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Saracatinib

Cat. No. M1659
Saracatinib Structure
Synonym:

AZD0530

Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 150 In stock
100mg USD 240 In stock
200mg USD 350 In stock
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Quality Control
Biological Activity

Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively.Saracatinib (AZD0530) demonstrated potent antimigratory and antiinvasive effects in vitro, and inhibited metastasis in a murine model of bladder cancer. Antiproliferative activity of AZD0530 in vitro varied between cell lines (IC50=0.2 ~10 mM).

Protocol
Cell Experiment
Cell lines Calu-6, A549, LoVo, SW 403, HT29, HCT 116 and other cells line
Preparation method Cell proliferation was assessed using a colorimetric 5-bromo- 20 -deoxyuridine (BrdU) Cell Proliferation ELISA kit (Roche Diagnostics GmbH), as described previously (Ple´ et al., 2004). Briefly, cells were plated onto 96-well plates (1.5*104 cells/ well), the following day 0.039–20 μM AZD0530 in DMSO (at a final concentration of 0.5%) was added and the cells were incubated for 24 h. The cells were pulse labeled with BrdU for 2 h and fixed. Cellular DNA was then denatured with the provided solution and incubated with antiBrdU peroxidase for 90 min. Following three washes with phosphate-buffered saline, tetramethylbenzidine substrate solution was added and the plates were incubated on a plate shaker for 10–30 min until the positive control absorbance at 690 nm was approximately 1.5 absorbance units.
Concentrations 0.039–20 μM
Incubation time 24 h
Animal Experiment
Animal models female nude mice bearing LoVo tumors, Src3T3 allografts and human NSCLC (Calu-6) xenografts
Formulation saline
Dosages 6.25–50 mg/kg for 10–91 days
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 542.03
Formula C27H32ClN5O5
CAS Number 379231-04-6
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Src inhibition with saracatinib reverses fulvestrant resistance in ER-positive ovarian cancer models in vitro and in vivo.
Simpkins et al. Clin Cancer Res. 2012 Aug 15. PMID: 22896656.

Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo.
Liu et al. Int J Cancer. 2012 May 24. PMID: 22623106.

Common PIK3CA mutants and a novel 3' UTR mutation are associated with increased sensitivity to saracatinib.
Arcaroli et al. Clin Cancer Res. 2012 May 1;18(9):2704-14. PMID: 22553375.

Phase I study of saracatinib (AZD0530) in combination with paclitaxel and/or carboplatin in patients with solid tumours.
Kaye et al. Br J Cancer. 2012 May 22;106(11):1728-34. PMID: 22531637.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Saracatinib, AZD0530 supplier, Src-bcr-Abl, inhibitors

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