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 M2HvU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwME[xOFMh|ryP MX7TRW5ITVJ?
LAMA-84 NVjvXHRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PIU2lEPTB;MD6xOVk6KM7:TR?= NVixeIh4W0GQR1XS
MEG-01 NX\iUlJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rZd2lEPTB;MD6yN|Y5QCEQvF2= MmTxV2FPT0WU
EM-2 NFnyfHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHrRVB[UUN3ME2wMlI3PSEQvF2= M1LvVnNCVkeHUh?=
TE-15 NF\CW5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFyyfIJKSzVyPUCuNlc1OTJizszN M1fF[3NCVkeHUh?=
NCI-H1648 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2qxN2lEPTB;MD6yPFEyPiEQvF2= MYfTRW5ITVJ?
TE-12 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjsTWM2OD1yLkOyOlgh|ryP NUT5eIpMW0GQR1XS
LB996-RCC MmXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTMTWM2OD1yLkS0NVk3KM7:TR?= NH\rdXZUSU6JRWK=
K-562 M{\uOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7qTWM2OD1yLkS0PVY4KM7:TR?= MVjTRW5ITVJ?
D-336MG NUDPNVE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVqxT4hoUUN3ME2wMlUxOzB2IN88US=> NILYRVJUSU6JRWK=
NOS-1 M4LScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvoNllKSzVyPUCuOlA2OjlizszN NHPl[3NUSU6JRWK=
EW-24 M3\0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PoVGlEPTB;MD62NlY6OyEQvF2= NV73NINlW0GQR1XS
BV-173 MmLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTNV5JKUUN3ME2wMlY2OjR7IN88US=> MoPZV2FPT0WU
NCCIT MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwN{OyNVgh|ryP MmrKV2FPT0WU
NCI-H1436 NVz4PXh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2m2S2lEPTB;MD63PVA1QSEQvF2= NIrBSWlUSU6JRWK=
BB30-HNC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\lemlEPTB;MD64OlIxOyEQvF2= M1nubnNCVkeHUh?=
TE-8 NXfDWIU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwOEeyO|Uh|ryP NX\VfGpyW0GQR1XS
A704 M2PDZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwOEmyNUDPxE1? MULTRW5ITVJ?
TK10 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPlRXZVUUN3ME2wMlkxPjZ7IN88US=> M1Psb3NCVkeHUh?=
KS-1 M1H0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTFwMUm3O|kh|ryP NYX1WG5wW0GQR1XS
C2BBe1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XadGlEPTB;MT6yNFUxPyEQvF2= MWTTRW5ITVJ?
RXF393 NVnX[21KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnYZ41KSzVyPUGuNlQ{PiEQvF2= NEe1bGlUSU6JRWK=
KGN MofHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFwMke2PFch|ryP NXLH[JlUW0GQR1XS
NB69 NEOxRmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nTPWlEPTB;MT6zO|Q6PyEQvF2= NVnwNpdDW0GQR1XS
TE-11 NFexZ41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwNEO0NVgh|ryP MWrTRW5ITVJ?
TE-1 NUjEZZFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfLTWM2OD1zLkS0NVA2KM7:TR?= NYHETHRzW0GQR1XS
ST486 NXqwe3ZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILGR2tKSzVyPUGuOFU5PTJizszN NHPSOItUSU6JRWK=
HOP-62 Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXP0[WYzUUN3ME2xMlUxOjR4IN88US=> MYTTRW5ITVJ?
EW-16 MnzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXUTWM2OD1zLkW1NFg{KM7:TR?= M{Pu[XNCVkeHUh?=
LB1047-RCC MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXPTWM2OD1zLkW1OFU{KM7:TR?= NXrMcoxrW0GQR1XS
TE-10 NVLmZWVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPzeJJOUUN3ME2xMlY3OjV{IN88US=> M3nCSXNCVkeHUh?=
RL95-2 Mm\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\MWJVKSzVyPUGuOlY6ODJizszN MWXTRW5ITVJ?
DOHH-2 M1LSOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnu[YhKSzVyPUGuO|E4QDJizszN NGfweZFUSU6JRWK=
MFH-ino MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\Nd3U3UUN3ME2xMlc4QDdizszN M2rQb3NCVkeHUh?=
GB-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLmTWM2OD1zLke5PFM{KM7:TR?= MWTTRW5ITVJ?
SK-N-DZ M2G1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLmfFZZUUN3ME2xMlg1Pjh6IN88US=> M4PhV3NCVkeHUh?=
OS-RC-2 MorxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoG3TWM2OD1zLki4OVc1KM7:TR?= NIPFWGpUSU6JRWK=
SW982 NHLaSJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGOyO3JKSzVyPUGuPVIxQTNizszN NXvEPVdPW0GQR1XS
KALS-1 M{K1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7p[GtKSzVyPUGuPVg4OjJizszN NInNeGxUSU6JRWK=
TGBC24TKB MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJwMEW5OVgh|ryP MkTlV2FPT0WU
GI-1 NGD0UmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr0NoV2UUN3ME2yMlE3ODh2IN88US=> MYnTRW5ITVJ?
SW962 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofxTWM2OD1{LkG3NVc5KM7:TR?= MVLTRW5ITVJ?
SW872 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\TTWM2OD1{LkG4OVA4KM7:TR?= MX;TRW5ITVJ?
NCI-H747 M2q3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTJwMkW3NVQh|ryP MkGxV2FPT0WU
MZ1-PC M1\RSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjuTWM2OD1{LkK5N|U3KM7:TR?= MVvTRW5ITVJ?
MSTO-211H MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\pTWM2OD1{LkO1O|I{KM7:TR?= M4XpfHNCVkeHUh?=
BL-70 M3jnWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmL6TWM2OD1{LkS3OFIzKM7:TR?= NWf0VXZ[W0GQR1XS
SW954 NGO3VIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f3ZWlEPTB;Mj61O|QxQCEQvF2= MlPJV2FPT0WU
SNB75 M3[xSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS0TWM2OD1{Lk[4OVk1KM7:TR?= MnPOV2FPT0WU
IST-SL2 NE\V[GhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHj2[IVKSzVyPUKuO|I{PzlizszN MnmxV2FPT0WU
GCIY M2jkRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nLNmlEPTB;Mj64O|AxPSEQvF2= NHL6XpNUSU6JRWK=
KU812 NUW3bVYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPOUI1KSzVyPUOuNFUzQTlizszN MYDTRW5ITVJ?
LXF-289 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\2[mtKSzVyPUOuNVIyODlizszN MYTTRW5ITVJ?
ETK-1 Mm\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHJPFJKSzVyPUOuNlA4PjdizszN M3r4VXNCVkeHUh?=
SF126 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTNwM{GxO|Qh|ryP MWTTRW5ITVJ?
LC-2-ad MkTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTNwNUW3JO69VQ>? MYXTRW5ITVJ?
KNS-42 MkS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HMZmlEPTB;Mz62OUDPxE1? MW\TRW5ITVJ?
OVCAR-4 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3nNXZMUUN3ME2zMlc{PDN|IN88US=> M4rQenNCVkeHUh?=
PF-382 NITkVlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\4WmlKSzVyPUOuPFM3QThizszN MoixV2FPT0WU
SH-4 Mne4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzobWpZUUN3ME20MlI2OjV7IN88US=> MkC2V2FPT0WU
KM12 NFPSc3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInqNHdKSzVyPUSuN|I1OTZizszN M3fXcXNCVkeHUh?=
NB5 NFvhTWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfmNWsxUUN3ME20MlQyQDZ2IN88US=> NV\jVIpHW0GQR1XS
KURAMOCHI NUXXNXhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn0XVdWUUN3ME20MlY2OjV4IN88US=> MUPTRW5ITVJ?
Becker NWnXcHNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXKTWM2OD12Lk[2OFE3KM7:TR?= MWrTRW5ITVJ?
MV-4-11 M3q4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofuTWM2OD12LkixN|Q1KM7:TR?= Mnu5V2FPT0WU
KINGS-1 NHrRSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2KzWWlEPTB;ND64NlM4OyEQvF2= NFHHZ4dUSU6JRWK=
LS-123 NUfCZ5VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfGTWM2OD13LkS5Olg1KM7:TR?= NXr3[YRSW0GQR1XS
SF268 NIPFZZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfITWM2OD13Lk[xNlYzKM7:TR?= NIPOTo9USU6JRWK=
A388 NEX1NmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXTeG03UUN3ME21MlY{PjZ5IN88US=> M1;wZnNCVkeHUh?=
NMC-G1 M{LuNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml74TWM2OD14LkCxPFEyKM7:TR?= M1S3d3NCVkeHUh?=
CGTH-W-1 M2rXd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;yVGlEPTB;Nj6wNlA4PSEQvF2= NHfqcmdUSU6JRWK=
ES4 NGTpT3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTZwNUOwO|Qh|ryP MmDKV2FPT0WU
SR NGO1bFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTZwNUi4NFch|ryP MXfTRW5ITVJ?
BB49-HNC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle2TWM2OD14LkezNlA3KM7:TR?= M1:weHNCVkeHUh?=
KLE MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\VTGlEPTB;Nj63PFM4PyEQvF2= MXfTRW5ITVJ?
HUTU-80 NH60UZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3hS|VKSzVyPU[uPVg1PjZizszN Ml\VV2FPT0WU
SNU-C2B NWPIXWRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2KybmlEPTB;Nz64Nlc{PyEQvF2= M4PLZnNCVkeHUh?=
BB65-RCC NVzlSY4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPlTWM2OD15Lkm0PVA1KM7:TR?= M4T6ZXNCVkeHUh?=
QIMR-WIL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HTWmlEPTB;OD60NlgxQCEQvF2= NYDF[I1nW0GQR1XS
GDM-1 MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfGbZRKSzVyPUiuPVczQTJizszN Mn7JV2FPT0WU
LC4-1 NUHTPZRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jqN2lEPTB;OT6wNFkyOSEQvF2= MnG4V2FPT0WU
MLMA NUj1No1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTlwMUWwNFYh|ryP MX3TRW5ITVJ?
EoL-1-cell MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PRSGlEPTB;OT6zNFE6OiEQvF2= Mm\0V2FPT0WU
BOKU M{\VO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jyOWlEPTB;OT65OlQ3PiEQvF2= NVrpVoFuW0GQR1XS
EVSA-T NITiSZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTFyLk[1Olgh|ryP M335N3NCVkeHUh?=
D-283MED M2mwVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTFyLkmxO|Yh|ryP MUHTRW5ITVJ?
NB1 NFr1SJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r0NWlEPTB;MUGuNFI1OiEQvF2= Mkj3V2FPT0WU
RPMI-8402 NHrDVGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X5dWlEPTB;MUGuNVc5KM7:TR?= MYXTRW5ITVJ?
NCI-H1355 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2m1VmlEPTB;MUGuNVgxPiEQvF2= MXjTRW5ITVJ?
NB7 MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\1TWM2OD1zMT6zNlk4KM7:TR?= Mn\5V2FPT0WU
RPMI-6666 M{PpXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfwTWM2OD1zMj65OVY4KM7:TR?= NIn3SINUSU6JRWK=
697 NXPIRmJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\KWmlEPTB;MUOuNlcxOSEQvF2= M3P6b3NCVkeHUh?=
CTB-1 NUnLTmtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLsTWM2OD1zMz61PVQ5KM7:TR?= M3PGN3NCVkeHUh?=
VA-ES-BJ MlP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEe1bYFKSzVyPUGzMlkzOzRizszN NH7KUY9USU6JRWK=
BE-13 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF2LkO5NVUh|ryP NEjzVlJUSU6JRWK=
SKM-1 NEezdlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\oPZRKSzVyPUG0MlQ1QTlizszN Mn76V2FPT0WU
TE-6 MkjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rCbWlEPTB;MUSuO|U6OSEQvF2= MorNV2FPT0WU
LB771-HNC MmL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF2Lke4PVgh|ryP M1PtXnNCVkeHUh?=
ECC4 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzWT2JzUUN3ME2xO{4xOjd5IN88US=> M4XVOXNCVkeHUh?=
ES3 MkHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTF5LkS2OVUh|ryP Mm[2V2FPT0WU
LB647-SCLC M1LqZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnFTWM2OD1zNz60PVQ6KM7:TR?= NVHhPZhUW0GQR1XS
NB10 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDTNVFKSzVyPUG4MlUzPTZizszN NXi1R3VzW0GQR1XS
L-540 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTF6LkixNFkh|ryP Ml;2V2FPT0WU
NCI-H2126 MlrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ThNmlEPTB;MUmuOVEh|ryP M1Tn[3NCVkeHUh?=
HH NETyRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTJyLkCwPVkh|ryP NE[wXFlUSU6JRWK=
MPP-89 M2Thfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTPV|dKSzVyPUKzMlIzQDlizszN NHvBSWhUSU6JRWK=
IST-MEL1 M33HdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJ|Lki2OVgh|ryP M3;ubHNCVkeHUh?=
KP-N-YS M{LESmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\vTWM2OD1{Mz65NlU2KM7:TR?= M3\zcHNCVkeHUh?=
EC-GI-10 M2P3fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4riSGlEPTB;MkSuOVk5QSEQvF2= MXXTRW5ITVJ?
EKVX NUPTSGRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH4TWM2OD1{Nj6wNlA{KM7:TR?= MWnTRW5ITVJ?
TGBC1TKB M{nGcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3MTWM2OD1{Nj60N|Qh|ryP MlzkV2FPT0WU
Daudi M4PEemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ5LkC3O|Mh|ryP Mly3V2FPT0WU
ALL-PO NF[3bolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;5NmlEPTB;MkeuNFgyKM7:TR?= MYXTRW5ITVJ?
NB6 M4HGSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zjeGlEPTB;MkeuOFg5KM7:TR?= NX64XmNIW0GQR1XS
ES6 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoSxTWM2OD1{Nz65NVI{KM7:TR?= MXnTRW5ITVJ?
COLO-320-HSR NWi4cHJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DTXmlEPTB;MkiuNFM4OyEQvF2= MVHTRW5ITVJ?
K5 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzhfoo2UUN3ME2yPE4yOjh5IN88US=> MX;TRW5ITVJ?
ES1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPoTWM2OD1{OD63O|c{KM7:TR?= NELldHlUSU6JRWK=
LC-1F NVi4WGZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXTbZR6UUN3ME2yPU44OzR4IN88US=> MWXTRW5ITVJ?
SCLC-21H MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTNyLkezNVch|ryP NHrjdFVUSU6JRWK=
SK-PN-DW NYizW4U4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTN{LkW1PVgh|ryP NWnDdIJvW0GQR1XS
D-247MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXXTWM2OD1|Mj65O|c{KM7:TR?= M{LoO3NCVkeHUh?=
TE-5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrLTWM2OD1|Mz6wN|YzKM7:TR?= MnP4V2FPT0WU
MONO-MAC-6 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTJRnltUUN3ME2zN{42ODR6IN88US=> NHjqO3lUSU6JRWK=
LB2518-MEL NULrUFNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTN|Lke2OlYh|ryP NGPrcpRUSU6JRWK=
LOXIMVI M3fERWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vkTmlEPTB;M{OuO|kzQCEQvF2= NFfEW4NUSU6JRWK=
NCI-H209 NXzzdYRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTN3LkG0OEDPxE1? NUnjZWxvW0GQR1XS
A253 NEW4XJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1mwT2lEPTB;M{WuO|QzQSEQvF2= NVm5ZZdQW0GQR1XS
HCC1599 MoXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3G1b2lEPTB;M{[uO|A2OyEQvF2= MWLTRW5ITVJ?
EB-3 NFfN[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LjXmlEPTB;M{[uPVUyQCEQvF2= MlzJV2FPT0WU
GOTO MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjwc3R3UUN3ME2zO{4{OjJ2IN88US=> MmPzV2FPT0WU
SW684 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLCTWM2OD12MT64OFk2KM7:TR?= M13sTXNCVkeHUh?=
DEL Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTR{LkC1NlIh|ryP M2PHVHNCVkeHUh?=
HT-144 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrQTWM2OD12Mj6xOlc3KM7:TR?= M2nMPXNCVkeHUh?=
TE-9 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXj3S29IUUN3ME20N{41PTl4IN88US=> MU\TRW5ITVJ?
KARPAS-45 MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjz[5ZKSzVyPUS0MlM6OjVizszN MX7TRW5ITVJ?
HAL-01 MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TYOmlEPTB;NESuOVA{PCEQvF2= MnPvV2FPT0WU
RCC10RGB Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHkV29PUUN3ME20OE44Ozl{IN88US=> NWDnOIpbW0GQR1XS
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NB17 NVH3c2lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTmcY9LUUN3ME20OU43PjR|IN88US=> NFXnTVVUSU6JRWK=
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JiyoyeP-2003 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[wbWlEPTB;NE[uNFEyQSEQvF2= NVjhTYVyW0GQR1XS
HCE-4 M2n1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\qTWM2OD12Nj61PVY5KM7:TR?= NHH6XmNUSU6JRWK=
NCI-H720 M2i4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nmUWlEPTB;NE[uO|Y5OiEQvF2= NHK4cmJUSU6JRWK=
KARPAS-422 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\OOWlEPTB;NEeuNFg6PSEQvF2= MVPTRW5ITVJ?
Ramos-2G6-4C10 NI\1cmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXvUYpKSzVyPUS3MlE3OjJizszN Mo\iV2FPT0WU
HCE-T M1:0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnmTWM2OD12Nz62PFI5KM7:TR?= MofCV2FPT0WU
PSN1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjXbGNKSzVyPUS3Mlc5OTNizszN M1rTZnNCVkeHUh?=

... 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 individually and in order:
2% DMSO+30% PEG 300+ddH2O
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)

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID