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AZD9496

CAS No.
1639042-08-2
Chemical Name:
AZD9496
Synonyms
AZD9496;CS-2107;AZD-9496;AZD 9496;AZD9496, 98%, a potent and selective estrogen receptor (ERα) antagonist;(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;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)-
CBNumber:
CB73041386
Molecular Formula:
C25H25F3N2O2
Molecular Weight:
442.47
MDL Number:
MFCD28902195
MOL File:
1639042-08-2.mol
Last updated:2023-09-20 16:43:00

AZD9496 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)
FDA UNII DA9P7LN909

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501
NFPA 704
0
2 0

AZD9496 price More Price(15)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 21805 AZD 9496 ≥98% 1639042-08-2 1mg $44 2024-03-01 Buy
Cayman Chemical 21805 AZD 9496 ≥98% 1639042-08-2 5mg $193 2024-03-01 Buy
Cayman Chemical 21805 AZD 9496 ≥98% 1639042-08-2 10mg $341 2024-03-01 Buy
Cayman Chemical 21805 AZD 9496 ≥98% 1639042-08-2 25mg $638 2024-03-01 Buy
AK Scientific 5289EA (E)-3-[3,5-Difluoro-4-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoicacid 1639042-08-2 50mg $640 2021-12-16 Buy
Product number Packaging Price Buy
21805 1mg $44 Buy
21805 5mg $193 Buy
21805 10mg $341 Buy
21805 25mg $638 Buy
5289EA 50mg $640 Buy

AZD9496 Chemical Properties,Uses,Production

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].

IC 50

0.82, 0.14 and 0.28 nm for erα binding, erα downregulation, erα antagonism, respectively

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

AZD9496 Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 86)Suppliers
Supplier Tel Email Country ProdList Advantage
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070 product@chemlin.com.cn CHINA 3012 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
Zhejiang ZETian Fine Chemicals Co. LTD
18957127338 stella@zetchem.com China 2141 58
BOC Sciences
+1-631-485-4226 inquiry@bocsci.com United States 19553 58
career henan chemical co
+86-0371-86658258 15093356674; factory@coreychem.com China 29826 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6313 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10523 58
CR Corporation Lomited
fred.wen@crcorporation.cn CHINA 12069 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6393 58
LEAP CHEM CO., LTD.
+86-852-30606658 market18@leapchem.com China 24738 58

View Lastest Price from AZD9496 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
AZD9496 pictures 2020-02-01 AZD9496
1639042-08-2
US $3.00 / KG 1KG 98% 100KG Career Henan Chemical Co
  • AZD9496 pictures
  • AZD9496
    1639042-08-2
  • US $3.00 / KG
  • 98%
  • Career Henan Chemical Co

AZD9496 Spectrum

1639042-08-2(AZD9496)Related Search:

(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)- 1639042-08-2 API