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 NUPD[ld7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTBwME[xOFMh|ryP NITwfIRUSU6JRWK=
LAMA-84 NF;XcXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PkVmlEPTB;MD6xOVk6KM7:TR?= NYXrT5hXW0GQR1XS
MEG-01 NXfhWo01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nvOGlEPTB;MD6yN|Y5QCEQvF2= NXTUPHpTW0GQR1XS
EM-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwMk[1JO69VQ>? NFT5c4tUSU6JRWK=
TE-15 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfYTWM2OD1yLkK3OFEzKM7:TR?= MmXKV2FPT0WU
NCI-H1648 NGHBSo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHjU2FKSzVyPUCuNlgyOTZizszN NV;uS3BFW0GQR1XS
TE-12 NW\lSG1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwM{K2PEDPxE1? M4LuTXNCVkeHUh?=
LB996-RCC NYDvZ4F1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD0TWM2OD1yLkS0NVk3KM7:TR?= Ml7RV2FPT0WU
K-562 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3SfZBPUUN3ME2wMlQ1QTZ5IN88US=> MVPTRW5ITVJ?
D-336MG M4HOWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHWx[YJKSzVyPUCuOVA{ODRizszN MX7TRW5ITVJ?
NOS-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwNkC1Nlkh|ryP Mn72V2FPT0WU
EW-24 NX7rcWJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW[yd|B{UUN3ME2wMlYzPjl|IN88US=> MoP3V2FPT0WU
BV-173 NUTOR5JZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LsVmlEPTB;MD62OVI1QSEQvF2= MYXTRW5ITVJ?
NCCIT NXTVd4tDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rTbWlEPTB;MD63N|IyQCEQvF2= NUHKZ25{W0GQR1XS
NCI-H1436 M2PWUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLCTWM2OD1yLke5NFQ6KM7:TR?= MorvV2FPT0WU
BB30-HNC M{OzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TrU2lEPTB;MD64OlIxOyEQvF2= M3frXHNCVkeHUh?=
TE-8 Moe2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITHTY5KSzVyPUCuPFczPzVizszN NX;kbVRrW0GQR1XS
A704 NFzLfnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LZ[WlEPTB;MD64PVIyKM7:TR?= NYP3cpUzW0GQR1XS
TK10 MlTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILPV5JKSzVyPUCuPVA3PjlizszN NVfYdmp3W0GQR1XS
KS-1 M2\CbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHwNoxKSzVyPUGuNVk4PzlizszN NXfm[VNIW0GQR1XS
C2BBe1 NWS3[VJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfZTWM2OD1zLkKwOVA4KM7:TR?= M{\6N3NCVkeHUh?=
RXF393 NX7OU2xUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFwMkSzOkDPxE1? M4G5VHNCVkeHUh?=
KGN MlzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjUTWM2OD1zLkK3Olg4KM7:TR?= MXrTRW5ITVJ?
NB69 NX;x[oQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfGTWM2OD1zLkO3OFk4KM7:TR?= NGLzUWNUSU6JRWK=
TE-11 MlnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPEZY9KSzVyPUGuOFM1OThizszN MXnTRW5ITVJ?
TE-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHT3OIxKSzVyPUGuOFQyODVizszN M{exSnNCVkeHUh?=
ST486 NHqzeWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jxS2lEPTB;MT60OVg2OiEQvF2= M3T5UXNCVkeHUh?=
HOP-62 NW\ieXFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{W5dGlEPTB;MT61NFI1PiEQvF2= NIHZ[ndUSU6JRWK=
EW-16 M{jCOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHZTWM2OD1zLkW1NFg{KM7:TR?= M3P4ZnNCVkeHUh?=
LB1047-RCC NUfGXW9TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTFwNUW0OVMh|ryP Mm\hV2FPT0WU
TE-10 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrGNlhKSzVyPUGuOlYzPTJizszN MUTTRW5ITVJ?
RL95-2 MmPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjQTWM2OD1zLk[2PVAzKM7:TR?= NX23[W1wW0GQR1XS
DOHH-2 M{Lscmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVftVHZ1UUN3ME2xMlcyPzh{IN88US=> MmSwV2FPT0WU
MFH-ino NULoeoQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG1TWM2OD1zLke3PFch|ryP M3vRUXNCVkeHUh?=
GB-1 NUTaZZY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTFwN{m4N|Mh|ryP MV;TRW5ITVJ?
SK-N-DZ M4LhOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrCTWM2OD1zLki0Olg5KM7:TR?= NXzw[mdtW0GQR1XS
OS-RC-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7KbXdKSzVyPUGuPFg2PzRizszN NWr2XHptW0GQR1XS
SW982 M3KxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrBd5dKSzVyPUGuPVIxQTNizszN M4L5cHNCVkeHUh?=
KALS-1 NWPYeVN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jFRWlEPTB;MT65PFczOiEQvF2= Mor1V2FPT0WU
TGBC24TKB NX3tdo5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJwMEW5OVgh|ryP NF:zXpVUSU6JRWK=
GI-1 NESwPI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4WzSWlEPTB;Mj6xOlA5PCEQvF2= NWi0[JhMW0GQR1XS
SW962 M4XoRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HEU2lEPTB;Mj6xO|E4QCEQvF2= NEnyN5BUSU6JRWK=
SW872 M{\0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LxW2lEPTB;Mj6xPFUxPyEQvF2= NYnVcIZ6W0GQR1XS
NCI-H747 NYjud2xTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFraZ|JKSzVyPUKuNlU4OTRizszN NG\CWWNUSU6JRWK=
MZ1-PC NGfKRopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH32bZVKSzVyPUKuNlk{PTZizszN NUXZSGo{W0GQR1XS
MSTO-211H Mn\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTJwM{W3NlMh|ryP MkSxV2FPT0WU
BL-70 NEXRT2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjNbVRKSzVyPUKuOFc1OjJizszN NYDydJJrW0GQR1XS
SW954 NWDuOJl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXOTWM2OD1{LkW3OFA5KM7:TR?= M3;PfXNCVkeHUh?=
SNB75 NX3NeWNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3VTWM2OD1{Lk[4OVk1KM7:TR?= MXzTRW5ITVJ?
IST-SL2 MkTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TpcmlEPTB;Mj63NlM4QSEQvF2= MmPJV2FPT0WU
GCIY NIPDWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzxS2tKSzVyPUKuPFcxODVizszN NVXnVnVKW0GQR1XS
KU812 NE\JcYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LRSmlEPTB;Mz6wOVI6QSEQvF2= MYnTRW5ITVJ?
LXF-289 MmLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTNwMUKxNFkh|ryP M{LETnNCVkeHUh?=
ETK-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHG[XdFUUN3ME2zMlIxPzZ5IN88US=> NGX5Xo5USU6JRWK=
SF126 NYHGbnYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoS5TWM2OD1|LkOxNVc1KM7:TR?= M370XHNCVkeHUh?=
LC-2-ad M2H3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rzXWlEPTB;Mz61OVch|ryP MWHTRW5ITVJ?
KNS-42 MlXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEX3[HFKSzVyPUOuOlUh|ryP MoTKV2FPT0WU
OVCAR-4 NYjiPWZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETWbZFKSzVyPUOuO|M1OzNizszN Mo\oV2FPT0WU
PF-382 NHTqOWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\QTWM2OD1|LkizOlk5KM7:TR?= NFL6N|lUSU6JRWK=
SH-4 M3LRcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULFdYhKUUN3ME20MlI2OjV7IN88US=> MnPYV2FPT0WU
KM12 MlWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvyTWM2OD12LkOyOFE3KM7:TR?= M{X6WnNCVkeHUh?=
NB5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LFfmlEPTB;ND60NVg3PCEQvF2= MljaV2FPT0WU
KURAMOCHI NGXIOJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTRwNkWyOVYh|ryP NVKwU3diW0GQR1XS
Becker MoLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vBVGlEPTB;ND62OlQyPiEQvF2= NEjrUW1USU6JRWK=
MV-4-11 M{\6b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTrTWM2OD12LkixN|Q1KM7:TR?= MoDXV2FPT0WU
KINGS-1 M1e5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTRwOEKzO|Mh|ryP NWXXcYJ{W0GQR1XS
LS-123 NVXMTYY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPuTWM2OD13LkS5Olg1KM7:TR?= M{DH[HNCVkeHUh?=
SF268 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTVwNkGyOlIh|ryP M3La[XNCVkeHUh?=
A388 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDBTWM2OD13Lk[zOlY4KM7:TR?= NHTzV|JUSU6JRWK=
NMC-G1 NYrT[m5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTZwMEG4NVEh|ryP NGTGdnVUSU6JRWK=
CGTH-W-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXKzRmZ2UUN3ME22MlAzODd3IN88US=> MnfZV2FPT0WU
ES4 NVzMU29UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGSxO|BKSzVyPU[uOVMxPzRizszN MXnTRW5ITVJ?
SR MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\uWIFKSzVyPU[uOVg5ODdizszN NWD2SHRJW0GQR1XS
BB49-HNC NUHTcmRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\ZbY9KSzVyPU[uO|MzODZizszN NYnCNXp[W0GQR1XS
KLE M3LBZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HiUGlEPTB;Nj63PFM4PyEQvF2= Ml7LV2FPT0WU
HUTU-80 Mn\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTZwOUi0OlYh|ryP M2rpSXNCVkeHUh?=
SNU-C2B MnLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HGVGlEPTB;Nz64Nlc{PyEQvF2= MWXTRW5ITVJ?
