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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Saracatinib

HY-10234

(AZD0530; AZD-0530; AZD 0530)

Saracatinib
Saracatinib Chemical Structure

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q).

Price and Availability of Saracatinib
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Saracatinib Data Sheet

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Purity: 99.85%

Saracatinib

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Biological Activity of Saracatinib

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q).
IC50 value: 2.7 nM(c-Src); 30 nM (v-Abl) [1]
Target: c-Src; v-Abl
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 signi?cantly 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].
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].

[1]. Chang YM, Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene, 2008, 27(49), 6365-6375.
[2]. Green TP, et al. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol, 2009, 3(3), 248-261.
[3]. Purnell PR, et al. The Src inhibitor AZD0530 blocks invasion and may act as a radiosensitizer in lung cancer cells. J Thorac Oncol, 2009, 4(4), 448-454.

Products are for research use only. Not for human use. We do not sell to patients.

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