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 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.

  • 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 M4G0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHYTWM2OD1yLkC2NVQ{KM7:TR?= MXLTRW5ITVJ?
LAMA-84 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHFNlRKSzVyPUCuNVU6QSEQvF2= NV;idFM3W0GQR1XS
MEG-01 MmHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rxeGlEPTB;MD6yN|Y5QCEQvF2= MVjTRW5ITVJ?
EM-2 NF3zW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXy[WxKSzVyPUCuNlY2KM7:TR?= MkHaV2FPT0WU
TE-15 M{j4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn2TotKSzVyPUCuNlc1OTJizszN MUHTRW5ITVJ?
NCI-H1648 Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLVTWM2OD1yLkK4NVE3KM7:TR?= NIjycWNUSU6JRWK=
TE-12 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoO2TWM2OD1yLkOyOlgh|ryP NWfZNGduW0GQR1XS
LB996-RCC MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkC3TWM2OD1yLkS0NVk3KM7:TR?= MWHTRW5ITVJ?
K-562 NGD5UW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnseHhKSzVyPUCuOFQ6PjdizszN MXvTRW5ITVJ?
D-336MG M1LIU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjQV4JKSzVyPUCuOVA{ODRizszN NEDOWoRUSU6JRWK=
NOS-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTBwNkC1Nlkh|ryP MVrTRW5ITVJ?
EW-24 NITDcoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLMO|lnUUN3ME2wMlYzPjl|IN88US=> MVXTRW5ITVJ?
BV-173 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDDc|lKSzVyPUCuOlUzPDlizszN MVPTRW5ITVJ?
NCCIT NEHyW5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjMTWM2OD1yLkezNlE5KM7:TR?= MWLTRW5ITVJ?
NCI-H1436 NEjqUJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nKVGlEPTB;MD63PVA1QSEQvF2= M4izN3NCVkeHUh?=
BB30-HNC MkK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLHW4RKSzVyPUCuPFYzODNizszN NXPiS|JLW0GQR1XS
TE-8 NEniRpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7WSXZKSzVyPUCuPFczPzVizszN NIDhemxUSU6JRWK=
A704 NEjxVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXrR3ZIUUN3ME2wMlg6OjFizszN MXvTRW5ITVJ?
TK10 Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXi0fG5VUUN3ME2wMlkxPjZ7IN88US=> NYrDdm9[W0GQR1XS
KS-1 NEDaSIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFwMUm3O|kh|ryP MoDiV2FPT0WU
C2BBe1 NFrL[JFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDTVppKSzVyPUGuNlA2ODdizszN M2TXcnNCVkeHUh?=
RXF393 NUDJO5RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwMkSzOkDPxE1? MYjTRW5ITVJ?
KGN MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MormTWM2OD1zLkK3Olg4KM7:TR?= NVH0cFJ7W0GQR1XS
NB69 M{nBTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfnbJlKSzVyPUGuN|c1QTdizszN NFfOfphUSU6JRWK=
TE-11 M4G3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT6d4ZKSzVyPUGuOFM1OThizszN NVHMeIRjW0GQR1XS
TE-1 MmfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL3dnlJUUN3ME2xMlQ1OTB3IN88US=> MlLRV2FPT0WU
ST486 M{PJOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXH3XJM4UUN3ME2xMlQ2QDV{IN88US=> M2\GUHNCVkeHUh?=
HOP-62 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr2TWM2OD1zLkWwNlQ3KM7:TR?= NH;CUFdUSU6JRWK=
EW-16 M4fWVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLVbWlKSzVyPUGuOVUxQDNizszN NYHs[5VEW0GQR1XS
LB1047-RCC M1;oUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIiwe29KSzVyPUGuOVU1PTNizszN NYXlUnVsW0GQR1XS
TE-10 NV3vR2o3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln3TWM2OD1zLk[2NlUzKM7:TR?= MXLTRW5ITVJ?
RL95-2 M1ftcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXq2OVd6UUN3ME2xMlY3QTB{IN88US=> NFHDb4dUSU6JRWK=
DOHH-2 MmfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFwN{G3PFIh|ryP MXfTRW5ITVJ?
MFH-ino MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC4SG5KSzVyPUGuO|c5PyEQvF2= NV2wZ2t{W0GQR1XS
GB-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrrTWM2OD1zLke5PFM{KM7:TR?= M1z6VnNCVkeHUh?=
SK-N-DZ NHvDVYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwOES2PFgh|ryP NF31W3dUSU6JRWK=
OS-RC-2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\GTIVKSzVyPUGuPFg2PzRizszN MofCV2FPT0WU
SW982 M1vzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHhOW1KSzVyPUGuPVIxQTNizszN MnzmV2FPT0WU
KALS-1 Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTFwOUi3NlIh|ryP NVm3bppYW0GQR1XS
TGBC24TKB MlXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTJwMEW5OVgh|ryP NYfwNnk4W0GQR1XS
GI-1 MkjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\XVXM{UUN3ME2yMlE3ODh2IN88US=> NEfCXY5USU6JRWK=