BB65-RCC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[xTWM2OD15Lkm0PVA1KM7:TR?= M{jONnNCVkeHUh?=
QIMR-WIL NXX5PI1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPqT5JKSzVyPUiuOFI5ODhizszN MmixV2FPT0WU
GDM-1 M1v5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDsPWxCUUN3ME24Mlk4Ojl{IN88US=> MnX2V2FPT0WU
LC4-1 Mln0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTlwMEC5NVEh|ryP NX;UNGhrW0GQR1XS
MLMA MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2naSGlEPTB;OT6xOVAxPiEQvF2= M2juTnNCVkeHUh?=
EoL-1-cell MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3DTpBlUUN3ME25MlMxOTl{IN88US=> MYHTRW5ITVJ?
BOKU M3vyVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnq3TWM2OD17Lkm2OFY3KM7:TR?= MoLZV2FPT0WU
EVSA-T NHX1UopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LPRmlEPTB;MUCuOlU3QCEQvF2= MWnTRW5ITVJ?
D-283MED NH7nNHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi1OG9KSzVyPUGwMlkyPzZizszN NXvKV2c4W0GQR1XS
NB1 M{fET2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\u[pVpUUN3ME2xNU4xOjR{IN88US=> MX7TRW5ITVJ?
RPMI-8402 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H5NGlEPTB;MUGuNVc5KM7:TR?= MWjTRW5ITVJ?
NCI-H1355 NYDQZ4xNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTwWpBKSzVyPUGxMlE5ODZizszN M1PHeXNCVkeHUh?=
NB7 MkPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTFzLkOyPVch|ryP MVnTRW5ITVJ?
RPMI-6666 NWLXdYxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTF{Lkm1Olch|ryP NI\vPG1USU6JRWK=
697 M{DXS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzjO5ZTUUN3ME2xN{4zPzBzIN88US=> M1;FS3NCVkeHUh?=
CTB-1 M{LxR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTF|LkW5OFgh|ryP NHHNSJBUSU6JRWK=
VA-ES-BJ MnvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TqfWlEPTB;MUOuPVI{PCEQvF2= NHrHSphUSU6JRWK=
BE-13 MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfNZmRUUUN3ME2xOE4{QTF3IN88US=> M4G2XHNCVkeHUh?=
SKM-1 NYO5VoF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4i3PWlEPTB;MUSuOFQ6QSEQvF2= MV3TRW5ITVJ?
TE-6 Mlm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;lO2lEPTB;MUSuO|U6OSEQvF2= NXqzfJRYW0GQR1XS
LB771-HNC NUP6boRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTFcnFKSzVyPUG0Mlc5QThizszN NIPmS2pUSU6JRWK=
ECC4 Ml:yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHi2fY1KSzVyPUG3MlAzPzdizszN MoXKV2FPT0WU
ES3 NH:0S4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlH5TWM2OD1zNz60OlU2KM7:TR?= MnPPV2FPT0WU
LB647-SCLC MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M135fGlEPTB;MUeuOFk1QSEQvF2= MVXTRW5ITVJ?
NB10 NGfsTZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;u[5BKSzVyPUG4MlUzPTZizszN MVTTRW5ITVJ?
L-540 M1rGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK4d|RWUUN3ME2xPE45OTB7IN88US=> M2O5T3NCVkeHUh?=
NCI-H2126 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vPUWlEPTB;MUmuOVEh|ryP NF3re5FUSU6JRWK=
HH MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;adlRjUUN3ME2yNE4xODl7IN88US=> NVzlRZR1W0GQR1XS
MPP-89 Mn;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofLTWM2OD1{Mz6yNlg6KM7:TR?= NHTQb2RUSU6JRWK=
IST-MEL1 M4X1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PtWmlEPTB;MkOuPFY2QCEQvF2= MYrTRW5ITVJ?
KP-N-YS NEDzVYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfXTWM2OD1{Mz65NlU2KM7:TR?= NVjZRZB3W0GQR1XS
EC-GI-10 Mon4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGK5VmtKSzVyPUK0MlU6QDlizszN M2\rNnNCVkeHUh?=
EKVX MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;TVoNqUUN3ME2yOk4xOjB|IN88US=> M1L0[XNCVkeHUh?=
TGBC1TKB NF\FO3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\BUWlEPTB;Mk[uOFM1KM7:TR?= NInqSWxUSU6JRWK=
Daudi NIizVm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfaTWM2OD1{Nz6wO|c{KM7:TR?= MY\TRW5ITVJ?
ALL-PO MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILLbZVKSzVyPUK3MlA5OSEQvF2= M2i3PXNCVkeHUh?=
NB6 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPjWnNkUUN3ME2yO{41QDhizszN MmLDV2FPT0WU
ES6 M{LiUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJ5LkmxNlMh|ryP NGrUZZFUSU6JRWK=
COLO-320-HSR NInrWYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTtV|B5UUN3ME2yPE4xOzd|IN88US=> MWXTRW5ITVJ?
K5 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjESZZKSzVyPUK4MlEzQDdizszN NIXaXldUSU6JRWK=
ES1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULoe4pwUUN3ME2yPE44Pzd|IN88US=> M13wR3NCVkeHUh?=
LC-1F NV[4R201T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTJ7LkezOFYh|ryP MXvTRW5ITVJ?
SCLC-21H NGmzZnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rpS2lEPTB;M{CuO|MyPyEQvF2= M{HIVHNCVkeHUh?=
SK-PN-DW MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml2zTWM2OD1|Mj61OVk5KM7:TR?= M{XjenNCVkeHUh?=
D-247MG NGP0TYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTN{Lkm3O|Mh|ryP MUDTRW5ITVJ?
TE-5 MkPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXyepB2UUN3ME2zN{4xOzZ{IN88US=> MYDTRW5ITVJ?
MONO-MAC-6 M1jzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17IfGlEPTB;M{OuOVA1QCEQvF2= MUnTRW5ITVJ?
LB2518-MEL NXLr[4NkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkG1TWM2OD1|Mz63OlY3KM7:TR?= Mn71V2FPT0WU
LOXIMVI NEfkNJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDNOZc2UUN3ME2zN{44QTJ6IN88US=> NILnPGZUSU6JRWK=
NCI-H209 M2W1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTN3LkG0OEDPxE1? M1jMNnNCVkeHUh?=
A253 NHjJNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPxRlRQUUN3ME2zOU44PDJ7IN88US=> MV;TRW5ITVJ?
HCC1599 NUHRdXNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K5bGlEPTB;M{[uO|A2OyEQvF2= MY\TRW5ITVJ?
EB-3 MnLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTN4Lkm1NVgh|ryP MYjTRW5ITVJ?
GOTO M1f4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTN5LkOyNlQh|ryP M3TVXnNCVkeHUh?=
SW684 MnvrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PXVGlEPTB;NEGuPFQ6PSEQvF2= MXLTRW5ITVJ?
DEL MnPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX36XFlQUUN3ME20Nk4xPTJ{IN88US=> MWfTRW5ITVJ?
HT-144 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TJWGlEPTB;NEKuNVY4PiEQvF2= MYrTRW5ITVJ?
TE-9 NWTFVZFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrQNW4yUUN3ME20N{41PTl4IN88US=> MmTlV2FPT0WU
KARPAS-45 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HpeWlEPTB;NESuN|kzPSEQvF2= MkX4V2FPT0WU
HAL-01 M2jkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq0TWM2OD12ND61NFM1KM7:TR?= MX\TRW5ITVJ?
RCC10RGB NHH4d3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\4[G5KSzVyPUS0Mlc{QTJizszN NX3xbW9nW0GQR1XS
CP67-MEL M{\JdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTR3Lk[yOFEh|ryP NY\CZVJKW0GQR1XS
NB17 NETMZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml72TWM2OD12NT62OlQ{KM7:TR?= MUDTRW5ITVJ?
SK-UT-1 NFrP[I9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;GcYRKSzVyPUS1Mlk1PjRizszN NEjYbZFUSU6JRWK=
JiyoyeP-2003 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPCclJQUUN3ME20Ok4xOTF7IN88US=> NVTpV4dzW0GQR1XS
HCE-4 NUnRR2htT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTR4LkW5Olgh|ryP NFGz[5pUSU6JRWK=
NCI-H720 NWLHbZVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz5b5RKSzVyPUS2Mlc3QDJizszN MYrTRW5ITVJ?
KARPAS-422 NXG5N4Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vIWmlEPTB;NEeuNFg6PSEQvF2= MlvFV2FPT0WU
Ramos-2G6-4C10 M1;JU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlL5TWM2OD12Nz6xOlIzKM7:TR?= M4izWnNCVkeHUh?=
HCE-T NGjwSo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDaXZlJUUN3ME20O{43QDJ6IN88US=> MXjTRW5ITVJ?
PSN1 NYfNT4t3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTR5Lke4NVMh|ryP MljRV2FPT0WU

... 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:
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
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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    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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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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID