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

9 Customer Reviews

  • 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 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIKw[JBKSzVyPUCuNFYyPDNizszN NYrhfoFkW0GQR1XS
LAMA-84 NUjNe4RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwMUW5PUDPxE1? M4e1PHNCVkeHUh?=
MEG-01 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f3WWlEPTB;MD6yN|Y5QCEQvF2= NVvxV4JUW0GQR1XS
EM-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz5[JdKSzVyPUCuNlY2KM7:TR?= MWLTRW5ITVJ?
TE-15 MmPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\VUmlEPTB;MD6yO|QyOiEQvF2= NHrzUlJUSU6JRWK=
NCI-H1648 NEnyR3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwMkixNVYh|ryP NV;oSHhsW0GQR1XS
TE-12 NFfy[VFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjwTWM2OD1yLkOyOlgh|ryP MorKV2FPT0WU
LB996-RCC NXHGTZdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPBO2I3UUN3ME2wMlQ1OTl4IN88US=> MVzTRW5ITVJ?
K-562 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLlOXo6UUN3ME2wMlQ1QTZ5IN88US=> MYnTRW5ITVJ?
D-336MG NYn4OFR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGH1Wm1KSzVyPUCuOVA{ODRizszN MUTTRW5ITVJ?
NOS-1 M3Ltb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwNkC1Nlkh|ryP MXXTRW5ITVJ?
EW-24 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP5[pV2UUN3ME2wMlYzPjl|IN88US=> MnLRV2FPT0WU
BV-173 M1zYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{mwUGlEPTB;MD62OVI1QSEQvF2= NHTv[HpUSU6JRWK=
NCCIT MnvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zq[GlEPTB;MD63N|IyQCEQvF2= NUPmbJRKW0GQR1XS
NCI-H1436 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTBwN{mwOFkh|ryP MXvTRW5ITVJ?
BB30-HNC NULReGk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrCUGtKSzVyPUCuPFYzODNizszN MXXTRW5ITVJ?
TE-8 NG\MPGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\Ld2lEPTB;MD64O|I4PSEQvF2= MXXTRW5ITVJ?
A704 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnUeXlmUUN3ME2wMlg6OjFizszN MmjNV2FPT0WU
TK10 M1jKRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjjTWM2OD1yLkmwOlY6KM7:TR?= MmfrV2FPT0WU
KS-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrIPW4yUUN3ME2xMlE6Pzd7IN88US=> Mn3SV2FPT0WU
C2BBe1 NWHwR4RwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T3[GlEPTB;MT6yNFUxPyEQvF2= M4q2fXNCVkeHUh?=
RXF393 MmPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPxeWhSUUN3ME2xMlI1OzZizszN MYPTRW5ITVJ?
KGN NEfrVpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzTboVKSzVyPUGuNlc3QDdizszN M3LNOnNCVkeHUh?=
NB69 NV24dHBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTrSVJKSzVyPUGuN|c1QTdizszN NGOzd3hUSU6JRWK=
TE-11 NV64[pJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkO0TWM2OD1zLkSzOFE5KM7:TR?= NGfNW4FUSU6JRWK=
TE-1 M1ux[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLaTWM2OD1zLkS0NVA2KM7:TR?= M{TuOnNCVkeHUh?=
ST486 NIKxcXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PKSGlEPTB;MT60OVg2OiEQvF2= NI\FSZZUSU6JRWK=
HOP-62 MmHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTFwNUCyOFYh|ryP Mn:zV2FPT0WU
EW-16 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\nTWM2OD1zLkW1NFg{KM7:TR?= MX7TRW5ITVJ?
LB1047-RCC NUfUZ2NOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fmUGlEPTB;MT61OVQ2OyEQvF2= MVXTRW5ITVJ?
TE-10 M2\mWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLITWM2OD1zLk[2NlUzKM7:TR?= M4i3UHNCVkeHUh?=
RL95-2 MkTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDDRZVGUUN3ME2xMlY3QTB{IN88US=> MVTTRW5ITVJ?
DOHH-2 NVPNZ3ZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXhTWM2OD1zLkexO|gzKM7:TR?= NEn5UJRUSU6JRWK=
MFH-ino Ml7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TKeGlEPTB;MT63O|g4KM7:TR?= M2L1T3NCVkeHUh?=
GB-1 M4XsT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfybVBKSzVyPUGuO|k5OzNizszN MWrTRW5ITVJ?
SK-N-DZ MnnWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjudY51UUN3ME2xMlg1Pjh6IN88US=> MnSyV2FPT0WU
OS-RC-2 NFjLWVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrxWm1KSzVyPUGuPFg2PzRizszN NWLLTXo3W0GQR1XS
SW982 MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonGTWM2OD1zLkmyNFk{KM7:TR?= Mk\JV2FPT0WU
KALS-1 MknnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXXTWM2OD1zLkm4O|IzKM7:TR?= NH\NOINUSU6JRWK=
TGBC24TKB MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJwMEW5OVgh|ryP Mn;6V2FPT0WU
GI-1 NV7GV5dIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJwMU[wPFQh|ryP MWXTRW5ITVJ?
SW962 NFvVOYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTJwMUexO|gh|ryP NIPGV2ZUSU6JRWK=
SW872 M{fYWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYK4[pp[UUN3ME2yMlE5PTB5IN88US=> NVyzdpV2W0GQR1XS
NCI-H747 NG\Lb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTNTWM2OD1{LkK1O|E1KM7:TR?= M{PlWHNCVkeHUh?=
MZ1-PC M{PPU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPGcYpKSzVyPUKuNlk{PTZizszN MUXTRW5ITVJ?
MSTO-211H NFPIRnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTJwM{W3NlMh|ryP NEWxfJFUSU6JRWK=
BL-70 NHfLT5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPFTWM2OD1{LkS3OFIzKM7:TR?= M{O2UHNCVkeHUh?=
SW954 NESybJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTFTWM2OD1{LkW3OFA5KM7:TR?= MXXTRW5ITVJ?
SNB75 M{nmSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fyVWlEPTB;Mj62PFU6PCEQvF2= MlX3V2FPT0WU
IST-SL2 MmHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJwN{KzO|kh|ryP MVjTRW5ITVJ?
GCIY NUDCVINXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfH[4p3UUN3ME2yMlg4ODB3IN88US=> MofXV2FPT0WU
KU812 NEDOTHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXOTWM2OD1|LkC1Nlk6KM7:TR?= MVvTRW5ITVJ?
LXF-289 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILnRnFKSzVyPUOuNVIyODlizszN NVjqW|J{W0GQR1XS
ETK-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLiWohOUUN3ME2zMlIxPzZ5IN88US=> NWHMN|lQW0GQR1XS
SF126 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDRb2RwUUN3ME2zMlMyOTd2IN88US=> M4[4THNCVkeHUh?=
LC-2-ad MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\JOWFKSzVyPUOuOVU4KM7:TR?= MX\TRW5ITVJ?
KNS-42 M4nSOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;ENXdKSzVyPUOuOlUh|ryP M13DRnNCVkeHUh?=
OVCAR-4 MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTNwN{O0N|Mh|ryP M4\xSnNCVkeHUh?=
PF-382 M1PiWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXL[nJKSzVyPUOuPFM3QThizszN NFSwe|RUSU6JRWK=
SH-4 NUjFeIJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlT0TWM2OD12LkK1NlU6KM7:TR?= M4fSenNCVkeHUh?=
KM12 M4XOeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILUbFNKSzVyPUSuN|I1OTZizszN MoOwV2FPT0WU
NB5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPDTWM2OD12LkSxPFY1KM7:TR?= M3;FOnNCVkeHUh?=
KURAMOCHI MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3IepJKSzVyPUSuOlUzPTZizszN NFjj[FdUSU6JRWK=
Becker MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTRwNk[0NVYh|ryP MlXkV2FPT0WU
MV-4-11 NF7WcYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLLZnJKSzVyPUSuPFE{PDRizszN MorYV2FPT0WU
KINGS-1 MkLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe2bIFUUUN3ME20MlgzOzd|IN88US=> NFjMfFFUSU6JRWK=
LS-123 MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTVwNEm2PFQh|ryP NGTpRWdUSU6JRWK=
SF268 NVvROnE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDsZoY5UUN3ME21MlYyOjZ{IN88US=> NFHFO5dUSU6JRWK=
A388 Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvqTWM2OD13Lk[zOlY4KM7:TR?= Ml60V2FPT0WU
NMC-G1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\wOVZKUUN3ME22MlAyQDFzIN88US=> NGexPY5USU6JRWK=
CGTH-W-1 M33EdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPnTWM2OD14LkCyNFc2KM7:TR?= Mn\mV2FPT0WU
ES4 NHnYSoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTJTWM2OD14LkWzNFc1KM7:TR?= M37UNXNCVkeHUh?=
SR NX7ocYRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELQTZdKSzVyPU[uOVg5ODdizszN M2nwcXNCVkeHUh?=
BB49-HNC NWfGeWx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG2TWM2OD14LkezNlA3KM7:TR?= MkXIV2FPT0WU
KLE NGDnRVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXPbJMxUUN3ME22Mlc5Ozd5IN88US=> M4LlN3NCVkeHUh?=
HUTU-80 M{e2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn6xTWM2OD14Lkm4OFY3KM7:TR?= NVT3Z4FrW0GQR1XS
SNU-C2B MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3STWM2OD15LkiyO|M4KM7:TR?= M1fvVXNCVkeHUh?=
BB65-RCC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELh[npKSzVyPUeuPVQ6ODRizszN M3TXTHNCVkeHUh?=
QIMR-WIL M1fndmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\FTWM2OD16LkSyPFA5KM7:TR?= NV3jTFdYW0GQR1XS
GDM-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XMdGlEPTB;OD65O|I6OiEQvF2= NYrxeYRHW0GQR1XS
LC4-1 NY\IUpZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUW4b3ppUUN3ME25MlAxQTFzIN88US=> NX\G[JloW0GQR1XS
MLMA M4D2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDpTWM2OD17LkG1NFA3KM7:TR?= MojCV2FPT0WU
EoL-1-cell NGjUR4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;wTWM2OD17LkOwNVkzKM7:TR?= Mk\0V2FPT0WU
BOKU NFXLTFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HXTmlEPTB;OT65OlQ3PiEQvF2= NHu3[ZNUSU6JRWK=
EVSA-T NYLRcpczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrrUllKSzVyPUGwMlY2PjhizszN NEGzdoRUSU6JRWK=
D-283MED MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33zUGlEPTB;MUCuPVE4PiEQvF2= M4ex[3NCVkeHUh?=
NB1 M3nDXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrxXpZKSzVyPUGxMlAzPDJizszN M4HwbnNCVkeHUh?=
RPMI-8402 NWjRcGNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TBbmlEPTB;MUGuNVc5KM7:TR?= M{Tv[XNCVkeHUh?=
NCI-H1355 MoOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnvWXVsUUN3ME2xNU4yQDB4IN88US=> M1\OTHNCVkeHUh?=
NB7 NHzQNFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTFzLkOyPVch|ryP M3viOXNCVkeHUh?=
RPMI-6666 NVn0RoNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHWxTGRKSzVyPUGyMlk2PjdizszN MoDGV2FPT0WU
697 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF|LkK3NFEh|ryP NV;i[mZbW0GQR1XS
CTB-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4mxOWlEPTB;MUOuOVk1QCEQvF2= NEPkb5NUSU6JRWK=
VA-ES-BJ NVHZbVVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrFXlFKSzVyPUGzMlkzOzRizszN MoDhV2FPT0WU
BE-13 NXTNfGF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTF2LkO5NVUh|ryP NX[0S4F3W0GQR1XS
SKM-1 M{\ONGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLTdFFKSzVyPUG0MlQ1QTlizszN MWLTRW5ITVJ?
TE-6 NXXFOmRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkH6TWM2OD1zND63OVkyKM7:TR?= MmXOV2FPT0WU
LB771-HNC M2i1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTF2Lke4PVgh|ryP MV\TRW5ITVJ?
ECC4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW3fotKSzVyPUG3MlAzPzdizszN NX;CdGVDW0GQR1XS
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LB647-SCLC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTF5LkS5OFkh|ryP MmTOV2FPT0WU
NB10 MkPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHJUGZKSzVyPUG4MlUzPTZizszN NVrJOFNnW0GQR1XS
L-540 NXrDWpJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHVTWM2OD1zOD64NVA6KM7:TR?= M3LiOHNCVkeHUh?=
NCI-H2126 MmTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDv[Hk3UUN3ME2xPU42OSEQvF2= MXHTRW5ITVJ?
HH NGe2bYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jvbGlEPTB;MkCuNFA6QSEQvF2= NX34NoVNW0GQR1XS
MPP-89 MknZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTJ|LkKyPFkh|ryP NWXTepFqW0GQR1XS
IST-MEL1 MkLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJ|Lki2OVgh|ryP NUi4N411W0GQR1XS
KP-N-YS NYPYXldUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\EcFk5UUN3ME2yN{46OjV3IN88US=> MlPkV2FPT0WU
EC-GI-10 MnfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPW[YxbUUN3ME2yOE42QTh7IN88US=> MWrTRW5ITVJ?
