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 MnrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwME[xOFMh|ryP M1myeXNCVkeHUh?=
LAMA-84 M2OxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7jOmlxUUN3ME2wMlE2QTlizszN Mn:yV2FPT0WU
MEG-01 NULVRXVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwMkO2PFgh|ryP MlvOV2FPT0WU
EM-2 NHjFZ45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwMk[1JO69VQ>? NEHUZYRUSU6JRWK=
TE-15 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnPTWM2OD1yLkK3OFEzKM7:TR?= NXjRVYJ5W0GQR1XS
NCI-H1648 NInLTmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L2W2lEPTB;MD6yPFEyPiEQvF2= NGL6dWpUSU6JRWK=
TE-12 MnL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnsTWM2OD1yLkOyOlgh|ryP NWLEb49xW0GQR1XS
LB996-RCC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M335T2lEPTB;MD60OFE6PiEQvF2= MV\TRW5ITVJ?
K-562 NInUTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7ITWM2OD1yLkS0PVY4KM7:TR?= M3vJT3NCVkeHUh?=
D-336MG NUC5O4tlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2D1N2lEPTB;MD61NFMxPCEQvF2= MULTRW5ITVJ?
NOS-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPVTWM2OD1yLk[wOVI6KM7:TR?= M{LMOHNCVkeHUh?=
EW-24 NUjOV4Y6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;vOGlEPTB;MD62NlY6OyEQvF2= NVPDfVRCW0GQR1XS
BV-173 MmLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjoepBXUUN3ME2wMlY2OjR7IN88US=> MXHTRW5ITVJ?
NCCIT NEXCXplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfGO4xKSzVyPUCuO|MzOThizszN NFrRd21USU6JRWK=
NCI-H1436 Ml\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\rZ4RKSzVyPUCuO|kxPDlizszN NFPqT|RUSU6JRWK=
BB30-HNC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHzTVgxUUN3ME2wMlg3OjB|IN88US=> M2G5XnNCVkeHUh?=
TE-8 NFXLWlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TPfmlEPTB;MD64O|I4PSEQvF2= NX;kUJVzW0GQR1XS
A704 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTBwOEmyNUDPxE1? MUPTRW5ITVJ?
TK10 M4fzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTBwOUC2Olkh|ryP NVzMVpNoW0GQR1XS
KS-1 NWnK[4N5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDrSXFKSzVyPUGuNVk4PzlizszN NVvQXmZRW0GQR1XS
C2BBe1 NX20NZVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PoVWlEPTB;MT6yNFUxPyEQvF2= M{XidXNCVkeHUh?=
RXF393 MnLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwMkSzOkDPxE1? Ml;zV2FPT0WU
KGN NHjqSnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[3WmlEPTB;MT6yO|Y5PyEQvF2= NFHLOWdUSU6JRWK=
NB69 NYLsPXVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nPcWlEPTB;MT6zO|Q6PyEQvF2= NEf4dYtUSU6JRWK=
TE-11 Mni3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[xTWM2OD1zLkSzOFE5KM7:TR?= MknZV2FPT0WU
TE-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPHRnBKSzVyPUGuOFQyODVizszN NUDZV5llW0GQR1XS
ST486 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX65dYJ{UUN3ME2xMlQ2QDV{IN88US=> NHjoOpZUSU6JRWK=
HOP-62 M{PzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG1[|lxUUN3ME2xMlUxOjR4IN88US=> NED5WHVUSU6JRWK=
EW-16 M2\wVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfUSmdKSzVyPUGuOVUxQDNizszN NWXpcXFnW0GQR1XS
LB1047-RCC NXLlV2p{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LJZmlEPTB;MT61OVQ2OyEQvF2= MlrRV2FPT0WU
TE-10 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnK0TWM2OD1zLk[2NlUzKM7:TR?= MonSV2FPT0WU
RL95-2 MkL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFwNk[5NFIh|ryP NVTCbmx{W0GQR1XS
DOHH-2 M1SzUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFS3d5VKSzVyPUGuO|E4QDJizszN M3fDXnNCVkeHUh?=
MFH-ino NWXvNnN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFwN{e4O{DPxE1? MlTjV2FPT0WU
GB-1 MoLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HmOWlEPTB;MT63PVg{OyEQvF2= M1zicnNCVkeHUh?=
SK-N-DZ MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGm1SG5KSzVyPUGuPFQ3QDhizszN MkXWV2FPT0WU
OS-RC-2 NUPzZpFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFwOEi1O|Qh|ryP NIXoU4JUSU6JRWK=
SW982 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDXTWM2OD1zLkmyNFk{KM7:TR?= MU\TRW5ITVJ?
KALS-1 M4fjPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzPWnZKSzVyPUGuPVg4OjJizszN NVezdXNbW0GQR1XS
TGBC24TKB NUL6bmlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzZNJlKSzVyPUKuNFU6PThizszN MmXhV2FPT0WU
GI-1 M3TBSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJwMU[wPFQh|ryP MWnTRW5ITVJ?
SW962 NEC5e|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fm[WlEPTB;Mj6xO|E4QCEQvF2= NWrK[2FVW0GQR1XS
SW872 MoPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn1bopIUUN3ME2yMlE5PTB5IN88US=> Mn7OV2FPT0WU
NCI-H747 NEPie|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTJwMkW3NVQh|ryP NEDxNVBUSU6JRWK=
MZ1-PC Mn[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jmUmlEPTB;Mj6yPVM2PiEQvF2= NVXLPZZ3W0GQR1XS
MSTO-211H NEDUeJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\udJRmUUN3ME2yMlM2PzJ|IN88US=> M1zSZnNCVkeHUh?=
BL-70 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzPTWM2OD1{LkS3OFIzKM7:TR?= MUXTRW5ITVJ?
SW954 NX30UnFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfKVZJKSzVyPUKuOVc1ODhizszN NXvrOGg6W0GQR1XS
SNB75 MoD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXIb3FKSzVyPUKuOlg2QTRizszN NUTV[ZFxW0GQR1XS
IST-SL2 MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\RPGlEPTB;Mj63NlM4QSEQvF2= M{\YWnNCVkeHUh?=
GCIY Mny3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnkdlVKSzVyPUKuPFcxODVizszN NUnQ[YNlW0GQR1XS
KU812 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfQdJNTUUN3ME2zMlA2Ojl7IN88US=> NIPpNHpUSU6JRWK=
LXF-289 M3jMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXueYxKSzVyPUOuNVIyODlizszN MnzTV2FPT0WU
ETK-1 MmS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVThVnc4UUN3ME2zMlIxPzZ5IN88US=> NU\XSI1YW0GQR1XS
SF126 MljpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjXTWM2OD1|LkOxNVc1KM7:TR?= MkDxV2FPT0WU
LC-2-ad MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnZXXJuUUN3ME2zMlU2PyEQvF2= NH\NcoxUSU6JRWK=
KNS-42 NGLPeW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDiTWM2OD1|Lk[1JO69VQ>? MYHTRW5ITVJ?
OVCAR-4 NGn1TmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH6TWM2OD1|LkezOFM{KM7:TR?= M4mzSXNCVkeHUh?=
PF-382 M1\5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILP[G5KSzVyPUOuPFM3QThizszN NYTSdHRWW0GQR1XS
SH-4 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17EW2lEPTB;ND6yOVI2QSEQvF2= MXTTRW5ITVJ?
KM12 M2TxOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzpPZU{UUN3ME20MlMzPDF4IN88US=> MmTVV2FPT0WU
NB5 NECyU2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTRwNEG4OlQh|ryP Mlm1V2FPT0WU
KURAMOCHI MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLnTWM2OD12Lk[1NlU3KM7:TR?= MlHjV2FPT0WU
Becker MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLkTWM2OD12Lk[2OFE3KM7:TR?= MVfTRW5ITVJ?
MV-4-11 NWiwR3RJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vjR2lEPTB;ND64NVM1PCEQvF2= NV:4WppXW0GQR1XS
KINGS-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTCTnk1UUN3ME20MlgzOzd|IN88US=> M2\hfHNCVkeHUh?=
LS-123 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG4TWM2OD13LkS5Olg1KM7:TR?= MVfTRW5ITVJ?
SF268 NELPVpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XpdGlEPTB;NT62NVI3OiEQvF2= NGDQSIpUSU6JRWK=
A388 NEixUGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4izV2lEPTB;NT62N|Y3PyEQvF2= NX;Z[oN1W0GQR1XS
NMC-G1 M1zJRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTZwMEG4NVEh|ryP NU\WR2tvW0GQR1XS
CGTH-W-1 NX3JfIc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPNcG9WUUN3ME22MlAzODd3IN88US=> MkDiV2FPT0WU
ES4 NIX0cHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWP1O|FFUUN3ME22MlU{ODd2IN88US=> MV3TRW5ITVJ?
SR MkPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XGOWlEPTB;Nj61PFgxPyEQvF2= MljpV2FPT0WU
BB49-HNC MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TnfmlEPTB;Nj63N|IxPiEQvF2= MoPRV2FPT0WU
KLE MknMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTZwN{izO|ch|ryP M1nodnNCVkeHUh?=
HUTU-80 M{jNbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTZwOUi0OlYh|ryP M{\J[XNCVkeHUh?=
SNU-C2B M2\ORWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTdwOEK3N|ch|ryP NXfEOYUxW0GQR1XS
BB65-RCC M3\mXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTdwOUS5NFQh|ryP NEnqR|lUSU6JRWK=
