CAS 5072-26-4|D,L-Buthionine-(S,R)-sulfoximine

Introduction:Basic information about CAS 5072-26-4|D,L-Buthionine-(S,R)-sulfoximine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameD,L-Buthionine-(S,R)-sulfoximine
CAS Number5072-26-4Molecular Weight222.30500
Density1.29g/cm3Boiling Point382.3ºC at 760 mmHg
Molecular FormulaC8H18N2O3SMelting Point215ºC (dec.)(lit.)
MSDSChineseUSAFlash Point185ºC
Symbol
GHS07
Signal WordWarning

Names

NameS-butyl-DL-homocysteine (S,R)-sulfoximine
SynonymMore Synonyms

D,L-Buthionine-(S,R)-sulfoximine BiologicalActivity

DescriptionD,L-Buthionine-(S,R)-sulfoximine is a potent inhibitor of glutamylcysteine synthetase biosynthesis.
Related CatalogSignaling Pathways >>Others >>OthersResearch Areas >>Cancer
Target

glutamylcysteine synthetase[1]

In VitroButhionine sulfoximine is an analogs of methionine sulfoximine and inhibits gamma-glutamylcysteine synthetase about 20 times more effectively than prothionine sulfoximine and at least 100 times more effectively than methionine sulfoximine[1].
In VivoTreatment of mice bearing HT1080 and HT1080/DR4 xenografts with a continuous i.v infusion of nontoxic doses of D,L-Buthionine-(S,R)-sulfoximine (300 and 600 mg/kg/day) produce a 60% reduction of GSH plasma levels and greater than 95 % reduction in GSH tumor levels in both parental and multidrug-resistant tumors[2].
Animal AdminMice[2] D,L-Buthionine-(S,R)-sulfoximine is dissolved in sterile 0.9% saline, filtered through a 0.2-p.m polysulfone membrane filter, and administered by 48-h continuous iv. infusion at a dose of 300 mg/kg/day and 600 mg/kg/day starting at 24 h before doxorubicin administration. In vivo GSH levels after treatment with D,L-Buthionine-(S,R)-sulfoximine at a dose of 300 mg/kg and 600 mg/kg for 24 h as an iv. continuous infusion in munine plasma and in tumor tissue of HT1080 and HT1080/DR4 xenografts is measured[2].
References

[1]. Griffith OW, et al. Potent and specific inhibition of glutathione synthesis by buthionine sulfoximine (S-n-butyl homocysteine sulfoximine). J Biol Chem. 1979 Aug 25;254(16):7558-60.

[2]. Vanhoefer U, et al. d,l-buthionine-(S,R)-sulfoximine potentiates in vivo the therapeutic efficacy of doxorubicin against multidrug resistance protein-expressing tumors. Clin Cancer Res. 1996 Dec;2(12):1961-8.

Chemical & Physical Properties

Density1.29g/cm3
Boiling Point382.3ºC at 760 mmHg
Melting Point215ºC (dec.)(lit.)
Molecular FormulaC8H18N2O3S
Molecular Weight222.30500
Flash Point185ºC
Exact Mass222.10400
PSA112.62000
LogP2.30100
Index of Refraction1.537
InChIKeyKJQFBVYMGADDTQ-UHFFFAOYSA-N
SMILESCCCCS(=N)(=O)CCC(N)C(=O)O
Storage condition2-8°C
Water SolubilityH2O: 50 mg/mL, clear, colorless

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
EK7713435
CHEMICAL NAME :
Butanoic acid, 2-amino-4-(S-butylsulfonimidoyl)-
CAS REGISTRY NUMBER :
5072-26-4
LAST UPDATED :
199612
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C8-H18-N2-O3-S
MOLECULAR WEIGHT :
222.34

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
1 gm/kg
SEX/DURATION :
female 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - other effects
REFERENCE :
REPTED Reproductive Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1987- Volume(issue)/page/year: 6,133,1992

Safety Information

Symbol
GHS07
Signal WordWarning
Hazard StatementsH315-H319-H335
Precautionary StatementsP305 + P351 + P338
Personal Protective Equipmentdust mask type N95 (US);Eyeshields;Gloves
Hazard CodesXi
Risk Phrases36/37/38
Safety Phrases26-36
RIDADRNONH for all modes of transport
WGK Germany3
RTECSEK7713435

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Synonyms

2-amino-4-(butylsulfonimidoyl)butanoic acid
DL-Buthionine (S,R)-sulfoximine
EINECS 246-685-1
MFCD00070309
D,L-Buthionine-(S,R)-sulfoximine
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