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Saracatinib, Free Base (N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(oxan-4-yloxy)quinazolin-4-amine, AZD-0530)

Cat no: S0097-50

Saracatinib, Free Base (N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(oxan-4-yloxy)quinazolin-4-amine, AZD-0530)

Saracatinib an orally available Src kinase inhibitor. Saracatinib inhibits c-Src and Abl enzymes at low nanomolar concentrations. Saracatinib blocked the tumor growth of a c-Src-transfected 3T3-fibroblast xenograft in vivo and increased significantly the survival of animals in a highly aggressive model of human pancreatic cancer.\n\nSolubility:\nSoluble in DMSO.\n\nMelting Point:\n81-97C\n\nElemental Anaylsis:\nCalculated: \nC=59.83%\nH=5.95%\nCl=6.54%\nN=12.92%\n\nStorage and Stability:\nLyophilized powder may be stored at -20 degrees C. Stable for 6 months.

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SPECIFICATIONS

Catalog Number

S0097-50

Size

10mg

Form

Supplied as a white to off-white crystalline powder.

Purity

HPLC: ~99%. TLC: ~99%

References

1. Hennequin, L.F., et al. \"N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.\" J. Med. Chem. 49:6465-6488 (2006). 2. Green, T.P., et al. \"Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530.\" Mol. Oncol. 3:248-261 (2009). 3. Gwanmesia, P.M., et al. \"The effect of the dual Src/Abl kinase inhibitor AZD0530 on Philadelphia positive leukaemia cell lines.\" BMC Cancer 9:53 (2009). 4. Herynk, M.H., et al. \"Cooperative action of tamoxifen and c-Src inhibition in preventing the growth of estrogen receptor-positive human breast cancer cells.\" Mol. Cancer Ther. 5:3023-3031 (2006). 5. Chang, Y.M., et al. \"Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530.\" Oncogene 27:6365-6375 (2008). 6. Lara, P.N. Jr., et al. \"A phase II trial of the Src-kinase inhibitor AZD0530 in patients with advanced castration-resistant prostate cancer: a California Cancer Consortium study.\" Anticancer Drugs 20:179-184 (2009).

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