Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222)

製品コードS2447 バッチS244702

印刷

化学情報

Synonyms

Antibiotic C 15003P3

Storage
(From the date of receipt)

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

化学式

C₃₂H₄₃ClN₂O₉

分子量

635.14

CAS No.

66584-72-3

Solubility (25°C)*

体外

DMSO

100 mg/mL (157.44 mM)

Ethanol

16 mg/mL (25.19 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	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 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	1.25mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 25 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	Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222, Antibiotic C 15003P3) is a potent inhibitor of tubulin polymerization with IC50 of 3.4 μM.
in vitro	Ansamitocin p-3 at 5 μM completely inhibits the polymerization of tubulin isolated from bovine brains, but in contrast to VCR, Ansamitocin p-3 at a high concentration of 80 μM does not leads to the aggregation of tubulin. Ansamitocin p-3 at 16 μM also potently depolymerizes the polymerized tubulin (IC50 = 3.8 μM). The addition of Ansamitocin p-3 to culture cells blocks the morphological alteration of AC cells from fibroepithelioid to a glial cell type caused by the exposure to a certain concentration of dibutyryl cyclic adenosine 3':5'-monophosphate. In addition, Ansamitocin p-3 treatment at 16 nM causes the well-defined network of cytoplasmic microtubules of A31 cells rapidly dispersed. Short-term Ansamitocin p-3 treatment also inhibits the synthesis of DNA in A31 cells or KB cells. These results confirm that Ansamitocin p-3 acts by interfering with the microtubule assembly system, thus resulting in an inhibition of mitotic spindle fiber formation and, ultimately, cytokilling. ^[1] Ansamitocin p-3 displays potent cytotoxicity against A-549, HT-29, and MCF-7 cells in a dose-dependent manner with ED50 of 4 ×10^-7, 4 × 10^-7, and 2 × 10^-6 μg/mL, respectively. ^[2] Ansamitocin p-3 also exhibits cytotoxicity against HCT-116 cells with a much low EC50 of 0.081 nM. ^[3] Ansamitocin p-3 enhances the effect of radiation both in Drosophila cells and human cancer cells in a p53 dependent manner. ^[4]
in vivo	Ansamitocin p-3 treatment (>1 μg) significantly suppresses the growth of leukemia SN36, and induces an increased arrest in metaphase of P388 leukemia cells. Ansamitocin p-3 treatment at 25 μg/kg/day significantly prolongs the survival time of mice bearing i.p. B16 melanoma by 130%. Ansamitocin p-3 treatment also significantly prolongs the survival time of mice bearing Ehrlich ascites carcinoma, Sarcoma 180, and P815 mastocytoma, while slightly prolongs the survival time of mice bearing ascites MOPC-104E myeloma,leukemia L1210, and leukemia C1498. ^[1]
特徴	Ansamitocin p-3 does not inhibit the growth of bacteria, but very markedly inhibits the growth of eukaryotic organisms.

プロトコル(参考用のみ)

キナーゼアッセイ	Polymerization inhibition assay
キナーゼアッセイ	After the addition of 100 μL of various concentrations of Ansamitocin p-3 solution (GTP minus MES buffer) or 1 M Tris buffer, pH 8.4 (for blank), to 400 μL of bovine tubulin solution (1 mg/mL in cold MES buffer), maintained at 0 °C for 10 to 15 minutes, the mixture is warmed in a water bath at 37 °C for 30 to 60 minutes. The polymerization of tubulin is followed by an increase in turbidity of the mixture during warming. The turbidity measurement is performed at 460 nm with a Hitachi type 101 spectrophotometer.
細胞アッセイ	細胞株	A31 and KB
	濃度	Dissolved in DMSO, final concentrations ~10 μM
	反応時間	~24 hours
	実験の流れ	Cells are synchronized, and then exposed to various concentrations of Ansamitocin p-3 for ~24 hours. Cells are labeled with [³H]thymidine (5 Ci/mM, 1 μCi/mL) in 1 mL of the medium. After pulse-labeling at 37 °C for 1 hour, the cells on coverslips are fixed with methanol:acetic acid (3:1). The acidsoluble fraction is washed out from the cells, and the radio activity of each coverslip is determined by a liquid scintillation counter.
動物実験	動物モデル	Female DBA/2 mice bearing P388, L1210, or P815 cells, C57BL/6 mice bearing B16, or C1498 cells, ICR mice bearing sarcoma 180 and EAC, and BALB/c mice bearing MOPC-104E cells
	投薬量	~200 μg/kg
	投与方法	Administered i.p. or i.v. daily

参考

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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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