ChemicalBook > CAS DataBase List > 1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-

1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-

Product Name
1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-
CAS No.
2092925-89-6
Chemical Name
1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-
Synonyms
OP-1250;Palazestrant;Palazestrant OP-1250;(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1-(4-((1-propylazetidin-3-yl)oxy)phenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole;1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-
CBNumber
CB48590116
Molecular Formula
C28H36FN3O
Formula Weight
449.6
MOL File
2092925-89-6.mol
More
Less

1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)- Property

Boiling point:
568.2±50.0 °C(Predicted)
Density 
1.134±0.06 g/cm3(Predicted)
solubility 
Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Slightly soluble: 0.1-1 mg/ml
form 
Solid
pka
17.73±0.60(Predicted)
color 
White to off-white
More
Less

Hazard and Precautionary Statements (GHS)

More
Less

1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)- Chemical Properties,Usage,Production

Description

Palazestrant is an antiestrogen and antineoplastic agent.

Uses

Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER+/HER2+ cancer[1][2][3].

in vivo

Palazestrant (0-100 mg/kg/day for 3 days. p.o.) alone or in combination with Palbociclib (HY-50767), Ribociclib (HY-15777) or Alpelisib (HY-15244) can effectively inhibit the proliferation and brain metastasis of ER-positive breast cancer[3].

IC 50

17b-estradiol (E2): 6.4 nM (IC50); ER

References

[1] Harmon CL, et al. Methods of treating estrogen receptor-associated diseases such as ER+/HER2+ cancer using an estrogen receptor antagonist: World Intellectual Property Organization, WO2023283329. 2023-01-12.
[2] WHO Drug Information-World Health Organization (WHO).
[3] Parisian AD, et al. Palazestrant (OP-1250), A Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination. Mol Cancer Ther. 2024 Mar 4;23(3):285-300. DOI:10.1158/1535-7163.MCT-23-0351

1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)- Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)- Suppliers

China 35 United States 1 Global 36
Taizhou Zhongzhi Biotechnology Co., Ltd
Tel
13012344321
Email
3995296515@qq.com
Country
China
ProdList
8439
Advantage
58
Bayee Biotech (Anqing) Co., Ltd.
Tel
0556-5032306 18917961636
Email
wtx@bayeebio.com
Country
China
ProdList
239
Advantage
61
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
15883
Advantage
64
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
ChengDu TongChuangYuan Pharmaceutical Co.Ltd
Tel
028-83379370 13880556291
Fax
028-87747383
Email
tcy@tcypharm.com
Country
China
ProdList
7218
Advantage
58
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9119
Advantage
58
Kaixin Chemical (Hong Kong) Limited
Tel
010-88886666-01 13112345678
Fax
CDXH21@126.com
Email
loyson@tcypharm.com
Country
China
ProdList
597
Advantage
55
Shanghai CR Corporation Limited
Tel
13062833949; 4006653949 4006653949
Fax
QQ: 2136646215
Email
fred.wen@crcorporation.cn
Country
China
ProdList
9758
Advantage
58
Jinan Kabotang Biological Technology Co.,Ltd.
Tel
0531-61320525 15866703830
Email
figo.gao@foxmail.com
Country
China
ProdList
5178
Advantage
58
Jinan Carbotang Biotech Co.,Ltd.
Tel
+8615866703830
Email
figo.gao@foxmail.com
Country
China
ProdList
8497
Advantage
58

2092925-89-6, 1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-Related Search:


  • 1H-Pyrido[3,4-b]indole, 2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-, (1R,3R)-
  • OP-1250
  • Palazestrant
  • (1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1-(4-((1-propylazetidin-3-yl)oxy)phenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
  • Palazestrant OP-1250
  • 2092925-89-6
  • C28H36FN3O