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 M{TrcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;2UoR{UUN3ME2wMlA3OTR|IN88US=> Mkn4V2FPT0WU
LAMA-84 M1zLNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzTTWM2OD1yLkG1PVkh|ryP NH[xbodUSU6JRWK=
MEG-01 M2nVXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXYTWM2OD1yLkKzOlg5KM7:TR?= MoTxV2FPT0WU
EM-2 MkDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXreZRKSzVyPUCuNlY2KM7:TR?= MUDTRW5ITVJ?
TE-15 M{XjSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPRTWM2OD1yLkK3OFEzKM7:TR?= MX7TRW5ITVJ?
NCI-H1648 Mmi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDLRVFoUUN3ME2wMlI5OTF4IN88US=> NVfMR|lWW0GQR1XS
TE-12 NFHoWJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;GUWlEPTB;MD6zNlY5KM7:TR?= MVXTRW5ITVJ?
LB996-RCC MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknuTWM2OD1yLkS0NVk3KM7:TR?= MnHBV2FPT0WU
K-562 NUW5VGo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX65ZVluUUN3ME2wMlQ1QTZ5IN88US=> MlW0V2FPT0WU
D-336MG MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoiwTWM2OD1yLkWwN|A1KM7:TR?= NY\NdVV{W0GQR1XS
NOS-1 NGPJ[3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7oOYZKSzVyPUCuOlA2OjlizszN NXGz[2tOW0GQR1XS
EW-24 NYW3W5d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNkK2PVMh|ryP MY\TRW5ITVJ?
BV-173 M1uxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwNkWyOFkh|ryP M1:0T3NCVkeHUh?=
NCCIT Ml3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnuZZFKSzVyPUCuO|MzOThizszN NILTfXZUSU6JRWK=
NCI-H1436 MlHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwN{mwOFkh|ryP NUjPblc4W0GQR1XS
BB30-HNC MkS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwOE[yNFMh|ryP NYe0RZE1W0GQR1XS
TE-8 M{[3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWSy[lU4UUN3ME2wMlg4Ojd3IN88US=> NHLHRmtUSU6JRWK=
A704 NWPZTHZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwOEmyNUDPxE1? M4HNOnNCVkeHUh?=
TK10 NHrybGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrlVHdKSzVyPUCuPVA3PjlizszN NVmwfph7W0GQR1XS
KS-1 NYX2V|NET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37UOmlEPTB;MT6xPVc4QSEQvF2= Mnq4V2FPT0WU
C2BBe1 NGjON29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\hbpFuUUN3ME2xMlIxPTB5IN88US=> MWPTRW5ITVJ?
RXF393 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzNSWt[UUN3ME2xMlI1OzZizszN M3jX[nNCVkeHUh?=
KGN NFz2eJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TaO2lEPTB;MT6yO|Y5PyEQvF2= MXPTRW5ITVJ?
NB69 M{nxWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoSwTWM2OD1zLkO3OFk4KM7:TR?= MXrTRW5ITVJ?
TE-11 Mn;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjaeVlKSzVyPUGuOFM1OThizszN M{XRTHNCVkeHUh?=
TE-1 M1z1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwNESxNFUh|ryP MnnlV2FPT0WU
ST486 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjuNGZSUUN3ME2xMlQ2QDV{IN88US=> M{CzcnNCVkeHUh?=
HOP-62 M3rDUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7VTWM2OD1zLkWwNlQ3KM7:TR?= MkLxV2FPT0WU
EW-16 M4KzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrXe41xUUN3ME2xMlU2ODh|IN88US=> NWrLbpVXW0GQR1XS
LB1047-RCC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvIW2NKSzVyPUGuOVU1PTNizszN M{PtTXNCVkeHUh?=
TE-10 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwNk[yOVIh|ryP NGjSNJRUSU6JRWK=
RL95-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DLSGlEPTB;MT62OlkxOiEQvF2= M4TXbXNCVkeHUh?=
DOHH-2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYKxbYJ4UUN3ME2xMlcyPzh{IN88US=> NWjjfIhQW0GQR1XS
MFH-ino MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzhTWM2OD1zLke3PFch|ryP NF7tRpFUSU6JRWK=
GB-1 NV3vW|ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\yd2lEPTB;MT63PVg{OyEQvF2= NIrhT2ZUSU6JRWK=
SK-N-DZ MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rSb2lEPTB;MT64OFY5QCEQvF2= NXGxVm9YW0GQR1XS
OS-RC-2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTFwOEi1O|Qh|ryP MXXTRW5ITVJ?
SW982 NWPYSmlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DXd2lEPTB;MT65NlA6OyEQvF2= MXnTRW5ITVJ?
KALS-1 NWXU[ZBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jmT2lEPTB;MT65PFczOiEQvF2= Mn[zV2FPT0WU
TGBC24TKB NIXVSHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJwMEW5OVgh|ryP M2m5fXNCVkeHUh?=
GI-1 M4LkXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3zTWM2OD1{LkG2NFg1KM7:TR?= MmK2V2FPT0WU
SW962 NFe0fVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILLRopKSzVyPUKuNVcyPzhizszN M37pXXNCVkeHUh?=
SW872 NUTRbmFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJwMUi1NFch|ryP MY\TRW5ITVJ?
NCI-H747 NIf2RnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjWcJF2UUN3ME2yMlI2PzF2IN88US=> NHq2NZNUSU6JRWK=
MZ1-PC Mmq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmf6TWM2OD1{LkK5N|U3KM7:TR?= MUDTRW5ITVJ?
MSTO-211H MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XUeWlEPTB;Mj6zOVczOyEQvF2= Mmi1V2FPT0WU
BL-70 M3zxOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJwNEe0NlIh|ryP M1zsbnNCVkeHUh?=
SW954 NFLtTWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfHTWM2OD1{LkW3OFA5KM7:TR?= NFHOO2dUSU6JRWK=
SNB75 NHnnd3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXwNoVKSzVyPUKuOlg2QTRizszN M3Lvb3NCVkeHUh?=
IST-SL2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LJdGlEPTB;Mj63NlM4QSEQvF2= MlvoV2FPT0WU
GCIY NHnBPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvIbmg6UUN3ME2yMlg4ODB3IN88US=> Ml3YV2FPT0WU
KU812 M1rD[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTNwMEWyPVkh|ryP MnuwV2FPT0WU
LXF-289 NXrLbnczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;0coNKSzVyPUOuNVIyODlizszN M4P5enNCVkeHUh?=
ETK-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPJTWM2OD1|LkKwO|Y4KM7:TR?= NEHGXWlUSU6JRWK=
SF126 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTNwM{GxO|Qh|ryP MkLHV2FPT0WU
LC-2-ad M172cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTNwNUW3JO69VQ>? MnjXV2FPT0WU
KNS-42 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\rTWM2OD1|Lk[1JO69VQ>? M2D1NXNCVkeHUh?=
OVCAR-4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvLflNKSzVyPUOuO|M1OzNizszN NVjH[JJSW0GQR1XS
PF-382 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XZ[mlEPTB;Mz64N|Y6QCEQvF2= NXTk[|doW0GQR1XS
SH-4 NHf6O4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnsRVZVUUN3ME20MlI2OjV7IN88US=> MWDTRW5ITVJ?
KM12 MofOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTRwM{K0NVYh|ryP MXnTRW5ITVJ?
NB5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\UUWlEPTB;ND60NVg3PCEQvF2= NGTKVVNUSU6JRWK=
KURAMOCHI Mn3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfl[|lyUUN3ME20MlY2OjV4IN88US=> M{XXVHNCVkeHUh?=
Becker MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfafFdKSzVyPUSuOlY1OTZizszN NFfHSWxUSU6JRWK=
MV-4-11 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn30TWM2OD12LkixN|Q1KM7:TR?= MnTpV2FPT0WU
KINGS-1 M3n3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfqcXRKSzVyPUSuPFI{PzNizszN NGXMVHpUSU6JRWK=
LS-123 MkjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;6bVNKSzVyPUWuOFk3QDRizszN MXPTRW5ITVJ?
SF268 MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XSXmlEPTB;NT62NVI3OiEQvF2= M1fMUHNCVkeHUh?=
A388 M3vmRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TUSmlEPTB;NT62N|Y3PyEQvF2= NGX3fmdUSU6JRWK=
NMC-G1 MkPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr1PVV7UUN3ME22MlAyQDFzIN88US=> Mo[zV2FPT0WU
CGTH-W-1 NGO1VVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1S3d2lEPTB;Nj6wNlA4PSEQvF2= NWC0cGMxW0GQR1XS
ES4 NGe3bIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYm5SmxIUUN3ME22MlU{ODd2IN88US=> Mlr1V2FPT0WU
SR Mn61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfYTWM2OD14LkW4PFA4KM7:TR?= M3z5cHNCVkeHUh?=
BB49-HNC NVf2dXhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHGfWxRUUN3ME22Mlc{OjB4IN88US=> NGTPcVVUSU6JRWK=
KLE NH\OOYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjEcGFKSzVyPU[uO|g{PzdizszN Ml3mV2FPT0WU
HUTU-80 NX3zTohnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\NTWM2OD14Lkm4OFY3KM7:TR?= NH;sXndUSU6JRWK=
SNU-C2B NH;QO5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi2TWM2OD15LkiyO|M4KM7:TR?= NFm4XGZUSU6JRWK=
BB65-RCC NUn2T|RNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTdwOUS5NFQh|ryP NIn5OmRUSU6JRWK=
QIMR-WIL MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3uzdGlEPTB;OD60NlgxQCEQvF2= M3\DbHNCVkeHUh?=
GDM-1 NIOzW3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\LTWM2OD16Lkm3NlkzKM7:TR?= NULJZXhNW0GQR1XS
LC4-1 MlrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrlOVhQUUN3ME25MlAxQTFzIN88US=> NVfMR5FPW0GQR1XS
MLMA NEjQR5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTlwMUWwNFYh|ryP M1rTV3NCVkeHUh?=
EoL-1-cell MmjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHWxWGpKSzVyPUmuN|AyQTJizszN M2\ZOHNCVkeHUh?=
BOKU MnK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTlwOU[0OlYh|ryP MUnTRW5ITVJ?
EVSA-T M4\Gc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTFyLk[1Olgh|ryP NF\0ZnRUSU6JRWK=
D-283MED NVKxboRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfMOlBYUUN3ME2xNE46OTd4IN88US=> MV3TRW5ITVJ?
NB1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTFzLkCyOFIh|ryP MkjvV2FPT0WU
RPMI-8402 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTFzLkG3PEDPxE1? MlTDV2FPT0WU
NCI-H1355 NXLESVdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Kyd2lEPTB;MUGuNVgxPiEQvF2= NIHLRldUSU6JRWK=
NB7 Mk\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFzLkOyPVch|ryP NYHWPGZtW0GQR1XS
RPMI-6666 MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF{Lkm1Olch|ryP MknnV2FPT0WU
697 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jlPGlEPTB;MUOuNlcxOSEQvF2= NFj4OnVUSU6JRWK=
CTB-1 NYjDe2g6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fWbGlEPTB;MUOuOVk1QCEQvF2= M1qyNnNCVkeHUh?=
VA-ES-BJ MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTF|LkmyN|Qh|ryP M{G1XnNCVkeHUh?=
BE-13 NF3LPIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELxRmRKSzVyPUG0MlM6OTVizszN NIPvPGdUSU6JRWK=
SKM-1 MoPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknYTWM2OD1zND60OFk6KM7:TR?= MmXHV2FPT0WU
TE-6 Ml3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHYPXRKSzVyPUG0Mlc2QTFizszN NVHnNllTW0GQR1XS
LB771-HNC MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PTOGlEPTB;MUSuO|g6QCEQvF2= NIXnTYtUSU6JRWK=
ECC4 MnjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvnTWM2OD1zNz6wNlc4KM7:TR?= MWDTRW5ITVJ?
ES3 MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF5LkS2OVUh|ryP NXnLWXRbW0GQR1XS
LB647-SCLC NFPmcJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXzcY5TUUN3ME2xO{41QTR7IN88US=> NXXEfJFLW0GQR1XS
NB10 M3LSfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTDOIlKSzVyPUG4MlUzPTZizszN NYC2UWp4W0GQR1XS
L-540 NXHpbXRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETOXZNKSzVyPUG4MlgyODlizszN NV;tSplmW0GQR1XS
NCI-H2126 NFHoTWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTF7LkWxJO69VQ>? MWnTRW5ITVJ?
HH M1HOW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOwVJIzUUN3ME2yNE4xODl7IN88US=> Ml\SV2FPT0WU
MPP-89 M2TwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTJ|LkKyPFkh|ryP NUf6ZZI1W0GQR1XS
IST-MEL1 MkHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK2TWM2OD1{Mz64OlU5KM7:TR?= Ml7qV2FPT0WU
KP-N-YS MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmm5TWM2OD1{Mz65NlU2KM7:TR?= M2LLOXNCVkeHUh?=
EC-GI-10 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1y4[WlEPTB;MkSuOVk5QSEQvF2= NHnJSFVUSU6JRWK=
EKVX NU\BXHBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXqzXWJjUUN3ME2yOk4xOjB|IN88US=> NXvEdZVIW0GQR1XS
TGBC1TKB NWLOenFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\LTWM2OD1{Nj60N|Qh|ryP NVjCcVB2W0GQR1XS
Daudi MmfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33oNWlEPTB;MkeuNFc4OyEQvF2= NF\uT4JUSU6JRWK=
ALL-PO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJ5LkC4NUDPxE1? M4XCWHNCVkeHUh?=
NB6 NHz5UWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDrTWM2OD1{Nz60PFgh|ryP NY\lWVdIW0GQR1XS
ES6 M3f2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTJ5LkmxNlMh|ryP NI\GVmdUSU6JRWK=
COLO-320-HSR MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLWVXdKSzVyPUK4MlA{PzNizszN MnraV2FPT0WU
K5 NGHKeGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTJ6LkGyPFch|ryP NUjTOHl3W0GQR1XS
ES1 NUfLPGp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrJNmJKSzVyPUK4Mlc4PzNizszN MWrTRW5ITVJ?
LC-1F M4XMTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3nTolKSzVyPUK5Mlc{PDZizszN MVPTRW5ITVJ?
SCLC-21H MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjHTWM2OD1|MD63N|E4KM7:TR?= NWPYXHdEW0GQR1XS
SK-PN-DW NXLNUZZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjQbWhKSzVyPUOyMlU2QThizszN MlrxV2FPT0WU
D-247MG M{Lybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTN{Lkm3O|Mh|ryP M1:2SnNCVkeHUh?=
TE-5 MorNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjhTWM2OD1|Mz6wN|YzKM7:TR?= MUnTRW5ITVJ?
MONO-MAC-6 MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTN|LkWwOFgh|ryP MlntV2FPT0WU
LB2518-MEL MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mke0TWM2OD1|Mz63OlY3KM7:TR?= NXXZUm5rW0GQR1XS
LOXIMVI NHXsPVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7VRVI6UUN3ME2zN{44QTJ6IN88US=> NVXSSIQ6W0GQR1XS
NCI-H209 NEfKOWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGntRppKSzVyPUO1MlE1PCEQvF2= NETOXXhUSU6JRWK=
A253 M{mzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{G2dmlEPTB;M{WuO|QzQSEQvF2= Mn7xV2FPT0WU
HCC1599 MlK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN4LkewOVMh|ryP NUK5OYZpW0GQR1XS
EB-3 NXnEPHhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTN4Lkm1NVgh|ryP NG\2WmpUSU6JRWK=
GOTO NEHYTJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXUSphKSzVyPUO3MlMzOjRizszN MlTZV2FPT0WU
SW684 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYK1WYQ5UUN3ME20NU45PDl3IN88US=> NGjGdINUSU6JRWK=
DEL NWHyT2NKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTR{LkC1NlIh|ryP M2DrOnNCVkeHUh?=
HT-144 MmjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXrdI9IUUN3ME20Nk4yPjd4IN88US=> NFHrTnhUSU6JRWK=
TE-9 NE\KPXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DMSWlEPTB;NEOuOFU6PiEQvF2= M2L2cnNCVkeHUh?=
KARPAS-45 M17S[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XXdmlEPTB;NESuN|kzPSEQvF2= MX7TRW5ITVJ?
HAL-01 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;sSW9KSzVyPUS0MlUxOzRizszN MX3TRW5ITVJ?
RCC10RGB NEL6c4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX6zOJF5UUN3ME20OE44Ozl{IN88US=> NWLQSnhLW0GQR1XS
CP67-MEL M3T3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzBZ5JxUUN3ME20OU43OjRzIN88US=> NXPm[JRKW0GQR1XS
NB17 NHjC[5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnMTWx7UUN3ME20OU43PjR|IN88US=> NVHkW2x1W0GQR1XS
SK-UT-1 Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[zTWM2OD12NT65OFY1KM7:TR?= MXXTRW5ITVJ?
JiyoyeP-2003 MoTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zlbWlEPTB;NE[uNFEyQSEQvF2= M{nQ[nNCVkeHUh?=
HCE-4 MnjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LWRWlEPTB;NE[uOVk3QCEQvF2= MX7TRW5ITVJ?
NCI-H720 NX3X[mhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTR4Lke2PFIh|ryP MkXUV2FPT0WU
KARPAS-422 NVPJZoJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPQR3pJUUN3ME20O{4xQDl3IN88US=> MmXVV2FPT0WU
Ramos-2G6-4C10 MljqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHpO|JsUUN3ME20O{4yPjJ{IN88US=> MmjuV2FPT0WU
HCE-T MkDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\LeXhpUUN3ME20O{43QDJ6IN88US=> NX\MUWh2W0GQR1XS
PSN1 NELLeHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHXSXJyUUN3ME20O{44QDF|IN88US=> NXrDOWhNW0GQR1XS

... 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 slightly soluble or insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+ddH2O
5mg/mL

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

Chemical Information

Molecular Weight 542.03
Formula

C27H32ClN5O5

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

  • Mass
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*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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID