Name | amino-[bis(2-chloroethyl)amino]phosphinic acid,cyclohexanamine |
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Synonyms |
n,n-bis(2-chloroethyl)phosphorodiamidic acid-cyclohexanamine(1:1)
Phosphorodiamidic acid,N,N-bis(2-chloroethyl)-,cyclohexylamine salt phosphoramide mustard cyclohexylammonium salt Cyclohexylammonium Hydrogen N,N-di-(2-chloroethyl)phosphorodiamidate Phosphoramide mustard cyclohexamine salt phosphoramide mustard cyclohexylamine salt Phosphorodiamidic acid,N,N-bis(2-chloroethyl)-,compd. with cyclohexanamine (1:1) OMF 59 cyclohexylamine,salt of/the/ N,N-bis-(2-chloro-ethyl)-diamidophosphoric acid Cyclohexylamin,Salz der N,N-Bis-(2-chlor-aethyl)-diamidophosphorsaeure N,N-bis(2-chloroethyl)phosphorodiamidic acid cyclohexylammonium salt |
Description | Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response[1][2]. |
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Related Catalog | |
In Vitro | Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication[1]. Phosphoramide mustard cyclohexanamine destroys rapidly dividing cells by forming NOR-G-OH, NOR-G and G-NOR-G adducts with DNA, potentially leading to DNA damage[1]. Phosphoramide mustard cyclohexanamine (3-6 μM; 48 hours) reduces cell viability in rat spontaneously immortalized granulosa cells (SIGCs)[1]. Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces DNA adduct formation[1]. Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces ovarian DNA damage in rat ovaries[1]. Phosphoramide mustard cyclohexanamine increases DNA damage responses (DDR) gene (Atm, Parp1, Prkdc, Xrcc6, Brca1, Rad51) mRNA expression level[1]. Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) increased DDR proteins[1]. Cell Viability Assay[1] 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[1] Cell Line: SIGCs Concentration: 3 μM, 6 μM Incubation Time: 24 hours, 48 hours Result: Increased DDR gene mRNA expression levels. Western Blot Analysis[1] Cell Line: SIGCs Concentration: 3 μM, 6 μM Incubation Time: 24 hours, 48 hours Result: Generally increased DDR proteins. |
In Vivo | Phosphoramide mustard cyclohexanamine (2.1-20.7 mg/kg; i.p.; daily; for 5 days) inhibits subcutaneous tumor growth in rats[2]. Phosphoramide mustard cyclohexanamine (86.0 mg/kg; i.v.) has a plasma disappearance half-life of 15.1 minutes[2]. Animal Model: Rat, subcutaneously implanted Walker 256 carcinosarcoma tumor[2] 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[2] Dosage: 86.0 mg/kg (Pharmacokinetic Analysis) Administration: Intravenous injection Result: Had a disappearance half-life of 15.1 minutes in plasma. |
References |
Boiling Point | 363.5ºC at 760mmHg |
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Melting Point | 100-103 °C |
Molecular Formula | C10H24Cl2N3O2P |
Molecular Weight | 320.19600 |
Flash Point | 173.6ºC |
Exact Mass | 319.09800 |
PSA | 102.39000 |
LogP | 3.50350 |
Vapour Pressure | 2.84E-06mmHg at 25°C |