AZD9496
- CAS NO.:1639042-08-2
- Empirical Formula: C25H25F3N2O2
- Molecular Weight: 442.47
- MDL number: MFCD28902195
- Update Date: 2024-11-01 18:09:03
What is AZD9496?
Description
AZD 9496 is a potent and selective estrogen receptor downregulator (SERD) with an IC50 value of 0.138 nM for estrogen receptor α (ERα) downregulation. It is selective for ERα compared to other nuclear hormone receptors with IC50 values of 0.0008, 0.54, 9.2, and 30 μM for ERα, progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR), respectively. AZD 9496 decreases ERα activity (IC50 = 0.282 nM), measured via quantification of downstream PR activity, and reduces proliferation of MCF-7 breast cancer cells (IC50 = 0.0398 nM). It also inhibits MCF-7 xenograft growth in mice in a dose-dependent manner. AZD 9496 is orally bioavailable and formulations containing it are under investigation in clinical trials for treatment of ER positive breast cancer.
in vitro
azd9496 was identified as a nonsteroidal small-molecule inhibitor of erα, which was a potent and selective antagonist and downregulator of erα. in addition, azd9496 could bind and downregulate clinically relevant esr1 mutants [1].
in vivo
animal study reported that significant tumor growth inhibition was observed as low as 0.5 mg/kg dose of azd9496 in the estrogen-dependent mcf-7 xenograft model, and such effect was accompanied by a dose-dependent decrease in pr protein levels, providing potent antagonist activity. in addition, the combination of azd9496 with pi3k pathway and cdk4/6 inhibitors resulted in further growth-inhibitory effects when compared with monotherapy alone. furthermore, the tumor regression was also observed in a long-term estrogen-deprived breast model, in which significant erα protein downregulation was found [1].
References
[1] weir hm et al. azd9496: an oral estrogen receptor inhibitor that blocks the growth of er-positive and esr1-mutant breast tumors in preclinical models. cancer res. 2016 jun 1;76(11):3307-18.
[2] https://clinicaltrials. gov/ct2/show/nct02780713 term=azd9496&rank=2
Properties of AZD9496
Boiling point: | 541.0±50.0 °C(Predicted) |
Density | 1.286±0.06 g/cm3(Predicted) |
storage temp. | 4°C, protect from light, stored under nitrogen |
solubility | Soluble in DMSO |
pka | 4.08±0.10(Predicted) |
form | A crystalline solid |
color | Light yellow to brown |
Safety information for AZD9496
Computed Descriptors for AZD9496
New Products
Bromine 99.5% AR (4 x 500ml) Fehling's Solution No. B Amino Acid Kit of 23 items set Ammonium Molybdate Reagent Solution Beam's Reagent Solution Ehrlich's Reagent For detection of urobillinogen 4-Hydroxy Carbazole 4-((2-isopropoxyethoxy)methyl)phenol 2 – Methoxy – 5- Sulfamoyl Benzoic acid Amino Salicylic Acid. U.S.P. 1,2,3,4-Tetrahydrocarbazol-4-one Acetone Isobutryl oxime ester Curcuma aromatica Oil Curry leaf Extract Terminalia bellirica Extract Aloe vera extract 200x Withania somnifera (Ashwagandha Extract) Citrus bioflavonoids Extract (S)-4-(4-(5-(Aminomethyl)-2-Oxooxazolidin-3-Yl)Phenyl)Mo Ethyl N-[[2-[[[4-(Aminoiminomethyl)Phenyl]Amino]Methyl] 5-Nitrosalicylaldehyde 5-(Difluoromethoxy)-2-Mercapto-1H-Benzimidazole- IP/BP/ Cypermethric Acid Chloride Methyl Di Chloride (Mdc)Related products of tetrahydrofuran
You may like
-
7726-95-6 Bromine 99.5% AR (4 x 500ml) 99%View Details
7726-95-6 -
Formamide 99%View Details
75-12-7 -
376608-65-0 2-[[(3Ar,4S,6R,6As)-6-Aminotetrahydro-2,2-Dimethyl-4H-Cy 99%View Details
376608-65-0 -
2, 4-Pyrimidinediamine 3-Oxide 99%View Details
74638-76-9 -
111974-72-2 99%View Details
111974-72-2 -
85-81-4 6-Methoxy-8-Nitroquinoline 99%View Details
85-81-4 -
3-Bromo-4,5-Dihydro-1H-Benzo[B]Azepin-2(3H)-One 99%View Details
86499-96-9 -
(−)-Dip-Chloride 85116-37-6 99%View Details
85116-37-6