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 NIriNZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;h[lRKSzVyPUCuNFYyPDNizszN NFPnNYVUSU6JRWK=
LAMA-84 M1;uSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\CTWM2OD1yLkG1PVkh|ryP Mk\sV2FPT0WU
MEG-01 NIXaWXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTBwMkO2PFgh|ryP NXfsfZVxW0GQR1XS
EM-2 NFLNNm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHTRZpKSzVyPUCuNlY2KM7:TR?= MVrTRW5ITVJ?
TE-15 NWLvOYRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3FNYVQUUN3ME2wMlI4PDF{IN88US=> NGLRcoRUSU6JRWK=
NCI-H1648 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwMkixNVYh|ryP NF;od3VUSU6JRWK=
TE-12 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwM{K2PEDPxE1? NX3YPHlMW0GQR1XS
LB996-RCC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELWR2xKSzVyPUCuOFQyQTZizszN MWjTRW5ITVJ?
K-562 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\JWGlEPTB;MD60OFk3PyEQvF2= NH72UnZUSU6JRWK=
D-336MG MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;xfllKSzVyPUCuOVA{ODRizszN MkLDV2FPT0WU
NOS-1 NXLLU|dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP5bXcyUUN3ME2wMlYxPTJ7IN88US=> NHezUlNUSU6JRWK=
EW-24 MnjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLZZ3BYUUN3ME2wMlYzPjl|IN88US=> MljPV2FPT0WU
BV-173 NIPLfGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELPUmlKSzVyPUCuOlUzPDlizszN MVfTRW5ITVJ?
NCCIT MkXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PQU2lEPTB;MD63N|IyQCEQvF2= NI[2UlJUSU6JRWK=
NCI-H1436 NHX3V2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HDdWlEPTB;MD63PVA1QSEQvF2= M3fyfXNCVkeHUh?=
BB30-HNC Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnTcpJLUUN3ME2wMlg3OjB|IN88US=> MVjTRW5ITVJ?
TE-8 NY\ZTJdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwOEeyO|Uh|ryP MWnTRW5ITVJ?
A704 MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXj4dnlyUUN3ME2wMlg6OjFizszN MlzYV2FPT0WU
TK10 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTZZ2pKSzVyPUCuPVA3PjlizszN MXnTRW5ITVJ?
KS-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjmTWM2OD1zLkG5O|c6KM7:TR?= NF35fXRUSU6JRWK=
C2BBe1 NHLxd3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPUS|E1UUN3ME2xMlIxPTB5IN88US=> M3TmfXNCVkeHUh?=
RXF393 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF6xdI5KSzVyPUGuNlQ{PiEQvF2= NHzMWlBUSU6JRWK=
KGN NVHOUoxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPSN2dKSzVyPUGuNlc3QDdizszN MWrTRW5ITVJ?
NB69 NX3tfJprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHhNnlKSzVyPUGuN|c1QTdizszN MWHTRW5ITVJ?
TE-11 MofQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXIbnZKSzVyPUGuOFM1OThizszN MXjTRW5ITVJ?
TE-1 MljKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLlPWZKSzVyPUGuOFQyODVizszN MlHiV2FPT0WU
ST486 MmX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrTTWM2OD1zLkS1PFUzKM7:TR?= NHf0TJNUSU6JRWK=
HOP-62 MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTFwNUCyOFYh|ryP NH3mWGdUSU6JRWK=
EW-16 NIHG[VhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLhXoZ[UUN3ME2xMlU2ODh|IN88US=> M3juXnNCVkeHUh?=
LB1047-RCC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1KzUGlEPTB;MT61OVQ2OyEQvF2= M1Tmd3NCVkeHUh?=
TE-10 MkjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\GTWM2OD1zLk[2NlUzKM7:TR?= M32xZnNCVkeHUh?=
RL95-2 NFXGb25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXifVJYUUN3ME2xMlY3QTB{IN88US=> NUS2cJdUW0GQR1XS
DOHH-2 MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqwTWM2OD1zLkexO|gzKM7:TR?= NIP4WWdUSU6JRWK=
MFH-ino M4DxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO5TWM2OD1zLke3PFch|ryP NEXCfFRUSU6JRWK=
GB-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFztcWJKSzVyPUGuO|k5OzNizszN NGfpOoJUSU6JRWK=
SK-N-DZ NVrkdFd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTCTVNFUUN3ME2xMlg1Pjh6IN88US=> MWrTRW5ITVJ?
OS-RC-2 NUP3VIRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3yzfWlEPTB;MT64PFU4PCEQvF2= MWfTRW5ITVJ?
SW982 NH;IdYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwOUKwPVMh|ryP NHG2d2VUSU6JRWK=
KALS-1 M2HjPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfmTWxQUUN3ME2xMlk5PzJ{IN88US=> NGTxTppUSU6JRWK=
TGBC24TKB MnTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fDc2lEPTB;Mj6wOVk2QCEQvF2= M4jG[3NCVkeHUh?=
GI-1 M4LIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq1TWM2OD1{LkG2NFg1KM7:TR?= M2\Hc3NCVkeHUh?=
SW962 NEHvOFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nkZ2lEPTB;Mj6xO|E4QCEQvF2= M2P4[nNCVkeHUh?=
SW872 MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTJwMUi1NFch|ryP Mn7pV2FPT0WU
NCI-H747 MlzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHhTWM2OD1{LkK1O|E1KM7:TR?= MXfTRW5ITVJ?
MZ1-PC M1Kyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;WemlEPTB;Mj6yPVM2PiEQvF2= Mm\aV2FPT0WU
MSTO-211H NYjHcpZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmmwTWM2OD1{LkO1O|I{KM7:TR?= MWjTRW5ITVJ?
BL-70 NYrJU2drT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HMbGlEPTB;Mj60O|QzOiEQvF2= M3jkcHNCVkeHUh?=
SW954 NV;MW|k{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXBTWM2OD1{LkW3OFA5KM7:TR?= NWPkOnd5W0GQR1XS
SNB75 NYnU[5h1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTJwNki1PVQh|ryP MkXxV2FPT0WU
IST-SL2 NWPZfWlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLMc25KSzVyPUKuO|I{PzlizszN NXLvWHloW0GQR1XS
GCIY M1jze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LtXWlEPTB;Mj64O|AxPSEQvF2= MXPTRW5ITVJ?
KU812 MlPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1OyPWlEPTB;Mz6wOVI6QSEQvF2= M2LDOXNCVkeHUh?=
LXF-289 NUK5PFdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TyT2lEPTB;Mz6xNlExQSEQvF2= MV;TRW5ITVJ?
ETK-1 NWq3fmM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoOwTWM2OD1|LkKwO|Y4KM7:TR?= M2PxPXNCVkeHUh?=
SF126 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTNwM{GxO|Qh|ryP MYfTRW5ITVJ?
LC-2-ad MnPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\yTWM2OD1|LkW1O{DPxE1? MXjTRW5ITVJ?
KNS-42 NUfVSXJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfw[4JKSzVyPUOuOlUh|ryP NUCybXJDW0GQR1XS
OVCAR-4 MnXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHvTWM2OD1|LkezOFM{KM7:TR?= M2jzdnNCVkeHUh?=
PF-382 MmrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTNwOEO2PVgh|ryP M4fQcXNCVkeHUh?=
SH-4 MkHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITveZdKSzVyPUSuNlUzPTlizszN M37qOnNCVkeHUh?=
KM12 NWfUXJpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Pnb2lEPTB;ND6zNlQyPiEQvF2= NV\qNWpjW0GQR1XS
NB5 M3;BT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPJO4ZKSzVyPUSuOFE5PjRizszN NGK4NIVUSU6JRWK=
KURAMOCHI MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MliyTWM2OD12Lk[1NlU3KM7:TR?= MV7TRW5ITVJ?
Becker MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe1Z4JJUUN3ME20MlY3PDF4IN88US=> NYXrOpJRW0GQR1XS
MV-4-11 NUjHTmtvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn6TWM2OD12LkixN|Q1KM7:TR?= NUPYbWRmW0GQR1XS
KINGS-1 NHzJcZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjVSJVJUUN3ME20MlgzOzd|IN88US=> M3HyT3NCVkeHUh?=
LS-123 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:yTWM2OD13LkS5Olg1KM7:TR?= NVzvXHdNW0GQR1XS
SF268 M4DBfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfGZ4FKSzVyPUWuOlEzPjJizszN NIjxeFFUSU6JRWK=
A388 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\PNJFrUUN3ME21MlY{PjZ5IN88US=> NGjkWZVUSU6JRWK=
NMC-G1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHpTWM2OD14LkCxPFEyKM7:TR?= NFG5WnFUSU6JRWK=
CGTH-W-1 NGrJcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzvTWM2OD14LkCyNFc2KM7:TR?= MW\TRW5ITVJ?
ES4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzQTWM2OD14LkWzNFc1KM7:TR?= MknDV2FPT0WU
SR NYLDfnNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojrTWM2OD14LkW4PFA4KM7:TR?= NFfvV3hUSU6JRWK=
BB49-HNC NGXuUnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPEZ5k{UUN3ME22Mlc{OjB4IN88US=> MYfTRW5ITVJ?
KLE NIThSHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTZwN{izO|ch|ryP MoHxV2FPT0WU
HUTU-80 NW\oTWZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTZwOUi0OlYh|ryP M1zxcHNCVkeHUh?=
SNU-C2B M4LBfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[ybJZKSzVyPUeuPFI4OzdizszN Ml60V2FPT0WU
BB65-RCC M3LId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjPTWM2OD15Lkm0PVA1KM7:TR?= NHfRUWRUSU6JRWK=
QIMR-WIL NGruXFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRThwNEK4NFgh|ryP MmOwV2FPT0WU
GDM-1 NFG2dZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTjTWM2OD16Lkm3NlkzKM7:TR?= M3;LZ3NCVkeHUh?=
LC4-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTlwMEC5NVEh|ryP M{nqTXNCVkeHUh?=
MLMA MlvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnxc4RKSzVyPUmuNVUxODZizszN M{jUOnNCVkeHUh?=
EoL-1-cell NVXGUnJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUT0XJFiUUN3ME25MlMxOTl{IN88US=> MYrTRW5ITVJ?
BOKU Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\FTWM2OD17Lkm2OFY3KM7:TR?= NHKzT|lUSU6JRWK=
EVSA-T MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnKTWM2OD1zMD62OVY5KM7:TR?= MU\TRW5ITVJ?
D-283MED MnvsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUC5SYpkUUN3ME2xNE46OTd4IN88US=> MYHTRW5ITVJ?
NB1 NWPMZ2FJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFzLkCyOFIh|ryP NWLFO|BPW0GQR1XS
RPMI-8402 M4XERWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHxTWM2OD1zMT6xO|gh|ryP NVXCUXhnW0GQR1XS
NCI-H1355 NIOzUWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFzLkG4NFYh|ryP M3PuTHNCVkeHUh?=
NB7 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPFTWM2OD1zMT6zNlk4KM7:TR?= NH3GeW1USU6JRWK=
RPMI-6666 M4\BcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLhOY1ZUUN3ME2xNk46PTZ5IN88US=> M1v0TnNCVkeHUh?=
697 Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz0T5l[UUN3ME2xN{4zPzBzIN88US=> NUTZO|lGW0GQR1XS
CTB-1 NFjMNJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfqTWM2OD1zMz61PVQ5KM7:TR?= M4W2eXNCVkeHUh?=
VA-ES-BJ M3GxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTF|LkmyN|Qh|ryP NFLHR5lUSU6JRWK=
BE-13 NXzqSmZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTFUY1{UUN3ME2xOE4{QTF3IN88US=> M3nQbHNCVkeHUh?=
SKM-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3UfmFKSzVyPUG0MlQ1QTlizszN NEfYR4hUSU6JRWK=
TE-6 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTF2Lke1PVEh|ryP M2q1bnNCVkeHUh?=
LB771-HNC MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHGTWM2OD1zND63PFk5KM7:TR?= NUTCUYtxW0GQR1XS
ECC4 NVr6RZd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\zfWQzUUN3ME2xO{4xOjd5IN88US=> NIHEWVJUSU6JRWK=
ES3 Mk\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTF5LkS2OVUh|ryP MUTTRW5ITVJ?
LB647-SCLC MmraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjwUXlKSzVyPUG3MlQ6PDlizszN MoDWV2FPT0WU
NB10 NFm2W25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvNTWM2OD1zOD61NlU3KM7:TR?= Mn7uV2FPT0WU
L-540 M2fJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknKTWM2OD1zOD64NVA6KM7:TR?= Mni1V2FPT0WU
NCI-H2126 MnrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\tTWM2OD1zOT61NUDPxE1? MofNV2FPT0WU
HH MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnGxTWM2OD1{MD6wNFk6KM7:TR?= NX:1UG1zW0GQR1XS
MPP-89 Mnm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3IcYVJUUN3ME2yN{4zOjh7IN88US=> MUHTRW5ITVJ?
IST-MEL1 NHXZWYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLLNFBKSzVyPUKzMlg3PThizszN MXLTRW5ITVJ?
KP-N-YS NHH3XY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmC4TWM2OD1{Mz65NlU2KM7:TR?= MXjTRW5ITVJ?
EC-GI-10 NEDIPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTJ2LkW5PFkh|ryP NV7GVGdPW0GQR1XS
EKVX MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T2VGlEPTB;Mk[uNFIxOyEQvF2= NX22[oo4W0GQR1XS
TGBC1TKB NVW4TYh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTJ4LkSzOEDPxE1? MXXTRW5ITVJ?
Daudi Mo[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmn2TWM2OD1{Nz6wO|c{KM7:TR?= MnixV2FPT0WU
ALL-PO NFvHOI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H1bGlEPTB;MkeuNFgyKM7:TR?= NXOwUFk3W0GQR1XS
NB6 MljhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjDPINKSzVyPUK3MlQ5QCEQvF2= MnztV2FPT0WU
ES6 NXzxUlF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnPbpNKSzVyPUK3MlkyOjNizszN NW[3XphUW0GQR1XS
COLO-320-HSR MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHCTWM2OD1{OD6wN|c{KM7:TR?= M1zBdnNCVkeHUh?=
K5 NFjRNXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nWTmlEPTB;MkiuNVI5PyEQvF2= MoO4V2FPT0WU
ES1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;KZpQ3UUN3ME2yPE44Pzd|IN88US=> NWHpOXFqW0GQR1XS
LC-1F M4LFdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIftbGZKSzVyPUK5Mlc{PDZizszN M3O5VHNCVkeHUh?=
SCLC-21H MoCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTNyLkezNVch|ryP NXH4c286W0GQR1XS
SK-PN-DW M{fzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PUbGlEPTB;M{KuOVU6QCEQvF2= NWqwXpJjW0GQR1XS
D-247MG NHn5O4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TOXWlEPTB;M{KuPVc4OyEQvF2= NUPPVGd2W0GQR1XS
TE-5 NYTrd4R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW4c4dkUUN3ME2zN{4xOzZ{IN88US=> MXTTRW5ITVJ?
MONO-MAC-6 NVHRcI15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnudlJKSzVyPUOzMlUxPDhizszN MlHYV2FPT0WU
LB2518-MEL NGi0NG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTN|Lke2OlYh|ryP MWrTRW5ITVJ?
LOXIMVI MmLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnSTWM2OD1|Mz63PVI5KM7:TR?= MYrTRW5ITVJ?
NCI-H209 MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnzbWE5UUN3ME2zOU4yPDRizszN NH\kXYNUSU6JRWK=
A253 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi2PFlqUUN3ME2zOU44PDJ7IN88US=> NGLifJdUSU6JRWK=
HCC1599 MoXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvUTWM2OD1|Nj63NFU{KM7:TR?= NH;3UlJUSU6JRWK=
EB-3 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7WTWM2OD1|Nj65OVE5KM7:TR?= MofpV2FPT0WU
GOTO NH\CRmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF72V3JKSzVyPUO3MlMzOjRizszN MULTRW5ITVJ?
SW684 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L6OmlEPTB;NEGuPFQ6PSEQvF2= NYj0eVRnW0GQR1XS
DEL MkHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILQV41KSzVyPUSyMlA2OjJizszN NEDG[XlUSU6JRWK=
HT-144 M3PlZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjFNZhKSzVyPUSyMlE3PzZizszN MYHTRW5ITVJ?
TE-9 M{nPZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33jNmlEPTB;NEOuOFU6PiEQvF2= NUjXRZFnW0GQR1XS
KARPAS-45 NHXmTGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r5bmlEPTB;NESuN|kzPSEQvF2= NEnSUFdUSU6JRWK=
HAL-01 NHjacnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1yxe2lEPTB;NESuOVA{PCEQvF2= MoL4V2FPT0WU
RCC10RGB M3XLcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTR2LkezPVIh|ryP NWexS|RDW0GQR1XS
CP67-MEL MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITuUndKSzVyPUS1MlYzPDFizszN MYDTRW5ITVJ?
NB17 M1;pRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrXVlZkUUN3ME20OU43PjR|IN88US=> NUPyXVlsW0GQR1XS
SK-UT-1 M2PZRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETvbFZKSzVyPUS1Mlk1PjRizszN NI\rOYJUSU6JRWK=
JiyoyeP-2003 NVWy[ohkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nT[WlEPTB;NE[uNFEyQSEQvF2= MknqV2FPT0WU
HCE-4 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\ZN2lEPTB;NE[uOVk3QCEQvF2= MoX1V2FPT0WU
NCI-H720 MkfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTR4Lke2PFIh|ryP NGG0T5BUSU6JRWK=
KARPAS-422 M2DtbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorlTWM2OD12Nz6wPFk2KM7:TR?= MWDTRW5ITVJ?
Ramos-2G6-4C10 Mof2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTR5LkG2NlIh|ryP Mkm0V2FPT0WU
HCE-T NYTxNZJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HZNWlEPTB;NEeuOlgzQCEQvF2= MVTTRW5ITVJ?
PSN1 M2nMdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\iWoVQUUN3ME20O{44QDF|IN88US=> MUHTRW5ITVJ?

... 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 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
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 )

  • 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):
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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

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