EKVX NYjmPYxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS3TWM2OD1{Nj6wNlA{KM7:TR?= NUnvb45WW0GQR1XS
TGBC1TKB MoC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTwTWM2OD1{Nj60N|Qh|ryP Mn7uV2FPT0WU
Daudi NFLxZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfYbIF5UUN3ME2yO{4xPzd|IN88US=> NGXPfVRUSU6JRWK=
ALL-PO MlexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\RWG9LUUN3ME2yO{4xQDFizszN MoHHV2FPT0WU
NB6 NX3kOldoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jMbWlEPTB;MkeuOFg5KM7:TR?= NHfCc|dUSU6JRWK=
ES6 NXnsd5E3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rO[2lEPTB;MkeuPVEzOyEQvF2= M1jub3NCVkeHUh?=
COLO-320-HSR NF\GeoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTJ6LkCzO|Mh|ryP M{fMSXNCVkeHUh?=
K5 M{TkU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3mO5lvUUN3ME2yPE4yOjh5IN88US=> MnPQV2FPT0WU
ES1 M33XXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULKc5FQUUN3ME2yPE44Pzd|IN88US=> MoG1V2FPT0WU
LC-1F MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTsTWM2OD1{OT63N|Q3KM7:TR?= NHzBSYRUSU6JRWK=
SCLC-21H MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLCSW5HUUN3ME2zNE44OzF5IN88US=> MnzpV2FPT0WU
SK-PN-DW NFTkOXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzVTYhrUUN3ME2zNk42PTl6IN88US=> NW\QWol2W0GQR1XS
D-247MG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjSTWM2OD1|Mj65O|c{KM7:TR?= MVXTRW5ITVJ?
TE-5 M1v6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjiNVNEUUN3ME2zN{4xOzZ{IN88US=> NYXxOIRzW0GQR1XS
MONO-MAC-6 M{HmOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTN|LkWwOFgh|ryP M33sVnNCVkeHUh?=
LB2518-MEL MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN|Lke2OlYh|ryP M1nwT3NCVkeHUh?=
LOXIMVI M361NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljaTWM2OD1|Mz63PVI5KM7:TR?= MnTtV2FPT0WU
NCI-H209 MmPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HrNWlEPTB;M{WuNVQ1KM7:TR?= MV;TRW5ITVJ?
A253 Ml3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVK4SVRkUUN3ME2zOU44PDJ7IN88US=> M{TLS3NCVkeHUh?=
HCC1599 NIfyTVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PPVmlEPTB;M{[uO|A2OyEQvF2= MY\TRW5ITVJ?
EB-3 MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPXTWM2OD1|Nj65OVE5KM7:TR?= NYLq[Ys6W0GQR1XS
GOTO NWHPO|dmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DEeGlEPTB;M{euN|IzPCEQvF2= MlTCV2FPT0WU
SW684 MoW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr2TWM2OD12MT64OFk2KM7:TR?= NH;wZYpUSU6JRWK=
DEL NULoSmVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHPVIRLUUN3ME20Nk4xPTJ{IN88US=> M3rzdnNCVkeHUh?=
HT-144 NYP5UFJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTR{LkG2O|Yh|ryP MlT2V2FPT0WU
TE-9 M1P2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17JRWlEPTB;NEOuOFU6PiEQvF2= NIfNVodUSU6JRWK=
KARPAS-45 NWD2RXZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTR2LkO5NlUh|ryP MYHTRW5ITVJ?
HAL-01 MljjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3uyb2lEPTB;NESuOVA{PCEQvF2= NYnwUWMyW0GQR1XS
RCC10RGB NYnkUIFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWD1NlhoUUN3ME20OE44Ozl{IN88US=> MnzlV2FPT0WU
CP67-MEL NVXTZpk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHYRZJMUUN3ME20OU43OjRzIN88US=> NELTd5hUSU6JRWK=
NB17 M1z1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon6TWM2OD12NT62OlQ{KM7:TR?= M4naZnNCVkeHUh?=
SK-UT-1 Ml:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\3NlZ1UUN3ME20OU46PDZ2IN88US=> Ml3vV2FPT0WU
JiyoyeP-2003 NV\TVGN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r1SWlEPTB;NE[uNFEyQSEQvF2= NVXoWVdvW0GQR1XS
HCE-4 NX\scm1xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfle2VxUUN3ME20Ok42QTZ6IN88US=> M4DHTHNCVkeHUh?=
NCI-H720 Mn3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHGfFRKSzVyPUS2Mlc3QDJizszN NGTjUndUSU6JRWK=
KARPAS-422 MnvsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX4TWM2OD12Nz6wPFk2KM7:TR?= MlfiV2FPT0WU
Ramos-2G6-4C10 NHfxNY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnu1TWM2OD12Nz6xOlIzKM7:TR?= MWjTRW5ITVJ?
HCE-T NFXjS5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPN[poxUUN3ME20O{43QDJ6IN88US=> MnzyV2FPT0WU
PSN1 M33nOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LmdmlEPTB;NEeuO|gyOyEQvF2= NXjReolkW0GQR1XS

... 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)

  • Mass
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    Volume
    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):
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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
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