AZD9496

CAS No. 1639042-08-2

AZD9496( AZD-9496 )

Catalog No. M12477 CAS No. 1639042-08-2

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 64 In Stock
5MG 106 In Stock
10MG 178 In Stock
25MG 333 In Stock
50MG 493 In Stock
100MG 713 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    AZD9496
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68.
  • Description
    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(In Vitro):The potency of AZD9496 with IC50 of 0.82 nM, 0.14 nM, and 0.28 nM in ERα binding, downregulation, and antagonism, respectively. AZD9496 significantly inhibits MCF-7 cell growth with EC50 of 0.04 nM. Selectivity of AZD9496 over other tested nuclear hormone receptors is high: androgen receptor (AR), IC50=30 μM; glucocorticoid receptor (GR), IC50=9.2 μM; progesterone receptor (PR), IC50=0.54 μM. (In Vivo):Significant tumor growth inhibition is observed as low as 0.5 mg/kg dose in the estrogen-dependent MCF-7 xenograft model, where this effect is accompanied by a dose-dependent decrease in PR protein levels, demonstrating potent antagonist activity. Combining AZD9496 with PI3K pathway and CDK4/6 inhibitors lead to further growth-inhibitory effects compared with monotherapy alone. AZD9496, given once daily orally at 5 and 25 mg/kg produced statistically significant increases in uterine weight compared with the ICI 182780 control (P<0.001) but significantly lower than ICI 47699 (P=0.001). AZD9496 is also tested in a long-term estrogen deprived model (LTED), using the HCC-1428 LTED cell line that grows in the absence of estrogen and is thought to best represent a model of aromatase inhibition. AZD9496 shows significant activity, with a dose of 5 mg/kg giving tumor regressions in this model.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    AZD-9496
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    ERα
  • Research Area
    Cancer
  • Indication
    Breast Cancer

Chemical Information

  • CAS Number
    1639042-08-2
  • Formula Weight
    442.4734
  • Molecular Formula
    C25H25F3N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 104.5 mg/mL
  • SMILES
    CC1CC2=C(C(N1CC(C)(C)F)C3=C(C=C(C=C3F)C=CC(=O)O)F)NC4=CC=CC=C24
  • Chemical Name
    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)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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