product name Procarbazine HCl
Description: Procarbazine HCl (also known as NSC-77213 HCl) is a hydrochloride salt form of procarbazine which is a polyfunctional alkylating compound. Procarbazine is an antineoplastic chemotherapy drug for the treatment of Hodgkins lymphoma and certain brain cancers; Procarbazine also inhibits MAO thus increasing the effects of sympathomimetics, TCAs, and tyramine. Procarbazine causes DNA damage through non-enzymatic formation of the Cu(I)-hydroperoxo complex and methyl radicals. Procarbazine has a strong clastogenic effect in hematopoietic cells and is mutagenic in a variety organs after high dose treatment.
References: Mutat Res. 2003 Aug 5;539(1-2):145-55; Arch Androl. 2002 Mar-Apr;48(2):91-100.
257.76
Formula
C12H19N3O.HCl
CAS No.
366-70-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: 52 mg/mL (201.7 mM)
Ethanol: 52 mg/mL (201.7 mM)
Solubility (In vivo)
Synonyms
NSC-77213 HCl
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19412176
| In Vitro |
In vitro activity: Procarbazine plus Cu(II) induce piperidine-labile and formamidopyrimidine-DNA glycosylase-sensitive lesions at the 5-ACG-3 sequence, complementary to a hotspot of the p53 gene, and the 5-TG-3 sequence. Procarbazine causes DNA damage through non-enzymatic formation of the Cu(I)-hydroperoxo complex and methyl radicals. Procarbazine has a strong clastogenic effect in hematopoietic cells and is mutagenic in a variety organs after high dose treatment. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Procarbazine causes significant decrease in testicular and epididymal weight and a drastic reduction in haploid cells and spermatogenic arrest, demonstrating variation among the test golden hamster. Procarbazine produces a dose-dependent potentiation of MAO A in brown adipose tissue, the elevation being more pronounced following monomethylhydrazine, with activity rising to 350% of that in control homogenates in rats. Procarbazine or monomethylhydrazine reduces metabolism of this amine by a similar degree as had been determined ex-vivo in blood vessel homogenates. Procarbazine is mutagenic, clastogenic and teratogenic in a wide range of test systems of varying complexity and a wide-spectrum carcinogen in rodents and monkeys, causing tumours of the haemopoietic system, the mammary gland, the lung and the nervous system. Procarbazine in vivo undergoes a complex series of metabolic changes that result in the generation of a number of chemically reactive species, including methylating agents and free radicals. |
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| Formulation & Dosage | |
| References | Mutat Res. 2003 Aug 5;539(1-2):145-55; Arch Androl. 2002 Mar-Apr;48(2):91-100. |
