Griseofulvin

製品コードS4071 バッチS407101

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C17H17ClO6

分子量 352.77 CAS No. 126-07-8
Solubility (25°C)* 体外 DMSO 50 mg/mL (141.73 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.
* <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 Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.
in vitro Griseofulvin is active against dermatophytes of different species in the genera Microsporum, Trichophyton and Epidermophyton. Other fungi such as Scopulariopsis brevicaulis and Hendersomula toruloidea are insensitive. This compound has little or no effect against yeasts and bacteria. The minimum inhibitory concentration of this chemical tested in vitro against various dermatophytes ranges between 0.14 and 0.6 μg/mL. Main effect of this compound on cell mitosis is disorganization of the spindle microtubules. It is also able to induce structural chromosomal aberrations in mammalian cells. [1] This compound inhibits the viability of human colon adenocarcinoma cells COLO 205 and HT 29, hepatoma cells Hep G2 and Hep 3B, leukemia cells HL 60, and normal keratinocytes (#76 KhGH) with IC50s of ~1 and ~5 μM, 5 and 5 μM, 1 μM, and 50 μM, respectively after a 30 hr incubation,. It (20 μM) induces a marked presence of abnormal mitotic spindle formation with mono-, bi-, and tripolar spindles of varying lengths in HT 29 cells, and causes G2/M cell cycle arrest at 24h through elevation of cyclin B1/cdc2 kinase activity and down-regulation of myt-1 protein expression. This chemical is able to induce apoptosis of HT 29 cells via caspase3 activation, Bcl-2 hyperphosphorylation and inhibition of the normal function of Bcl-2 associated with Bax. [2]
in vivo Griseofulvin displays potent anti-infection activity in vivo. The minimum effective dose of this compound given daily per os is 250 mg/kg (6 days) in mice with a cutaneous infection of Trichophyton quinckeanum and 25 mg/kg (12 days) in guinea pigs with a cutaneous infection of Trichophyton mentagrophytes. [1] This compound (50 mg/kg) is able to suppress COLO 205 tumor xenografts growth. Treatment with this chemical and nocodazole (5 mg/kg) together significantly enhances the efficacy of nocodazole, leading to cessation of tumor growth. [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human hepatoma cells HepG2
濃度 ~50 μM
反応時間 30 hours
実験の流れ

The cells (5× 103/mL) are incubated in triplicate in a 96-well plate in the presence or absence of indicated concentration of Griseofulvin in a final volume of 0.2 mL for different time intervals at 37 ℃. Thereafter, 20 μL MTT solution (5 mg/mL in PBS) is added to each well. After a 2-hour incubation at 37 ℃, 0.1 mL lysis buffer (20% SDS, 50% dimethylformamide) is added, incubation is continued overnight at 37 ℃, and then the optical density at 570 nm is measured by plate reader.

動物実験 動物モデル Human colon adenocarcinoma xenografts COLO 205
投薬量 50 mg/kg
投与方法 i.p. 3 times per week for 6 weeks

参考

  • https://pubmed.ncbi.nlm.nih.gov/3277037/
  • https://pubmed.ncbi.nlm.nih.gov/11169965/
  • https://pubmed.ncbi.nlm.nih.gov/21131551/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

The Eμ-Ret mouse is a novel model of hyperdiploid B-cell acute lymphoblastic leukemia [ Leukemia, 2024, 38(5):969-980] PubMed: 38519798
Lactate Promotes Hypoxic Granulosa Cells' Autophagy by Activating the HIF-1α/BNIP3/Beclin-1 Signaling Axis [ Genes (Basel), 2024, 16(1)14] PubMed: 39858561

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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