Pyroxamide (NSC 696085)

製品コードS2190 バッチS219001

印刷

化学情報

Synonyms

NSC-696085

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₃H₁₉N₃O₃

分子量

265.31

CAS No.

382180-17-8

Solubility (25°C)*

体外

DMSO

17 mg/mL (64.07 mM)

Ethanol

2 mg/mL (7.53 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.85mg/ml	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	0.85mg/ml	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Pyroxamide(NSC 696085) is a potent inhibitor of affinity-purified HDAC1 with ID50 of 100 nM. It also induces growth suppression and cell death in human rhabdomyosarcoma in vitro.
in vitro	Pyroxamide causes the accumulation of acetylated core histones in MEL cells cultured with the agent. Pyroxamide, at micromolar concentrations, induces terminal differentiation and inhibits proliferation of murine erythroleukemia(MEL) cells. Pyroxamide (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. ^[1] 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 Pyroxamide. ^[2] Pyroxamide 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 Pyroxamide incubation are 2-6 μM. ^[3]
in vivo	Administration of 100 or 200 mg/kg of Pyroxamide daily for 21 days causes significant, dose-dependent suppression of the growth of the tumor xenograft. A dose of 300 mg/kg Pyroxamide is lethal to all of the mice in the treatment group within 1 week. After in vivo administration of Pyroxamide, accumulation of acetylated histones and a dose-dependent increase in the expression of p21/WAF1 protein level are observed. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	HDAC Inhibition Assays
キナーゼアッセイ	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 (10 to 100,000 nM) for 30 minutes at 4 °
細胞アッセイ	細胞株	MEL Ds19/Sc9 cells
	濃度	0.625-8 μM
	反応時間	5 days
	実験の流れ	1-2 × 10⁵ cells/mL MEL Ds19/Sc9 cells are cultured with increasing concentrations of Pyroxamide (0.625-8 μM) for 5 days, at which time the Benzidine positivity is determined as an indicator of terminal differentiation. MEL cell density is measured using a Coulter counter and viability is assessed by trypan blue exclusion.
動物実験	動物モデル	Human CWR22 prostate cancer xenograft is s.c. injected in nude mice.
	投薬量	100, 200, or 300 mg/kg
	投与方法	Administered daily via i.p. injection.

参考

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。