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 NXLN[I1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m2bGlEPTB;MD6wOlE1OyEQvF2= M4fGSnNCVkeHUh?=
LAMA-84 NXjTSJlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlqxTWM2OD1yLkG1PVkh|ryP MoC2V2FPT0WU
MEG-01 NXPLPW5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXrTWM2OD1yLkKzOlg5KM7:TR?= M2DOT3NCVkeHUh?=
EM-2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TyU2lEPTB;MD6yOlUh|ryP NIPoSYdUSU6JRWK=
TE-15 NFSy[49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwMke0NVIh|ryP NHXaO2dUSU6JRWK=
NCI-H1648 Mnz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPsTWM2OD1yLkK4NVE3KM7:TR?= NYrqWpc1W0GQR1XS
TE-12 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwM{K2PEDPxE1? MoftV2FPT0WU
LB996-RCC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLoVIk5UUN3ME2wMlQ1OTl4IN88US=> NITxfYZUSU6JRWK=
K-562 Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrnTFdPUUN3ME2wMlQ1QTZ5IN88US=> M{T2T3NCVkeHUh?=
D-336MG M3rIPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjVOod[UUN3ME2wMlUxOzB2IN88US=> NGezdllUSU6JRWK=
NOS-1 M{f6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwNkC1Nlkh|ryP NFPacmtUSU6JRWK=
EW-24 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwNkK2PVMh|ryP NHjwbIFUSU6JRWK=
BV-173 M37tRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwNkWyOFkh|ryP NEjHNIxUSU6JRWK=
NCCIT MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3NO5Y{UUN3ME2wMlc{OjF6IN88US=> NUXZXpNOW0GQR1XS
NCI-H1436 M3q3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3vfWJKSzVyPUCuO|kxPDlizszN MVLTRW5ITVJ?
BB30-HNC MmXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXPO4k2UUN3ME2wMlg3OjB|IN88US=> M3znT3NCVkeHUh?=
TE-8 M2XlNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFznRY1KSzVyPUCuPFczPzVizszN M3nZcnNCVkeHUh?=
A704 Ml7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfoTWM2OD1yLki5NlEh|ryP NXrQb3IzW0GQR1XS
TK10 NWX3Tm5WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXKTWM2OD1yLkmwOlY6KM7:TR?= M4jMWnNCVkeHUh?=
KS-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwMUm3O|kh|ryP MnHsV2FPT0WU
C2BBe1 Mlr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rtbWlEPTB;MT6yNFUxPyEQvF2= MXzTRW5ITVJ?
RXF393 NWW4SnZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLtTWM2OD1zLkK0N|Yh|ryP NVfQUolTW0GQR1XS
KGN NIHTVWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFwMke2PFch|ryP NVXJV5RKW0GQR1XS
NB69 NVHhfFhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHq0b3ZKSzVyPUGuN|c1QTdizszN MUXTRW5ITVJ?
TE-11 M3i0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkC4TWM2OD1zLkSzOFE5KM7:TR?= MnLRV2FPT0WU
TE-1 NIPVWYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrtd5VoUUN3ME2xMlQ1OTB3IN88US=> NULiZZpLW0GQR1XS
ST486 NWHqWohpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fpcmlEPTB;MT60OVg2OiEQvF2= NV\KWWJbW0GQR1XS
HOP-62 M3vyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\aemlEPTB;MT61NFI1PiEQvF2= MoXoV2FPT0WU
EW-16 NWDZZVJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfpdJdFUUN3ME2xMlU2ODh|IN88US=> NFuyWZNUSU6JRWK=
LB1047-RCC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLvdWZrUUN3ME2xMlU2PDV|IN88US=> NYHNV2NWW0GQR1XS
TE-10 NGPybVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLBTWM2OD1zLk[2NlUzKM7:TR?= NXPVfolTW0GQR1XS
RL95-2 MoPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFwNk[5NFIh|ryP NIfnZ5dUSU6JRWK=
DOHH-2 NITCPHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTaSmx4UUN3ME2xMlcyPzh{IN88US=> M3Xie3NCVkeHUh?=
MFH-ino MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTFwN{e4O{DPxE1? NHPneldUSU6JRWK=
GB-1 NIrW[FZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLJSplKUUN3ME2xMlc6QDN|IN88US=> NEDXW2NUSU6JRWK=
SK-N-DZ M3Pme2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorETWM2OD1zLki0Olg5KM7:TR?= M2OyNnNCVkeHUh?=
OS-RC-2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTFwOEi1O|Qh|ryP MorpV2FPT0WU
SW982 NWHq[5J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFwOUKwPVMh|ryP NIDvbYpUSU6JRWK=
KALS-1 NIXid3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHMS|RKSzVyPUGuPVg4OjJizszN MnrpV2FPT0WU
TGBC24TKB NX\hcXV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJwMEW5OVgh|ryP NIO2UIVUSU6JRWK=
GI-1 NFO3R|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTlTWM2OD1{LkG2NFg1KM7:TR?= NWPMXnZxW0GQR1XS
SW962 NWPCN2xoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJwMUexO|gh|ryP MlPrV2FPT0WU
SW872 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zXUWlEPTB;Mj6xPFUxPyEQvF2= M{i0dHNCVkeHUh?=
NCI-H747 NF3seZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jMSGlEPTB;Mj6yOVcyPCEQvF2= NULQS3d{W0GQR1XS
MZ1-PC NH7sbppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTJwMkmzOVYh|ryP MmrhV2FPT0WU
MSTO-211H NI\kO2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M335VWlEPTB;Mj6zOVczOyEQvF2= NGqwb4NUSU6JRWK=
BL-70 NFnIV2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLFTWM2OD1{LkS3OFIzKM7:TR?= M3G5cXNCVkeHUh?=
SW954 Mk\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PIWmlEPTB;Mj61O|QxQCEQvF2= NUDWUZlVW0GQR1XS
SNB75 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXre5B6UUN3ME2yMlY5PTl2IN88US=> MYDTRW5ITVJ?
IST-SL2 M{DhSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTJwN{KzO|kh|ryP M4LURXNCVkeHUh?=
GCIY Mmi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3JTWM2OD1{Lki3NFA2KM7:TR?= MlzUV2FPT0WU
KU812 NVHOcYxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHuw[XpKSzVyPUOuNFUzQTlizszN MUjTRW5ITVJ?
LXF-289 NG\0b4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjlNYRDUUN3ME2zMlEzOTB7IN88US=> M37mcHNCVkeHUh?=
ETK-1 MoX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTNwMkC3Olch|ryP NFizWFBUSU6JRWK=
SF126 NXraS5ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLSZ4pKSzVyPUOuN|EyPzRizszN NELsSFlUSU6JRWK=
LC-2-ad Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTNwNUW3JO69VQ>? M3XkUHNCVkeHUh?=
KNS-42 NXHEXHdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH1b5dKSzVyPUOuOlUh|ryP M1PjT3NCVkeHUh?=
OVCAR-4 NV\tSVdZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;VO2lEPTB;Mz63N|Q{OyEQvF2= MmnSV2FPT0WU
PF-382 M4WwVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHWXYRTUUN3ME2zMlg{Pjl6IN88US=> M4PJenNCVkeHUh?=
SH-4 NGnEVXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrE[JhKSzVyPUSuNlUzPTlizszN MXzTRW5ITVJ?
KM12 MkPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HzOGlEPTB;ND6zNlQyPiEQvF2= NFPib5BUSU6JRWK=
NB5 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHaTWM2OD12LkSxPFY1KM7:TR?= NWi1cJJvW0GQR1XS
KURAMOCHI MojuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTRwNkWyOVYh|ryP NHrDdpBUSU6JRWK=
Becker Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TyO2lEPTB;ND62OlQyPiEQvF2= MmnKV2FPT0WU
MV-4-11 NEn1O|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofCTWM2OD12LkixN|Q1KM7:TR?= NI\tNHFUSU6JRWK=
KINGS-1 MlHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK0TWM2OD12LkiyN|c{KM7:TR?= M4PUb3NCVkeHUh?=
LS-123 MkL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLOXYN[UUN3ME21MlQ6Pjh2IN88US=> NWHNXpNSW0GQR1XS
SF268 NU\uNVFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DC[WlEPTB;NT62NVI3OiEQvF2= NEfhXXNUSU6JRWK=
A388 NGjDVHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LnbGlEPTB;NT62N|Y3PyEQvF2= MnSzV2FPT0WU
NMC-G1 NWnQVIlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{i4XWlEPTB;Nj6wNVgyOSEQvF2= MojUV2FPT0WU
CGTH-W-1 NYLMSnU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUP5cIk5UUN3ME22MlAzODd3IN88US=> NGPYVYhUSU6JRWK=
ES4 NYnI[pB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf1VYFwUUN3ME22MlU{ODd2IN88US=> NEnTS5BUSU6JRWK=
SR NUHQPFlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVH1UY1QUUN3ME22MlU5QDB5IN88US=> M2HYS3NCVkeHUh?=
BB49-HNC MmfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWiwNIxzUUN3ME22Mlc{OjB4IN88US=> MXXTRW5ITVJ?
KLE NXv6VXJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTZwN{izO|ch|ryP NWXoXm1HW0GQR1XS
HUTU-80 NXvvfo5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTZwOUi0OlYh|ryP MW\TRW5ITVJ?
SNU-C2B NUfFUHlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTdwOEK3N|ch|ryP M4T2NnNCVkeHUh?=
BB65-RCC NXLOPFJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfDWmZKSzVyPUeuPVQ6ODRizszN NVrI[mxTW0GQR1XS
QIMR-WIL NX3oR2lMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUmyPJNuUUN3ME24MlQzQDB6IN88US=> M{jXRnNCVkeHUh?=
GDM-1 MmHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRThwOUeyPVIh|ryP M3X0T3NCVkeHUh?=
LC4-1 M3:xR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13L[GlEPTB;OT6wNFkyOSEQvF2= NFfMS3FUSU6JRWK=
MLMA NYXoWYhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LhWGlEPTB;OT6xOVAxPiEQvF2= M2LGW3NCVkeHUh?=
EoL-1-cell MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDCUVlnUUN3ME25MlMxOTl{IN88US=> NWjDOmh3W0GQR1XS
BOKU NW[2cZdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K3NGlEPTB;OT65OlQ3PiEQvF2= M1zRPHNCVkeHUh?=
EVSA-T MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrZS|NKSzVyPUGwMlY2PjhizszN NWHVTpRXW0GQR1XS
D-283MED NE\qVJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTPNlVKSzVyPUGwMlkyPzZizszN NF;QOGZUSU6JRWK=
NB1 M{TOemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITYVmVKSzVyPUGxMlAzPDJizszN NEDIVnpUSU6JRWK=
RPMI-8402 MlLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjBbYVKSzVyPUGxMlE4QCEQvF2= NVrHNIxyW0GQR1XS
NCI-H1355 NWqy[5lxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XLU2lEPTB;MUGuNVgxPiEQvF2= MWTTRW5ITVJ?
NB7 NGfqTmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrrfYdKSzVyPUGxMlMzQTdizszN MUnTRW5ITVJ?
RPMI-6666 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPU[oZsUUN3ME2xNk46PTZ5IN88US=> M1Tw[HNCVkeHUh?=
697 NH\tPHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3iwNGlEPTB;MUOuNlcxOSEQvF2= NVvKUFQ{W0GQR1XS
CTB-1 MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITDVGZKSzVyPUGzMlU6PDhizszN MlPaV2FPT0WU
VA-ES-BJ NH3IVGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXVTnNKSzVyPUGzMlkzOzRizszN MXzTRW5ITVJ?
BE-13 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDhTWM2OD1zND6zPVE2KM7:TR?= MmOyV2FPT0WU
SKM-1 M{m5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTF2LkS0PVkh|ryP MkS1V2FPT0WU
TE-6 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTF2Lke1PVEh|ryP MW\TRW5ITVJ?
LB771-HNC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\DOlNwUUN3ME2xOE44QDl6IN88US=> NWLJVnFDW0GQR1XS
ECC4 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLoTWM2OD1zNz6wNlc4KM7:TR?= NWq5V2ZOW0GQR1XS
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LB647-SCLC NUe1VYpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF5LkS5OFkh|ryP M3rVWHNCVkeHUh?=
NB10 M1zlb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe4c5dKSzVyPUG4MlUzPTZizszN NVjadWhQW0GQR1XS
L-540 M1W4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XRNWlEPTB;MUiuPFExQSEQvF2= NXvVcZl3W0GQR1XS
NCI-H2126 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGn2fnlKSzVyPUG5MlUyKM7:TR?= NVjPZYU2W0GQR1XS
HH M4HRZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX6fWdKSzVyPUKwMlAxQTlizszN NFXOZ4NUSU6JRWK=
MPP-89 NXnLXYxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXhTWM2OD1{Mz6yNlg6KM7:TR?= M3rHRnNCVkeHUh?=
IST-MEL1 M4HLVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJ|Lki2OVgh|ryP M2nJdXNCVkeHUh?=
KP-N-YS NH;x[|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTkTWM2OD1{Mz65NlU2KM7:TR?= M4rrXHNCVkeHUh?=
EC-GI-10 NGPGPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInHbZdKSzVyPUK0MlU6QDlizszN MWLTRW5ITVJ?
EKVX NWHXfFFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfwcldWUUN3ME2yOk4xOjB|IN88US=> Mn[2V2FPT0WU
TGBC1TKB MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOzR2N[UUN3ME2yOk41OzRizszN MmT0V2FPT0WU
Daudi MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ5LkC3O|Mh|ryP MnHMV2FPT0WU
ALL-PO NUK4ZldUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC3TWM2OD1{Nz6wPFEh|ryP NUOwUJJDW0GQR1XS
NB6 M4XteGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LqemlEPTB;MkeuOFg5KM7:TR?= M1rzUHNCVkeHUh?=
ES6 NYDDNIFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonMTWM2OD1{Nz65NVI{KM7:TR?= M1r5N3NCVkeHUh?=
COLO-320-HSR MlvqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfCTWM2OD1{OD6wN|c{KM7:TR?= M4PPVHNCVkeHUh?=
K5 NHr4ZZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW2TWM2OD1{OD6xNlg4KM7:TR?= NUG1VYIxW0GQR1XS
ES1 NV[2Z3VFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHm3[5hKSzVyPUK4Mlc4PzNizszN NUiyd3Y5W0GQR1XS
LC-1F NVfPNIpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTJ7LkezOFYh|ryP MX;TRW5ITVJ?
SCLC-21H NULDNnFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHH3NJVKSzVyPUOwMlc{OTdizszN MnThV2FPT0WU
SK-PN-DW NYfhbmNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLpTWM2OD1|Mj61OVk5KM7:TR?= MlvpV2FPT0WU
D-247MG NEDPXYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGO4[|FKSzVyPUOyMlk4PzNizszN M4fzT3NCVkeHUh?=
TE-5 M1e0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP5bmtKSzVyPUOzMlA{PjJizszN M2fObHNCVkeHUh?=
MONO-MAC-6 NWrKO|JTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;Zb3ZRUUN3ME2zN{42ODR6IN88US=> MXzTRW5ITVJ?
LB2518-MEL MnTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPrfZRKSzVyPUOzMlc3PjZizszN M1LCSXNCVkeHUh?=
LOXIMVI M{LrOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTN|Lke5Nlgh|ryP NW\4dnlVW0GQR1XS
NCI-H209 Mof6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFP6VGlKSzVyPUO1MlE1PCEQvF2= M1jucHNCVkeHUh?=
A253 NWjxUldOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTN3Lke0Nlkh|ryP MUHTRW5ITVJ?
HCC1599 NWnLVYJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PWb2lEPTB;M{[uO|A2OyEQvF2= NH\2RVdUSU6JRWK=
EB-3 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nobWlEPTB;M{[uPVUyQCEQvF2= Mn7GV2FPT0WU
GOTO M1\RPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mne0TWM2OD1|Nz6zNlI1KM7:TR?= M1nDdHNCVkeHUh?=
SW684 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC2WWNKSzVyPUSxMlg1QTVizszN NHrMRWJUSU6JRWK=
DEL MnfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXFSmRKSzVyPUSyMlA2OjJizszN MorZV2FPT0WU
HT-144 MkDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HMWGlEPTB;NEKuNVY4PiEQvF2= MonUV2FPT0WU
TE-9 MlOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHPbFlQUUN3ME20N{41PTl4IN88US=> Ml;GV2FPT0WU
KARPAS-45 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1znTGlEPTB;NESuN|kzPSEQvF2= NFPsSIdUSU6JRWK=
HAL-01 M1;FRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjrS2FKSzVyPUS0MlUxOzRizszN M36zW3NCVkeHUh?=
RCC10RGB NF;mRoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzt[nRTUUN3ME20OE44Ozl{IN88US=> M2C0bHNCVkeHUh?=
CP67-MEL M{LGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD0b|U3UUN3ME20OU43OjRzIN88US=> NULVc3BDW0GQR1XS
NB17 NY\iflRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vaeGlEPTB;NEWuOlY1OyEQvF2= MWrTRW5ITVJ?
SK-UT-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjVbmNkUUN3ME20OU46PDZ2IN88US=> MU\TRW5ITVJ?
JiyoyeP-2003 NUm0OZBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLFb4JKSzVyPUS2MlAyOTlizszN M3XmenNCVkeHUh?=
HCE-4 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnDU2kzUUN3ME20Ok42QTZ6IN88US=> NFqxfphUSU6JRWK=
NCI-H720 NX7Md45KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnjTWM2OD12Nj63OlgzKM7:TR?= MY\TRW5ITVJ?
KARPAS-422 M2S0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFu4V5VKSzVyPUS3MlA5QTVizszN Moj6V2FPT0WU
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HCE-T NEfDUoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTQN4RKSzVyPUS3MlY5OjhizszN NXrKR412W0GQR1XS
PSN1 M4O1WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7TTWM2OD12Nz63PFE{KM7:TR?= M3zpfHNCVkeHUh?=

... 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 )

  • 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):
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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

Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID