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Saracatinib

Cat. No. M1659
Saracatinib Structure
Synonym:

AZD0530

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
5mg USD 40  USD40 In stock
10mg USD 55  USD55 In stock
50mg USD 150  USD150 In stock
100mg USD 265  USD265 In stock
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Quality Control & Documentation
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 (for reference only)
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
Chemical Information
Molecular Weight 542.03
Formula C27H32ClN5O5
CAS Number 379231-04-6
Solubility (25°C) DMSO 33 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Simpkins et al. Clin Cancer Res. Src inhibition with saracatinib reverses fulvestrant resistance in ER-positive ovarian cancer models in vitro and in vivo.

[2] Liu et al. Int J Cancer. Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo.

[3] Arcaroli et al. Clin Cancer Res. Common PIK3CA mutants and a novel 3' UTR mutation are associated with increased sensitivity to saracatinib.

[4] Kaye et al. Br J Cancer. Phase I study of saracatinib (AZD0530) in combination with paclitaxel and/or carboplatin in patients with solid tumours.

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


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