Saracatinib (AZD0530)

Catalog No.S1006 Batch:S100615

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Technical Data

Formula

C27H32ClN5O5
Molecular Weight 542.03 CAS No. 379231-04-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (184.49 mM)
Ethanol 100 mg/mL (184.49 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
1.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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). Saracatinib induces autophagy. Phase 2/3.
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)		 View More
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]
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]
Features The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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
Animal Study:

[1]
  • Animal Models

    CB17 mice are implanted with DU145 cells.

  • Dosages

    25 mg/kg

  • Administration

    Orally administered daily

Customer Product Validation

Data from [Cancer Res, 2013, 71, 7547-57]

Data from [J Biomol Screen, 2013, 18, 54-66]

Data from [J Biomol Screen, 2013, 18, 54-66]

Data from [Cancer Res, 2012, 71, 7547-57]

Selleck's Saracatinib (AZD0530) has been cited by 340 publications

Heterogeneity-driven phenotypic plasticity and treatment response in branched-organoid models of pancreatic ductal adenocarcinoma [ Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9] PubMed: 39658630
The pro-oncogenic noncanonical activity of a RAS•GTP:RanGAP1 complex facilitates nuclear protein export [ Nat Cancer, 2024, ] PubMed: 39528835
Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src [ Nat Commun, 2024, 15(1):1300] PubMed: 38346942
The proto-oncogene tyrosine kinase c-SRC facilitates glioblastoma progression by remodeling fatty acid synthesis [ Nat Commun, 2024, 15(1):7455] PubMed: 39198451
Viral infection induces inflammatory signals that coordinate YAP regulation of dysplastic cells in lung alveoli [ J Clin Invest, 2024, 134(19)e176828] PubMed: 39352385
The SRC-family serves as a therapeutic target in triple negative breast cancer with acquired resistance to chemotherapy [ Br J Cancer, 2024, 131(10):1656-1667] PubMed: 39390250
RAPSYN-mediated neddylation of BCR-ABL alternatively determines the fate of Philadelphia chromosome-positive leukemia [ Elife, 2024, 12RP88375] PubMed: 38865175
Gender-different effect of Src family kinases antagonism on photophobia and trigeminal ganglion activity [ J Headache Pain, 2024, 25(1):175] PubMed: 39390364
Merkel cell polyomavirus protein ALTO modulates TBK1 activity to support persistent infection [ PLoS Pathog, 2024, 20(7):e1012170] PubMed: 39074144
EGFRvIII Confers Sensitivity to Saracatinib in a STAT5-Dependent Manner in Glioblastoma [ Int J Mol Sci, 2024, 25(11)6279] PubMed: 38892466

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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