmUHNUSU6JRWK=
MZ1-PC Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJwMkmzOVYh|ryP NUT2Smo6W0GQR1XS
MSTO-211H NVG2c4JoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDXOm5KSzVyPUKuN|U4OjNizszN MnTnV2FPT0WU
BL-70 MluwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7BTWM2OD1{LkS3OFIzKM7:TR?= NHrWS|dUSU6JRWK=
SW954 NHu1fJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnUTWM2OD1{LkW3OFA5KM7:TR?= NWfZN214W0GQR1XS
SNB75 NEXTTGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfkTWM2OD1{Lk[4OVk1KM7:TR?= NHfFVpNUSU6JRWK=
IST-SL2 NU\KWoRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmxUpVxUUN3ME2yMlczOzd7IN88US=> M3zyfHNCVkeHUh?=
GCIY MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELvSm1KSzVyPUKuPFcxODVizszN NULsZos6W0GQR1XS
KU812 NVvVR5BRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnLTWM2OD1|LkC1Nlk6KM7:TR?= NF;IZ4RUSU6JRWK=
LXF-289 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjjTWM2OD1|LkGyNVA6KM7:TR?= M1;rWHNCVkeHUh?=
ETK-1 NWfQ[WJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;jTWM2OD1|LkKwO|Y4KM7:TR?= NGHid|BUSU6JRWK=
SF126 M2ntdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPYPWJKSzVyPUOuN|EyPzRizszN MUHTRW5ITVJ?
LC-2-ad MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml6wTWM2OD1|LkW1O{DPxE1? NIi2dFlUSU6JRWK=
KNS-42 NX3QOpRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvwPWFKSzVyPUOuOlUh|ryP NV\xZoxbW0GQR1XS
OVCAR-4 M2DqeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoKzTWM2OD1|LkezOFM{KM7:TR?= NV7VdlA4W0GQR1XS
PF-382 M{T3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmraTWM2OD1|LkizOlk5KM7:TR?= MnizV2FPT0WU
SH-4 NIriNFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDu[XZKSzVyPUSuNlUzPTlizszN MUfTRW5ITVJ?
KM12 NWnWVpM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1qyWmlEPTB;ND6zNlQyPiEQvF2= MWTTRW5ITVJ?
NB5 MnXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfXVYZ3UUN3ME20MlQyQDZ2IN88US=> NX;nNnVMW0GQR1XS
KURAMOCHI M{[0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXhfXN2UUN3ME20MlY2OjV4IN88US=> MY\TRW5ITVJ?
Becker MmTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XvfGlEPTB;ND62OlQyPiEQvF2= M2\3UnNCVkeHUh?=
MV-4-11 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfCcYViUUN3ME20MlgyOzR2IN88US=> M4r2N3NCVkeHUh?=
KINGS-1 NUPXRWRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfMdlVtUUN3ME20MlgzOzd|IN88US=> M4LEeXNCVkeHUh?=
LS-123 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HxW2lEPTB;NT60PVY5PCEQvF2= M1fHSnNCVkeHUh?=
SF268 M1PtXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TC[mlEPTB;NT62NVI3OiEQvF2= M{S2NnNCVkeHUh?=
A388 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTVwNkO2Olch|ryP NF3N[YJUSU6JRWK=
NMC-G1 NFTudY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzw[YFKSzVyPU[uNFE5OTFizszN MXLTRW5ITVJ?
CGTH-W-1 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojiTWM2OD14LkCyNFc2KM7:TR?= Mkf2V2FPT0WU
ES4 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjKTWM2OD14LkWzNFc1KM7:TR?= Mk[zV2FPT0WU
SR NEnHeVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTZwNUi4NFch|ryP M3rLfnNCVkeHUh?=
BB49-HNC M{K5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlOwTWM2OD14LkezNlA3KM7:TR?= M3vrOHNCVkeHUh?=
KLE MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jHXmlEPTB;Nj63PFM4PyEQvF2= M2XVRXNCVkeHUh?=
HUTU-80 NVnvVYJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFG3blNKSzVyPU[uPVg1PjZizszN NIPoZVdUSU6JRWK=
SNU-C2B MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDORld6UUN3ME23MlgzPzN5IN88US=> Ml\3V2FPT0WU
BB65-RCC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXjfVlmUUN3ME23Mlk1QTB2IN88US=> NHHCXY9USU6JRWK=
QIMR-WIL MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LmZmlEPTB;OD60NlgxQCEQvF2= MV;TRW5ITVJ?
GDM-1 NUfOUXdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC0TWM2OD16Lkm3NlkzKM7:TR?= M{jXSHNCVkeHUh?=
LC4-1 NFvyR5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP2VVdCUUN3ME25MlAxQTFzIN88US=> MVHTRW5ITVJ?
MLMA NWj1TIt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXi2d25xUUN3ME25MlE2ODB4IN88US=> NHLzcnlUSU6JRWK=
EoL-1-cell MnXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLiTWM2OD17LkOwNVkzKM7:TR?= Mn3WV2FPT0WU
BOKU MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnONnRKSzVyPUmuPVY1PjZizszN NVLHbJBjW0GQR1XS
EVSA-T NVXMeJFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfrRY9KSzVyPUGwMlY2PjhizszN NXHpU4NMW0GQR1XS
D-283MED M4nkOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XBO2lEPTB;MUCuPVE4PiEQvF2= M{LtUHNCVkeHUh?=
NB1 M3;iTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1mweWlEPTB;MUGuNFI1OiEQvF2= NEPMcFZUSU6JRWK=
RPMI-8402 NUXyW5BIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHX2d4lKSzVyPUGxMlE4QCEQvF2= NFrRXHpUSU6JRWK=
NCI-H1355 NVfCVoNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULQR4JwUUN3ME2xNU4yQDB4IN88US=> MoT3V2FPT0WU
NB7 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILSeFVKSzVyPUGxMlMzQTdizszN NYW2UnQyW0GQR1XS
RPMI-6666 M{\5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTF{Lkm1Olch|ryP MWPTRW5ITVJ?
697 M2XtSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPBSYpKSzVyPUGzMlI4ODFizszN M4PZSnNCVkeHUh?=
CTB-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:3[|hKSzVyPUGzMlU6PDhizszN MkC0V2FPT0WU
VA-ES-BJ Ml7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTF|LkmyN|Qh|ryP M3rOV3NCVkeHUh?=
BE-13 NWT6[ox6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWwflV3UUN3ME2xOE4{QTF3IN88US=> NX;BTVF7W0GQR1XS
SKM-1 NF7k[ppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;HTWM2OD1zND60OFk6KM7:TR?= M2XSV3NCVkeHUh?=
TE-6 M13GXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvoVm1KSzVyPUG0Mlc2QTFizszN NH;3[JFUSU6JRWK=
LB771-HNC M2[ycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fGTWlEPTB;MUSuO|g6QCEQvF2= MmfkV2FPT0WU
ECC4 M1\nbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LUb2lEPTB;MUeuNFI4PyEQvF2= NX;2NFRXW0GQR1XS
ES3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXVTWM2OD1zNz60OlU2KM7:TR?= M1\jV3NCVkeHUh?=
LB647-SCLC Mlj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFWxeGtKSzVyPUG3MlQ6PDlizszN NF[2W4JUSU6JRWK=
NB10 MlfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTF6LkWyOVYh|ryP MYLTRW5ITVJ?
L-540 MljRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3DTWM2OD1zOD64NVA6KM7:TR?= MXLTRW5ITVJ?
NCI-H2126 NUjZOHp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTF7LkWxJO69VQ>? M1fHdHNCVkeHUh?=
HH NXm0O2ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTJyLkCwPVkh|ryP MkHVV2FPT0WU
MPP-89 MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfvTWM2OD1{Mz6yNlg6KM7:TR?= NIS0dWZUSU6JRWK=
IST-MEL1 M4\EdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjBZ5VRUUN3ME2yN{45PjV6IN88US=> NEDxUVBUSU6JRWK=
KP-N-YS NELqXoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTJ|LkmyOVUh|ryP NELoRlRUSU6JRWK=
EC-GI-10 M{nPdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWL5eI9xUUN3ME2yOE42QTh7IN88US=> MU\TRW5ITVJ?
EKVX MojwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfqSpZKSzVyPUK2MlAzODNizszN Mn\JV2FPT0WU
TGBC1TKB NF\NTZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTJ4LkSzOEDPxE1? NFTkZmVUSU6JRWK=
Daudi NX24b2pYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn5VINwUUN3ME2yO{4xPzd|IN88US=> MmTRV2FPT0WU
ALL-PO NFXDZplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTJ5LkC4NUDPxE1? MVnTRW5ITVJ?
NB6 NV3vRVVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jydGlEPTB;MkeuOFg5KM7:TR?= M1i0bXNCVkeHUh?=
ES6 NW\QdG5MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHKzT4hKSzVyPUK3MlkyOjNizszN MonEV2FPT0WU
COLO-320-HSR MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D3d2lEPTB;MkiuNFM4OyEQvF2= MmroV2FPT0WU
K5 M2rHfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIL1eIJKSzVyPUK4MlEzQDdizszN NEHLc29USU6JRWK=
ES1 Mk\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;EVGZHUUN3ME2yPE44Pzd|IN88US=> M3;wTXNCVkeHUh?=
LC-1F M1\vXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfrPZE2UUN3ME2yPU44OzR4IN88US=> MojwV2FPT0WU
SCLC-21H NE[0Z2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTNyLkezNVch|ryP M1nYeHNCVkeHUh?=
SK-PN-DW NIjzbXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDU[HNLUUN3ME2zNk42PTl6IN88US=> M3zXO3NCVkeHUh?=
D-247MG NH3kV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLjTWM2OD1|Mj65O|c{KM7:TR?= M1zRb3NCVkeHUh?=
TE-5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPQc4dKSzVyPUOzMlA{PjJizszN NXPs[olXW0GQR1XS
MONO-MAC-6 NGP3cWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTN|LkWwOFgh|ryP M3vqXnNCVkeHUh?=
LB2518-MEL NEnaVIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K4OWlEPTB;M{OuO|Y3PiEQvF2= NXnhdFY3W0GQR1XS
LOXIMVI M3vnNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzy[nNKSzVyPUOzMlc6OjhizszN MYTTRW5ITVJ?
NCI-H209 M3y5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTN3LkG0OEDPxE1? NV;GS5c1W0GQR1XS
A253 M1nCTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXmTWM2OD1|NT63OFI6KM7:TR?= MXrTRW5ITVJ?
HCC1599 NX;jOG96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nS[mlEPTB;M{[uO|A2OyEQvF2= MXHTRW5ITVJ?
EB-3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTJO|FKSzVyPUO2Mlk2OThizszN MknXV2FPT0WU
GOTO NIK4OZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTN5LkOyNlQh|ryP M1rx[XNCVkeHUh?=
SW684 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvLNZlKSzVyPUSxMlg1QTVizszN Ml3CV2FPT0WU
DEL Ml60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTR{LkC1NlIh|ryP MWXTRW5ITVJ?
HT-144 M{nqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnyd4NKSzVyPUSyMlE3PzZizszN NHi1dFFUSU6JRWK=
TE-9 MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvpN|l4UUN3ME20N{41PTl4IN88US=> Ml7JV2FPT0WU
KARPAS-45 MnT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Oyd2lEPTB;NESuN|kzPSEQvF2= NHjR[HpUSU6JRWK=
HAL-01 MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHHTWM2OD12ND61NFM1KM7:TR?= NHvVWodUSU6JRWK=
RCC10RGB MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\QTWM2OD12ND63N|kzKM7:TR?= M2HGcHNCVkeHUh?=
CP67-MEL NIKwcmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLCVXN4UUN3ME20OU43OjRzIN88US=> MnT6V2FPT0WU
NB17 M{LaOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTRWJNiUUN3ME20OU43PjR|IN88US=> NFjLUY9USU6JRWK=
SK-UT-1 NV\v[G5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXodWxKSzVyPUS1Mlk1PjRizszN NHTucotUSU6JRWK=
JiyoyeP-2003 NI\WSpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\acppwUUN3ME20Ok4xOTF7IN88US=> MVLTRW5ITVJ?
HCE-4 M37wUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR4LkW5Olgh|ryP NXXjNmx3W0GQR1XS
NCI-H720 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\HfmtKSzVyPUS2Mlc3QDJizszN NYLLUnk6W0GQR1XS
KARPAS-422 NVHVSJI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TiSGlEPTB;NEeuNFg6PSEQvF2= NF;NSHNUSU6JRWK=
Ramos-2G6-4C10 M4H4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\meWlEPTB;NEeuNVYzOiEQvF2= MmrXV2FPT0WU
HCE-T Mlq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LmN2lEPTB;NEeuOlgzQCEQvF2= MWrTRW5ITVJ?
PSN1 MnTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfNOIs4UUN3ME20O{44QDF|IN88US=> M{CxUHNCVkeHUh?=

... 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(Data is from Selleck tests instead of citations):
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
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 )

  • 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):
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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
NCT03661125 Not yet recruiting Parkinson Disease Psychosis King''s College London|AstraZeneca|King''s College Hospital NHS Trust April 11 2019 Early Phase 1
NCT03661125 Not yet recruiting Parkinson Disease Psychosis King''s College London|AstraZeneca|King''s College Hospital NHS Trust April 11 2019 Early Phase 1
NCT02955186 Recruiting Alcohol Drinking Yale University May 9 2017 Phase 2
NCT02955186 Recruiting Alcohol Drinking Yale University May 9 2017 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Women''s Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Women''s Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2

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

Src Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID