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Procarbazine HCl DNA/RNA Synthesis inhibitor

Name: Procarbazine HCl
Brand: Selleck Chemicals
SKU: S1995
Availability: InStock
Rating: 5 (10 reviews)

Cat.No.S1995

Procarbazine HCl (NSC-77213) is a hydrochloride salt form of procarbazine which is a polyfunctional alkylating compound, used for the treatment of Hodgkin's lymphoma.

Chemical Structure

Molecular Weight: 257.76

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.45%

99.45

Related Targets	HDAC Topoisomerase PPAR PARP Sirtuin ATM/ATR Casein Kinase eIF MDM2/MDMX DNA-PK DHFR Nucleoside Analog/Antimetabolite DNA alkylator Telomerase Thymidylate Synthase CRISPR/Cas9 RAD51 BMI-1 LIM kinase RNR Alkylating Agent NUDIX High-mobility Group OGG1 MTH1 G-quadruplex SMN FENs WRN Pax
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Chemical Information, Storage & Stability

Molecular Weight	257.76	Formula	C₁₂H₁₉N₃O.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	366-70-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC-77213 HCl			Smiles	CC(C)NC(=O)C1=CC=C(C=C1)CNNC.Cl

Solubility

In vitro
Batch:

Water : 52 mg/mL

Ethanol : 52 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.55mg/ml (9.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 51 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.36mg/ml (1.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 7.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro	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. ^[1] Procarbazine has a strong clastogenic effect in hematopoietic cells and is mutagenic in a variety organs after high dose treatment. ^[2]
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. ^[3] 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. ^[4] 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. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/12948823/ [2] https://pubmed.ncbi.nlm.nih.gov/10521668/ [3] https://pubmed.ncbi.nlm.nih.gov/11868631/ [4] https://pubmed.ncbi.nlm.nih.gov/8583353/ [5] https://pubmed.ncbi.nlm.nih.gov/9395220/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00003564	Withdrawn	Brain and Central Nervous System Tumors	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)		Phase 3

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