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AZD9496

CAT: 0013-GTR19163769-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163769-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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.
CAS Number
1639042-08-2
Product Name Alternative
AZD-9496
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
Molecular Formula
C25H25F3N2O2
Molecular Weight
442.4734
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
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) -

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