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 NUjrW5dkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fX[WlEPTB;MD6wOlE1OyEQvF2= NWLP[oxSW0GQR1XS
LAMA-84 M1vQV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVG2PG15UUN3ME2wMlE2QTlizszN NEf6XpVUSU6JRWK=
MEG-01 M1\MOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrkUGpKSzVyPUCuNlM3QDhizszN M4[ycnNCVkeHUh?=
EM-2 NX3S[5RUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwMk[1JO69VQ>? NFiyTI9USU6JRWK=
TE-15 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r4SmlEPTB;MD6yO|QyOiEQvF2= NX3ZZ5hVW0GQR1XS
NCI-H1648 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrPNlNKSzVyPUCuNlgyOTZizszN M{LuS3NCVkeHUh?=
TE-12 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjZTWM2OD1yLkOyOlgh|ryP MUHTRW5ITVJ?
LB996-RCC MoHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fHXGlEPTB;MD60OFE6PiEQvF2= NU\p[nhnW0GQR1XS
K-562 NUT5c5BKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHETWM2OD1yLkS0PVY4KM7:TR?= NYnuPJVnW0GQR1XS
D-336MG MmjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXSV5l2UUN3ME2wMlUxOzB2IN88US=> NWOwTIhGW0GQR1XS
NOS-1 NF7MVlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPVfYpKSzVyPUCuOlA2OjlizszN NYXRR2NpW0GQR1XS
EW-24 MojZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrETWM2OD1yLk[yOlk{KM7:TR?= NIHZS3lUSU6JRWK=
BV-173 NGj5SpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWqyS4Q6UUN3ME2wMlY2OjR7IN88US=> NEHWWWJUSU6JRWK=
NCCIT NH\n[YdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvVN45sUUN3ME2wMlc{OjF6IN88US=> NYfNSIVHW0GQR1XS
NCI-H1436 NW\rXHY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwN{mwOFkh|ryP Ml7xV2FPT0WU
BB30-HNC MmH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjTdW1LUUN3ME2wMlg3OjB|IN88US=> MmjrV2FPT0WU
TE-8 NX7XUYhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33sUWlEPTB;MD64O|I4PSEQvF2= MWfTRW5ITVJ?
A704 NV7zZm9lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwOEmyNUDPxE1? NYrndFZWW0GQR1XS
TK10 NI\SSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUK2UXF1UUN3ME2wMlkxPjZ7IN88US=> MYPTRW5ITVJ?
KS-1 NEPWPJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf2cW5OUUN3ME2xMlE6Pzd7IN88US=> NGK0UlRUSU6JRWK=
C2BBe1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPRUY1kUUN3ME2xMlIxPTB5IN88US=> NGq2W2ZUSU6JRWK=
RXF393 NUDJNXdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIK5b5NKSzVyPUGuNlQ{PiEQvF2= NVnIdpBbW0GQR1XS
KGN M3ew[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX6yZVY4UUN3ME2xMlI4Pjh5IN88US=> NEGxfZNUSU6JRWK=
NB69 NH3icJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz6R5dKSzVyPUGuN|c1QTdizszN NGW4SZFUSU6JRWK=
TE-11 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTFwNEO0NVgh|ryP MnroV2FPT0WU
TE-1 NX7KdlBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;HS5JmUUN3ME2xMlQ1OTB3IN88US=> MV7TRW5ITVJ?
ST486 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nKOWlEPTB;MT60OVg2OiEQvF2= M{T0XHNCVkeHUh?=
HOP-62 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvtTWM2OD1zLkWwNlQ3KM7:TR?= MYrTRW5ITVJ?
EW-16 M4rKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXKwd5NbUUN3ME2xMlU2ODh|IN88US=> M2jZb3NCVkeHUh?=
LB1047-RCC NXPR[4FoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[5TWM2OD1zLkW1OFU{KM7:TR?= MXrTRW5ITVJ?
TE-10 NV\YfG14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\B[INiUUN3ME2xMlY3OjV{IN88US=> Ml;xV2FPT0WU
RL95-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\NNog{UUN3ME2xMlY3QTB{IN88US=> Mn3qV2FPT0WU
DOHH-2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjsWHZKSzVyPUGuO|E4QDJizszN MVjTRW5ITVJ?
MFH-ino M1rITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFwN{e4O{DPxE1? NVLITnhNW0GQR1XS
GB-1 NWrVelJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfOTWM2OD1zLke5PFM{KM7:TR?= MY\TRW5ITVJ?
SK-N-DZ M17jSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HUTmlEPTB;MT64OFY5QCEQvF2= M2rQN3NCVkeHUh?=
OS-RC-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGftNmdKSzVyPUGuPFg2PzRizszN M4P2SHNCVkeHUh?=
SW982 MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYS1SocxUUN3ME2xMlkzODl|IN88US=> MnjwV2FPT0WU
KALS-1 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFwOUi3NlIh|ryP Mn62V2FPT0WU
TGBC24TKB MkjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTJwMEW5OVgh|ryP NFrKd2tUSU6JRWK=
GI-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTJwMU[wPFQh|ryP NE\3R|hUSU6JRWK=
SW962 M4Hs[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfBcHFKSzVyPUKuNVcyPzhizszN M17zenNCVkeHUh?=
SW872 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkO4TWM2OD1{LkG4OVA4KM7:TR?= NULGVmIyW0GQR1XS
NCI-H747 NGO2UnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJwMkW3NVQh|ryP MlzEV2FPT0WU
MZ1-PC M3joUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvuSGVOUUN3ME2yMlI6OzV4IN88US=> NFjqOlRUSU6JRWK=
MSTO-211H NF63e5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPpepRKSzVyPUKuN|U4OjNizszN M1G4fHNCVkeHUh?=
BL-70 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILqTXBKSzVyPUKuOFc1OjJizszN M1uyPXNCVkeHUh?=
SW954 NHv4WoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHXb2hUUUN3ME2yMlU4PDB6IN88US=> MYjTRW5ITVJ?
SNB75 NGTrZnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\sfXBlUUN3ME2yMlY5PTl2IN88US=> NIHQcIlUSU6JRWK=
IST-SL2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jTeGlEPTB;Mj63NlM4QSEQvF2= M1TKbHNCVkeHUh?=
GCIY M1[yNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTJwOEewNFUh|ryP MoXBV2FPT0WU
KU812 NWX3VoRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3H0eGlEPTB;Mz6wOVI6QSEQvF2= NYKwUoQ2W0GQR1XS
LXF-289 NFLseplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlz5TWM2OD1|LkGyNVA6KM7:TR?= M1\CSXNCVkeHUh?=
ETK-1 MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPoUFBJUUN3ME2zMlIxPzZ5IN88US=> MnXvV2FPT0WU
SF126 NYTiT|FmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzBTWM2OD1|LkOxNVc1KM7:TR?= NHjwOFdUSU6JRWK=
LC-2-ad NFvO[plIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTNwNUW3JO69VQ>? NUnmSm8zW0GQR1XS
KNS-42 M1Pt[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTNwNkWg{txO MXnTRW5ITVJ?
OVCAR-4 NEWxd4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTNwN{O0N|Mh|ryP M3\wSHNCVkeHUh?=
PF-382 Mk\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\IT2NKSzVyPUOuPFM3QThizszN M1vt[HNCVkeHUh?=
SH-4 M3ryOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnFXZRKSzVyPUSuNlUzPTlizszN MoDQV2FPT0WU
KM12 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3L1SGlEPTB;ND6zNlQyPiEQvF2= NH;mfWFUSU6JRWK=
NB5 M{K4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonYTWM2OD12LkSxPFY1KM7:TR?= NVzEZmExW0GQR1XS
KURAMOCHI MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7TcZRCUUN3ME20MlY2OjV4IN88US=> M{jpcHNCVkeHUh?=
Becker NXn5e3JMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HpO2lEPTB;ND62OlQyPiEQvF2= NX61PJB6W0GQR1XS
MV-4-11 M3vQNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULqT3FWUUN3ME20MlgyOzR2IN88US=> M{PUfnNCVkeHUh?=
KINGS-1 MnXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HqOmlEPTB;ND64NlM4OyEQvF2= MmHiV2FPT0WU
LS-123 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LiVGlEPTB;NT60PVY5PCEQvF2= M2jzfnNCVkeHUh?=
SF268 M3[xNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHxTWM2OD13Lk[xNlYzKM7:TR?= NX7QcoV3W0GQR1XS
A388 NYjv[mljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3oTWM2OD13Lk[zOlY4KM7:TR?= NVnLXW9iW0GQR1XS
NMC-G1 MnK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TWUWlEPTB;Nj6wNVgyOSEQvF2= NIXFZ4ZUSU6JRWK=
CGTH-W-1 NHrjd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHiTWM2OD14LkCyNFc2KM7:TR?= NUPrXWxMW0GQR1XS
ES4 NIruV2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDjTWM2OD14LkWzNFc1KM7:TR?= M{PwdXNCVkeHUh?=
SR MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjLfVlnUUN3ME22MlU5QDB5IN88US=> M{LuWXNCVkeHUh?=
BB49-HNC Mm\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn32TWM2OD14LkezNlA3KM7:TR?= MWHTRW5ITVJ?
KLE MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTZwN{izO|ch|ryP Mly2V2FPT0WU
HUTU-80 MoCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ziUGlEPTB;Nj65PFQ3PiEQvF2= NGL6b|lUSU6JRWK=
SNU-C2B NIPRR|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\m[GhKSzVyPUeuPFI4OzdizszN NVq1RpV4W0GQR1XS
BB65-RCC NX;uUFVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHQflJrUUN3ME23Mlk1QTB2IN88US=> M3vHTHNCVkeHUh?=
QIMR-WIL MofaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRThwNEK4NFgh|ryP NFnu[5lUSU6JRWK=
GDM-1 NHjxPHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWntVmg2UUN3ME24Mlk4Ojl{IN88US=> NGTzS2dUSU6JRWK=
LC4-1 Mn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTlwMEC5NVEh|ryP NX\zZnZ6W0GQR1XS
MLMA MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3BR3pKSzVyPUmuNVUxODZizszN NX3pUlN7W0GQR1XS
EoL-1-cell MmDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTlwM{CxPVIh|ryP NH;NXnpUSU6JRWK=
BOKU M4HpTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3riSGlEPTB;OT65OlQ3PiEQvF2= NXnHSmNUW0GQR1XS
EVSA-T NHfxcnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrPTWM2OD1zMD62OVY5KM7:TR?= MXjTRW5ITVJ?
D-283MED M1fSOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFyLkmxO|Yh|ryP NGLJT5VUSU6JRWK=
NB1 NGXH[I5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFzLkCyOFIh|ryP Moq1V2FPT0WU
RPMI-8402 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO3TWM2OD1zMT6xO|gh|ryP MXrTRW5ITVJ?
NCI-H1355 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH75c4tKSzVyPUGxMlE5ODZizszN NHvVVm5USU6JRWK=
NB7 NUmwfnNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;aTJdKSzVyPUGxMlMzQTdizszN Mke2V2FPT0WU
RPMI-6666 NHPX[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XaTWlEPTB;MUKuPVU3PyEQvF2= NWr2SHB{W0GQR1XS
697 NV36NFdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz2TWt3UUN3ME2xN{4zPzBzIN88US=> NGmx[FBUSU6JRWK=
CTB-1 NVLCbFBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\rVnR4UUN3ME2xN{42QTR6IN88US=> M1\kO3NCVkeHUh?=
VA-ES-BJ MnvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3kUIdFUUN3ME2xN{46OjN2IN88US=> MmOwV2FPT0WU
BE-13 NV3hSVk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTF2LkO5NVUh|ryP M3[zOnNCVkeHUh?=
SKM-1 NHTFZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPh[3hCUUN3ME2xOE41PDl7IN88US=> NFvJdpRUSU6JRWK=
TE-6 M4rCTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;qR|V1UUN3ME2xOE44PTlzIN88US=> MX;TRW5ITVJ?
LB771-HNC NHfXUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF2Lke4PVgh|ryP NFPRZWZUSU6JRWK=
ECC4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XJU2lEPTB;MUeuNFI4PyEQvF2= MlztV2FPT0WU
ES3 NUnE[Wd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTF5LkS2OVUh|ryP M4jnWHNCVkeHUh?=
LB647-SCLC NICzWY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:zTWM2OD1zNz60PVQ6KM7:TR?= MUfTRW5ITVJ?
NB10 NXv4eZBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTF6LkWyOVYh|ryP MYfTRW5ITVJ?
L-540 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\zUWlEPTB;MUiuPFExQSEQvF2= MVjTRW5ITVJ?
NCI-H2126 NI\nb2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1T2ZWlEPTB;MUmuOVEh|ryP M17uZXNCVkeHUh?=
HH MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjoZ3dFUUN3ME2yNE4xODl7IN88US=> MoTOV2FPT0WU
MPP-89 M3rSUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\6eXJKSzVyPUKzMlIzQDlizszN M3\1cXNCVkeHUh?=
IST-MEL1 M4XSPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mle4TWM2OD1{Mz64OlU5KM7:TR?= MkDnV2FPT0WU
KP-N-YS NUCweJNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPTTWM2OD1{Mz65NlU2KM7:TR?= NWKxSml4W0GQR1XS
EC-GI-10 M1HLSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJ2LkW5PFkh|ryP NGj5R4ZUSU6JRWK=
EKVX NHnRT2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4C3W2lEPTB;Mk[uNFIxOyEQvF2= M1zhVnNCVkeHUh?=
TGBC1TKB M17TU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[1cmlEPTB;Mk[uOFM1KM7:TR?= Mk\PV2FPT0WU
Daudi Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlqzTWM2OD1{Nz6wO|c{KM7:TR?= M2LTc3NCVkeHUh?=
ALL-PO NVnMeWxHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn5SpdVUUN3ME2yO{4xQDFizszN NIixZ2NUSU6JRWK=
NB6 NIi1V45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2OwUWlEPTB;MkeuOFg5KM7:TR?= MYXTRW5ITVJ?
ES6 NXXhW4VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DLZmlEPTB;MkeuPVEzOyEQvF2= MofiV2FPT0WU
COLO-320-HSR MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXHTWM2OD1{OD6wN|c{KM7:TR?= NEi2dWhUSU6JRWK=
K5 NF\DNGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXpTWM2OD1{OD6xNlg4KM7:TR?= Ml;tV2FPT0WU
ES1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXNcGRKSzVyPUK4Mlc4PzNizszN MoLsV2FPT0WU
LC-1F M{PJWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjoeVZKSzVyPUK5Mlc{PDZizszN NEDPSYJUSU6JRWK=
SCLC-21H MonJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnUWm1KSzVyPUOwMlc{OTdizszN NHTiTJhUSU6JRWK=
SK-PN-DW M2i1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;WTWM2OD1|Mj61OVk5KM7:TR?= NEHNW2dUSU6JRWK=
D-247MG M{Lrc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XvXmlEPTB;M{KuPVc4OyEQvF2= Mm\3V2FPT0WU
TE-5 NXHpOld{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;HUWlEPTB;M{OuNFM3OiEQvF2= M2XhU3NCVkeHUh?=
MONO-MAC-6 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTN|LkWwOFgh|ryP MWTTRW5ITVJ?
LB2518-MEL NHnHOG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3roSWlEPTB;M{OuO|Y3PiEQvF2= NGTCOIxUSU6JRWK=
LOXIMVI NILKWFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\nVWlEPTB;M{OuO|kzQCEQvF2= NULVZ2lVW0GQR1XS
NCI-H209 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTN3LkG0OEDPxE1? NHT5dGZUSU6JRWK=
A253 NWnVWFBNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPtT5lKSzVyPUO1Mlc1OjlizszN NFTiTXlUSU6JRWK=
HCC1599 MorYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTN4LkewOVMh|ryP MYnTRW5ITVJ?
EB-3 MlXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;EO5ZKSzVyPUO2Mlk2OThizszN MYLTRW5ITVJ?
GOTO MnW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyyVJl3UUN3ME2zO{4{OjJ2IN88US=> MkTaV2FPT0WU
SW684 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTRzLki0PVUh|ryP NHLUTodUSU6JRWK=
DEL NUfCOHZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\hTWM2OD12Mj6wOVIzKM7:TR?= Mn7iV2FPT0WU
HT-144 M{PwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTR{LkG2O|Yh|ryP MmLYV2FPT0WU
TE-9 M2CyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTR|LkS1PVYh|ryP M4\LSHNCVkeHUh?=
KARPAS-45 NYHWe5U4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTR2LkO5NlUh|ryP NES1NIdUSU6JRWK=
HAL-01 Ml3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXvVYRKSzVyPUS0MlUxOzRizszN NXG4[ohwW0GQR1XS
RCC10RGB MonQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILHfHBKSzVyPUS0Mlc{QTJizszN MlLGV2FPT0WU
CP67-MEL NIT4dVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTR3Lk[yOFEh|ryP NXm4Om1KW0GQR1XS
NB17 M33mTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DiTmlEPTB;NEWuOlY1OyEQvF2= M{e2dXNCVkeHUh?=
SK-UT-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfO[lFKSzVyPUS1Mlk1PjRizszN NILkZnpUSU6JRWK=
JiyoyeP-2003 NF\oNIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPvTWM2OD12Nj6wNVE6KM7:TR?= MX;TRW5ITVJ?
HCE-4 NUPnW5JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXqdZRKSzVyPUS2MlU6PjhizszN NGOwfGNUSU6JRWK=
NCI-H720 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTR4Lke2PFIh|ryP NVvldXRWW0GQR1XS
KARPAS-422 NFjDTldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR5LkC4PVUh|ryP MonkV2FPT0WU
Ramos-2G6-4C10 M{XESmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTR5LkG2NlIh|ryP MWHTRW5ITVJ?
HCE-T NXLrbVVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDNTWM2OD12Nz62PFI5KM7:TR?= NV24cGN1W0GQR1XS
PSN1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEOydXpKSzVyPUS3Mlc5OTNizszN NVW1Oo06W0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo Saracatinib shows great tumor growth inhibition in Src3T3 allografts and a moderate growth delay in Calu-6, MDA-MB-231, AsPc-1 and BT474C xenografts. [1] Saracatinib shows great antitumor activity in orthotopic DU145 xenograft mice at a dose of 25mg/kg (orally administered, daily). [2]

Protocol

Kinase Assay:[1]
+ Expand

Kinase Assay:

IC50 of tyrosine kinase activity is measured by an enzyme-linked immunosorbent assay (ELISA) with recombinant catalytic domains of a panel of receptor and non-receptor tyrosine kinases (in some cases only part of the catalytic domain is used). Saracatinib dose ranges from 0.001-10 mM. Specificity assays against a panel of serine/threonine kinases are performed using a filter capture assay with 32P. Briefly, multidrop 384 plates containing 0.5 μL Saracatinib or controls (DMSO) alone or pH 3.0 buffer controls) are incubated with 15 μL of enzyme plus peptide/protein substrate for 5 min before the reaction is initiated by the addition of 10 μL of 20 mM Mg-ATP. For all enzymes the final concentration is approximated to the Michaelis constant (Km). Assays are carried out for 30min at room temperature before termination by the addition of 5 μL orthophosphoric acid. After mixing, the well contents are harvested onto a P81 Unifilter plate, using orthophosphoric acid as the wash buffer. Then IC50 is calculated.
Cell Research:[1]
+ Expand
  • Cell lines: PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 and RWPE-1 cells
  • Concentrations: 62.5 nM - 16 mM
  • Incubation Time: 1, 3 and 5 days
  • Method: Cells are seeded at a density of 2× 103 in 96-well plates and incubated overnight. Then Saracatinib (62.5 nM-16 mM) is added to the cells. After 1, 3 and 5 days, culture medium is removed followed by addition of 0.2 mL DMSO per well and continuous shaking of plates at 200 rotations per minute for 15min. Then IC50 is measured by MTT metho
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: CB17 mice are implanted with DU145 cells.
  • Formulation: Dissolved in 0.5% hydroxypropyl methylcellulose, 0.1% Tween 80
  • Dosages: 25 mg/kg
  • Administration: Orally administered daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL warmed (64.57 mM)
Ethanol 31 mg/mL (57.19 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
5mg/mL

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

Chemical Information

Molecular Weight 542.03
Formula

C27H32ClN5O5

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

  • Mass
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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):
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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