PHOSPHORAMIDEMUSTARD
| 中文名称 | PHOSPHORAMIDEMUSTARD |
|---|---|
| 中文同义词 | PHOSPHAMIDE MUSTARD CYCLOHEXAMINE SALT;磷酰胺氮芥环己盐;N,N-双(2-氯乙基)磷二酰胺酸环己胺盐;N,N-BIS(2-CHLOROETHYL)PHOSPHORODIAMIDIC ACID COMPOUND WITH CYCLOHEXANAMINE (1:1) |
| 英文名称 | PHOSPHORAMIDEMUSTARD |
| 英文同义词 | Ai3-51834;Phosphorodiamidic acid, N,N-bis(2-chloroethyl)-, compd. with cyclohexanamine(1:1) (9ci);Phosphorodiamidic acid, N,N-bis(2-chloroethyl)-, compound with cyclohexanamine (1:1);N,N-Bis(2-chloroethyl)phosphorodiaMidic Acid CyclohexylaMine Salt;amino-[bis(2-chloroethyl)amino]phosphinic acid,cyclohexanamine;Phosphamide Mustard;Phosphamide Mustard Cyclohexamine Salt;Phosphoramide mustard cyclohexylammonium salt |
| CAS号 | 1566-15-0 |
| 分子式 | C10H24Cl2N3O2P |
| 分子量 | 320.196221 |
| EINECS号 | |
| 相关类别 | Amino Acids & Derivatives, Heterocycles, Metabolites & Impurities, Pharmaceuticals, Intermediates & Fine Chemicals |
| Mol文件 | 1566-15-0.mol |
| 结构式 |  |
PHOSPHORAMIDEMUSTARD 性质
| 熔点 | 100-103°C |
|---|---|
| 储存条件 | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| 溶解度 | 可溶于氯仿（少许）、甲醇（少许） |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
| 稳定性 | 湿气敏感 |
Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication.
Phosphoramide mustard cyclohexanamine (3-6 μM; 48 hours) reduces cell viability in rat spontaneously immortalized granulosa cells (SIGCs).
Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces DNA adduct formation and ovarian DNA damage.
Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) increases DNA damage responses (DDR) gene mRNA expression levels and DDR proteins.
Cell Viability Assay
| Cell Line: | SIGCs |
| Concentration: | 0.5 μM, 1 μM, 3 μM, 6 μM |
| Incubation Time: | 48 hours |
| Result: | Reduced cell viability at concentrations of 3 μM and higher. |
RT-PCR
| Cell Line: | SIGCs |
| Concentration: | 3 μM, 6 μM |
| Incubation Time: | 24 hours, 48 hours |
| Result: | Increased DDR gene mRNA expression levels. |
Western Blot Analysis
| Cell Line: | SIGCs |
| Concentration: | 3 μM, 6 μM |
| Incubation Time: | 24 hours, 48 hours |
| Result: | Generally increased DDR proteins. |
Phosphoramide mustard cyclohexanamine (2.1-20.7 mg/kg; i.p.; daily; for 5 days) inhibits subcutaneous tumor growth in rats.
Phosphoramide mustard cyclohexanamine exhibits terminal elimination half-lives (rat 15.1 min) following intravenous administration (rat 59.4 mg/kg).
| Animal Model: | Rat, subcutaneously implanted Walker 256 carcinosarcoma tumor |
| Dosage: | 2.1 mg/kg, 4.8 mg/kg, 10.4 mg/kg, 20.7 mg/kg |
| Administration: | Intraperitoneal injection, once daily, for 5 consecutive days |
| Result: | Required to produce 50% inhibition of subcutaneous tumor growth with dose of 12 mg/kg. |
| Animal Model: | Rats |
| Dosage: | 86.0 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Intravenous injection |
| Result: | T 1/2 (15.1 min). |