CAS 52128-35-5|Trimetrexate

Introduction：Basic information about CAS 52128-35-5|Trimetrexate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Trimetrexate BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

Common Name	Trimetrexate
CAS Number	52128-35-5	Molecular Weight	369.41800
Density	1.305g/cm3	Boiling Point	647ºC at 760mmHg
Molecular Formula	C₁₉H₂₃N₅O₃	Melting Point	/
MSDS	/	Flash Point	345.1ºC

Names

Name	5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline-2,4-diamine
Synonym	More Synonyms

Trimetrexate BiologicalActivity

Description	Trimetrexate(CI-898) is a potent competitive inhibitor of bacterial, protozoan, and mammalian dihydrofolate reductase.IC50 value:Target: Antibiotic Trimetrexate therapy had minimal toxicity; transient neutropenia or thrombocytopenia occurred in 12 patients and mild elevation of serum aminotransferases in 4. We conclude that the combination of trimetrexate and leucovorin is safe and effective for the initial treatment of pneumocystis pneumonia in patients with AIDS and for the treatment of patients with intolerance or lack of response to standard therapies [1]. In noncomparative trials trimetrexate was effective in the treatment of P. carinii pneumonia (PCP) in patients with AIDS who were intolerant of or refractory to cotrimoxazole (trimethoprim/sulfamethoxazole) and pentamidine treatment. In these patients, 2- to 4-week survival rates of 48 to 69% were reported. In a comparative trial in the initial therapy of PCP, trimetrexate was less effective than cotrimoxazole in moderate to severe disease as evidenced by a significantly higher failure rate [2]. trimetrexate plus leucovorin was effective, albeit inferior to TMP-SMZ, for moderately severe P. carinii pneumonia but was better tolerated than TMP-SMZ [3].
Related Catalog	Signaling Pathways >>Anti-infection >>BacterialResearch Areas >>Infection
References	[1]. Allegra CJ, et al. Trimetrexate for the treatment of Pneumocystis carinii pneumonia in patients with the acquired immunodeficiency syndrome. N Engl J Med. 1987 Oct 15;317(16):978-85. [2]. Fulton B, et al. Trimetrexate. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the treatment of Pneumocystis carinii pneumonia. Drugs. 1995 Apr;49(4):563-76. [3]. Sattler FR, et al. Trimetrexate with leucovorin versus trimethoprim-sulfamethoxazole for moderate to severe episodes of Pneumocystis carinii pneumonia in patients with AIDS: a prospective, controlled multicenter investigation of the AIDS Clinical Trials Group Protocol 029/031. J Infect Dis. 1994 Jul;170(1):165-72.

Description

Trimetrexate(CI-898) is a potent competitive inhibitor of bacterial, protozoan, and mammalian dihydrofolate reductase.IC50 value:Target: Antibiotic Trimetrexate therapy had minimal toxicity; transient neutropenia or thrombocytopenia occurred in 12 patients and mild elevation of serum aminotransferases in 4. We conclude that the combination of trimetrexate and leucovorin is safe and effective for the initial treatment of pneumocystis pneumonia in patients with AIDS and for the treatment of patients with intolerance or lack of response to standard therapies [1]. In noncomparative trials trimetrexate was effective in the treatment of P. carinii pneumonia (PCP) in patients with AIDS who were intolerant of or refractory to cotrimoxazole (trimethoprim/sulfamethoxazole) and pentamidine treatment. In these patients, 2- to 4-week survival rates of 48 to 69% were reported. In a comparative trial in the initial therapy of PCP, trimetrexate was less effective than cotrimoxazole in moderate to severe disease as evidenced by a significantly higher failure rate [2]. trimetrexate plus leucovorin was effective, albeit inferior to TMP-SMZ, for moderately severe P. carinii pneumonia but was better tolerated than TMP-SMZ [3].

Related Catalog

Signaling Pathways >>Anti-infection >>BacterialResearch Areas >>Infection

References

[1]. Allegra CJ, et al. Trimetrexate for the treatment of Pneumocystis carinii pneumonia in patients with the acquired immunodeficiency syndrome. N Engl J Med. 1987 Oct 15;317(16):978-85.

[2]. Fulton B, et al. Trimetrexate. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the treatment of Pneumocystis carinii pneumonia. Drugs. 1995 Apr;49(4):563-76.

[3]. Sattler FR, et al. Trimetrexate with leucovorin versus trimethoprim-sulfamethoxazole for moderate to severe episodes of Pneumocystis carinii pneumonia in patients with AIDS: a prospective, controlled multicenter investigation of the AIDS Clinical Trials Group Protocol 029/031. J Infect Dis. 1994 Jul;170(1):165-72.

Chemical & Physical Properties

Density	1.305g/cm3
Boiling Point	647ºC at 760mmHg
Molecular Formula	C₁₉H₂₃N₅O₃
Molecular Weight	369.41800
Flash Point	345.1ºC
Exact Mass	369.18000
PSA	117.54000
LogP	3.97590
InChIKey	NOYPYLRCIDNJJB-UHFFFAOYSA-N
SMILES	COc1cc(NCc2ccc3nc(N)nc(N)c3c2C)cc(OC)c1OC
Storage condition	2-8℃

Safety Information

HS Code	2933990090

Customs

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Synonyms

Trimetrexato

Trimetrexate

CI-898

Trimetrexatum

Jb-11

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