Melphalan is an effective DNA alkylating agent, with potent antitumor activity.

DNA Alkylator/Crosslinker^[1]

Melphalan is a DNA alkylating agent, used for multiple myeloma^[1]. Melphalan-DNA adducts can be visualised in both cultured cells and solid tumour tissue^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Melphalan (12 mg/kg, i.p.) increases pharmacological activity with heat in SD rats^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

305.20

C₁₃H₁₈Cl₂N₂O₂

148-82-3

马法兰；马尔法兰；米尔法兰；美法仑；左旋溶肉瘤素；左旋苯丙氨酸氮芥

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

In Vitro: 

DMSO : 5 mg/mL (16.38 mM; Need ultrasonic)

H₂O : 4 mg/mL (13.11 mM; ultrasonic and adjust pH to 2 with HCl)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

• [1]. BLUMBERG BS, et al. AN ALKYLATING AGENT FOR MULTIPLE MYELOMA: MELPHALAN. JAMA. 1965 Feb 15;191:547-9.

  [2]. Glehen O, et al. Hyperthermia modifies pharmacokinetics and tissue distribution of intraperitoneal melphalan in a rat model. Cancer Chemother Pharmacol. 2004 Jul;54(1):79-84.

  [3]. Rothbarth J, et al. Immunohistochemical detection of melphalan-DNA adducts in colon cancer cells in vitro and human colorectal liver tumours in vivo. Biochem Pharmacol. 2004 May 1;67(9):1771-8.

Melphalan cytotoxicity is determined by an MTT assay. The cells are seeded at 1000 cells per well in a 96-well microtitre plate in 100 μL culture medium to obtain approximately 4000 cells per well after 2 days at 37°C, 5% CO₂. Then, the cells are washed and exposed to 0, 10, 25, 50, 100, 250 or 500 μM melphalan for 1 h at 37°C, 5% CO₂. To control for cytotoxicity from hydrochloric acid, the solvent for melphalan, cells are also exposed to hydrochloric acid at a concentration adjusted to the highest concentration of melphalan (500 μM). After treatment the cells are washed twice with culture medium and 100 μL fresh culture medium is added. The day after exposure to melphalan another 100 μL fresh culture medium is added. After an additional 2 days the culture medium is removed and 200 μL fresh culture medium is added. At day 4 after treatment the culture medium is removed and cells are incubated for 4 h with 100 μL fresh culture medium and 10 μL MTT-labelling agent. Subsequently, 100 μL solubilisation solution (10% (v/v) in 0.01 M HCl) is added. After incubation overnight the absorbance at 590 nm is measured by a microtitre-plate reader^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Rats^[2]
Twenty rats are randomized into two groups according to the intraperitoneal temperature. The normothermic (NT) group receives intraperitoneal chemotherapy with intraperitoneal temperatures maintained between 32.5 and 34.5°C, and the hyperthermic (HT) group receives intraperitoneal chemotherapy with intraperitoneal temperatures maintained between 41.5 and 42.5°C. Melphalan at a dose of 12 mg/kg is diluted in 150 mL 0.9% NaCl solution immediately before administration. A closed perfusion system is utilized. The perfusate is heated in a tube coil in a thermostatically regulated water bath and infused into the peritoneal cavity with a roller pump at a rate of 80 mL/min for 90 min. Rhythmic massage of the abdomen is used to facilitate uniform heat distribution within the peritoneal cavity. When the proper temperature for the experiment is reached inside the peritoneal cavity, melphalan is added to the perfusate in the reservoir. For each animal, 0.5 mL peritoneal fluid and 0.5 mL blood are collected at 5, 15, 30, 60, and 90 min after the initiation of chemotherapy. The venous catheter is flushed with 0.2 mL of heparinized saline after each blood sampling. At the end of the procedure the rats are killed and tissues samples are taken^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. BLUMBERG BS, et al. AN ALKYLATING AGENT FOR MULTIPLE MYELOMA: MELPHALAN. JAMA. 1965 Feb 15;191:547-9.

  [2]. Glehen O, et al. Hyperthermia modifies pharmacokinetics and tissue distribution of intraperitoneal melphalan in a rat model. Cancer Chemother Pharmacol. 2004 Jul;54(1):79-84.

  [3]. Rothbarth J, et al. Immunohistochemical detection of melphalan-DNA adducts in colon cancer cells in vitro and human colorectal liver tumours in vivo. Biochem Pharmacol. 2004 May 1;67(9):1771-8.