Saracatinib (AZD0530)

CAS No. : 379231-04-6

Saracatinib (AZD0530),379231-04-6
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I003391
Molecular Formula:C₂₇H₃₂ClN₅O₅
Molecular Weight:542.03
IC50:2.7 nM(c-Src); 30 nM (v-Abl)
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Cat No:I003391
Cas No:379231-04-6
Product-Name:Saracatinib (AZD0530)
MDL No:MFCD09832698

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).

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 signicantly 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:Importance of the novel organic cation transporter 1 for tyrosine kinase inhibition by saracatinib in rheumatoid arthritis synovial fibroblasts. Harrach S, Edemir B, Schmidt-Lauber C, Pap T, Bertrand J, Ciarimboli G.Sci Rep. 2017 Apr 28;7(1):1258. doi: 10.1038/s41598-017-01438-4. PMID: 28455521 Free PMC Article
2:Cytochrome P450 Mediated Bioactivation of Saracatinib. Chen J, Peng Y, Zheng J.Chem Res Toxicol. 2016 Nov 21;29(11):1835-1842. Epub 2016 Nov 3. PMID: 27769111
3:PTTG1 Levels Are Predictive of Saracatinib Sensitivity in Ovarian Cancer Cell Lines. Nakachi I, Helfrich BA, Spillman MA, Mickler EA, Olson CJ, Rice JL, Coldren CD, Heasley LE, Geraci MW, Stearman RS.Clin Transl Sci. 2016 Dec;9(6):293-301. doi: 10.1111/cts.12413. Epub 2016 Oct 20. PMID: 27766744
4:Combined SRC inhibitor saracatinib and anti-ErbB2 antibody H2-18 produces a synergistic antitumor effect on trastuzumab-resistant breast cancer. Wang L, Yu X, Dong J, Meng Y, Yang Y, Wang H, Wang C, Zhang Y, Zhao Y, Zhao J, Wang H, Lu C, Li B.Biochem Biophys Res Commun. 2016 Oct 21;479(3):563-570. doi: 10.1016/j.bbrc.2016.09.111. Epub 2016 Sep 22. PMID: 27666484
5:Effect of saracatinib on pulmonary metastases from hepatocellular carcinoma. Xiong J, Wu JS, Mao SS, Yu XN, Huang XX.Oncol Rep. 2016 Sep;36(3):1483-90. doi: 10.3892/or.2016.4968. Epub 2016 Jul 22. PMID: 27460949
6:SRC kinase inhibition with saracatinib limits the development of osteolytic bone disease in multiple myeloma. Heusschen R, Muller J, Binsfeld M, Marty C, Plougonven E, Dubois S, Mahli N, Moermans K, Carmeliet G, Léonard A, Baron F, Beguin Y, Menu E, Cohen-Solal M, Caers J.Oncotarget. 2016 May 24;7(21):30712-29. doi: 10.18632/oncotarget.8750. PMID: 27095574 Free PMC Article
7:A randomized, double-blind phase II study evaluating cediranib versus cediranib and saracatinib in patients with relapsed metastatic clear-cell renal cancer (COSAK). Powles T, Brown J, Larkin J, Jones R, Ralph C, Hawkins R, Chowdhury S, Boleti E, Bhal A, Fife K, Webb A, Crabb S, Geldart T, Hill R, Dunlop J, Hall PE, McLaren D, Ackerman C, Beltran L, Nathan P.Ann Oncol. 2016 May;27(5):880-6. doi: 10.1093/annonc/mdw014. Epub 2016 Jan 22. PMID: 26802156
8:Saracatinib as a metastasis inhibitor in metastatic castration-resistant prostate cancer: A University of Chicago Phase 2 Consortium and DOD/PCF Prostate Cancer Clinical Trials Consortium Study. Posadas EM, Ahmed RS, Karrison T, Szmulewitz RZ, O/'Donnell PH, Wade JL 3rd, Shen J, Gururajan M, Sievert M, Stadler WM.Prostate. 2016 Feb 15;76(3):286-93. doi: 10.1002/pros.23119. Epub 2015 Oct 23. PMID: 26493492 Free PMC Article
9:Effectiveness of inhibitor rapamycin, saracatinib, linsitinib and JNJ-38877605 against human prostate cancer cells. Li W, Wang Z, Wang L, He X, Wang G, Liu H, Guo F, Wang Z, Chen G.Int J Clin Exp Med. 2015 Apr 15;8(4):6563-7. eCollection 2015. PMID: 26131286 Free PMC Article
10:Phase II study of saracatinib (AZD0530) in patients with previously treated metastatic colorectal cancer. Reddy SM, Kopetz S, Morris J, Parikh N, Qiao W, Overman MJ, Fogelman D, Shureiqi I, Jacobs C, Malik Z, Jimenez CA, Wolff RA, Abbruzzese JL, Gallick G, Eng C.Invest New Drugs. 2015 Aug;33(4):977-84. doi: 10.1007/s10637-015-0257-z. Epub 2015 Jun 12. PMID: 26062928
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