2-Hydroxyflutamide

Names

[ Name ]:
2-Hydroxyflutamide

[Synonym ]:
2-hydroxy Flutamide
2-Hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
Propanamide, 2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-
2-Hydroxy-2-methyl-N-(4-nitro-3-(trifluoromethyl)phenyl)propanamide
Hydroxyflutamide
2-Hydroxy-flutamide

Biological Activity

[Description]:

Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC50=700 nM). Hydroxyflutamide can be used for the research of prostate cancer[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Others >> Androgen Receptor

[Target]

IC50: 700 nM (androgen receptor)[1]

[References]

[1]. Furr BJ, et, al. Casodex: preclinical studies and controversies. Ann N Y Acad Sci. 1995 Jun 12;761:79-96.

[2]. Liu HL, et, al. A Molecular Modeling Study of the Hydroxyflutamide Resistance Mechanism Induced by Androgen Receptor Mutations. Int J Mol Sci. 2017 Aug 23;18(9):1823.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
443.8±45.0 °C at 760 mmHg

[ Melting Point ]:
125-130â„ƒ

[ Molecular Formula ]:
C₁₁H₁₁F₃N₂O₄

[ Molecular Weight ]:
292.211

[ Flash Point ]:
222.2±28.7 °C

[ Exact Mass ]:
292.067078

[ PSA ]:
95.15000

[ LogP ]:
3.16

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.546

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TX1466250

CHEMICAL NAME :: Propanamide, 2-hydroxy-2-methyl-N-(4-nitro-3-(trifluoromethyl)phen yl)-

CAS REGISTRY NUMBER :: 52806-53-8

LAST UPDATED :: 199706

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C11-H11-F3-O2-N4

MOLECULAR WEIGHT :: 288.26

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg/6D-I

TOXIC EFFECTS :: Endocrine - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - dehydrogenases

REFERENCE :: JJATDK JAT, Journal of Applied Toxicology. (John Wiley & Sons Ltd., Baffins Lane, Chichester, W. Sussex PO19 1UD, UK) V.1- 1981- Volume(issue)/page/year: 1,297,1981 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6 gm/kg

SEX/DURATION :: female 11-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - other effects on male

REFERENCE :: CJPPA3 Canadian Journal of Physiology and Pharmacology. (National Research Council of Canada, Publication Sales and Distribution, Ottawa ON K1A OR6, Canada) V.42- 1964- Volume(issue)/page/year: 73,1582,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2400 mg/kg

SEX/DURATION :: female 15-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands Reproductive - Paternal Effects - other effects on male

REFERENCE :: CJPPA3 Canadian Journal of Physiology and Pharmacology. (National Research Council of Canada, Publication Sales and Distribution, Ottawa ON K1A OR6, Canada) V.42- 1964- Volume(issue)/page/year: 73,1582,1995

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
TX1466250

[ HS Code ]:
2924299090

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2924299090

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

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