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Home > products > L-Glutamicacid, N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-

L-Glutamicacid, N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]- cas no:59-05-2

Synonyms: Glutamicacid, N-[p-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-, L-(+)-(8CI);(+)-Amethopterin;Amethopterin;Amethopterine;Antifolan;CL 14377;EMT 25299;Emtexate;Emthexate PF;L-Amethopterin;L-Methotrexate;Ledertrexate;Metatrexan;Mexate;N-[p-[[2,4-Diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-(+)-glutamicacid;NSC 740;R 9985;Rheumatrex;Trexall;

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Identification
NameL-Glutamicacid, N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-
CAS59-05-2
SynonymsGlutamicacid, N-[p-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-, L-(+)-(8CI);(+)-Amethopterin;Amethopterin;Amethopterine;Antifolan;CL 14377;EMT 25299;Emtexate;Emthexate PF;L-Amethopterin;L-Methotrexate;Ledertrexate;Metatrexan;Mexate;N-[p-[[2,4-Diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-(+)-glutamicacid;NSC 740;R 9985;Rheumatrex;Trexall;
EINECS(EC#)200-413-8
Molecular FormulaC20H22N8O5
Molecular Weight454.44
Chemical Properties
Appearanceyellow crystalline powder
storage temp?20°C
Globally Harmonized System of Classification adn Labelling of Chemicals(GHS)
Hazardclass6.1(b)
Safety Data

Hazard T:Toxic
Risk R61;R25;R36/38
Safety

A human poison by intraspinal route. Poison experimentally by ingestion, intravenous, subcutaneous, and intraperitoneal routes. Human teratogenic effects by ingestion: developmental abnormalities of the craniofacial area and the musculoskeletal system. Human systemic effects by multiple routes: thrombocytopenia (decrease in the number of blood platelets), bone marrow changes, other blood changes, cerebral spinal fluid effects, eye effects, blood pressure lowering, cough, dyspnea, fibrosis (pneumoconiosis), cyanosis, gastrointestinal effects, fatty liver degeneration, hepatitis, impairment of liver function tests, other liver changes, fever, effects on inflammation or mediation of inflammation, leukopenia. Human mutation data reported. Experimental reproductive effects. A human eye irritant. Questionable human carcinogen producing leukemia, Hodgkin's disease, and skin tumors. An FDA proprietary drug. A chemotherapeutic agent. When heated to decomposition it emits toxic fumes including NOx.
Hazard Codes:?T
Risk Statements: 61-25-36/38-46?
R61: May cause harm to the unborn child.?
R25: Toxic if swallowed.?
R36/38: Irritating to eyes and skin.?
R46: May cause heritable genetic damage.
Safety Statements: 53-26-36/37-45-36/37/39
S53: Avoid exposure - obtain special instructions before use.?
S26: In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.?
S36/37: Wear suitable protective clothing and gloves.?
S45: In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.)?
S36/37/39: Wear suitable protective clothing, gloves and eye/face protection.
RIDADR: UN 2811 6.1/PG 3
WGK Germany: 3
RTECS: MA1225000
F: 3-8-10
HazardClass: 6.1(b)
PackingGroup: III


HS Code 29335995

Toxicity

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
child TDLo intravenous 100mg/kg/4H (100mg/kg) BLOOD: THROMBOCYTOPENIA

BLOOD: OTHER CHANGES		 Cancer Vol. 33, Pg. 1151, 1974.
child TDLo oral 2mg/kg/12D (2mg/kg) LUNGS, THORAX, OR RESPIRATION: COUGH

LUNGS, THORAX, OR RESPIRATION: DYSPNEA		 JAMA, Journal of the American Medical Association. Vol. 209, Pg. 1861, 1969.
human TDLo intramuscular 35mg/kg/28W (35mg/kg) VASCULAR: BP LOWERING NOT CHARACTERIZED IN AUTONOMIC SECTION

LUNGS, THORAX, OR RESPIRATION: DYSPNEA

LUNGS, THORAX, OR RESPIRATION: CYANOSIS		 British Medical Journal. Vol. 2, Pg. 156, 1970.
human TDLo intramuscular 200mg/kg/5Y (200mg/kg) LIVER: "HEPATITIS, FIBROUS (CIRRHOSIS, POST-NECROTIC SCARRING)" Archives of Dermatology. Vol. 100, Pg. 531, 1969.
human TDLo intravenous 4650ug/kg/4W- (4.65mg/kg) LIVER: FATTY LIVER DEGERATION

LIVER: LIVER FUNCTION TESTS IMPAIRED		 Proceedings of the American Association for Cancer Research. Vol. 5, Pg. 26, 1964.
human TDLo intravenous 7143ug/kg (7.143mg/kg) GASTROINTESTINAL: NAUSEA OR VOMITING

BLOOD: CHANGES IN PLATELET COUNT

BLOOD: CHANGES IN LEUCOCYTE (WBC) COUNT		 Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. Vol. 27, Pg. 673, 1992.
human TDLo oral 43mg/kg/5Y (43mg/kg) LIVER: LIVER FUNCTION TESTS IMPAIRED

LIVER: OTHER CHANGES		 Archives of Dermatology. Vol. 100, Pg. 523, 1969.
man TDLo intramuscular 214ug/kg/12D- (0.214mg/kg) SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE" Clinical and Experimental Rheumatology. Vol. 14, Pg. 450, 1996.
man TDLo intravenous 740mg/kg (740mg/kg) GASTROINTESTINAL: OTHER CHANGES Archives of Internal Medicine. Vol. 136, Pg. 1321, 1976.
man TDLo oral 643ug/kg/6W-I (0.643mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD Journal of Rheumatology. Vol. 14, Pg. 74, 1987.
man TDLo oral 4286ug/kg/2.7 (4.286mg/kg) LUNGS, THORAX, OR RESPIRATION: "FIBROSIS, FOCAL (PNEUMOCONIOSIS)"

LUNGS, THORAX, OR RESPIRATION: RESPIRATORY OBSTRUCTION

BLOOD: APLASTIC ANEMIA		 Clinical Rheumatology. Vol. 12, Pg. 535, 1993.
mouse LD50 intraperitoneal 50mg/kg (50mg/kg) ? Anatomical Record. Vol. 178, Pg. 465, 1974.
mouse LD50 intravenous 65mg/kg (65mg/kg) ? Drugs in Japan Vol. 6, Pg. 841, 1982.
mouse LD50 oral 146mg/kg (146mg/kg) ? Drugs in Japan Vol. 6, Pg. 841, 1982.
mouse LD50 subcutaneous 250mg/kg (250mg/kg) ? National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program. Vol. JAN1986,
mouse LD50 unreported 69mg/kg (69mg/kg) ? Cancer Research. Vol. 46, Pg. 2703, 1986.
Link to PubMed
rat LD50 intraperitoneal 6mg/kg (6mg/kg) ? Drugs in Japan Vol. 6, Pg. 841, 1982.
rat LD50 intravenous 14mg/kg (14mg/kg) ? Arzneimittel-Forschung. Drug Research. Vol. 20, Pg. 1467, 1970.
Link to PubMed
rat LD50 oral 135mg/kg (135mg/kg) ? Drugs in Japan Vol. 6, Pg. 841, 1982.
rat LD50 subcutaneous 58mg/kg (58mg/kg) ? Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 23, Pg. 93, 1992.
rat LD50 unreported 133ug/kg (0.133mg/kg) ? United States Patent Document. Vol. #4746662,
women LDLo intraspinal 36mg/kg/15D (36mg/kg) SPINAL CORD: OTHER DEGENERATIVE CHANGES

GASTROINTESTINAL: NAUSEA OR VOMITING		 New England Journal of Medicine. Vol. 289, Pg. 770, 1973.
women TDLo oral 800ug/kg/4D-I (0.8mg/kg) BLOOD: LEUKOPENIA

BLOOD: THROMBOCYTOPENIA

BLOOD: OXIDANT RELATED (GPD DEFICIENT) ANEMIA		 Medical Journal of Australia. Vol. 155, Pg. 493, 1991.
women TDLo oral 2mg/kg/17W-I (2mg/kg) LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

BLOOD: LEUKOPENIA		 Journal of Rheumatology. Vol. 14, Pg. 74, 1987.
women TDLo parenteral 2600ug/kg (2.6mg/kg) BRAIN AND COVERINGS: CHANGES IN CEREBRAL SPINAL FLUID

LUNGS, THORAX, OR RESPIRATION: "FIBROSIS, FOCAL (PNEUMOCONIOSIS)"

LUNGS, THORAX, OR RESPIRATION: DYSPNEA		 Cancer Vol. 38, Pg. 1529, 1976.
women TDLo unreported 11400ug/kg/44 (11.4mg/kg) LUNGS, THORAX, OR RESPIRATION: "FIBROSIS, FOCAL (PNEUMOCONIOSIS)" Clinical and Experimental Rheumatology. Vol. 15, Pg. 583, 1997.
women TDLo unreported 150mg/kg (150mg/kg) SENSE ORGANS AND SPECIAL SENSES: OTHER: EYE Cancer Vol. 48, Pg. 2158, 1981.

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