Saracatinib Inhibitor CAS No. 379231-04-6

Cat. No.	Name	Size	Price
KI0072	Saracatinib	10 mg	$112
	Saracatinib	25 mg	$272
	Saracatinib	200 mg	$1072

Chemical Characteristic

Product Name	Saracatinib
Synonyms	AZD0530
CAS No.	379231-04-6
Molecular Weight	542.03
Formula	C₂₇H₃₂ClN₅O₅
Chemical Name	N-(5-chlorobenzo[d][1,3]dioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine
Smiles	n1cnc(c2c(cc(cc12)OCCN1CCN(CC1)C)OC1CCOCC1)Nc1c2OCOc2ccc1Cl
Chemical Structure

Biological activities

Saracatinib is a novel Src family kinase/Abl dual-kinase inhibitor for c-Src and v-Abl with IC50 values of 2.7 and 30 nM, respectively. Saracatinib also inhibits epidermal growth factor receptor (EGFR) with an IC50 value of 66 nM. In five of the human cancer cell lines (tumor types: colon, prostate, lung, and leukemia), saracatinib has IC50 values of 0.2-0.7 µM. Saracatinib inhibits growth of PC-9 cells with an IC50 of 0.23 µM. Saracatinib inhibits proliferation of the Bcr??bl-driven human leukemia cell line K562 with an IC50 of 0.22 µM. Saracatinib reduces the migration of human lung cancer A549 cells in a concentration-dependent manner with an IC50 of 0.14 µM. Saracatinib (10-500 nM) has a dose-dependent antimigratory effect compared with untreated controls in monolayer scratch assays of human breast cancer MDA-MB-231 cells. Saracatinib also dose dependently inhibits the epidermal growth factor- (EGF-) and collagen-stimulated migration of NBT-II bladder cancer cells. Moreover, saracatinib (0.25 µM) consistently inhibits migration of bladder cancer cell lines T24, SCaBER, and 1A6 by 31 %, 37 % and 78 %, respectively. Saracatinib treatment (1 µM) induces a relocalization of paxillin from the cell membrane into the cell cytoplasm.^[1] Saracatinib at concentrations of 5.0 and 10.0 µM significantly inhibits ⁴⁵Ca release by 30% and 50% from cultured fetal calvarial mouse bone explants. Saracatinib dose-dependently inhibits osteoclast formation in osteoblast/ PBMC (peripheral blood mononuclear cells) cocultures.^[2] Saracatinib treatment of DU145 and PC3 respectively increases the proportion of G0/G1 cells by 21 and 11% and concurrently decreases S cells by 22 and 10% in the cell cycle, respectively. Saracatinib inhibits DU145 and PC3 migration in the Boyden chamber in a dose-dependent manner.^[3] In Src3T3 allografts and xenografts models, saracatinib (??6 mg/kg/day) has 60% inhibition of tumor growth in mice and 98% inhibition of tumor growth in rats versus animals treated with vehicle. Besides, in human tumor cell MDA-MB-231 and AsPc-1 xenografts models, saracatinib (50 mg/kg) has mean inhibition of tumor volume relative to control by 40 % and 42 %, respectively.^[1] In prostate cancer DU145 xenografts model, saracatinib (25 mg/kg) has an average 45% smaller tumor than control mice.^[3]

Protocols

Saracatinib is dissolved in DMSO.^[1]

References

[1] Green TP, et al. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol. 2009, 3(3): 248-261. [2] de Vries TJ, et al. The Src inhibitor AZD0530 reversibly inhibits the formation and activity of human osteoclasts. Mol Cancer Res. 2009, 7(4): 476-488. [3] Chang YM, et al. Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene. 2008, 27(49): 6365-6375.

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