SW962 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3L6cWlEPTB;Mj6xO|E4QCEQvF2= MWTTRW5ITVJ?
SW872 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHsTWNKSzVyPUKuNVg2ODdizszN MX3TRW5ITVJ?
NCI-H747 MkfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTJwMkW3NVQh|ryP NFTtfGZUSU6JRWK=
MZ1-PC MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rVSGlEPTB;Mj6yPVM2PiEQvF2= MkP4V2FPT0WU
MSTO-211H M{LMd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXhdndKSzVyPUKuN|U4OjNizszN M2P3N3NCVkeHUh?=
BL-70 M4nYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rQ[GlEPTB;Mj60O|QzOiEQvF2= NV3MNXNRW0GQR1XS
SW954 MmDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e5bWlEPTB;Mj61O|QxQCEQvF2= NEn4OIpUSU6JRWK=
SNB75 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPReZBLUUN3ME2yMlY5PTl2IN88US=> NFHOXGZUSU6JRWK=
IST-SL2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrKbGNKSzVyPUKuO|I{PzlizszN M{DuN3NCVkeHUh?=
GCIY M1PWeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3XdJhWUUN3ME2yMlg4ODB3IN88US=> NV\ZNGdoW0GQR1XS
KU812 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\TdpVtUUN3ME2zMlA2Ojl7IN88US=> MVzTRW5ITVJ?
LXF-289 NYe4VYtjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTNwMUKxNFkh|ryP MYrTRW5ITVJ?
ETK-1 Ml;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2P4b2lEPTB;Mz6yNFc3PyEQvF2= NE\UdIlUSU6JRWK=
SF126 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTNwM{GxO|Qh|ryP M1\Ie3NCVkeHUh?=
LC-2-ad NX7zXIc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7B[2hKSzVyPUOuOVU4KM7:TR?= MV\TRW5ITVJ?
KNS-42 M{Hwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNwNkWg{txO M4nMN3NCVkeHUh?=
OVCAR-4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTNwN{O0N|Mh|ryP M2Hh[nNCVkeHUh?=
PF-382 MkXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTNwOEO2PVgh|ryP M2ToUHNCVkeHUh?=
SH-4 NXvFfWRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfnS2pzUUN3ME20MlI2OjV7IN88US=> M3jwOnNCVkeHUh?=
KM12 M3K5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFWyc|ZKSzVyPUSuN|I1OTZizszN NFq0R3BUSU6JRWK=
NB5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTRwNEG4OlQh|ryP MoH5V2FPT0WU
KURAMOCHI NEi3Zm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvzeGFKSzVyPUSuOlUzPTZizszN MV7TRW5ITVJ?
Becker Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17sZmlEPTB;ND62OlQyPiEQvF2= NX3DOo1nW0GQR1XS
MV-4-11 M4\TNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3zTWM2OD12LkixN|Q1KM7:TR?= M1LvVHNCVkeHUh?=
KINGS-1 NYP6OlU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTMTWM2OD12LkiyN|c{KM7:TR?= NXiz[HBCW0GQR1XS
LS-123 NGPofnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\ETWM2OD13LkS5Olg1KM7:TR?= NIXwS5JUSU6JRWK=
SF268 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;IOGlEPTB;NT62NVI3OiEQvF2= NH7KcFJUSU6JRWK=
A388 NXHRXXRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTVwNkO2Olch|ryP MVPTRW5ITVJ?
NMC-G1 M{\INWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTPe4ZKSzVyPU[uNFE5OTFizszN MUPTRW5ITVJ?
CGTH-W-1 NHqzXVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm2TWM2OD14LkCyNFc2KM7:TR?= NX;RcZM4W0GQR1XS
ES4 NXLM[4hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTZwNUOwO|Qh|ryP MnjxV2FPT0WU
SR MlzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HVWGlEPTB;Nj61PFgxPyEQvF2= MVHTRW5ITVJ?
BB49-HNC NIfxOVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn65TWM2OD14LkezNlA3KM7:TR?= NFS2em5USU6JRWK=
KLE MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:3NIVKSzVyPU[uO|g{PzdizszN NEnLe|FUSU6JRWK=
HUTU-80 NFH1T3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXkbmN1UUN3ME22Mlk5PDZ4IN88US=> M17WbHNCVkeHUh?=
SNU-C2B NXLKNlE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTre|dKSzVyPUeuPFI4OzdizszN M1frRnNCVkeHUh?=
BB65-RCC MnTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPYTWM2OD15Lkm0PVA1KM7:TR?= NGXFdXRUSU6JRWK=
QIMR-WIL NXfjdIRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P1Z2lEPTB;OD60NlgxQCEQvF2= MlzHV2FPT0WU
GDM-1 NHzQb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfjTWM2OD16Lkm3NlkzKM7:TR?= MmjYV2FPT0WU
LC4-1 M3rzVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;4W49YUUN3ME25MlAxQTFzIN88US=> NITwSZRUSU6JRWK=
MLMA MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTlwMUWwNFYh|ryP M4D2[nNCVkeHUh?=
EoL-1-cell NWnIUXZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTlwM{CxPVIh|ryP MVHTRW5ITVJ?
BOKU M{Didmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzCTWM2OD17Lkm2OFY3KM7:TR?= NFrhWmxUSU6JRWK=
EVSA-T M{TUcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fsNWlEPTB;MUCuOlU3QCEQvF2= NF3xWY9USU6JRWK=
D-283MED MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nKbmlEPTB;MUCuPVE4PiEQvF2= MlrVV2FPT0WU
NB1 NFH3WodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPWT5JKSzVyPUGxMlAzPDJizszN NHPLTXVUSU6JRWK=
RPMI-8402 NHHqfWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mni1TWM2OD1zMT6xO|gh|ryP NVm3UYNCW0GQR1XS
NCI-H1355 Mm\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPvbIFTUUN3ME2xNU4yQDB4IN88US=> MVvTRW5ITVJ?
NB7 M1nPRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Gw[2lEPTB;MUGuN|I6PyEQvF2= NYLEOFNyW0GQR1XS
RPMI-6666 Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH5dGNKSzVyPUGyMlk2PjdizszN MXHTRW5ITVJ?
697 NFOxNW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorlTWM2OD1zMz6yO|AyKM7:TR?= M4fVeXNCVkeHUh?=
CTB-1 MoXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLiTWM2OD1zMz61PVQ5KM7:TR?= MlPmV2FPT0WU
VA-ES-BJ M33Ocmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF|LkmyN|Qh|ryP NV3uUmhOW0GQR1XS
BE-13 Mki1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGC4TGNKSzVyPUG0MlM6OTVizszN NVXhWGZ1W0GQR1XS
SKM-1 NUPs[3RTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnWyTWM2OD1zND60OFk6KM7:TR?= MXPTRW5ITVJ?
TE-6 MluzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDjc29KUUN3ME2xOE44PTlzIN88US=> NXKwRnM4W0GQR1XS
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EKVX MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\YTWM2OD1{Nj6wNlA{KM7:TR?= NUPF[ZlXW0GQR1XS
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ES6 Mn\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HxOGlEPTB;MkeuPVEzOyEQvF2= NVjTcFZJW0GQR1XS
COLO-320-HSR NV3VbYdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTJ6LkCzO|Mh|ryP M{T0XXNCVkeHUh?=
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LC-1F M{\TWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXXPGN1UUN3ME2yPU44OzR4IN88US=> NXTPbnFMW0GQR1XS
SCLC-21H MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLLTWM2OD1|MD63N|E4KM7:TR?= NH;ZVVJUSU6JRWK=
SK-PN-DW Mor4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzw[HhKSzVyPUOyMlU2QThizszN M2WwbXNCVkeHUh?=
D-247MG MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHOyT4hKSzVyPUOyMlk4PzNizszN NELnPHJUSU6JRWK=
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LOXIMVI NVPjdVJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\5cJdKSzVyPUOzMlc6OjhizszN MVLTRW5ITVJ?
NCI-H209 NFjSe2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\hNmlEPTB;M{WuNVQ1KM7:TR?= NH3WSZRUSU6JRWK=
A253 Mk\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTN3Lke0Nlkh|ryP M4TLcXNCVkeHUh?=
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EB-3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTN4Lkm1NVgh|ryP NFviNnFUSU6JRWK=
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SW684 NF7Y[mFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTRzLki0PVUh|ryP M1rXOnNCVkeHUh?=
DEL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nEdmlEPTB;NEKuNFUzOiEQvF2= NF23N5lUSU6JRWK=
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HCE-4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\oTWM2OD12Nj61PVY5KM7:TR?= MVjTRW5ITVJ?
NCI-H720 Mo\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTR4Lke2PFIh|ryP MVPTRW5ITVJ?
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HCE-T NH31W2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTR5Lk[4Nlgh|ryP Mnm1V2FPT0WU
PSN1 NXHZNmRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj0XYdZUUN3ME20O{44QDF|IN88US=> NFK3bYxUSU6JRWK=

... 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 )

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

The Serial Dilution Calculator Equation

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  • Computed Result

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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

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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 December 1 2018 Early Phase 1
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
NCT02732587 Completed Alcohol Drinking Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) November 2015 Phase 1
NCT02167256 Completed Alzheimer''s Disease Yale University|Alzheimer''s Therapeutic Research Institute December 2014 Phase 2
NCT02262026 Recruiting Alcoholism Yale University November 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

Src Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID