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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NWK0SlJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIW1fZRKSzVyPUCuNFYyPDNizszN MUXTRW5ITVJ?
LAMA-84 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfzSo4xUUN3ME2wMlE2QTlizszN NEKzVo5USU6JRWK=
MEG-01 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjIWIFKSzVyPUCuNlM3QDhizszN MnvEV2FPT0WU
EM-2 NXnZUWc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkKxTWM2OD1yLkK2OUDPxE1? NWfyPFZGW0GQR1XS
TE-15 M{Xze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHxdlVFUUN3ME2wMlI4PDF{IN88US=> M4nYRXNCVkeHUh?=
NCI-H1648 NIewW5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwMkixNVYh|ryP NFiwSHpUSU6JRWK=
TE-12 NUCyOJNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfLdItyUUN3ME2wMlMzPjhizszN M3roRXNCVkeHUh?=
LB996-RCC MoHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvHTWM2OD1yLkS0NVk3KM7:TR?= MmW0V2FPT0WU
K-562 M2nOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnl[VdwUUN3ME2wMlQ1QTZ5IN88US=> MnLSV2FPT0WU
D-336MG Mnv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\YbZpKSzVyPUCuOVA{ODRizszN M2HlU3NCVkeHUh?=
NOS-1 M373eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zlSWlEPTB;MD62NFUzQSEQvF2= MoK0V2FPT0WU
EW-24 M{TRcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwNkK2PVMh|ryP M3rjTHNCVkeHUh?=
BV-173 NILyeZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTrdItKSzVyPUCuOlUzPDlizszN M1i0UXNCVkeHUh?=
NCCIT MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwN{OyNVgh|ryP NF;3W4JUSU6JRWK=
NCI-H1436 NUTwNnlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELGbWxKSzVyPUCuO|kxPDlizszN NIHnTYNUSU6JRWK=
BB30-HNC NFy0bIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwOE[yNFMh|ryP NWXuXWRWW0GQR1XS
TE-8 NHHOXmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfsR3lKSzVyPUCuPFczPzVizszN NEn5ZVJUSU6JRWK=
A704 MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwOEmyNUDPxE1? MXPTRW5ITVJ?
TK10 NXHnNo12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHkTWM2OD1yLkmwOlY6KM7:TR?= NYTudlVnW0GQR1XS
KS-1 MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTFwMUm3O|kh|ryP NV25SpFjW0GQR1XS
C2BBe1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLQTWM2OD1zLkKwOVA4KM7:TR?= NGXL[|NUSU6JRWK=
RXF393 M17pNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TpNWlEPTB;MT6yOFM3KM7:TR?= M2\JeXNCVkeHUh?=
KGN MkP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwMke2PFch|ryP NEXleVdUSU6JRWK=
NB69 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFwM{e0PVch|ryP MV;TRW5ITVJ?
TE-11 NXfZc4lDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFwNEO0NVgh|ryP MmrWV2FPT0WU
TE-1 NGrtT4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL4ZmhWUUN3ME2xMlQ1OTB3IN88US=> NX7GS3RZW0GQR1XS
ST486 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\We5dKSzVyPUGuOFU5PTJizszN MmW4V2FPT0WU
HOP-62 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nNW2lEPTB;MT61NFI1PiEQvF2= M1W4RnNCVkeHUh?=
EW-16 NXLndXdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLYOGNKSzVyPUGuOVUxQDNizszN NIn4RphUSU6JRWK=
LB1047-RCC M3rVfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\NOWlEPTB;MT61OVQ2OyEQvF2= NETVcZZUSU6JRWK=
TE-10 NGPXSWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2O3cmlEPTB;MT62OlI2OiEQvF2= M3LIfnNCVkeHUh?=
RL95-2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DrUGlEPTB;MT62OlkxOiEQvF2= NX7E[ld5W0GQR1XS
DOHH-2 NV7EdGlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7hTWM2OD1zLkexO|gzKM7:TR?= Mmn6V2FPT0WU
MFH-ino NX;jOmN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVriRYpwUUN3ME2xMlc4QDdizszN NGfk[ndUSU6JRWK=
GB-1 Mn7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rmV2lEPTB;MT63PVg{OyEQvF2= NYWweWhsW0GQR1XS
SK-N-DZ Ml\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rJRWlEPTB;MT64OFY5QCEQvF2= MW\TRW5ITVJ?
OS-RC-2 NIDOV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnVXnRKSzVyPUGuPFg2PzRizszN NVzoeFhpW0GQR1XS
SW982 NHrFbGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jTU2lEPTB;MT65NlA6OyEQvF2= M17EO3NCVkeHUh?=
KALS-1 NF76PYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYCxdJFzUUN3ME2xMlk5PzJ{IN88US=> NULQNYwxW0GQR1XS
TGBC24TKB MofSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknrTWM2OD1{LkC1PVU5KM7:TR?= Mn\OV2FPT0WU
GI-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\QPGlEPTB;Mj6xOlA5PCEQvF2= MWDTRW5ITVJ?
SW962 NVjFUG9lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJwMUexO|gh|ryP NInKUmdUSU6JRWK=
SW872 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTvTpNKSzVyPUKuNVg2ODdizszN M3LubHNCVkeHUh?=
NCI-H747 M{LRUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJwMkW3NVQh|ryP M{TMeXNCVkeHUh?=
MZ1-PC MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DSOGlEPTB;Mj6yPVM2PiEQvF2= NUjVfpg3W0GQR1XS
MSTO-211H NV\yTIJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\hbVVKSzVyPUKuN|U4OjNizszN MXjTRW5ITVJ?
BL-70 M2PteWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE[ycnhKSzVyPUKuOFc1OjJizszN Ml;CV2FPT0WU
SW954 M1G1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJwNUe0NFgh|ryP NWHEe4g5W0GQR1XS
SNB75 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K3V2lEPTB;Mj62PFU6PCEQvF2= NWfo[|N3W0GQR1XS
IST-SL2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXZTWM2OD1{LkeyN|c6KM7:TR?= MnHzV2FPT0WU
GCIY NVv2W2xjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknJTWM2OD1{Lki3NFA2KM7:TR?= MUfTRW5ITVJ?
KU812 MoK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\TZWxKSzVyPUOuNFUzQTlizszN NE\vPFRUSU6JRWK=
LXF-289 M{PUSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrKTWM2OD1|LkGyNVA6KM7:TR?= NF3ZNHFUSU6JRWK=
ETK-1 NYDpS|hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLnO3dKSzVyPUOuNlA4PjdizszN NET5WYNUSU6JRWK=
SF126 M2jMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIeyVGtKSzVyPUOuN|EyPzRizszN Mn[1V2FPT0WU
LC-2-ad NGDyWnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom2TWM2OD1|LkW1O{DPxE1? MVHTRW5ITVJ?
KNS-42 NUHMSohiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnXTWM2OD1|Lk[1JO69VQ>? NGnBNWNUSU6JRWK=
OVCAR-4 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MluyTWM2OD1|LkezOFM{KM7:TR?= M{HPSnNCVkeHUh?=
PF-382 MnjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn5RZdKSzVyPUOuPFM3QThizszN M1rJOXNCVkeHUh?=
SH-4 NFvmZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnIUpk1UUN3ME20MlI2OjV7IN88US=> MVvTRW5ITVJ?
KM12 NGm4NWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjDUodUUUN3ME20MlMzPDF4IN88US=> NVvKR|Q4W0GQR1XS
NB5 NFizU2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTRwNEG4OlQh|ryP MljVV2FPT0WU
KURAMOCHI NVHjflhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPYTWM2OD12Lk[1NlU3KM7:TR?= NXvhVYVIW0GQR1XS
Becker M3zZ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPsTWM2OD12Lk[2OFE3KM7:TR?= M2POfHNCVkeHUh?=
MV-4-11 NHrJXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTRwOEGzOFQh|ryP MV3TRW5ITVJ?
KINGS-1 MkDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPtTWM2OD12LkiyN|c{KM7:TR?= MkftV2FPT0WU
LS-123 M2\MTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzKTm1vUUN3ME21MlQ6Pjh2IN88US=> NU\O[Yw4W0GQR1XS
SF268 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTVwNkGyOlIh|ryP MVjTRW5ITVJ?
A388 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXUTY5KSzVyPUWuOlM3PjdizszN NEHodXZUSU6JRWK=
NMC-G1 M2fZdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXZeXRsUUN3ME22MlAyQDFzIN88US=> NGXqXGFUSU6JRWK=
CGTH-W-1 MkPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTZwMEKwO|Uh|ryP MkXSV2FPT0WU
ES4 NFrvPWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvzWXd3UUN3ME22MlU{ODd2IN88US=> M4nqU3NCVkeHUh?=
SR MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTxdXlWUUN3ME22MlU5QDB5IN88US=> NIf5dXNUSU6JRWK=
BB49-HNC MkmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrxXYZYUUN3ME22Mlc{OjB4IN88US=> NWDJVotYW0GQR1XS
KLE MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj2TWM2OD14Lke4N|c4KM7:TR?= NVTEbnUzW0GQR1XS
HUTU-80 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTZwOUi0OlYh|ryP NULpeZZZW0GQR1XS
SNU-C2B NVjwWINjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIW5cmVKSzVyPUeuPFI4OzdizszN NFzTcI9USU6JRWK=
BB65-RCC NYnvdWU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjiTWM2OD15Lkm0PVA1KM7:TR?= MnLzV2FPT0WU
QIMR-WIL Mn3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRThwNEK4NFgh|ryP NVuybGNFW0GQR1XS
GDM-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\zTWM2OD16Lkm3NlkzKM7:TR?= NYrENIkzW0GQR1XS
LC4-1 MlrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\jTWM2OD17LkCwPVEyKM7:TR?= M3zHUXNCVkeHUh?=
MLMA Ml3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn1S3poUUN3ME25MlE2ODB4IN88US=> MkfjV2FPT0WU
EoL-1-cell MkHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rY[2lEPTB;OT6zNFE6OiEQvF2= NY\rWmU6W0GQR1XS
BOKU Ml7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzpcopKSzVyPUmuPVY1PjZizszN MVLTRW5ITVJ?
EVSA-T M4XpdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfRO25lUUN3ME2xNE43PTZ6IN88US=> NFPNfIZUSU6JRWK=
D-283MED MnixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLRTmRKSzVyPUGwMlkyPzZizszN NXXZbYZtW0GQR1XS
NB1 NY\pW3JTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjMXFZKSzVyPUGxMlAzPDJizszN MkTLV2FPT0WU
RPMI-8402 M13S[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLFZpVYUUN3ME2xNU4yPzhizszN NEjwV5BUSU6JRWK=
NCI-H1355 Ml3jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHC[HBKSzVyPUGxMlE5ODZizszN M4\JVnNCVkeHUh?=
NB7 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTFzLkOyPVch|ryP NG\CPXVUSU6JRWK=
RPMI-6666 Mn;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTlXnZvUUN3ME2xNk46PTZ5IN88US=> M1z0R3NCVkeHUh?=
697 NVPNeYQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnaRVlHUUN3ME2xN{4zPzBzIN88US=> M4DiZXNCVkeHUh?=
CTB-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTF|LkW5OFgh|ryP MlTkV2FPT0WU
VA-ES-BJ NYHCO4NsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mke3TWM2OD1zMz65NlM1KM7:TR?= MYjTRW5ITVJ?
BE-13 NUXwVo5xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF2LkO5NVUh|ryP MXPTRW5ITVJ?
SKM-1 M1;LbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS0TWM2OD1zND60OFk6KM7:TR?= Mn7rV2FPT0WU
TE-6 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle5TWM2OD1zND63OVkyKM7:TR?= NGXVXHlUSU6JRWK=
LB771-HNC NYLlcGpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTF2Lke4PVgh|ryP NHP3d3BUSU6JRWK=
ECC4 NH2wNndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\UNodKSzVyPUG3MlAzPzdizszN MmnDV2FPT0WU
ES3 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX33TZo5UUN3ME2xO{41PjV3IN88US=> NGCwWlVUSU6JRWK=
LB647-SCLC M{TCSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\s[4E2UUN3ME2xO{41QTR7IN88US=> NWC3N3ZUW0GQR1XS
NB10 M{nUOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm4eXhKSzVyPUG4MlUzPTZizszN NYTtT|YzW0GQR1XS
L-540 NX22[3N[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF6LkixNFkh|ryP NFrWfmRUSU6JRWK=
NCI-H2126 NGHHSYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF7LkWxJO69VQ>? NYjCc3RXW0GQR1XS
HH M3HHfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTBT|RPUUN3ME2yNE4xODl7IN88US=> NUXReI05W0GQR1XS
MPP-89 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XiOGlEPTB;MkOuNlI5QSEQvF2= NGTkPHhUSU6JRWK=
IST-MEL1 M2LSTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PMT2lEPTB;MkOuPFY2QCEQvF2= MoCzV2FPT0WU
KP-N-YS MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jibmlEPTB;MkOuPVI2PSEQvF2= MVTTRW5ITVJ?
EC-GI-10 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJ2LkW5PFkh|ryP MXzTRW5ITVJ?
EKVX M1G2[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTHTWM2OD1{Nj6wNlA{KM7:TR?= NVz3OnpjW0GQR1XS
TGBC1TKB Mnn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJ4LkSzOEDPxE1? MluyV2FPT0WU
Daudi NEHkT2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTJ5LkC3O|Mh|ryP Mmq2V2FPT0WU
ALL-PO M4DCSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2S3XGlEPTB;MkeuNFgyKM7:TR?= M2D0OnNCVkeHUh?=
NB6 NWX2NJBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[3PWlEPTB;MkeuOFg5KM7:TR?= NGDySIFUSU6JRWK=
ES6 NULpWWpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjLTFBKSzVyPUK3MlkyOjNizszN MXfTRW5ITVJ?
COLO-320-HSR NUDSPGRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTJ6LkCzO|Mh|ryP Ml\QV2FPT0WU
K5 NXX1fFJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmezTWM2OD1{OD6xNlg4KM7:TR?= MlXVV2FPT0WU
ES1 NI\FcGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXS0cIlzUUN3ME2yPE44Pzd|IN88US=> NEfYbphUSU6JRWK=
LC-1F M2fKemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLXR2JuUUN3ME2yPU44OzR4IN88US=> NV34NZNiW0GQR1XS
SCLC-21H MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTZW2NTUUN3ME2zNE44OzF5IN88US=> NXSwcY5jW0GQR1XS
SK-PN-DW MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7DfoNkUUN3ME2zNk42PTl6IN88US=> M3:4fXNCVkeHUh?=
D-247MG NUG2XnZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnMNYdKSzVyPUOyMlk4PzNizszN M{\tbHNCVkeHUh?=
TE-5 NF7qXHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4KwSGlEPTB;M{OuNFM3OiEQvF2= M13DNXNCVkeHUh?=
MONO-MAC-6 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTN|LkWwOFgh|ryP NV;rZVN[W0GQR1XS
LB2518-MEL MnXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkn0TWM2OD1|Mz63OlY3KM7:TR?= MljiV2FPT0WU
LOXIMVI MlXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjMTWM2OD1|Mz63PVI5KM7:TR?= NF3sSJFUSU6JRWK=
NCI-H209 NFT1SFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHDOWhKSzVyPUO1MlE1PCEQvF2= NIT2TI5USU6JRWK=
A253 MoPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPFWZJKSzVyPUO1Mlc1OjlizszN MnvTV2FPT0WU
HCC1599 M1X5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fEfmlEPTB;M{[uO|A2OyEQvF2= M{P5cXNCVkeHUh?=
EB-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HxTmlEPTB;M{[uPVUyQCEQvF2= MXjTRW5ITVJ?
GOTO MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknpTWM2OD1|Nz6zNlI1KM7:TR?= NGe0SYZUSU6JRWK=
SW684 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke3TWM2OD12MT64OFk2KM7:TR?= NXrHSXA1W0GQR1XS
DEL MnXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTR{LkC1NlIh|ryP NIXN[GhUSU6JRWK=
HT-144 M2L3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4mzOWlEPTB;NEKuNVY4PiEQvF2= M4W2ZXNCVkeHUh?=
TE-9 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\aTWM2OD12Mz60OVk3KM7:TR?= MYXTRW5ITVJ?
KARPAS-45 NIHKdVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu0XVM1UUN3ME20OE4{QTJ3IN88US=> NHn5TGtUSU6JRWK=
HAL-01 NV7KTFczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTyTWM2OD12ND61NFM1KM7:TR?= MmHWV2FPT0WU
RCC10RGB M{nwUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTyXG9KSzVyPUS0Mlc{QTJizszN M{HzRnNCVkeHUh?=
CP67-MEL NG\hZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmq3TWM2OD12NT62NlQyKM7:TR?= NEe4dnhUSU6JRWK=
NB17 Mo\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTR3Lk[2OFMh|ryP MUPTRW5ITVJ?
SK-UT-1 M1u2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C2cGlEPTB;NEWuPVQ3PCEQvF2= Mmf3V2FPT0WU
JiyoyeP-2003 M3L3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnxTWM2OD12Nj6wNVE6KM7:TR?= MYTTRW5ITVJ?
HCE-4 NWXGNG9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\CfpBrUUN3ME20Ok42QTZ6IN88US=> MXXTRW5ITVJ?
NCI-H720 NW\DOJBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jtOWlEPTB;NE[uO|Y5OiEQvF2= MlHHV2FPT0WU
KARPAS-422 M172dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTR5LkC4PVUh|ryP NHnCfmxUSU6JRWK=
Ramos-2G6-4C10 NIm4bGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXWWoh{UUN3ME20O{4yPjJ{IN88US=> MXLTRW5ITVJ?
HCE-T NYrHXlh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTR5Lk[4Nlgh|ryP M3nUN3NCVkeHUh?=
PSN1 NGXPTIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGKzV4tKSzVyPUS3Mlc5OTNizszN MX7TRW5ITVJ?

... 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
+ 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
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  • 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
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  • 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 (64.57 mM) warming
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
    Concentration
    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):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    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
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 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
NCT02085603 Recruiting Cancer Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca March 2014 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.

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Frequently Asked Questions

  • Question 1:

    What is the half-life of Saracatinib?

  • Answer:

    Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID