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  1. Anti-infection Apoptosis Metabolic Enzyme/Protease Cytoskeleton Cell Cycle/DNA Damage
  2. Fungal Apoptosis Antibiotic Endogenous Metabolite Microtubule/Tubulin Wee1 Caspase Bcl-2 Family
  3. Griseofulvin

Griseofulvin  (Synonyms: 灰黃霉素)

目錄號(hào): HY-17583 純度: 99.05%
COA 產(chǎn)品使用指南

Griseofulvin 是一種具有口服活性的抗真菌類(lèi)抗生素 (antibiotic),具有抗腫瘤活性。Griseofulvin 誘導(dǎo)癌細(xì)胞凋亡 (apoptosis) 和 G2/M 細(xì)胞周期阻滯。此外,Griseofulvin 也具有心血管系統(tǒng)調(diào)節(jié)活性,可減少心絞痛發(fā)作,緩解與甲真菌病相關(guān)的手部動(dòng)脈痙攣,以及諸如肩手綜合征等周?chē)芗膊 ?

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Griseofulvin Chemical Structure

Griseofulvin Chemical Structure

CAS No. : 126-07-8

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Customer Review

Other Forms of Griseofulvin:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Griseofulvin is an orally active antifungal antibiotic with antitumor activity. Griseofulvin induces apoptosis and G2/M cell cycle arrest in cancer cells. Griseofulvin also has cardiovascular modulatory activity, reducing angina pectoris, relieving hand artery spasm associated with onychomycosis, and peripheral vascular diseases such as shoulder-hand syndrome[1][2][3][4][5][6].

IC50 & Target

Microbial Metabolite

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
> 10 μM
Compound: 8
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31359750]
CCRF-CEM IC50
10 μM
Compound: Griseofulvin
Cytotoxicity against human CEM cells after 96 hrs
Cytotoxicity against human CEM cells after 96 hrs
[PMID: 16124785]
HCC1937 IC50
> 10 μM
Compound: Griseofulvin
Antiproliferative activity against exponentially growing adherent human HCC1937 cells assessed as inhibition of cell proliferation after 72 hrs by luminescence detection based ATPlite assay
Antiproliferative activity against exponentially growing adherent human HCC1937 cells assessed as inhibition of cell proliferation after 72 hrs by luminescence detection based ATPlite assay
[PMID: 25872984]
HEK293 IC50
7.3 μM
Compound: Griseofulvin
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
[PMID: 28230985]
HeLa IC50
75 μM
Compound: 1
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 27061984]
HT-29 IC50
> 20 μM
Compound: 15
Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
[PMID: 28409637]
Huh7.5.1 IC50
10 μM
Compound: 1; isolated
Cytotoxicity against human Huh7.5.1 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
Cytotoxicity against human Huh7.5.1 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
[PMID: 28802670]
L5178Y IC50
> 10 μM
Compound: 8
Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31359750]
MCF7 IC50
13.9 μM
Compound: 15
Cytotoxicity against human MCF7 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 3 days by sulforhodamine B assay
[PMID: 28409637]
MDA-MB-231 IC50
18 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay
[PMID: 22191585]
MDA-MB-231 IC50
25 μM
Compound: 1
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter-Glo luminescent assay
[PMID: 28258034]
MDA-MB-231 IC50
25.33 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by celltiter Glo assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by celltiter Glo assay
[PMID: 27061984]
MDA-MB-435 IC50
6.4 μM
Compound: 1; isolated
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
[PMID: 28802670]
OVCAR-3 IC50
48.5 μM
Compound: 1; isolated
Cytotoxicity against human OVCAR3 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
Cytotoxicity against human OVCAR3 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
[PMID: 28802670]
U2OS IC50
22.4 μM
Compound: 1
Antiproliferative activity against human U2OS cells after 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human U2OS cells after 72 hrs by CellTiter-Glo luminescent assay
[PMID: 28258034]
U2OS IC50
22.44 μM
Compound: 1
Cytotoxicity against human U2OS cells assessed as reduction in cell viability after 72 hrs by celltiter Glo assay
Cytotoxicity against human U2OS cells assessed as reduction in cell viability after 72 hrs by celltiter Glo assay
[PMID: 27061984]
體外研究
(In Vitro)

Griseofulvin 對(duì)紅色毛癬菌 (T. rubrum)、斷發(fā)毛癬菌 (T tonsurans) 和須癬毛癬菌 (T mentagrophytes) 在浮游生物和生物膜生長(zhǎng)中的最低抑菌濃度 (MIC) 分別為 0.0078-0.0156 μg/ml, 1-4 μg/mL 和 1-4 μg/mL[1]。
Griseofulvin 抑制 KMS 18, OPM-2, RPMI-8226, U-266, MPC-11, Primary CLL cells, Raji, RAW 264,7, Oci Ly 8 Lam 53, SU DHL 4 細(xì)胞系生長(zhǎng)的 IC50 值分別為 9 μM, 45 μM, 26 μM, 18 μM, 44 μM, 80 μM, 33 μM, 28 μM, 30 μM, 22 μM[2]。
Griseofulvin (10-100 μM; 72 h) 以濃度依賴(lài)的方式抑制人骨髓瘤細(xì)胞的活力[2]
Griseofulvin (0-50 μM; 30 h) 劑量依賴(lài)性誘導(dǎo)結(jié)腸癌細(xì)胞 (COLO 205 和 HT 29)、肝癌細(xì)胞 (Hep G2 和 Hep 3B) 和白血病細(xì)胞 HL 60 的凋亡[6]。
Griseofulvin (0-20 μM; 24 h) 誘導(dǎo) HT 29 細(xì)胞異常微管聚合[6]
Griseofulvin (5-60 μM; 24 h) 在較低劑量下可誘導(dǎo)細(xì)胞凋亡,但對(duì) G2/M 細(xì)胞周期無(wú)阻滯作用[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2]

Cell Line: OPM-2 and KMS-18 cells
Concentration: 10, 50 and 100 μM
Incubation Time: 72 h
Result: Induced apoptosis in KMS-18 cells at a dose of 10 mM.

Western Blot Analysis[6]

Cell Line: HT 29 cells
Concentration: 0, 1, 10, 20, 30, 40, 50 and 60 μM
Incubation Time: 24 h
Result: Down-regulated myt-1 protein expression, activated caspase 3 and caused hyperphosphorylation of Bcl-2.
體內(nèi)研究
(In Vivo)

Griseofulvin (0.5-3 mg/kg 用于雜交犬;2 和 5 mg/kg 用于大鼠;i.v.) 增加狗和大鼠的心室收縮力并增加心臟冠狀動(dòng)脈血流量[5]。
Griseofulvin (50 mg/kg; i.p.; 每周注射 3 次,持續(xù) 6 周) 減小 COLO 205 異種移小鼠體內(nèi)的腫瘤體積[6]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

352.77

Formula

C17H17ClO6

CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱(chēng)

灰黃霉素;灰霉素;微晶灰黃霉素

結(jié)構(gòu)分類(lèi)
初始來(lái)源

Penicillium

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 33.33 mg/mL (94.48 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.8347 mL 14.1735 mL 28.3471 mL
5 mM 0.5669 mL 2.8347 mL 5.6694 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.09 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.09 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.05%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8347 mL 14.1735 mL 28.3471 mL 70.8677 mL
5 mM 0.5669 mL 2.8347 mL 5.6694 mL 14.1735 mL
10 mM 0.2835 mL 1.4174 mL 2.8347 mL 7.0868 mL
15 mM 0.1890 mL 0.9449 mL 1.8898 mL 4.7245 mL
20 mM 0.1417 mL 0.7087 mL 1.4174 mL 3.5434 mL
25 mM 0.1134 mL 0.5669 mL 1.1339 mL 2.8347 mL
30 mM 0.0945 mL 0.4725 mL 0.9449 mL 2.3623 mL
40 mM 0.0709 mL 0.3543 mL 0.7087 mL 1.7717 mL
50 mM 0.0567 mL 0.2835 mL 0.5669 mL 1.4174 mL
60 mM 0.0472 mL 0.2362 mL 0.4725 mL 1.1811 mL
80 mM 0.0354 mL 0.1772 mL 0.3543 mL 0.8858 mL
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產(chǎn)品名稱(chēng):
Griseofulvin
目錄號(hào):
HY-17583
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