Methotrexate CAS#59-05-2
Broad Anti-Tumor Activity – It is effective against multiple cancers, including leukemia, lymphoma, lung cancer, breast cancer, cervical cancer, and osteosarcoma.
Wide Clinical Application Scope – It is used in the treatment of various malignant diseases such as squamous cell carcinoma, choriocarcinoma, and hydatidiform mole.
Rapid Elimination from the Body – Approximately 90% of the drug is excreted in urine within 12 hours after oral administration, indicating fast metabolic clearance.
Defined Pharmacological Profile – It has a known active metabolite (7-hydroxymethotrexate) and documented toxicity data (rat intravenous LD50: 14 mg/kg), supporting its studied pharmacokinetic characteristics.
Products Description of Methotrexate CAS#59-05-2
Methotrexate is an effective anti-tumor drug used in the treatment of acute lymphoblastic leukemia, lymphoma, malignant hydatidiform mole, choriocarcinoma, squamous cell carcinoma, lung cancer, cervical cancer, breast cancer, and osteosarcoma.
After oral administration, approximately 90% of the original drug is excreted in urine within 12 hours, with 7-hydroxymethotrexate as its main metabolite.
The LD50 of methotrexate via intravenous injection in rats 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: Traditionally, treatment was administered daily. Adults typically take 2.5–10 mg per day orally, with a total dose of 50–150 mg. Children receive 1.25–5 mg per day. Recent practice tends toward intermittent high-dose therapy, given orally or intramuscularly twice a week at 0.25–0.75 mg/kg per dose; adults are generally given 20–25 mg per dose. For intrathecal injection, the dosage is 10–15 mg per time for adults, while children receive 6–12 mg depending on age. Treatment is usually given once daily for 3 days, repeated every 4–8 weeks for maintenance or prevention.
Choriocarcinoma: Adults are typically given 10–30 mg orally or intramuscularly once daily for 5 consecutive days. The treatment course may be repeated depending on patient response.
Solid Tumors: Continuous intra-arterial infusion is preferred, combined with intermittent intramuscular administration of leucovorin (CF). The usual dosage is 25–50 mg/day of this product, along with 6–9 mg CF, administered intramuscularly every 4–6 hours.
Osteosarcoma: High-dose therapy is used in combination with CF rescue therapy. The dosage is generally 3–20 g/m², dissolved in 500–1000 mL of 5% glucose solution and infused intravenously over 4 hours. CF is started 2–6 hours after infusion at 6–12 mg intramuscularly (or orally), repeated every 6 hours for a total of 3 days. To ensure rapid drug elimination, electrolytes, fluids, and sodium bicarbonate should be supplemented on the first day and every 1–2 days thereafter, maintaining urine output above 3000 mL per day and ensuring alkalization. Liver function, kidney function, blood counts, and plasma methotrexate levels should be monitored daily.
Psoriasis: Due to significant side effects, it is rarely used. When applied, the dosage is 1.25 mg orally per dose, 2–3 times daily, with a treatment course of 6–9 days.
