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SR-16157

Chemical Structure : SR-16157

CAS No.: 943344-76-1

SR-16157 (NSC 732011;SR16157;HLX 801)

Catalog No.: PC-61433Not For Human Use, Lab Use Only.

A novel dual-acting steroid sulfatase inhibitor (IC50=0.1 uM) and selective ERα modulator (SERM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A novel dual-acting steroid sulfatase inhibitor (IC50=0.1 uM) and selective ERα modulator (SERM); exerts STS inhibition and antiestrogenic effects, 10 times more potent than the antiestrogens SR-16137 and tamoxifen in cell growth and ERα function test in MCF-7 breast cancer cells; displays profoundly improved ERα binding affinity and antiestrogenic effects on expression of estrogen-regulated genes.

Breast Cancer

Phase 2 Clinical

Physicochemical Properties

M.Wt 492.719
Formula C27H44N2O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(7R,17R)-17-(2-(2-(diethylamino)ethoxy)ethyl)-7,13-dimethyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl sulfamate

References

1. Rasmussen LM, et al. Breast Cancer Res Treat. 2007 Dec;106(2):191-203.

2. Rausch L, et al. Cancer Chemother Pharmacol. 2011 Jun;67(6):1341-52.

3. Wang J, et al. J Pharm Biomed Anal. 2007 Nov 30;45(4):572-82.

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