Actinomycin D (Dactinomycin)

製品コードS8964 バッチS896402

印刷

化学情報

Synonyms

Act D, RASP-101

Storage
(From the date of receipt)

3 years -20°C(in the dark) powder

化学式

C₆₂H₈₆N₁₂O₁₆

分子量

1255.42

CAS No.

50-76-0

Solubility (25°C)*

体外

DMSO

100 mg/mL (79.65 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.750mg/ml (2.99mM)	Taking the 1 mL working solution as an example, add 50 μL 75 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. 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	Actinomycin D (Dactinomycin, Act D, RASP-101)は、ストレプトマイセス属の土壌細菌から単離された重要なポリペプチド系抗生物質です。Actinomycin D (Dactinomycin)は、DNA修復を阻害し、G1期で細胞周期を停止させ、それぞれのIC50値は0.42 μMおよび0.4 nMです。Actinomycin Dは、細菌のタンパク質合成を抑制できるRNAおよびタンパク質合成阻害剤です。Actinomycin Dはオートファジー活性化剤であり、p53非依存性細胞死を誘導し、高リスクの慢性リンパ性白血病における生存期間を延長します。本製品は有害化学物質（急性毒性／可燃性／皮膚腐食性）です。保護マスク、手袋、保護衣を着用してご使用ください。
in vitro	Actinomycin D (Dactinomycin) markedly reduces the SMC proliferation via the inhibition of BrdU incorporation at 80 nM. This is further supported by the G1-phase arrest using a flowcytometric analysis. The protein expression levels of proliferating cell nuclear antigen (PCNA), focal adhesion kinase (FAK), and Raf are all suppressed by this compound. Extracellular signalregulated kinases (Erk) involved in cell-cycle arrest are found to be increased by it.
in vivo	Actinomycin D (Dactinomycin) targets survival proteins TOSO, BCL2 and MCL1 and is active in two different mouse models that are characterized by either unmutated B-cell receptor or inactive p53 function, both of which are known negative prognostic factors in CLL.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	A10 cells (Vascular SMC)
	濃度	80 nM, 800 nM, 8 μM
	反応時間	18-24 h
	実験の流れ	Cultured SMC are starved for 24 h followed by incubation with various doses of actinomycin D (dactinomycin) at 37℃. Drug treatment is carried out for 18-24 h. Since it is dissolved in 0.1% DMSO, a vehicle control containing DMSO is also included.
動物実験	動物モデル	C57BL/6 wild-type mice engrafted with tumor cells from Em-TCL-1 transgenic mice
	投薬量	0.06 mg/kg
	投与方法	IP

参考

https://pubmed.ncbi.nlm.nih.gov/15959627/
https://pubmed.ncbi.nlm.nih.gov/9450493/
https://pubmed.ncbi.nlm.nih.gov/22743622/

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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。

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