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 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwME[xOFMh|ryP NFLuW4RUSU6JRWK=
LAMA-84 NWHQZ2pOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[2cWlEPTB;MD6xOVk6KM7:TR?= NIHJeXZUSU6JRWK=
MEG-01 MnHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHzTWM2OD1yLkKzOlg5KM7:TR?= NVK3UIlCW0GQR1XS
EM-2 NH\zclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLOTWM2OD1yLkK2OUDPxE1? NGrVRZBUSU6JRWK=
TE-15 MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwMke0NVIh|ryP NHX0Rm9USU6JRWK=
NCI-H1648 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwMkixNVYh|ryP NXfrdmo4W0GQR1XS
TE-12 NFnwWWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3yzbGlEPTB;MD6zNlY5KM7:TR?= NH\ZWopUSU6JRWK=
LB996-RCC NFW2OZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\IOWlEPTB;MD60OFE6PiEQvF2= M3nsTXNCVkeHUh?=
K-562 M4PTNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXaTndKSzVyPUCuOFQ6PjdizszN M2LxTHNCVkeHUh?=
D-336MG MmHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwNUCzNFQh|ryP M3\4XnNCVkeHUh?=
NOS-1 M{O2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwNkC1Nlkh|ryP NE\3ZVRUSU6JRWK=
EW-24 MmL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjxTWM2OD1yLk[yOlk{KM7:TR?= MkXHV2FPT0WU
BV-173 NFjDbI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXUb41KSzVyPUCuOlUzPDlizszN NXXkcY5kW0GQR1XS
NCCIT MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjMWlZKSzVyPUCuO|MzOThizszN MYfTRW5ITVJ?
NCI-H1436 NVfZUmdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH1UphKSzVyPUCuO|kxPDlizszN MlPFV2FPT0WU
BB30-HNC NYj6WINmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjJUFdVUUN3ME2wMlg3OjB|IN88US=> NYrH[|hTW0GQR1XS
TE-8 NULv[lcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7sT5JKSzVyPUCuPFczPzVizszN M4fE[HNCVkeHUh?=
A704 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\ZTWM2OD1yLki5NlEh|ryP NIjacm9USU6JRWK=
TK10 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\JTWM2OD1yLkmwOlY6KM7:TR?= NGT5RVVUSU6JRWK=
KS-1 M1m2bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlP0TWM2OD1zLkG5O|c6KM7:TR?= NHi0PHFUSU6JRWK=
C2BBe1 NVTkVFdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFwMkC1NFch|ryP NGfaWnRUSU6JRWK=
RXF393 Ml[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mle3TWM2OD1zLkK0N|Yh|ryP MlPGV2FPT0WU
KGN NUTjPIhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPTTWM2OD1zLkK3Olg4KM7:TR?= Mkn4V2FPT0WU
NB69 NGjUTYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HtV2lEPTB;MT6zO|Q6PyEQvF2= M1HuV3NCVkeHUh?=
TE-11 NELOW3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLETWM2OD1zLkSzOFE5KM7:TR?= MUjTRW5ITVJ?
TE-1 NGn3cm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7IVWFKSzVyPUGuOFQyODVizszN MUjTRW5ITVJ?
ST486 M1i3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknyTWM2OD1zLkS1PFUzKM7:TR?= M2PHU3NCVkeHUh?=
HOP-62 M1XTcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTFwNUCyOFYh|ryP MkDJV2FPT0WU
EW-16 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTFwNUWwPFMh|ryP NF7sbo1USU6JRWK=
LB1047-RCC NVXoVnp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXvTWM2OD1zLkW1OFU{KM7:TR?= NU[0UlV[W0GQR1XS
TE-10 NFrDXHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvuTWM2OD1zLk[2NlUzKM7:TR?= M4Tyb3NCVkeHUh?=
RL95-2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlf5TWM2OD1zLk[2PVAzKM7:TR?= NHfS[ZdUSU6JRWK=
