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 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXROXpKSzVyPUCuNFYyPDNizszN NHHjOGpUSU6JRWK=
LAMA-84 Mny4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu1TWM2OD1yLkG1PVkh|ryP M2jMbXNCVkeHUh?=
MEG-01 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXDfmR{UUN3ME2wMlI{Pjh6IN88US=> MWnTRW5ITVJ?
EM-2 M4TlRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTTTWM2OD1yLkK2OUDPxE1? M2fXUHNCVkeHUh?=
TE-15 NVTTRY1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jCXmlEPTB;MD6yO|QyOiEQvF2= NUnrfIVHW0GQR1XS
NCI-H1648 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\RVFFKSzVyPUCuNlgyOTZizszN Ml;WV2FPT0WU
TE-12 NULLeHBvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;CTWM2OD1yLkOyOlgh|ryP NELjR2lUSU6JRWK=
LB996-RCC NXW3b2tnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf3PIo5UUN3ME2wMlQ1OTl4IN88US=> MW\TRW5ITVJ?
K-562 NVLvUFlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELR[YtKSzVyPUCuOFQ6PjdizszN MX;TRW5ITVJ?
D-336MG M4nweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PwTmlEPTB;MD61NFMxPCEQvF2= MkXHV2FPT0WU
NOS-1 Mn3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LDUmlEPTB;MD62NFUzQSEQvF2= NFK4T|BUSU6JRWK=
EW-24 NYTLXlh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz6b4NKSzVyPUCuOlI3QTNizszN MXTTRW5ITVJ?
BV-173 M33IRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moi1TWM2OD1yLk[1NlQ6KM7:TR?= MknhV2FPT0WU
NCCIT MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjneHRKSzVyPUCuO|MzOThizszN M{PUbnNCVkeHUh?=
NCI-H1436 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoS1TWM2OD1yLke5NFQ6KM7:TR?= NIqzRo1USU6JRWK=
BB30-HNC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLaO|J{UUN3ME2wMlg3OjB|IN88US=> M3;meHNCVkeHUh?=
TE-8 MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnZeHg2UUN3ME2wMlg4Ojd3IN88US=> M1PyXnNCVkeHUh?=
A704 Mo\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3vb41KSzVyPUCuPFkzOSEQvF2= NFLoU4hUSU6JRWK=
TK10 NYDkbINiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjwTHRKSzVyPUCuPVA3PjlizszN NIPs[|hUSU6JRWK=
KS-1 NWCyUIVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTFwMUm3O|kh|ryP NV\5[41ZW0GQR1XS
C2BBe1 NWPrV4x[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3yTWM2OD1zLkKwOVA4KM7:TR?= MYjTRW5ITVJ?
RXF393 M2nM[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO4N4hzUUN3ME2xMlI1OzZizszN NX7aeG5sW0GQR1XS
KGN NIX1bGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\ZUo9HUUN3ME2xMlI4Pjh5IN88US=> MkjkV2FPT0WU
NB69 M1[3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\WPYRLUUN3ME2xMlM4PDl5IN88US=> NV63dY57W0GQR1XS
TE-11 MkXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTFwNEO0NVgh|ryP MoroV2FPT0WU
TE-1 NUSzdJpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\DTWM2OD1zLkS0NVA2KM7:TR?= MXPTRW5ITVJ?
ST486 NVvYdmQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfkU2JKSzVyPUGuOFU5PTJizszN Ml;YV2FPT0WU
HOP-62 NFzGUnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfvXlhKSzVyPUGuOVAzPDZizszN NYH5XXBsW0GQR1XS
EW-16 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFwNUWwPFMh|ryP MlzCV2FPT0WU
LB1047-RCC MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwNUW0OVMh|ryP MYfTRW5ITVJ?
TE-10 NWPFfnZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfWTWM2OD1zLk[2NlUzKM7:TR?= M120NnNCVkeHUh?=
RL95-2 M1\SZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fsWmlEPTB;MT62OlkxOiEQvF2= NHXSO49USU6JRWK=
DOHH-2 MmDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITwNWJKSzVyPUGuO|E4QDJizszN MorBV2FPT0WU
MFH-ino M3fB[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3j3[GlEPTB;MT63O|g4KM7:TR?= MYTTRW5ITVJ?
GB-1 M1rIWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfqSo5KSzVyPUGuO|k5OzNizszN Moi5V2FPT0WU
SK-N-DZ MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFwOES2PFgh|ryP NX\1W|dbW0GQR1XS
OS-RC-2 MkPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPCfJpKSzVyPUGuPFg2PzRizszN MYfTRW5ITVJ?
SW982 NHGyTlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ns[2lEPTB;MT65NlA6OyEQvF2= MVHTRW5ITVJ?
KALS-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXHXHRKSzVyPUGuPVg4OjJizszN NYDNPYVxW0GQR1XS
TGBC24TKB MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJwMEW5OVgh|ryP MVHTRW5ITVJ?
GI-1 Mn3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nTbGlEPTB;Mj6xOlA5PCEQvF2= Mn7zV2FPT0WU
SW962 NF32cYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fL[mlEPTB;Mj6xO|E4QCEQvF2= M32xU3NCVkeHUh?=
SW872 NXrkN5l7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojpTWM2OD1{LkG4OVA4KM7:TR?= NHT4OIZUSU6JRWK=
NCI-H747 M{jiXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHaTWM2OD1{LkK1O|E1KM7:TR?= NYTGSGNRW0GQR1XS
MZ1-PC NEPG[JpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTJwMkmzOVYh|ryP NUnqZXJCW0GQR1XS
MSTO-211H NFe5U41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnYUZJtUUN3ME2yMlM2PzJ|IN88US=> NVfjZ201W0GQR1XS
BL-70 M1jxfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjmZVc4UUN3ME2yMlQ4PDJ{IN88US=> MVvTRW5ITVJ?
SW954 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jIRWlEPTB;Mj61O|QxQCEQvF2= M4r3RnNCVkeHUh?=
SNB75 M1;QUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7JblVKSzVyPUKuOlg2QTRizszN MmflV2FPT0WU
IST-SL2 NXTMSHZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1G0VGlEPTB;Mj63NlM4QSEQvF2= NXyzfZA6W0GQR1XS
GCIY MlvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGC5bmhKSzVyPUKuPFcxODVizszN M4rjUnNCVkeHUh?=
KU812 MoXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M164cWlEPTB;Mz6wOVI6QSEQvF2= MojZV2FPT0WU
LXF-289 MlniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3RTWM2OD1|LkGyNVA6KM7:TR?= MWLTRW5ITVJ?
ETK-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTNwMkC3Olch|ryP M3rUd3NCVkeHUh?=
SF126 M37EbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\3SY5TUUN3ME2zMlMyOTd2IN88US=> NYDYTHF1W0GQR1XS
LC-2-ad NIPZZXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUL3[HRZUUN3ME2zMlU2PyEQvF2= NWf4ZllMW0GQR1XS
KNS-42 M3XYN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjYeZVQUUN3ME2zMlY2KM7:TR?= MYnTRW5ITVJ?
OVCAR-4 NGe5cphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHWxXGFKSzVyPUOuO|M1OzNizszN MmrxV2FPT0WU
PF-382 NYTnN2RGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j2RmlEPTB;Mz64N|Y6QCEQvF2= MVTTRW5ITVJ?
SH-4 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\Ee5BKSzVyPUSuNlUzPTlizszN NXXXZZhFW0GQR1XS
KM12 M3;Nbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;JZ2lEPTB;ND6zNlQyPiEQvF2= M4D1[XNCVkeHUh?=
NB5 NIPKNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfQTWM2OD12LkSxPFY1KM7:TR?= NXjsPGVQW0GQR1XS
KURAMOCHI M4njXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXvdYNHUUN3ME20MlY2OjV4IN88US=> NYL5PHNXW0GQR1XS
Becker MnvjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvLWJJKSzVyPUSuOlY1OTZizszN MXXTRW5ITVJ?
MV-4-11 NEmyO3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Ds[2lEPTB;ND64NVM1PCEQvF2= MnPyV2FPT0WU
KINGS-1 NX;1cmF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTRwOEKzO|Mh|ryP NVLNbllMW0GQR1XS
LS-123 NWjZXpFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTVwNEm2PFQh|ryP Mlj1V2FPT0WU
SF268 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7Gdo11UUN3ME21MlYyOjZ{IN88US=> M4XYdXNCVkeHUh?=
A388 M{noOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT1TWM2OD13Lk[zOlY4KM7:TR?= NUjqSZlWW0GQR1XS
NMC-G1 M2fTTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzUXGFKSzVyPU[uNFE5OTFizszN NXOyPIRmW0GQR1XS
CGTH-W-1 MkjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTZwMEKwO|Uh|ryP MUnTRW5ITVJ?
ES4 Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2OzTWlEPTB;Nj61N|A4PCEQvF2= NV3hcZk5W0GQR1XS
SR M1:xO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnf0TWM2OD14LkW4PFA4KM7:TR?= MmnjV2FPT0WU
BB49-HNC NEOzTWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTZwN{OyNFYh|ryP NGjaXYVUSU6JRWK=
KLE MormS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzFU5hKUUN3ME22Mlc5Ozd5IN88US=> NWPvXYFYW0GQR1XS
HUTU-80 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4r1[WlEPTB;Nj65PFQ3PiEQvF2= NXf1SoZvW0GQR1XS
SNU-C2B MoG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPES3NZUUN3ME23MlgzPzN5IN88US=> M2CzfHNCVkeHUh?=
BB65-RCC NEm4ZY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTdwOUS5NFQh|ryP NIDDOolUSU6JRWK=
QIMR-WIL M2TqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;DfWlEPTB;OD60NlgxQCEQvF2= M{X3cnNCVkeHUh?=
GDM-1 NYnTe2hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLGRW9KSzVyPUiuPVczQTJizszN NIDu[oZUSU6JRWK=
LC4-1 NH20eFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fzUWlEPTB;OT6wNFkyOSEQvF2= M2PVWnNCVkeHUh?=
MLMA MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPBXI9KSzVyPUmuNVUxODZizszN MXrTRW5ITVJ?
EoL-1-cell MlPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTlwM{CxPVIh|ryP MlTiV2FPT0WU
BOKU NWfjWm11T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf1TWM2OD17Lkm2OFY3KM7:TR?= NUPofnV[W0GQR1XS
EVSA-T M3LDfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDPdIVyUUN3ME2xNE43PTZ6IN88US=> NGHobpZUSU6JRWK=
D-283MED MoLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m1[mlEPTB;MUCuPVE4PiEQvF2= MYjTRW5ITVJ?
NB1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFzLkCyOFIh|ryP M2fkOXNCVkeHUh?=
RPMI-8402 M13nfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTFzLkG3PEDPxE1? NEfUNWJUSU6JRWK=
NCI-H1355 M3H5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFzLkG4NFYh|ryP MoDQV2FPT0WU
NB7 NF\oVpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLrTWM2OD1zMT6zNlk4KM7:TR?= MXTTRW5ITVJ?
RPMI-6666 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7xTGZKSzVyPUGyMlk2PjdizszN M{HYUXNCVkeHUh?=
697 NIjBephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTF|LkK3NFEh|ryP NGTYPWJUSU6JRWK=
CTB-1 NU\hNJJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL3fIpKSzVyPUGzMlU6PDhizszN Mn7IV2FPT0WU
VA-ES-BJ M3;hS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrscGJNUUN3ME2xN{46OjN2IN88US=> NVLTWodGW0GQR1XS
BE-13 M2\nXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfyOHZKSzVyPUG0MlM6OTVizszN NUHWbnd5W0GQR1XS
SKM-1 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFL0XZJKSzVyPUG0MlQ1QTlizszN NGO1NodUSU6JRWK=
TE-6 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf1V4pNUUN3ME2xOE44PTlzIN88US=> NIHRWIlUSU6JRWK=
LB771-HNC NVvYTlRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHJOlZKSzVyPUG0Mlc5QThizszN MoLSV2FPT0WU
ECC4 NVTTbIJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTF5LkCyO|ch|ryP MlX1V2FPT0WU
ES3 NXn3Rmd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLMTWM2OD1zNz60OlU2KM7:TR?= NHLCXZFUSU6JRWK=
LB647-SCLC NHHpS2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\pWnZlUUN3ME2xO{41QTR7IN88US=> NGn1OlhUSU6JRWK=
NB10 NHjUXXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzXTWM2OD1zOD61NlU3KM7:TR?= NYnZU4NbW0GQR1XS
L-540 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvqTWM2OD1zOD64NVA6KM7:TR?= MWPTRW5ITVJ?
NCI-H2126 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWzTWM2OD1zOT61NUDPxE1? MUnTRW5ITVJ?
HH MlHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJyLkCwPVkh|ryP NXXkOlhYW0GQR1XS
MPP-89 Mlj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnSRlV2UUN3ME2yN{4zOjh7IN88US=> MkHaV2FPT0WU
IST-MEL1 NEKwO5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LzU2lEPTB;MkOuPFY2QCEQvF2= NFnze5lUSU6JRWK=
KP-N-YS NXPMN45tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTJ|LkmyOVUh|ryP MknPV2FPT0WU
EC-GI-10 MmLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGe3PGRKSzVyPUK0MlU6QDlizszN NULkfIF[W0GQR1XS
EKVX NGPTc|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJ4LkCyNFMh|ryP NXTEVXA4W0GQR1XS
TGBC1TKB NVTNWFZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJ4LkSzOEDPxE1? NVLUdpZ7W0GQR1XS
Daudi M1PkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJ5LkC3O|Mh|ryP M13OOXNCVkeHUh?=
ALL-PO NFT0VFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfKTWM2OD1{Nz6wPFEh|ryP M{\xUnNCVkeHUh?=
NB6 M1ziNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;LW3hEUUN3ME2yO{41QDhizszN MWnTRW5ITVJ?
ES6 MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ5LkmxNlMh|ryP MlvCV2FPT0WU
COLO-320-HSR NGnNVmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTJ6LkCzO|Mh|ryP MVTTRW5ITVJ?
K5 NYHZWWFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLYd|BKUUN3ME2yPE4yOjh5IN88US=> MomwV2FPT0WU
ES1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jxOGlEPTB;MkiuO|c4OyEQvF2= NYDMO4o6W0GQR1XS
LC-1F MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTJ7LkezOFYh|ryP MVnTRW5ITVJ?
SCLC-21H NFPIVndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTNyLkezNVch|ryP MojvV2FPT0WU
SK-PN-DW NGLqUJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTN{LkW1PVgh|ryP MU\TRW5ITVJ?
D-247MG NXS0e5RJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoD3TWM2OD1|Mj65O|c{KM7:TR?= NUjiNZVLW0GQR1XS
TE-5 NEHQXY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTN|LkCzOlIh|ryP M2\pT3NCVkeHUh?=
MONO-MAC-6 NHHUNVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorFTWM2OD1|Mz61NFQ5KM7:TR?= NHzkWmtUSU6JRWK=
LB2518-MEL NHrZS4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rscGlEPTB;M{OuO|Y3PiEQvF2= MnTHV2FPT0WU
LOXIMVI NXXzNWJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoL0TWM2OD1|Mz63PVI5KM7:TR?= MXnTRW5ITVJ?
NCI-H209 MmLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH75eIxKSzVyPUO1MlE1PCEQvF2= NVT0S3BoW0GQR1XS
A253 M4foTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHub29KSzVyPUO1Mlc1OjlizszN NHj4fnJUSU6JRWK=
HCC1599 MlO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LaOmlEPTB;M{[uO|A2OyEQvF2= MXHTRW5ITVJ?
EB-3 M4r4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTN4Lkm1NVgh|ryP M4DsRnNCVkeHUh?=
GOTO MlOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYWzdWV4UUN3ME2zO{4{OjJ2IN88US=> NIfmcm5USU6JRWK=
SW684 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\j[WlEPTB;NEGuPFQ6PSEQvF2= NV;TSYYyW0GQR1XS
DEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjMTWM2OD12Mj6wOVIzKM7:TR?= M2\kdXNCVkeHUh?=
HT-144 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnETWM2OD12Mj6xOlc3KM7:TR?= NFX4SmdUSU6JRWK=
TE-9 NGPXN2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTR|LkS1PVYh|ryP MkfkV2FPT0WU
KARPAS-45 MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELCZZZKSzVyPUS0MlM6OjVizszN M{XUOHNCVkeHUh?=
HAL-01 NF;6doVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3jOHhKSzVyPUS0MlUxOzRizszN NYnhVoVPW0GQR1XS
RCC10RGB M1\WW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGzSGFxUUN3ME20OE44Ozl{IN88US=> M4TOb3NCVkeHUh?=
CP67-MEL MkL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTR3Lk[yOFEh|ryP M{C1T3NCVkeHUh?=
NB17 M{fPTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S0[2lEPTB;NEWuOlY1OyEQvF2= NEXYN|ZUSU6JRWK=
SK-UT-1 NF7VbGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXxTWM2OD12NT65OFY1KM7:TR?= M3LhfHNCVkeHUh?=
JiyoyeP-2003 NXLUeIluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\ERWlEPTB;NE[uNFEyQSEQvF2= NETIRXlUSU6JRWK=
HCE-4 NUXveWZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nRbWlEPTB;NE[uOVk3QCEQvF2= NV3BbmZYW0GQR1XS
NCI-H720 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD4UmFqUUN3ME20Ok44Pjh{IN88US=> NHjIc5hUSU6JRWK=
KARPAS-422 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnwcJl3UUN3ME20O{4xQDl3IN88US=> NFvnPIFUSU6JRWK=
Ramos-2G6-4C10 NEL6S|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTR5LkG2NlIh|ryP M1rITHNCVkeHUh?=
HCE-T M4DlXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTR5Lk[4Nlgh|ryP NGr1XW1USU6JRWK=
PSN1 MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr0TWVLUUN3ME20O{44QDF|IN88US=> M4raS3NCVkeHUh?=

... 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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    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):
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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