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 Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPxXmVGUUN3ME2wMlA3OTR|IN88US=> NIfITJdUSU6JRWK=
LAMA-84 Ml24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHSbG5KSzVyPUCuNVU6QSEQvF2= MXfTRW5ITVJ?
MEG-01 NWPscFljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFGzVIpKSzVyPUCuNlM3QDhizszN NEH2U3pUSU6JRWK=
EM-2 M3n0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTTd4FMUUN3ME2wMlI3PSEQvF2= M4rMOnNCVkeHUh?=
TE-15 NEDiU29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXryPFJsUUN3ME2wMlI4PDF{IN88US=> NELwNVlUSU6JRWK=
NCI-H1648 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HrSmlEPTB;MD6yPFEyPiEQvF2= NVnZT5ZHW0GQR1XS
TE-12 NFnPNJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojXTWM2OD1yLkOyOlgh|ryP MULTRW5ITVJ?
LB996-RCC MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGW3Vm1KSzVyPUCuOFQyQTZizszN MnPJV2FPT0WU
K-562 MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTxTWM2OD1yLkS0PVY4KM7:TR?= NUfiV2RQW0GQR1XS
D-336MG MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInsW41KSzVyPUCuOVA{ODRizszN Mlq4V2FPT0WU
NOS-1 NWPIRpFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoS3TWM2OD1yLk[wOVI6KM7:TR?= MUfTRW5ITVJ?
EW-24 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DTTWlEPTB;MD62NlY6OyEQvF2= Mn7OV2FPT0WU
BV-173 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H5[mlEPTB;MD62OVI1QSEQvF2= MmnaV2FPT0WU
NCCIT MkSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwN{OyNVgh|ryP Moj5V2FPT0WU
NCI-H1436 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVeyR3JuUUN3ME2wMlc6ODR7IN88US=> NIr3S5NUSU6JRWK=
BB30-HNC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLh[2tCUUN3ME2wMlg3OjB|IN88US=> M33OcXNCVkeHUh?=
TE-8 M3Wz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwOEeyO|Uh|ryP M3zE[3NCVkeHUh?=
A704 M1\PV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnToTWM2OD1yLki5NlEh|ryP NVjRfHg{W0GQR1XS
TK10 NHPwUJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLTUJpkUUN3ME2wMlkxPjZ7IN88US=> NWTCNmhQW0GQR1XS
KS-1 NHGx[phIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13JNmlEPTB;MT6xPVc4QSEQvF2= NUXpN2ppW0GQR1XS
C2BBe1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHoTWM2OD1zLkKwOVA4KM7:TR?= MnvQV2FPT0WU
RXF393 Mn7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYP2NJRMUUN3ME2xMlI1OzZizszN NEDUclJUSU6JRWK=
KGN MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTFwMke2PFch|ryP NWjUVlF4W0GQR1XS
NB69 NXfjN3FvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;jTWM2OD1zLkO3OFk4KM7:TR?= NIH5S2NUSU6JRWK=
TE-11 M3:5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvpcFF{UUN3ME2xMlQ{PDF6IN88US=> NHHnT2dUSU6JRWK=
TE-1 M120SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrMW3BKSzVyPUGuOFQyODVizszN NHnkXmpUSU6JRWK=
ST486 NFfqSJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTFwNEW4OVIh|ryP MmDnV2FPT0WU
HOP-62 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfkTWM2OD1zLkWwNlQ3KM7:TR?= MnXsV2FPT0WU
EW-16 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnsVoRXUUN3ME2xMlU2ODh|IN88US=> NXnYVJY4W0GQR1XS
LB1047-RCC NFXxWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHCOoJKSzVyPUGuOVU1PTNizszN MmHKV2FPT0WU
TE-10 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInnVoRKSzVyPUGuOlYzPTJizszN NXG1Xm1RW0GQR1XS
RL95-2 NIfoSItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4i0NGlEPTB;MT62OlkxOiEQvF2= NF;wPYxUSU6JRWK=
DOHH-2 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Xvd2lEPTB;MT63NVc5OiEQvF2= MXzTRW5ITVJ?
MFH-ino MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTFwN{e4O{DPxE1? NH3HNXVUSU6JRWK=
GB-1 NFvjUJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfmTWM2OD1zLke5PFM{KM7:TR?= M{GybXNCVkeHUh?=
SK-N-DZ NITNdm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTFwOES2PFgh|ryP M4C3RXNCVkeHUh?=
OS-RC-2 NFfGZ21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfsTWM2OD1zLki4OVc1KM7:TR?= MlPUV2FPT0WU
SW982 NH7BOFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T4bGlEPTB;MT65NlA6OyEQvF2= M2rON3NCVkeHUh?=
KALS-1 M1n2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfXO|JLUUN3ME2xMlk5PzJ{IN88US=> MmjlV2FPT0WU
TGBC24TKB Mm\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XvV2lEPTB;Mj6wOVk2QCEQvF2= NHO0fmZUSU6JRWK=
GI-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\nZVFYUUN3ME2yMlE3ODh2IN88US=> MXTTRW5ITVJ?
SW962 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTJwMUexO|gh|ryP NYHjdIRQW0GQR1XS
SW872 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jTRmlEPTB;Mj6xPFUxPyEQvF2= MVrTRW5ITVJ?
NCI-H747 NX3Qe2N3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnFe5dKSzVyPUKuNlU4OTRizszN MX;TRW5ITVJ?
MZ1-PC MorXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXP[oR2UUN3ME2yMlI6OzV4IN88US=> M4W2cHNCVkeHUh?=
MSTO-211H MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;XTWM2OD1{LkO1O|I{KM7:TR?= M2\ucHNCVkeHUh?=
BL-70 NF3lfHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnX1TWM2OD1{LkS3OFIzKM7:TR?= NGLBOJRUSU6JRWK=
SW954 MoLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli5TWM2OD1{LkW3OFA5KM7:TR?= NG\hS3NUSU6JRWK=
SNB75 M3HXT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn5XnZKSzVyPUKuOlg2QTRizszN NXfPVVl6W0GQR1XS
IST-SL2 Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJwN{KzO|kh|ryP NH[wV3dUSU6JRWK=
GCIY MnrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzZUnU6UUN3ME2yMlg4ODB3IN88US=> MnLCV2FPT0WU
KU812 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTNwMEWyPVkh|ryP M1rjcHNCVkeHUh?=
LXF-289 NVT5TYRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojmTWM2OD1|LkGyNVA6KM7:TR?= M3Xs[XNCVkeHUh?=
ETK-1 M321dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHuW25HUUN3ME2zMlIxPzZ5IN88US=> MWLTRW5ITVJ?
SF126 M1vnPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnO1TWM2OD1|LkOxNVc1KM7:TR?= MYHTRW5ITVJ?
LC-2-ad NF76PZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInBc45KSzVyPUOuOVU4KM7:TR?= NYD6RVNKW0GQR1XS
KNS-42 NYO0OFMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jCZmlEPTB;Mz62OUDPxE1? MUjTRW5ITVJ?
OVCAR-4 NE\HflNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTiTWM2OD1|LkezOFM{KM7:TR?= MnPzV2FPT0WU
PF-382 NX;IfldYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTNwOEO2PVgh|ryP NF3SUlBUSU6JRWK=
SH-4 NUG0e4dPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTRwMkWyOVkh|ryP NWrxbYZOW0GQR1XS
KM12 NW\hSFV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnYTWM2OD12LkOyOFE3KM7:TR?= NFmxVJpUSU6JRWK=
NB5 NGPqOIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHkSJIzUUN3ME20MlQyQDZ2IN88US=> NEf6T2RUSU6JRWK=
KURAMOCHI NGPod2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHtTWM2OD12Lk[1NlU3KM7:TR?= MV;TRW5ITVJ?
Becker MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;yTWM2OD12Lk[2OFE3KM7:TR?= MnS1V2FPT0WU
MV-4-11 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXvXFRKSzVyPUSuPFE{PDRizszN M1HjU3NCVkeHUh?=
KINGS-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTRwOEKzO|Mh|ryP M4TBTnNCVkeHUh?=
LS-123 MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPxTWM2OD13LkS5Olg1KM7:TR?= Moe1V2FPT0WU
SF268 NYjCOZJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[xUHBKSzVyPUWuOlEzPjJizszN M1T5UnNCVkeHUh?=
A388 NXjJN3JTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnD[pNsUUN3ME21MlY{PjZ5IN88US=> MUTTRW5ITVJ?
NMC-G1 NFrhZo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnB[pZKSzVyPU[uNFE5OTFizszN NIj1UYdUSU6JRWK=
CGTH-W-1 NX7JeI9bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXQW|lKSzVyPU[uNFIxPzVizszN NHKyPW1USU6JRWK=
ES4 NGPmU|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PsS2lEPTB;Nj61N|A4PCEQvF2= NGPpbHdUSU6JRWK=
SR MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTZwNUi4NFch|ryP MWDTRW5ITVJ?
BB49-HNC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[ySZA5UUN3ME22Mlc{OjB4IN88US=> NUDjW3hzW0GQR1XS
KLE NG\McmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTzb5ZKSzVyPU[uO|g{PzdizszN MWPTRW5ITVJ?
HUTU-80 NVXaSpJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFv5OZRKSzVyPU[uPVg1PjZizszN Ml7jV2FPT0WU
SNU-C2B MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHMTWM2OD15LkiyO|M4KM7:TR?= MXLTRW5ITVJ?
BB65-RCC NV3NRpBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[1TWM2OD15Lkm0PVA1KM7:TR?= M2jG[XNCVkeHUh?=
QIMR-WIL MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4e2OWlEPTB;OD60NlgxQCEQvF2= NXHkbXU2W0GQR1XS
GDM-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrrVYJpUUN3ME24Mlk4Ojl{IN88US=> M1:5WXNCVkeHUh?=
LC4-1 NVvQd29GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV62WHlMUUN3ME25MlAxQTFzIN88US=> MlHqV2FPT0WU
MLMA Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;GTWM2OD17LkG1NFA3KM7:TR?= MXXTRW5ITVJ?
EoL-1-cell NEXsbXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7qTWM2OD17LkOwNVkzKM7:TR?= MmXzV2FPT0WU
BOKU Ml:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[xUG9KSzVyPUmuPVY1PjZizszN M{nReHNCVkeHUh?=
EVSA-T NHroNHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFyLk[1Olgh|ryP Mn2xV2FPT0WU
D-283MED NH\2fFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFyLkmxO|Yh|ryP M2nGdnNCVkeHUh?=
NB1 NXG3XVZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1W4N2lEPTB;MUGuNFI1OiEQvF2= MV;TRW5ITVJ?
RPMI-8402 NXzacnh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP0TWM2OD1zMT6xO|gh|ryP NH\ad4lUSU6JRWK=
NCI-H1355 M2DLR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFzLkG4NFYh|ryP MmL2V2FPT0WU
NB7 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;ESWlEPTB;MUGuN|I6PyEQvF2= NYHWOYZ[W0GQR1XS
RPMI-6666 NF;OOldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rEW2lEPTB;MUKuPVU3PyEQvF2= MXrTRW5ITVJ?
697 M1Xtbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfYbJQyUUN3ME2xN{4zPzBzIN88US=> MoDDV2FPT0WU
CTB-1 MonwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTF|LkW5OFgh|ryP NH;qdZRUSU6JRWK=
VA-ES-BJ MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DrdmlEPTB;MUOuPVI{PCEQvF2= M{XmVnNCVkeHUh?=
BE-13 MmqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF2LkO5NVUh|ryP MUPTRW5ITVJ?
SKM-1 Mm\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\Bc2lEPTB;MUSuOFQ6QSEQvF2= NETEcoFUSU6JRWK=
TE-6 Mn\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHnbnJKSzVyPUG0Mlc2QTFizszN NYPmOpZCW0GQR1XS
LB771-HNC MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe2fIdrUUN3ME2xOE44QDl6IN88US=> Mo\hV2FPT0WU
ECC4 NIfG[HhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTF5LkCyO|ch|ryP MV3TRW5ITVJ?
ES3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fMdGlEPTB;MUeuOFY2PSEQvF2= NUjqOnFkW0GQR1XS
LB647-SCLC MnGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPOZ4lWUUN3ME2xO{41QTR7IN88US=> NYHU[3g2W0GQR1XS
NB10 NVP3NJg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHoOIVKSzVyPUG4MlUzPTZizszN NWLzZ4V7W0GQR1XS
L-540 MojZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTF6LkixNFkh|ryP MV\TRW5ITVJ?
NCI-H2126 NI[4PWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nLTmlEPTB;MUmuOVEh|ryP MYHTRW5ITVJ?
HH M2HuSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;rUWhUUUN3ME2yNE4xODl7IN88US=> MkS4V2FPT0WU
MPP-89 NWHaUpVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJ|LkKyPFkh|ryP MWLTRW5ITVJ?
IST-MEL1 NYe1b|FCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTJ|Lki2OVgh|ryP NELTe5hUSU6JRWK=
KP-N-YS MoWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ|LkmyOVUh|ryP NF3KRWRUSU6JRWK=
EC-GI-10 MnziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTJ2LkW5PFkh|ryP Mnj2V2FPT0WU
EKVX M3rZSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTJ4LkCyNFMh|ryP NYLRPIdpW0GQR1XS
TGBC1TKB NI\YOGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDFWFVKSzVyPUK2MlQ{PCEQvF2= M3nNbHNCVkeHUh?=
Daudi NGTkV|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LNPWlEPTB;MkeuNFc4OyEQvF2= M4\oVnNCVkeHUh?=
ALL-PO NFvQc|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MliyTWM2OD1{Nz6wPFEh|ryP NEKz[JJUSU6JRWK=
NB6 MlfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe2U5VKSzVyPUK3MlQ5QCEQvF2= NYDRUFhEW0GQR1XS
ES6 NVvwc|Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILyemhKSzVyPUK3MlkyOjNizszN M1OzT3NCVkeHUh?=
COLO-320-HSR NFTJTZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u0XWlEPTB;MkiuNFM4OyEQvF2= M2jkbnNCVkeHUh?=
K5 M{XJemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJ6LkGyPFch|ryP NVzMeXVXW0GQR1XS
ES1 NYLiOIRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJ6Lke3O|Mh|ryP MVzTRW5ITVJ?
LC-1F NFjWbVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJ7LkezOFYh|ryP MYLTRW5ITVJ?
SCLC-21H M2LBS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTNyLkezNVch|ryP Mn:xV2FPT0WU
SK-PN-DW M4K0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXu3TXhRUUN3ME2zNk42PTl6IN88US=> M1;0bHNCVkeHUh?=
D-247MG MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\ZUpFKSzVyPUOyMlk4PzNizszN MnTyV2FPT0WU
TE-5 NYrTbVg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjiTWM2OD1|Mz6wN|YzKM7:TR?= M4fq[nNCVkeHUh?=
MONO-MAC-6 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLsNVZKSzVyPUOzMlUxPDhizszN NYj5OVl7W0GQR1XS
LB2518-MEL NIq1NYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHHN5VKSzVyPUOzMlc3PjZizszN NIjXUnVUSU6JRWK=
LOXIMVI MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W1R2lEPTB;M{OuO|kzQCEQvF2= MmixV2FPT0WU
NCI-H209 NXmybYwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\WOVNKSzVyPUO1MlE1PCEQvF2= NU\sT3VtW0GQR1XS
A253 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe3[FJKSzVyPUO1Mlc1OjlizszN M1nTVXNCVkeHUh?=
HCC1599 NEnLbJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4O2[2lEPTB;M{[uO|A2OyEQvF2= NWS0Z4xJW0GQR1XS
EB-3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjqc3plUUN3ME2zOk46PTF6IN88US=> M1m4fnNCVkeHUh?=
GOTO MmnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzJTWM2OD1|Nz6zNlI1KM7:TR?= MYfTRW5ITVJ?
SW684 NV70TpFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;mPGFKSzVyPUSxMlg1QTVizszN NWPiUm9NW0GQR1XS
DEL MoTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjiTWM2OD12Mj6wOVIzKM7:TR?= NHW5T4xUSU6JRWK=
HT-144 MmTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nkbGlEPTB;NEKuNVY4PiEQvF2= MoPQV2FPT0WU
TE-9 NUOwdoY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknyTWM2OD12Mz60OVk3KM7:TR?= MkLqV2FPT0WU
KARPAS-45 NVnYbnU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHiXVNKSzVyPUS0MlM6OjVizszN MWfTRW5ITVJ?
HAL-01 M4K2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTmUI44UUN3ME20OE42ODN2IN88US=> NWDSS4I4W0GQR1XS
RCC10RGB MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTR2LkezPVIh|ryP M2nOOXNCVkeHUh?=
CP67-MEL NH3FbHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjPVZVoUUN3ME20OU43OjRzIN88US=> MoDkV2FPT0WU
NB17 NX;hWnN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTR3Lk[2OFMh|ryP NV7u[VJVW0GQR1XS
SK-UT-1 Mlj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkG0TWM2OD12NT65OFY1KM7:TR?= MU\TRW5ITVJ?
JiyoyeP-2003 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXvTWM2OD12Nj6wNVE6KM7:TR?= M4XFNnNCVkeHUh?=
HCE-4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvjPVJmUUN3ME20Ok42QTZ6IN88US=> M4TueXNCVkeHUh?=
NCI-H720 MkHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTR4Lke2PFIh|ryP MoK1V2FPT0WU
KARPAS-422 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\ERmlEPTB;NEeuNFg6PSEQvF2= NVvSRmhXW0GQR1XS
Ramos-2G6-4C10 M1L4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GxZmlEPTB;NEeuNVYzOiEQvF2= MlO5V2FPT0WU
HCE-T M{nid2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTR5Lk[4Nlgh|ryP M3LGOHNCVkeHUh?=
PSN1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnvbXlKSzVyPUS3Mlc5OTNizszN NH72[3VUSU6JRWK=

... 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(Data is from Selleck tests instead of citations):
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
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 )

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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):
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    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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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 Recruiting Alcohol Drinking Yale University May 9 2017 Phase 2
NCT01216176 Completed Breast Cancer Joyce Marie Slingerland|Stanford University|University of Miami October 21 2008 Phase 1|Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Women''s Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2
NCT02732587 Completed Alcohol Drinking Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) November 2015 Phase 1
NCT02167256 Completed Alzheimer''s Disease Yale University|Alzheimer''s Therapeutic Research Institute December 2014 Phase 2
NCT02262026 Recruiting Alcoholism Yale University November 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID