1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMelphalanCat. No.: HY-17575CAS No.: 148-82-3Synonyms: L-PAM分式: CHClNO分量: 305.2作靶點(diǎn): DNA Alkylator/Crosslinker作通路: Cell Cycle/DNA Damage儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性

2、數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 6 mg/mL (19.66 mM; Need ultrasonic)H2O : 4 mg/mL (13.11 mM; ultrasonic and adjust pH to 2 with HCl)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.2765 mL 16.3827 mL 32.7654 mL5 mM 0.6553 mL 3.2765 mL 6.5531 mL10 mM 0.3277 mL 1.6383 mL 3.2765 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液

3、的保存式和期限。BIOLOGICAL ACTIVITY物活性 Melphalan種有效的 DNA 烷化劑 (DNA alkylator)，具有抗腫瘤活性。IC50 & Target DNA Alkylator/Crosslinker 1體外研究 Melphalan is a DNA alkylating agent, used for multiple myeloma 1. Melphalan-DNA adducts can bevisualised in both cultured cells and solid tumour tissue 3.1/3 Master of Small Mol

4、ecules 您邊的抑制劑師www.MedChemE體內(nèi)研究 Melphalan (12 mg/kg, i.p.) increases pharmacological activity with heat in SD rats 2.PROTOCOLCell Assay 3 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 L culture medium to obtain a

5、pproximately 4000 cells per well after 2 days at37C, 5% CO2. Then, the cells are washed and exposed to 0, 10, 25, 50, 100, 250 or 500 M melphalan for1 h at 37C, 5% CO2. To control for cytotoxicity from hydrochloric acid, the solvent for melphalan, cells arealso exposed to hydrochloric acid at a conc

6、entration adjusted to the highest concentration of melphalan (500M). After treatment the cells are washed twice with culture medium and 100 L fresh culture medium isadded. The day after exposure to melphalan another 100 L fresh culture medium is added. After anadditional 2 days the culture medium is

7、 removed and 200 L fresh culture medium is added. At day 4 aftertreatment the culture medium is removed and cells are incubated for 4 h with 100 L fresh culture mediumand 10 L MTT-labelling agent. Subsequently, 100 L solubilisation solution (10% (v/v) in 0.01 M HCl) isadded. After incubation overnig

8、ht the absorbance at 590 nm is measured by a microtitre-plate reader 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 2Administration 2 Twenty rats are randomized into two groups according to the intraperitoneal temperature. The normothermi

9、c(NT) group receives intraperitoneal chemotherapy with intraperitoneal temperatures maintained between32.5 and 34.5C, and the hyperthermic (HT) group receives intraperitoneal chemotherapy with intraperitonealtemperatures maintained between 41.5 and 42.5C. Melphalan at a dose of 12 mg/kg is diluted i

10、n 150 mL0.9% NaCl solution immediately before administration. A closed perfusion system is utilized. The perfusate isheated in a tube coil in a thermostatically regulated water bath and infused into the peritoneal cavity with aroller pump at a rate of 80 mL/min for 90 min. Rhythmic massage of the ab

11、domen is used to facilitate uniformheat distribution within the peritoneal cavity. When the proper temperature for the experiment is reachedinside the peritoneal cavity, melphalan is added to the perfusate in the reservoir. For each animal, 0.5 mLperitoneal fluid and 0.5 mL blood are collected at 5,

12、 15, 30, 60, and 90 min after the initiation ofchemotherapy. 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.MCE has not independently confirmed the accuracy of these methods. T

13、hey are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Oncol (Dordr). 2016 Dec;39(6):511-522. J Mol Med (Berl). 2019 Jun 14.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. BLUMBERG BS, et al. AN ALKYLATING AGENT FOR MULTIPLE MYELOMA: MELPHALAN. JAMA. 1965 Feb 15;191:547-9.2/3 Master of Sm

14、all Molecules 您邊的抑制劑師www.MedChemE2. Glehen O, et al. Hyperthermia modifies pharmacokinetics and tissue distribution of intraperitoneal melphalan in a rat model. CancerChemother 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 livertumours in vivo. Biochem Pharmacol. 2004 May 1;