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  1. Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis
  2. HDAC Autophagy Apoptosis
  3. Mocetinostat

Mocetinostat (MGCD0103)是一種有效,可口服和同種型選擇性的 HDAC (Class I/IV) 抑制劑,抑制HDAC1,HDAC2,HDAC3HDAC11IC50分別為0.15,0.29,1.66 和 0.59 μM。 Mocetinostat對(duì)HDAC4,HDAC5,HDAC6,HDAC7或HDAC8沒(méi)有抑制作用。

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)

Mocetinostat Chemical Structure

Mocetinostat Chemical Structure

CAS No. : 726169-73-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥698
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1 mg ¥363
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5 mg ¥800
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10 mg ¥1100
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25 mg ¥1900
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50 mg ¥2700
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100 mg ¥4300
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Customer Review

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.

IC50 & Target[1]

HDAC1

0.15 μM (IC50)

HDAC2

0.29 μM (IC50)

HDAC11

0.59 μM (IC50)

HDAC3

1.66 μM (IC50)

體外研究
(In Vitro)

Mocetinostat is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8. Mocetinostat (MGCD0103) exhibits potent and selective antiproliferative activities against a broad spectrum of human cancer cell lines in vitro, and HDAC inhibitory activity is required for these effects. In all cell lines tested, Mocetinostat (MGCD0103) partially inhibits cellular HDAC enzyme activity although the maximal inhibition of activity varies among cell lines from 75% to 85% of total activity. The IC50 of Mocetinostat in intact cancer cells is independent of tissue origin. In A549 cells, MGCD0103 shows dose-dependent inhibition of HDAC activity in whole cells. At high concentrations in A549 cells, Mocetinostat inhibits a maximum of 80% of total activity. In HCT116 cells, Mocetinostat induces a significant S-phase depletion and both G1 and G2-M accumulation[1].

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

體內(nèi)研究
(In Vivo)

Mocetinostat (MGCD0103) significantly inhibits growth of human tumor xenografts in nude mice in a dose-dependent manner and the antitumor activity correlated with induction of histone acetylation in tumors. The p.o. administration of Mocetinostat (MGCD0103) (2HBr salt) significantly reduces growth of implanted advanced A549 tumors in nude mice in a dose-dependent manner after 13 days of daily administration. Mocetinostat (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blocks growth of tumors compared with vehicle treatment alone (P<0.05 in post-ANOVA Dunnett's test) with no change in body weight[1].

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

Clinical Trial
分子量

396.44

Formula

C23H20N6O

CAS 號(hào)
性狀

固體

顏色

White to off-white

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 : 50 mg/mL (126.12 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 2.5224 mL 12.6122 mL 25.2245 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 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: ≥ 2.08 mg/mL (5.25 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.25 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

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: 99.68%

參考文獻(xiàn)
Cell Assay
[1]

Cells in 96-well plates are incubated with Mocetinostat at various concentrations for 72 h at 37°C in 5% CO2. MTT is added at a final concentration of 0.5 mg/mL and incubated with the cells for 4 h before an equal volume of solubilization buffer [50% N,N-dimethylformamide, 20% SDS (pH 4.7)] is added. After overnight incubation, solubilized dye is quantified by reading at 570 nm using a reference at 630 nm. Absorbance values are converted to cell numbers according to a standard growth curve of the relevant cell line. The concentration which reduces cell numbers to 50% relative to DMSO-treated cells is determined as MTT IC50[1].

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

Animal Administration
[1][2]

Mice[1]
Female CD-1 nude mice, ages 8 to 10 wk are used. Tumor fragments (30 mg), which have been serially passaged thrice in vivo in minimal, are implanted s.c. through a small surgical incision on the flank of the mice while under general anesthesia. Mocetinostat is dissolved in vehicle (PBS acidified with 0.1 N HCl or PEG400/0.2 N HCl saline, 40:60) and dosed p.o. as solutions daily. Tumor volumes and body weight are monitored thrice weekly for at least 2 wk. Each experimental group containe six to eight animals. For pharmacokinetic study, blood is collected from animals at various time points, and plasma samples are analyzed.
Rats[2]
Forty rats (220±20 g) are randomly divided into four different dosages of Mocetinostat groups (Low group, Medium group, High group, and control group with 10 rats in each group). Mocetinostat is dissolved in corn oil as suspension at three different concentrations (20, 40, and 80 mg/mL). Three different Mocetinostat groups (Low group, Medium group, and High group) are respectively given Mocetinostat 20, 40, and 80 mg/kg one time by intragastric administration at every morning and last for 7 days. Control group are given saline by same administration method. At 8 days morning, six probe drugs, Bupropion, Phenacetin, Tolbutamide, Metoprolol, Testosterone, and Omeprazole, are mixed in corn oil and given to the rats of three Mocetinostat groups and control group by intragastric administration at a single dosage of 10 mg/kg for Bupropion, Phenacetin, Metoprolol, Testosterone, and Omeprazole and 1 mg/kg for Tolbutamide.

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

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 2.5224 mL 12.6122 mL 25.2245 mL 63.0612 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL 12.6122 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL 6.3061 mL
15 mM 0.1682 mL 0.8408 mL 1.6816 mL 4.2041 mL
20 mM 0.1261 mL 0.6306 mL 1.2612 mL 3.1531 mL
25 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5224 mL
30 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1020 mL
40 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5765 mL
50 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.2612 mL
60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0510 mL
80 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7883 mL
100 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6306 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱:
Mocetinostat
目錄號(hào):
HY-12164
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