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Products are for research use only. Not for human use. We do not sell to patients.
(AZD0530; AZD-0530; AZD 0530)
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).
IC50 value: 2.7 nM(c-Src); 30 nM (v-Abl) 
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 . 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 . Saracatinib gives a potent and sustained blockage of AKT and enhances the sensitivity to irradiation in A549 and Calu-6 cells .
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 . Saracatinib shows great antitumor activity in orthotopic DU145 xenograft mice at a dose of 25mg/kg (orally administered, daily) .
|M.Wt||542.03||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
|1 mg||5 mg||10 mg|
|1 mM||1.8449 mL||9.2246 mL||18.4492 mL|
|5 mM||0.3690 mL||1.8449 mL||3.6898 mL|
|10 mM||0.1845 mL||0.9225 mL||1.8449 mL|
1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 (mu)M for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
1NM-PP1(PP1 Analog II) is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors(IC50=28 uM vSrc; 4.2 nM v-Src-as1 I338G).
A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.
AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.
CPDA is a novel potent SHIP2 inhibitor that can effectively ameliorate insulin resistance in 3T3-L1 adipocytes.
KX1-004 is a potent small molecule inhibitor of Src-PTK as a potential protective drug for NIHL.
Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.
PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFR(alpha) and no activity on InsR and PKC.
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