Broad-Spectrum Antitumor Effect – It exhibits therapeutic activity against a variety of cancers, such as leukemia, lymphoma, lung cancer, breast cancer, cervical cancer and osteosarcoma.
Extensive Clinical Use – It is indicated for the management of malignant conditions including squamous cell carcinoma, choriocarcinoma and hydatidiform mole.
Fast In Vivo Clearance – Roughly 90% of the substance is eliminated via urine within 12 hours following oral intake, featuring rapid metabolic excretion.
Well-Characterized Pharmacological Property – Its active metabolite 7-hydroxymethotrexate has been identified, and toxicity data is available (rat intravenous LD50: 14 mg/kg), which validates its established pharmacokinetic features.
Methotrexate is a potent antitumor agent indicated for the treatment of acute lymphoblastic leukemia, lymphoma, malignant hydatidiform mole, choriocarcinoma, squamous cell carcinoma, lung cancer, cervical cancer, breast cancer and osteosarcoma.
Following oral administration, around 90% of the parent compound is excreted through urine within 12 hours, and 7-hydroxymethotrexate is its primary metabolite.
Its intravenous LD50 value in rat tests is 14 mg/kg.
Product Parameters of Methotrexate CAS#59-05-2
Density
1.536
Melting point
195℃
Boiling point
561.26°C (rough estimate)
Refractive index
1.6910 (estimate)
Flash Point
11℃
Precise Quality
454.171
PSA
210.54
logP
1.8217
Solubility
H2O: insoluble
Appearance
yellow crystalline powder
Storage
Store at -20°C. Hygroscopic. Light Sensitive.
Color/Form
Pale-yellow to Yellow-brown Solid
Decomposition
When heated to decomposition it emits toxic fumes including /nitrogen oxides/.
pKa
pKa 3.04/4.99(H2O,t =25,I=0.0025) (Uncertain)
Water Solubility
Insoluble.
Spectral Properties
Specific 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
Stability
Stable, but light sensitive and hygroscopic. Incompatible with strong acids, strong oxidizing agents. Store at -15C or below.
StorageTemp
−20°C
Product Application of Methotrexate CAS#59‑05‑2
Leukemia Treatment: Historically, daily‑dose regimens were adopted. Adult oral dosage falls within 2.5‑10 mg per day with a cumulative total dose of 50‑150 mg, whereas children take 1.25‑5 mg daily. Modern clinical protocols favor intermittent high‑dose therapy, either oral or intramuscular, dosed at 0.25‑0.75 mg/kg twice weekly; the typical adult single‑dose is 20‑25 mg. For intrathecal injection, adults receive 10‑15 mg per administration, and pediatric doses range from 6‑12 mg adjusted according to age. Therapy is commonly delivered once daily over three consecutive days, and cycles recur every 4‑8 weeks for maintenance or prophylactic purposes.
Choriocarcinoma: Adult patients generally receive 10‑30 mg via oral or intramuscular route once daily for five successive days. Treatment cycles can be repeated subject to individual patient therapeutic responses.
Solid Tumors: Continuous intra‑arterial infusion is the preferred approach, paired with intermittent intramuscular leucovorin (CF) rescue. The routine dosage for methotrexate is 25‑50 mg per day, alongside 6‑9 mg CF injected intramuscularly every 4‑6 hours.
Osteosarcoma: High‑dose treatment is implemented together with CF rescue intervention. The common dosage ranges from 3‑20 g/m², dissolved in 500‑1000 mL 5% glucose solution and administered through intravenous infusion over 4‑hour periods. CF rescue is initiated 2‑6 hours post‑infusion at 6‑12 mg intramuscularly or orally, repeated every six hours for three full days. Adequate fluid, electrolyte and alkalizing‑agent supplementation are required on day one and at 1‑2‑day intervals afterwards to accelerate drug clearance, sustaining daily urine output above 3000 mL and achieving urinary alkalinization. Daily monitoring of liver function, renal function, blood cell counts and plasma methotrexate concentration is mandatory.
Psoriasis: This indication sees limited clinical application due to pronounced adverse‑reaction risks. If prescribed, the oral dose is 1.25 mg per time, taken 2‑3 times each day for a 6‑9‑day treatment cycle.
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