DOHH-2 Mn3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37QS2lEPTB;MT63NVc5OiEQvF2= NFT1eGNUSU6JRWK=
MFH-ino NIXiPHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjFTWM2OD1zLke3PFch|ryP NVTl[3NLW0GQR1XS
GB-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXX[5dDUUN3ME2xMlc6QDN|IN88US=> MVTTRW5ITVJ?
SK-N-DZ NFm2[npIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\UTIdrUUN3ME2xMlg1Pjh6IN88US=> M3G0ZXNCVkeHUh?=
OS-RC-2 MkG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{eycWlEPTB;MT64PFU4PCEQvF2= NV;sNppMW0GQR1XS
SW982 M3LwWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHjVY5VUUN3ME2xMlkzODl|IN88US=> M{DMR3NCVkeHUh?=
KALS-1 M4HHOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELuNmJKSzVyPUGuPVg4OjJizszN NHTwU3BUSU6JRWK=
TGBC24TKB NWS4Xm81T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3y2VGlEPTB;Mj6wOVk2QCEQvF2= M1jzVHNCVkeHUh?=
GI-1 M4H6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHzeJpbUUN3ME2yMlE3ODh2IN88US=> NETx[WFUSU6JRWK=
SW962 NGLpcGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTJwMUexO|gh|ryP NFjvXoRUSU6JRWK=
SW872 NVjHb|NtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTJwMUi1NFch|ryP NI\IOGtUSU6JRWK=
NCI-H747 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7xV3lKSzVyPUKuNlU4OTRizszN NWqwVVBEW0GQR1XS
MZ1-PC M1jhRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Hsc2lEPTB;Mj6yPVM2PiEQvF2= Mny0V2FPT0WU
MSTO-211H MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlGxTWM2OD1{LkO1O|I{KM7:TR?= NVfSSlBxW0GQR1XS
BL-70 M2HxdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJwNEe0NlIh|ryP M13lPHNCVkeHUh?=
SW954 NYfMR3dRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\RTWM2OD1{LkW3OFA5KM7:TR?= MXXTRW5ITVJ?
SNB75 NYXwVnI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjid4tKSzVyPUKuOlg2QTRizszN MlX2V2FPT0WU
IST-SL2 M37Sdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;WUYhKSzVyPUKuO|I{PzlizszN MnfPV2FPT0WU
GCIY MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\2dWlEPTB;Mj64O|AxPSEQvF2= NHrPeJlUSU6JRWK=
KU812 M2[2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M360TmlEPTB;Mz6wOVI6QSEQvF2= MXnTRW5ITVJ?
LXF-289 NH6z[3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{D5OGlEPTB;Mz6xNlExQSEQvF2= NIrnNGhUSU6JRWK=
ETK-1 M17Ob2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnVcWVJUUN3ME2zMlIxPzZ5IN88US=> MUPTRW5ITVJ?
SF126 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPydW5KSzVyPUOuN|EyPzRizszN MXPTRW5ITVJ?
LC-2-ad NUXW[5NsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXIUIdKSzVyPUOuOVU4KM7:TR?= MVfTRW5ITVJ?
KNS-42 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTGTWM2OD1|Lk[1JO69VQ>? MVLTRW5ITVJ?
OVCAR-4 M1:xVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnpTWM2OD1|LkezOFM{KM7:TR?= NX2yUWJ1W0GQR1XS
PF-382 M4rBfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TZW2lEPTB;Mz64N|Y6QCEQvF2= M{f1OXNCVkeHUh?=
SH-4 NEnnOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTRwMkWyOVkh|ryP NUT2bnljW0GQR1XS
KM12 NEHLcXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH33RmtKSzVyPUSuN|I1OTZizszN MU\TRW5ITVJ?
NB5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfNdXJKSzVyPUSuOFE5PjRizszN NGnuNm1USU6JRWK=
KURAMOCHI MoCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfDTWM2OD12Lk[1NlU3KM7:TR?= NWLFTYVxW0GQR1XS
Becker NFKzZZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjnOYxKSzVyPUSuOlY1OTZizszN NF\oemVUSU6JRWK=
MV-4-11 MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPoSoZKSzVyPUSuPFE{PDRizszN NWPyZ4RUW0GQR1XS
KINGS-1 M1;Ld2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;Jbpc{UUN3ME20MlgzOzd|IN88US=> MXzTRW5ITVJ?
LS-123 Mkm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDJVmpKSzVyPUWuOFk3QDRizszN M{\zVHNCVkeHUh?=
SF268 M4nyd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVWxUmh4UUN3ME21MlYyOjZ{IN88US=> MnHTV2FPT0WU
A388 M2rDU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjzco9KSzVyPUWuOlM3PjdizszN M2Xn[HNCVkeHUh?=
NMC-G1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTZwMEG4NVEh|ryP MmjDV2FPT0WU
CGTH-W-1 M1yycWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1KwWGlEPTB;Nj6wNlA4PSEQvF2= NHPQNJdUSU6JRWK=
ES4 M2m5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTZwNUOwO|Qh|ryP MVHTRW5ITVJ?
SR NWf4bYRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3wU3pKSzVyPU[uOVg5ODdizszN MkHDV2FPT0WU
BB49-HNC NIDsPVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXzSnpiUUN3ME22Mlc{OjB4IN88US=> MmfmV2FPT0WU
KLE NGXDc4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P5WmlEPTB;Nj63PFM4PyEQvF2= NEHmd4VUSU6JRWK=
HUTU-80 M4nmcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1y5UmlEPTB;Nj65PFQ3PiEQvF2= MnfsV2FPT0WU
SNU-C2B MmHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzUd|dKSzVyPUeuPFI4OzdizszN NIKybWlUSU6JRWK=
BB65-RCC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTdwOUS5NFQh|ryP MXrTRW5ITVJ?
QIMR-WIL MkTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvlfnVKSzVyPUiuOFI5ODhizszN NVSyRXF6W0GQR1XS
GDM-1 NYXZc|lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRThwOUeyPVIh|ryP MXLTRW5ITVJ?
LC4-1 M{HkUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTlwMEC5NVEh|ryP MUPTRW5ITVJ?
MLMA MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nybmlEPTB;OT6xOVAxPiEQvF2= MYHTRW5ITVJ?
EoL-1-cell NFHYUGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\xeWdvUUN3ME25MlMxOTl{IN88US=> M{DOU3NCVkeHUh?=
BOKU NYP0T|RUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X6e2lEPTB;OT65OlQ3PiEQvF2= NHSyfXVUSU6JRWK=
EVSA-T NXPQN5lUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTFyLk[1Olgh|ryP NEHFeWJUSU6JRWK=
D-283MED MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjXT29wUUN3ME2xNE46OTd4IN88US=> MnzFV2FPT0WU
NB1 MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXJWlExUUN3ME2xNU4xOjR{IN88US=> M2XoO3NCVkeHUh?=
RPMI-8402 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvCVpI5UUN3ME2xNU4yPzhizszN NGXBPY1USU6JRWK=
NCI-H1355 M4CzZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfSTVZKUUN3ME2xNU4yQDB4IN88US=> M2LyWXNCVkeHUh?=
NB7 MmnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHER2lKSzVyPUGxMlMzQTdizszN MWPTRW5ITVJ?
RPMI-6666 NXP1Wo9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PNcGlEPTB;MUKuPVU3PyEQvF2= MVLTRW5ITVJ?
697 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF|LkK3NFEh|ryP NFrTUFlUSU6JRWK=
CTB-1 NVHCdIxRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni4TWM2OD1zMz61PVQ5KM7:TR?= NV7xS3ljW0GQR1XS
VA-ES-BJ Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfuZ4VPUUN3ME2xN{46OjN2IN88US=> NWnBZXFOW0GQR1XS
BE-13 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M16xXmlEPTB;MUSuN|kyPSEQvF2= NWq5dG93W0GQR1XS
SKM-1 M3fRSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHDTWtKSzVyPUG0MlQ1QTlizszN MoP0V2FPT0WU
TE-6 NXfzRVBvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvTTWM2OD1zND63OVkyKM7:TR?= MoHhV2FPT0WU
LB771-HNC NVy5W3UxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jKdWlEPTB;MUSuO|g6QCEQvF2= MVjTRW5ITVJ?
ECC4 NXj4N5kzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjqXlBKSzVyPUG3MlAzPzdizszN NFjWWHZUSU6JRWK=
ES3 NHOxTFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHvZVNLUUN3ME2xO{41PjV3IN88US=> MmLHV2FPT0WU
LB647-SCLC NYHhZ3BtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH2yNmJKSzVyPUG3MlQ6PDlizszN M1npbnNCVkeHUh?=
NB10 NIjwcJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK4c4pKSzVyPUG4MlUzPTZizszN NGC5SHdUSU6JRWK=
L-540 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[4UmlEPTB;MUiuPFExQSEQvF2= MmPMV2FPT0WU
NCI-H2126 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nvfmlEPTB;MUmuOVEh|ryP MmfaV2FPT0WU
HH MonvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[yUGlEPTB;MkCuNFA6QSEQvF2= M1nQR3NCVkeHUh?=
MPP-89 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nIeWlEPTB;MkOuNlI5QSEQvF2= NYe2eGlPW0GQR1XS
IST-MEL1 MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;zTWlEPTB;MkOuPFY2QCEQvF2= NE\hR4hUSU6JRWK=
KP-N-YS Ml\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILoS3NKSzVyPUKzMlkzPTVizszN Mlv4V2FPT0WU
EC-GI-10 M3HXTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILGeFdKSzVyPUK0MlU6QDlizszN MnH1V2FPT0WU
EKVX NV\PNZc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEOyNINKSzVyPUK2MlAzODNizszN MXzTRW5ITVJ?
TGBC1TKB Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjkR3VKSzVyPUK2MlQ{PCEQvF2= MYrTRW5ITVJ?
Daudi NH7ZXWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrvbZRKSzVyPUK3MlA4PzNizszN NVTI[po1W0GQR1XS
ALL-PO NYruV24yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PiXWlEPTB;MkeuNFgyKM7:TR?= MX7TRW5ITVJ?
NB6 NVvYc5dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPnc5pKSzVyPUK3MlQ5QCEQvF2= MWHTRW5ITVJ?
ES6 M1fWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrncpRKSzVyPUK3MlkyOjNizszN MkXKV2FPT0WU
COLO-320-HSR NUK0NHNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTJ6LkCzO|Mh|ryP NFntc4FUSU6JRWK=
K5 MorDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ridmlEPTB;MkiuNVI5PyEQvF2= MofwV2FPT0WU
ES1 MoHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ6Lke3O|Mh|ryP M3rHcHNCVkeHUh?=
LC-1F NIT3VWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzmTWM2OD1{OT63N|Q3KM7:TR?= MkLOV2FPT0WU
SCLC-21H M4XRSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTNyLkezNVch|ryP MoDHV2FPT0WU
SK-PN-DW M1nMSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TXcGlEPTB;M{KuOVU6QCEQvF2= Mo\IV2FPT0WU
D-247MG NXq2[3ZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\Le3hKSzVyPUOyMlk4PzNizszN MlT6V2FPT0WU
TE-5 M{XBSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3z5TWlEPTB;M{OuNFM3OiEQvF2= MVzTRW5ITVJ?
MONO-MAC-6 NWLHZYtET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4W5bWlEPTB;M{OuOVA1QCEQvF2= MkTZV2FPT0WU
LB2518-MEL Mnz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HkW2lEPTB;M{OuO|Y3PiEQvF2= M{OzVHNCVkeHUh?=
LOXIMVI NWjHRpIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XNeGlEPTB;M{OuO|kzQCEQvF2= NVSxTVcyW0GQR1XS
NCI-H209 NIjrfJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HhUGlEPTB;M{WuNVQ1KM7:TR?= NXGz[5dbW0GQR1XS
A253 MljSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj6SnVUUUN3ME2zOU44PDJ7IN88US=> MVPTRW5ITVJ?
HCC1599 Mnj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlznTWM2OD1|Nj63NFU{KM7:TR?= NEnvPVlUSU6JRWK=
