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Fadrozole

Fadrozole structure

Fadrozole 

structure
  • CAS No:

    102676-47-1

  • Formula:

    C14H13N3

  • Chemical Name:

    Fadrozole

  • Synonyms:

    Benzonitrile,4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)-;Imidazo[1,5-a]pyridine,benzonitrile deriv.;4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile;Fadrozole;131833-76-6

  • Categories:

    Active Pharmaceutical Ingredients  >  Antineoplastic Agents

Description

Fadrozole is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.


4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile is an imidazopyridine.|A selective aromatase inhibitor effective in the treatment of estrogen-dependent disease including breast cancer.

Fadrozole Basic Attributes

223.27

223.27

DTXSID5034141

2933990090

Characteristics

41.6

1.88

1.2

117-118 °C

0°C

0°C

1.662

Safety Information

3439

20/21/22

22-24/25

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P312, P321, P322, P330, P332+P313, P337+P313, P362, P363, P403+P233, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

Antineoplastic agents that are used to treat hormone-sensitive tumors. Hormone-sensitive tumors may be hormone-dependent, hormone-responsive, or both. A hormone-dependent tumor regresses on removal of the hormonal stimulus, by surgery or pharmacological block. Hormone-responsive tumors may regress when pharmacologic amounts of hormones are administered regardless of whether previous signs of hormone sensitivity were observed. The major hormone-responsive cancers include carcinomas of the breast, prostate, and endometrium; lymphomas; and certain leukemias. (From AMA Drug Evaluations Annual 1994, p2079) (See all compounds classified as Antineoplastic Agents, Hormonal.)|Compounds that inhibit AROMATASE in order to reduce production of estrogenic steroid hormones. (See all compounds classified as Aromatase Inhibitors.)|Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds. (See all compounds classified as Estrogen Antagonists.)

CGS 020286A

Fadrozole Use and Manufacturing

Methods of Manufacturing

From the corresponding carboxylic acid compound in dichloroethane, in the presence of concentrated sulfuric acid, through the introduction of ammonia gas for aminolysis.

Uses

Antineoplastic

Computed Properties

Molecular Weight:223.27
XLogP3:2.1
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:1
Exact Mass:223.110947427
Monoisotopic Mass:223.110947427
Topological Polar Surface Area:41.6
Heavy Atom Count:17
Complexity:311
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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