AZD9496 CAS 1639042-08-2

Product Description:

Product Name: AZD9496 CAS NO: 1639042-08-2

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;

Chemical & Physical Properties:

Appearance: Crystalline solid

Assay :≥99.0%

Density: 1.286±0.06 g/cm3 (Predicted)

Boiling Point: 541.0±50.0℃ (Predicted)

PKa: 4.08±0.10 (Predicted)

Flash Point: 281.0±30.1℃

Vapor Pressure: 0.0±1.5 mmHg at 25℃

Index of Refraction: 1.612

AZD9496 is an oral estrog-en receptor inhibitor that inhibits the growth of ER-positive and ESR1-carrying breast tumors in a clinical tumor model. AZD9496 exhibited equal binding ability to both ER-α and ER-β isoforms, both in the pmol range.

AZD9496 directly targets and downregulates ERα in vitro. AZD9496 antagonized and down-regulated ER mutants in in vitro and in vivo Chemicalbook tests. The IC50 of AZD9496 binding, down-regulating and antagonistic to ERα were 0.82, 0.14 and 0.28nM, respectively. AZD9496 has high oral bioavailability in a variety of animals (63%, 91% and 74% in rats, mice and dogs, respectively), and low blood volume and clearance (higher in mice).

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