EB-3 NILLN|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjsW4hxUUN3ME2zOk46PTF6IN88US=> M3HzeXNCVkeHUh?=
GOTO M4O0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPRflNKSzVyPUO3MlMzOjRizszN M1z5N3NCVkeHUh?=
SW684 MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TmUmlEPTB;NEGuPFQ6PSEQvF2= NY\lRmRDW0GQR1XS
DEL Mn\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;CbGZzUUN3ME20Nk4xPTJ{IN88US=> NVvtZ2Z3W0GQR1XS
HT-144 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXyc3ZUUUN3ME20Nk4yPjd4IN88US=> M362eHNCVkeHUh?=
TE-9 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTR|LkS1PVYh|ryP M2PBbXNCVkeHUh?=
KARPAS-45 MojsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXOTWM2OD12ND6zPVI2KM7:TR?= NYr3[opJW0GQR1XS
HAL-01 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfXV|RxUUN3ME20OE42ODN2IN88US=> MmrxV2FPT0WU
RCC10RGB MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmz[o9KSzVyPUS0Mlc{QTJizszN MX;TRW5ITVJ?
CP67-MEL NXW5fmM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jqOWlEPTB;NEWuOlI1OSEQvF2= NFLwSIVUSU6JRWK=
NB17 Ml7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjSNGM2UUN3ME20OU43PjR|IN88US=> Ml;EV2FPT0WU
SK-UT-1 NIe3OHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPkTWM2OD12NT65OFY1KM7:TR?= NEPaT4tUSU6JRWK=
JiyoyeP-2003 Mor6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTR4LkCxNVkh|ryP MV\TRW5ITVJ?
HCE-4 NEPPRlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTR4LkW5Olgh|ryP M2PqdXNCVkeHUh?=
NCI-H720 Mnq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTR4Lke2PFIh|ryP NH\Se|JUSU6JRWK=
KARPAS-422 NIHVN3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDyTWM2OD12Nz6wPFk2KM7:TR?= NH\YfWdUSU6JRWK=
Ramos-2G6-4C10 M{[4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHxfW1KSzVyPUS3MlE3OjJizszN MXrTRW5ITVJ?
HCE-T NUTVVoc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq5TWM2OD12Nz62PFI5KM7:TR?= Ml24V2FPT0WU
PSN1 NEDHSFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\nTWM2OD12Nz63PFE{KM7:TR?= M{DQSXNCVkeHUh?=

... 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 <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 542.03
Formula

C27H32ClN5O5

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

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

Dilution Calculator

Dilution Calculator

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

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

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

  • C1
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    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02955186 Not yet recruiting Alcohol Drinking Yale University January 2017 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Womens Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2
NCT02732587 Active, not recruiting Alcohol Drinking Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) November 2015 Phase 1
NCT02167256 Active, not recruiting Alzheimers Disease Yale University|Alzheimers Therapeutic Research Institute December 2014 Phase 2
NCT02262026 Recruiting Alcoholism Yale University November 2014 Phase 1
NCT02116712 Completed Pulmonary Lymphangioleiomyomatosis Tony Eissa|University of Texas|University of Cincinnati|Baylor College of Medicine August 2014 Phase 1

Tech Support

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

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID