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
USD 70 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

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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 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PFUmlEPTB;MD6wOlE1OyEQvF2= M2O0T3NCVkeHUh?=
LAMA-84 M2\lT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnkZ|RKSzVyPUCuNVU6QSEQvF2= NYO0e3NCW0GQR1XS
MEG-01 M4O2c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWflTZNbUUN3ME2wMlI{Pjh6IN88US=> NYfBU2hCW0GQR1XS
EM-2 NXfIb4o5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjycJRKSzVyPUCuNlY2KM7:TR?= MmrqV2FPT0WU
TE-15 NGe0bm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnRcZNoUUN3ME2wMlI4PDF{IN88US=> NXnNVZczW0GQR1XS
NCI-H1648 MlfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwMkixNVYh|ryP M4PGe3NCVkeHUh?=
TE-12 NIfuPJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrlSIFKSzVyPUCuN|I3QCEQvF2= M1XHZnNCVkeHUh?=
LB996-RCC NV3kSJVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWT6XFJzUUN3ME2wMlQ1OTl4IN88US=> M1jOXHNCVkeHUh?=
K-562 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSxenRqUUN3ME2wMlQ1QTZ5IN88US=> MnzxV2FPT0WU
D-336MG M1PvZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoL0TWM2OD1yLkWwN|A1KM7:TR?= MnvyV2FPT0WU
NOS-1 M1PXdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwNkC1Nlkh|ryP NVz4UmtlW0GQR1XS
EW-24 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\kXmlEPTB;MD62NlY6OyEQvF2= NV;jUpl4W0GQR1XS
BV-173 NFzEdllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwNkWyOFkh|ryP MmLJV2FPT0WU
NCCIT MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonKTWM2OD1yLkezNlE5KM7:TR?= NYLLdJp7W0GQR1XS
NCI-H1436 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwN{mwOFkh|ryP MnzPV2FPT0WU
BB30-HNC NGH4[JJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7mfnBKSzVyPUCuPFYzODNizszN MVLTRW5ITVJ?
TE-8 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwOEeyO|Uh|ryP M1i1RnNCVkeHUh?=
A704 NFP3ZoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Lnb2lEPTB;MD64PVIyKM7:TR?= MYTTRW5ITVJ?
TK10 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{OzPGlEPTB;MD65NFY3QSEQvF2= M3:wfHNCVkeHUh?=
KS-1 NXfz[2xJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPTTWM2OD1zLkG5O|c6KM7:TR?= MUPTRW5ITVJ?
C2BBe1 NF;6SnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXDTWM2OD1zLkKwOVA4KM7:TR?= MlrmV2FPT0WU
RXF393 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHrS4pKSzVyPUGuNlQ{PiEQvF2= MV7TRW5ITVJ?
KGN NYDMR5RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDmTYJKSzVyPUGuNlc3QDdizszN NWfkUmQ4W0GQR1XS
NB69 NWTIXI1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTFwM{e0PVch|ryP NETicYJUSU6JRWK=
TE-11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHmb3NKSzVyPUGuOFM1OThizszN MXXTRW5ITVJ?
TE-1 NXnXRYZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTFwNESxNFUh|ryP NHL0Nm5USU6JRWK=
ST486 NGj5VmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXDTWM2OD1zLkS1PFUzKM7:TR?= NHT1cHJUSU6JRWK=
HOP-62 NYLnZVJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTFwNUCyOFYh|ryP M{nTbnNCVkeHUh?=
EW-16 NIrhOZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT1N4ZFUUN3ME2xMlU2ODh|IN88US=> NHrDUY5USU6JRWK=
LB1047-RCC MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfJc|JKSzVyPUGuOVU1PTNizszN MonXV2FPT0WU
TE-10 M4D4cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zaN2lEPTB;MT62OlI2OiEQvF2= M2ry[XNCVkeHUh?=
RL95-2 NGXSRXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXMW29KSzVyPUGuOlY6ODJizszN NHTmXZRUSU6JRWK=
DOHH-2 NID2WndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf2TWM2OD1zLkexO|gzKM7:TR?= M4DmWHNCVkeHUh?=
MFH-ino NYXJWGhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDtWoxKSzVyPUGuO|c5PyEQvF2= M{[1XnNCVkeHUh?=
GB-1 NVXBVIVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFwN{m4N|Mh|ryP M1LQRXNCVkeHUh?=
SK-N-DZ MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTFwOES2PFgh|ryP MVXTRW5ITVJ?
OS-RC-2 Mn62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnITWM2OD1zLki4OVc1KM7:TR?= M1jpbnNCVkeHUh?=
SW982 MoLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL2WmZKSzVyPUGuPVIxQTNizszN M3yycnNCVkeHUh?=
KALS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfXTWM2OD1zLkm4O|IzKM7:TR?= NFHPSZlUSU6JRWK=
TGBC24TKB MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUC5RYVmUUN3ME2yMlA2QTV6IN88US=> NXraUWhrW0GQR1XS
GI-1 M1PCOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfQd2xKSzVyPUKuNVYxQDRizszN MYnTRW5ITVJ?
SW962 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJwMUexO|gh|ryP NEP1XHNUSU6JRWK=
SW872 M{XaSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;2UIlKSzVyPUKuNVg2ODdizszN NI\CN2pUSU6JRWK=
NCI-H747 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXreI57UUN3ME2yMlI2PzF2IN88US=> M2LsZXNCVkeHUh?=
MZ1-PC MoruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe2fHJKSzVyPUKuNlk{PTZizszN NXHnZ4FFW0GQR1XS
MSTO-211H M2OxeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTJwM{W3NlMh|ryP NGXFd5VUSU6JRWK=
BL-70 M2rqN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTxTWM2OD1{LkS3OFIzKM7:TR?= NXzQPGJEW0GQR1XS
SW954 M123TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\QfFQ2UUN3ME2yMlU4PDB6IN88US=> NGPOSlBUSU6JRWK=
SNB75 NF\WPGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TxeGlEPTB;Mj62PFU6PCEQvF2= M{DiT3NCVkeHUh?=
IST-SL2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJwN{KzO|kh|ryP NIHXTnZUSU6JRWK=
GCIY NUnIeot1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DwTGlEPTB;Mj64O|AxPSEQvF2= MYfTRW5ITVJ?
KU812 NF\LXYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTNwMEWyPVkh|ryP MlLGV2FPT0WU
LXF-289 MoHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TLfGlEPTB;Mz6xNlExQSEQvF2= MX\TRW5ITVJ?
ETK-1 MlfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3P6XmlEPTB;Mz6yNFc3PyEQvF2= MnzxV2FPT0WU
SF126 MkHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzMXFBxUUN3ME2zMlMyOTd2IN88US=> MYLTRW5ITVJ?
LC-2-ad Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTNwNUW3JO69VQ>? NYLOZZNZW0GQR1XS
KNS-42 NVn1dopjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1z5SmlEPTB;Mz62OUDPxE1? NYnKOJJFW0GQR1XS
OVCAR-4 M3rEXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTNwN{O0N|Mh|ryP MljJV2FPT0WU
PF-382 MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILWUoZKSzVyPUOuPFM3QThizszN MnTQV2FPT0WU
SH-4 NFyzPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHqWoxUUUN3ME20MlI2OjV7IN88US=> NGTCe|ZUSU6JRWK=
KM12 NU\TcYFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jZNWlEPTB;ND6zNlQyPiEQvF2= NVrTVG96W0GQR1XS
NB5 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\rblRKSzVyPUSuOFE5PjRizszN MVjTRW5ITVJ?
KURAMOCHI MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGG3R21KSzVyPUSuOlUzPTZizszN M3qzS3NCVkeHUh?=
Becker NIXrTJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ezb2lEPTB;ND62OlQyPiEQvF2= NFficolUSU6JRWK=
MV-4-11 NYHZSGJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPRTWM2OD12LkixN|Q1KM7:TR?= M2X4OHNCVkeHUh?=
KINGS-1 MkfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HqbWlEPTB;ND64NlM4OyEQvF2= MXnTRW5ITVJ?
LS-123 NF7mRVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\LSmlEPTB;NT60PVY5PCEQvF2= M2qyc3NCVkeHUh?=
SF268 M2XaRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTVwNkGyOlIh|ryP MlPiV2FPT0WU
A388 MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrGfHFKSzVyPUWuOlM3PjdizszN NXfm[JJSW0GQR1XS
NMC-G1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvpTItvUUN3ME22MlAyQDFzIN88US=> NWjsTmFXW0GQR1XS
CGTH-W-1 NVHnWGNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHieJVKSzVyPU[uNFIxPzVizszN NE\hZYNUSU6JRWK=
ES4 M1X1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLT[XVwUUN3ME22MlU{ODd2IN88US=> M4DGVHNCVkeHUh?=
SR M{P0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDCNpFSUUN3ME22MlU5QDB5IN88US=> MUDTRW5ITVJ?
BB49-HNC NWDoRnRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O5bWlEPTB;Nj63N|IxPiEQvF2= Mm\3V2FPT0WU
KLE MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDyW41jUUN3ME22Mlc5Ozd5IN88US=> M2XMSHNCVkeHUh?=
HUTU-80 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfTTWM2OD14Lkm4OFY3KM7:TR?= MYrTRW5ITVJ?
SNU-C2B NUPZTJY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO4[5dKSzVyPUeuPFI4OzdizszN MkK4V2FPT0WU
BB65-RCC NInDTYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrnTWM2OD15Lkm0PVA1KM7:TR?= MUnTRW5ITVJ?
QIMR-WIL Mk[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRThwNEK4NFgh|ryP MWDTRW5ITVJ?
GDM-1 NWfzTVJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRThwOUeyPVIh|ryP NFXOPWxUSU6JRWK=
LC4-1 NVvTW2FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3Je4RTUUN3ME25MlAxQTFzIN88US=> M2TSXHNCVkeHUh?=
MLMA MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDYNHpKSzVyPUmuNVUxODZizszN NG\mb29USU6JRWK=
EoL-1-cell NWHFSm0{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4q1eGlEPTB;OT6zNFE6OiEQvF2= MmHCV2FPT0WU
BOKU MojHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTlwOU[0OlYh|ryP NFnzNYpUSU6JRWK=
EVSA-T NF;0WJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;kVmlEPTB;MUCuOlU3QCEQvF2= NGP3U41USU6JRWK=
D-283MED MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\jfnRKSzVyPUGwMlkyPzZizszN NYf1d|RUW0GQR1XS
NB1 M4fjbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rOR2lEPTB;MUGuNFI1OiEQvF2= M{nrVnNCVkeHUh?=
RPMI-8402 M2r3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTFzLkG3PEDPxE1? M{H6dHNCVkeHUh?=
NCI-H1355 NEfBNmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTFzLkG4NFYh|ryP Ml7VV2FPT0WU
NB7 M2mwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfvTWM2OD1zMT6zNlk4KM7:TR?= NUmySIloW0GQR1XS
RPMI-6666 NYfjVYdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz0TWM2OD1zMj65OVY4KM7:TR?= NHLKT|FUSU6JRWK=
697 MlGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TFeWlEPTB;MUOuNlcxOSEQvF2= M2LrS3NCVkeHUh?=
CTB-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj4TYJKSzVyPUGzMlU6PDhizszN M2jKW3NCVkeHUh?=
VA-ES-BJ MlfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4H0XmlEPTB;MUOuPVI{PCEQvF2= M1jNUHNCVkeHUh?=
BE-13 M1jXbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF2LkO5NVUh|ryP NEjCdnhUSU6JRWK=
SKM-1 NIfFV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLI[FF[UUN3ME2xOE41PDl7IN88US=> NVTpd4ZoW0GQR1XS
TE-6 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jF[WlEPTB;MUSuO|U6OSEQvF2= NFTxUm5USU6JRWK=
LB771-HNC NV3McHpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTF2Lke4PVgh|ryP NETQdG1USU6JRWK=
ECC4 NUSxW5VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXhSHRKSzVyPUG3MlAzPzdizszN NUCxb2hOW0GQR1XS
ES3 Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr0eZBKSzVyPUG3MlQ3PTVizszN NWK5UnRIW0GQR1XS
LB647-SCLC M4fyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF5LkS5OFkh|ryP NXy1XZp[W0GQR1XS
NB10 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Lsb2lEPTB;MUiuOVI2PiEQvF2= NXLGdnFlW0GQR1XS
L-540 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV65c2o2UUN3ME2xPE45OTB7IN88US=> M4DvZXNCVkeHUh?=
NCI-H2126 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXpTWM2OD1zOT61NUDPxE1? NVz5OYVmW0GQR1XS
HH Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli3TWM2OD1{MD6wNFk6KM7:TR?= M1HXN3NCVkeHUh?=
MPP-89 NXXUUohYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJ|LkKyPFkh|ryP NFKxNWxUSU6JRWK=
IST-MEL1 NHva[nlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPKSlI1UUN3ME2yN{45PjV6IN88US=> MlizV2FPT0WU
KP-N-YS MnLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHkZYhUUUN3ME2yN{46OjV3IN88US=> NU\RS4JzW0GQR1XS
EC-GI-10 M4LaNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXno[ItGUUN3ME2yOE42QTh7IN88US=> NYPTTmI2W0GQR1XS
EKVX MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;zR2lEPTB;Mk[uNFIxOyEQvF2= M{LoU3NCVkeHUh?=
TGBC1TKB MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfSc|B2UUN3ME2yOk41OzRizszN M1nt[XNCVkeHUh?=
Daudi MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLRTWM2OD1{Nz6wO|c{KM7:TR?= NIjEUmhUSU6JRWK=
ALL-PO MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJ5LkC4NUDPxE1? M{HYPHNCVkeHUh?=
NB6 NVjDfJJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILaZohKSzVyPUK3MlQ5QCEQvF2= MXPTRW5ITVJ?
ES6 MkHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVOwTIhDUUN3ME2yO{46OTJ|IN88US=> M3nJXXNCVkeHUh?=
COLO-320-HSR NVW2S49oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrXTWM2OD1{OD6wN|c{KM7:TR?= NUf5VWpUW0GQR1XS
K5 M17Remdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Xyc2lEPTB;MkiuNVI5PyEQvF2= M3Xy[HNCVkeHUh?=
ES1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvRc2NKSzVyPUK4Mlc4PzNizszN MW\TRW5ITVJ?
LC-1F NIfX[YFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPSb4ZKSzVyPUK5Mlc{PDZizszN MU\TRW5ITVJ?
SCLC-21H MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnTZZlJUUN3ME2zNE44OzF5IN88US=> NFHjSJpUSU6JRWK=
SK-PN-DW MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfvTWM2OD1|Mj61OVk5KM7:TR?= MmHFV2FPT0WU
D-247MG MkfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:2[2lEPTB;M{KuPVc4OyEQvF2= MV;TRW5ITVJ?
TE-5 NIjyc4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTN|LkCzOlIh|ryP NXT6VYE{W0GQR1XS
MONO-MAC-6 NV3vcG4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTN|LkWwOFgh|ryP MXTTRW5ITVJ?
LB2518-MEL MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;TW2lEPTB;M{OuO|Y3PiEQvF2= MUnTRW5ITVJ?
LOXIMVI MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXtUGpMUUN3ME2zN{44QTJ6IN88US=> NIjONXdUSU6JRWK=
NCI-H209 NWTtO5RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTlfpFWUUN3ME2zOU4yPDRizszN MXvTRW5ITVJ?
A253 NF;ue3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnm[po3UUN3ME2zOU44PDJ7IN88US=> M1Ta[XNCVkeHUh?=
HCC1599 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPoTWM2OD1|Nj63NFU{KM7:TR?= MVLTRW5ITVJ?
EB-3 NFuwc2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:0UJJKSzVyPUO2Mlk2OThizszN NIn0fodUSU6JRWK=
GOTO MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHqWWZKSzVyPUO3MlMzOjRizszN MlvUV2FPT0WU
SW684 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTRzLki0PVUh|ryP NYqzWG9TW0GQR1XS
DEL NYS2XVdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnIXlNSUUN3ME20Nk4xPTJ{IN88US=> MkjSV2FPT0WU
HT-144 NHzwNGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrvVYJKSzVyPUSyMlE3PzZizszN MYHTRW5ITVJ?
TE-9 Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTR|LkS1PVYh|ryP NGLIe2pUSU6JRWK=
KARPAS-45 NEPvVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTR2LkO5NlUh|ryP M2PRTHNCVkeHUh?=
HAL-01 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1faZmlEPTB;NESuOVA{PCEQvF2= M2\UVnNCVkeHUh?=
RCC10RGB MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTsTWM2OD12ND63N|kzKM7:TR?= MWLTRW5ITVJ?
CP67-MEL M4XYfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTR3Lk[yOFEh|ryP MUfTRW5ITVJ?
NB17 MlPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrmTWM2OD12NT62OlQ{KM7:TR?= NEKyVmZUSU6JRWK=
SK-UT-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\FZ2lEPTB;NEWuPVQ3PCEQvF2= MkXKV2FPT0WU
JiyoyeP-2003 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;ZdGlEPTB;NE[uNFEyQSEQvF2= MVzTRW5ITVJ?
HCE-4 NX\hb5VLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHPe5FKSzVyPUS2MlU6PjhizszN NE\IVo9USU6JRWK=
NCI-H720 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\XOmpKSzVyPUS2Mlc3QDJizszN M3vLWXNCVkeHUh?=
KARPAS-422 Ml3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nrSGlEPTB;NEeuNFg6PSEQvF2= NUPjeY5uW0GQR1XS
Ramos-2G6-4C10 M4jaXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjzS29KSzVyPUS3MlE3OjJizszN NH;TV5NUSU6JRWK=
HCE-T MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTR5Lk[4Nlgh|ryP MXXTRW5ITVJ?
PSN1 MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWwUW1KSzVyPUS3Mlc5OTNizszN NIrjRXhUSU6JRWK=

... 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
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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

  • 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