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AZD9496 maleate

Chemical Structure : AZD9496 maleate

CAS No.: 1639042-28-6

AZD9496 maleate (AZD-9496 maleate)

Catalog No.: PC-43271Not For Human Use, Lab Use Only.

A potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68; shows pM equipotent binding to both ERα and ERβ isoforms, highly selective binding compared with progesterone (∼650-fold), glucocorticoid (∼11,223-fold), and androgen (∼36,375-fold) receptor LBDs; downregulator of ERα in vitro and in vivo in ER-positive models of breast cancer and orally available.

Breast Cancer

Phase 1 Clinical

Physicochemical Properties

M.Wt 558.5456
Formula C29H29F3N2O6
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

2-Propenoic acid, 3-[3,5-difluoro-4-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]phenyl]-, (2E)-, (2Z)-2-butenedioate (1:1)

References

1. De Savi C, et al. J Med Chem. 2015 Oct 22;58(20):8128-40.

2. Weir HM, et al. Cancer Res. 2016 Jun 1;76(11):3307-18.

3. Toy W, et al. Cancer Discov. 2017 Mar;7(3):277-287.

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