Methotrexate CAS#59-05-2

  1. Potent and selective DHFR inhibition, well-established classic anti-folate agent.

  2. Dual therapeutic effect: anti-tumor and immunosuppressive activity.

  3. Mature synthesis route, stable quality, complying with USP/EP pharmacopoeia standards.

  4. Widely recognized clinical efficacy, long market application history.

  5. Can be formulated into tablets, injections for flexible dosage forms.

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Product Description

Methotrexate (MTX), CAS No. 59-05-2, is an important pharmaceutical active ingredient (API) commonly appearing as a yellow crystalline powder. It is a folate antagonist that inhibits dihydrofolate reductase (DHFR), interfering with folate metabolism and DNA synthesis. Due to its pharmacological properties, Methotrexate is widely used in pharmaceutical formulations for the treatment of certain cancers, autoimmune diseases, and inflammatory conditions. It is slightly soluble in dilute alkaline solutions and poorly soluble in water, requiring appropriate formulation and processing techniques. As a critical medicinal raw material, MTX is subject to strict quality control, GMP manufacturing standards, and pharmaceutical regulatory requirements to ensure its purity, consistency, and safety. It is classified as UN2811, Class 6.1 (Toxic Substance), Packing Group III. 

Methotrexat

Chemical Properties

Density1.536
Melting point195℃
Boiling point561.26°C (rough estimate)
Refractive index1.6910 (estimate)
Flash Point11℃
Precise Quality454.171
PSA210.54
logP1.8217
SolubilityH2O: insoluble
Appearanceyellow crystalline powder
StorageStore at -20°C. Hygroscopic. Light Sensitive.
Color/FormPale-yellow to Yellow-brown Solid
DecompositionWhen heated to decomposition it emits toxic fumes including /nitrogen oxides/.
pKapKa 3.04/4.99(H2O,t =25,I=0.0025) (Uncertain)
Water SolubilityInsoluble.
Spectral PropertiesSpecific optical rotation: 20.4 + or - 0.6 deg at 21 deg C/589 D (concentration by 0.1 N sodium hydroxide) maximum absorption: 243nm, A1= 388;307 nm, A1 = 475 (in 0.1 n hydrogen chloride). 258 nm, A1= 544; 303 nm, A1= 546; 372 nm, A1= 177 (in 0.1 N sodium hydroxide)UV max (0.1N HCl) 244, 307 nm; UV max (0.1N NaOH) 257, 302, 370 nm
StabilityStable, but light sensitive and hygroscopic. Incompatible with strong acids, strong oxidizing agents. Store at -15C or below.
StorageTemp−20°C

Product Application

Methotrexate (MTX) is used in the treatment of various malignancies, including leukemia, choriocarcinoma, and solid tumors. Depending on the disease type and clinical protocol, it may be administered orally, intramuscularly, intrathecally, or through intra-arterial infusion. Treatment regimens vary according to patient age, disease progression, and therapeutic response. In certain chemotherapy protocols, Methotrexate is combined with leucovorin (calcium folinate) rescue therapy to help protect normal cells and reduce drug-related toxicity. It is also an important component of high-dose chemotherapy regimens for osteosarcoma, requiring carefully controlled administration and supportive treatment.

In high-dose Methotrexate therapy, appropriate hydration, urine alkalinization, and leucovorin rescue are essential components of patient management. Close monitoring of liver and kidney function, blood counts, electrolyte balance, and plasma Methotrexate concentrations is necessary to evaluate drug clearance and minimize potential adverse effects. Methotrexate has also been used in the treatment of severe psoriasis, although its application is limited by potential toxicity and significant side effects. Across these therapeutic applications, dosage and administration schedules must be determined by qualified healthcare professionals in accordance with established clinical guidelines and individual patient requirements.

Methotrexate

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