Name: Pyroxamide (NSC 696085)
Brand: Selleck Chemicals
SKU: S2190
Availability: InStock
Rating: 5 (1 reviews)

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Quality Control

Batch: S219001 DMSO]17 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 98.99%

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COA
HPLC
SDS
Datasheet

98.99

Related Targets	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other HDAC Products	Entinostat (MS-275) Trichostatin A (TSA) RGFP966 Tubastatin A Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A HCl Fimepinostat (CUDC-907) Givinostat (ITF-2357) Hydrochloride Monohydrate Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

Solubility

In vitro
Batch:

DMSO : 17 mg/mL (64.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.	0.850mg/ml (3.20mM)	Taking the 1 mL working solution as an example, add 50 μL of 17 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.	0.850mg/ml (3.20mM)	Taking the 1 mL working solution as an example, add 50 μL of 17 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.

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

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%

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.

Chemical Information, Storage & Stability

Molecular Weight	265.31	Formula	C₁₃H₁₉N₃O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	382180-17-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	HDAC1 100 nM(ID50)
In vitro	Pyroxamide (NSC 696085) causes the accumulation of acetylated core histones in MEL cells cultured with the agent. At micromolar concentrations, it induces terminal differentiation and inhibits proliferation of murine erythroleukemia(MEL) cells. This compound (1.25-20 mM) causes dose-dependent inhibition of growth by cell cycle arrest of prostate carcinoma (LNCaP), neuroblastoma (KCN-69n), and bladder carcinoma (T24) cells in culture, with similar efficacy in all of the cell lines. A concentration of 1.25-20.0 μM Pyroxamide causes a dose-dependent decrease in viable cell number and an increase in percentage of dead cells over time in two Rhabdomyosarcoma cell lines, RD (embryonal ) and RH30B (alveolar). Accumulation of acetylated histones and induction of p21/WAF1 expression are obersevd in cells exposed to it. It shows a dose- and time-dependent proliferation inhibition, induction of apoptosis and histone H4 hyperacetylation in three B-cell precursor (BCP)-acute lymphoblastic leukemia (ALL) cell lines (Reh, Nalm6, Z33). The calculated IC50 after 96 hours of its incubation are 2-6 μM.
Kinase Assay	HDAC Inhibition Assays
Kinase Assay	A MEL cell line expressing the epitope Flag-tagged HDAC1 is generated. HDAC1-Flag is affinity purified by immune-precipitation using M2 anti-Flag antibody-coated agarose, followed by elution from the agarose using the Flag peptide. [³H]acetate-labeled cellular histones are prepared from MEL cells and are used as a substrate for the HDAC activity assay. Released [³H] acetic acid is quantified by scintillation counting. For inhibition studies, the enzyme preparations are preincubated with Pyroxamide (NSC 696085) (10 to 100,000 nM) for 30 minutes at 4 °
In vivo	Administration of 100 or 200 mg/kg of Pyroxamide (NSC 696085) daily for 21 days causes significant, dose-dependent suppression of the growth of the tumor xenograft. A dose of 300 mg/kg of this compound is lethal to all of the mice in the treatment group within 1 week. After in vivo administration, accumulation of acetylated histones and a dose-dependent increase in the expression of p21/WAF1 protein level are observed.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11309347/ [2] https://pubmed.ncbi.nlm.nih.gov/14654560/ [3] https://pubmed.ncbi.nlm.nih.gov/16810202/

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Pyroxamide (NSC 696085) HDAC inhibitor

Chemical Structure

Molecular Weight: 265.31