QIMR-WIL NWHZXmRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHVTWM2OD16LkSyPFA5KM7:TR?= NGfqNWFUSU6JRWK=
GDM-1 NGfoeYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fSXmlEPTB;OD65O|I6OiEQvF2= MWTTRW5ITVJ?
LC4-1 MnzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HKfGlEPTB;OT6wNFkyOSEQvF2= NEi5Z|RUSU6JRWK=
MLMA MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPXcXVKSzVyPUmuNVUxODZizszN NYD1TnZ{W0GQR1XS
EoL-1-cell MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrOTWM2OD17LkOwNVkzKM7:TR?= MorqV2FPT0WU
BOKU M3\kU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTlwOU[0OlYh|ryP MmHXV2FPT0WU
EVSA-T NFLBNGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\tTWM2OD1zMD62OVY5KM7:TR?= M4W5eHNCVkeHUh?=
D-283MED NETZZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zHfGlEPTB;MUCuPVE4PiEQvF2= MmL5V2FPT0WU
NB1 M{jyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFzLkCyOFIh|ryP Mn;HV2FPT0WU
RPMI-8402 NVLRcXVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\VcZpKSzVyPUGxMlE4QCEQvF2= MWPTRW5ITVJ?
NCI-H1355 MofGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvjNIx2UUN3ME2xNU4yQDB4IN88US=> NY[wflE6W0GQR1XS
NB7 NF;mc2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFzLkOyPVch|ryP NWi4dGVVW0GQR1XS
RPMI-6666 NFr3SHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[wVWlEPTB;MUKuPVU3PyEQvF2= NH;QXW5USU6JRWK=
697 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfV[JhKSzVyPUGzMlI4ODFizszN MWDTRW5ITVJ?
CTB-1 NUfWbJMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF|LkW5OFgh|ryP MUPTRW5ITVJ?
VA-ES-BJ M4r1c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvDZ21KSzVyPUGzMlkzOzRizszN NF7BT5BUSU6JRWK=
BE-13 Ml;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWOzWYNOUUN3ME2xOE4{QTF3IN88US=> NIfSSHNUSU6JRWK=
SKM-1 M3nrT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TkdGlEPTB;MUSuOFQ6QSEQvF2= NEXzS2xUSU6JRWK=
TE-6 M1fTWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkCzTWM2OD1zND63OVkyKM7:TR?= M4PQNnNCVkeHUh?=
LB771-HNC NUO3SItCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXpU3VKSzVyPUG0Mlc5QThizszN NICySVdUSU6JRWK=
ECC4 NFnoRmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDxTWM2OD1zNz6wNlc4KM7:TR?= MYLTRW5ITVJ?
ES3 NED6PYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjiTWM2OD1zNz60OlU2KM7:TR?= NXLEUFQ3W0GQR1XS
LB647-SCLC NUXUXmxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\hNm1KSzVyPUG3MlQ6PDlizszN NW\PVnZSW0GQR1XS
NB10 MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTF6LkWyOVYh|ryP MoDvV2FPT0WU
L-540 M2LK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTF6LkixNFkh|ryP NXvlNIJRW0GQR1XS
NCI-H2126 NHS1b2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvDdGhrUUN3ME2xPU42OSEQvF2= NGHz[GVUSU6JRWK=
HH MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;nZmlEPTB;MkCuNFA6QSEQvF2= M2fIdHNCVkeHUh?=
MPP-89 NGrZV4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3oTHVDUUN3ME2yN{4zOjh7IN88US=> M{C2e3NCVkeHUh?=
IST-MEL1 NX\FOGRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLySY84UUN3ME2yN{45PjV6IN88US=> M4S2b3NCVkeHUh?=
KP-N-YS MojzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXue2lMUUN3ME2yN{46OjV3IN88US=> MX\TRW5ITVJ?
EC-GI-10 M2\jbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXHZWRKSzVyPUK0MlU6QDlizszN NF;pSHBUSU6JRWK=
EKVX M3\tVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTJ4LkCyNFMh|ryP M1H0TnNCVkeHUh?=
TGBC1TKB NVHTbGN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{i2NWlEPTB;Mk[uOFM1KM7:TR?= M2fVbHNCVkeHUh?=
Daudi NUmyfpVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJ5LkC3O|Mh|ryP NVfZR|d2W0GQR1XS
ALL-PO NX:5dXNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlOyTWM2OD1{Nz6wPFEh|ryP NF\oe4RUSU6JRWK=
NB6 NH3FbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTaZlNKSzVyPUK3MlQ5QCEQvF2= Mm\NV2FPT0WU
ES6 NV7wN|hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1yyemlEPTB;MkeuPVEzOyEQvF2= MnnNV2FPT0WU
COLO-320-HSR NFixWohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7XfHpKSzVyPUK4MlA{PzNizszN M4\CbHNCVkeHUh?=
K5 NH\zcoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2GwdWlEPTB;MkiuNVI5PyEQvF2= NGCzbnJUSU6JRWK=
ES1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHMNIVKSzVyPUK4Mlc4PzNizszN M1zqPXNCVkeHUh?=
LC-1F NWPyVpc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTJ7LkezOFYh|ryP NYOwZ5JtW0GQR1XS
SCLC-21H NHKwVFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHHVJlPUUN3ME2zNE44OzF5IN88US=> M1HERnNCVkeHUh?=
SK-PN-DW M4faOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HoPWlEPTB;M{KuOVU6QCEQvF2= MUfTRW5ITVJ?
D-247MG MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3W5OGlEPTB;M{KuPVc4OyEQvF2= NY[4XHBGW0GQR1XS
TE-5 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfhbm5SUUN3ME2zN{4xOzZ{IN88US=> M13qR3NCVkeHUh?=
MONO-MAC-6 NIjae2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3RTWM2OD1|Mz61NFQ5KM7:TR?= M1nQO3NCVkeHUh?=
LB2518-MEL M1PmSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzBU4ZKSzVyPUOzMlc3PjZizszN NUjtWpJyW0GQR1XS
LOXIMVI M{TjUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXVTWM2OD1|Mz63PVI5KM7:TR?= MWnTRW5ITVJ?
NCI-H209 NYPQ[49GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN3LkG0OEDPxE1? MWjTRW5ITVJ?
A253 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7COXlLUUN3ME2zOU44PDJ7IN88US=> NF3oUpFUSU6JRWK=
HCC1599 M{XZTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTSUFlUUUN3ME2zOk44ODV|IN88US=> MVzTRW5ITVJ?
EB-3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j4TmlEPTB;M{[uPVUyQCEQvF2= NIrQd2xUSU6JRWK=
GOTO MoHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVGwfHN1UUN3ME2zO{4{OjJ2IN88US=> MnvWV2FPT0WU
SW684 NX3ZRox3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfrVoJGUUN3ME20NU45PDl3IN88US=> NID6VmZUSU6JRWK=
DEL NEnTPIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnFc5FKSzVyPUSyMlA2OjJizszN MV\TRW5ITVJ?
HT-144 NYTrfmVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTR{LkG2O|Yh|ryP M4DOTHNCVkeHUh?=
TE-9 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTR|LkS1PVYh|ryP NUfzN2EyW0GQR1XS
KARPAS-45 Ml;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTzWXVKSzVyPUS0MlM6OjVizszN NUPqS2RyW0GQR1XS
HAL-01 MlfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7aR3NJUUN3ME20OE42ODN2IN88US=> MmjqV2FPT0WU
RCC10RGB M1\Q[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTR2LkezPVIh|ryP MnqzV2FPT0WU
CP67-MEL NXTJdHlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LKR2lEPTB;NEWuOlI1OSEQvF2= NY\PcJVJW0GQR1XS
NB17 NVz4bZhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\qTWM2OD12NT62OlQ{KM7:TR?= NV;sXVRsW0GQR1XS
SK-UT-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz4[XVKSzVyPUS1Mlk1PjRizszN MnqwV2FPT0WU
JiyoyeP-2003 M3:5V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37JTmlEPTB;NE[uNFEyQSEQvF2= MofYV2FPT0WU
HCE-4 NXfBVWhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPYeXZCUUN3ME20Ok42QTZ6IN88US=> NVzDXItDW0GQR1XS
NCI-H720 NVXHd4FWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrM[FdKSzVyPUS2Mlc3QDJizszN NGLKclNUSU6JRWK=
KARPAS-422 NIDZVWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WxZ2lEPTB;NEeuNFg6PSEQvF2= MnvtV2FPT0WU
Ramos-2G6-4C10 NWjaeWVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILxNYZKSzVyPUS3MlE3OjJizszN NWi1TlBnW0GQR1XS
HCE-T NF7tNXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i1cWlEPTB;NEeuOlgzQCEQvF2= NES3ZZFUSU6JRWK=
PSN1 M1;6W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXQNnZDUUN3ME20O{44QDF|IN88US=> M3eyWHNCVkeHUh?=

... 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 (64.57 mM) warming
Ethanol 31 mg/mL (57.19 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL

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

Chemical Information

Molecular Weight 542.03
Formula

C27H32ClN5O5

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

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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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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

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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