AZD9496
- ₹0
- Product name: AZD9496
- CAS: 1639042-08-2
- MF: C25H25F3N2O2
- MW: 442.47
- EINECS:
- MDL Number:MFCD28902195
- Synonyms:(E)-3-[3,5-Difluoro-4-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl]phenyl]acrylic 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]-2-propenoic acid;AZD9496;AZD9496, 98%, a potent and selective estrogen receptor (ERα) antagonist;CS-2107;AZD-9496;AZD 9496;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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Properties
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
form :A crystalline solid
pka :4.08±0.10(Predicted)
color :Light yellow to brown
Density :1.286±0.06 g/cm3(Predicted)
storage temp. :4°C, protect from light, stored under nitrogen
solubility :Soluble in DMSO
form :A crystalline solid
pka :4.08±0.10(Predicted)
color :Light yellow to brown
Safety Information
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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.Related product price
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