ChemicalBook > CAS DataBase List > AZD9496

AZD9496

Product Name
AZD9496
CAS No.
1639042-08-2
Chemical Name
AZD9496
Synonyms
CS-2107;AZD9496;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
Formula Weight
442.47
MOL File
1639042-08-2.mol
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AZD9496 Property

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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21805
Product name
AZD 9496
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
21805
Product name
AZD 9496
Purity
≥98%
Packaging
5mg
Price
$193
Updated
2024/03/01
Cayman Chemical
Product number
21805
Product name
AZD 9496
Purity
≥98%
Packaging
10mg
Price
$341
Updated
2024/03/01
Cayman Chemical
Product number
21805
Product name
AZD 9496
Purity
≥98%
Packaging
25mg
Price
$638
Updated
2024/03/01
AK Scientific
Product number
5289EA
Product name
(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
Packaging
50mg
Price
$640
Updated
2021/12/16
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AZD9496 Chemical Properties,Usage,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

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AZD9496 Suppliers

China 74 India 2 United States 10 Global 86
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19179
Advantage
64
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
Shanghai Xingui Biotechnology Co., Ltd.
Tel
17501653715
Email
xingui2022@126.com
Country
China
ProdList
10015
Advantage
58
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4566
Advantage
55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
1005
Advantage
55
Shanghai Synchem Pharma Co., ltd
Tel
21-619849051-1 18521059765
Email
synchempharma@aliyun.com
Country
China
ProdList
6463
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9806
Advantage
58
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View Lastest Price from AZD9496 manufacturers

Career Henan Chemical Co
Product
AZD9496 1639042-08-2
Price
US $3.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
100KG
Release date
2020-01-29

1639042-08-2, AZD9496Related Search:

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  • (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, 98%, a potent and selective estrogen receptor (ERα) antagonist
  • AZD9496
  • 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