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  1. Apoptosis
  2. Thymidylate Synthase
  3. Fosifloxuridine nafalbenamide

Fosifloxuridine nafalbenamide  (Synonyms: NUC-3373)

目錄號(hào): HY-109115 純度: 96.05%
COA 產(chǎn)品使用指南 技術(shù)支持

Fosifloxuridine nafalbenamide (NUC-3373) 屬于嘧啶核苷酸類似物,是一種胸腺嘧啶合酶 (Thymidylate synthase) 抑制劑。Fosifloxuridine nafalbenamide 具有抗癌活性。Fosifloxuridine nafalbenamide 具有誘發(fā)宿主免疫反應(yīng)和增強(qiáng)免疫研究的潛力。

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Fosifloxuridine nafalbenamide Chemical Structure

Fosifloxuridine nafalbenamide Chemical Structure

CAS No. : 1332837-31-6

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10 mM * 1 mL in DMSO ¥2700
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1 mg ¥1000
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5 mg ¥2000
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10 mg ¥2800
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25 mg ¥5000
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Fosifloxuridine nafalbenamide (NUC-3373), a pyrimidine nucleotide analogue, is a Thymidylate synthase inhibitor. Fosifloxuridine nafalbenamide has anticancer activity. Fosifloxuridine nafalbenamide has the potential to evoke a host immune response and enhance immunoresearch[1][2].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM IC50
0.05 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting
Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting
[PMID: 21892829]
CCRF-CEM IC50
0.068 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against human CEM/0 cells after 72 hrs by cell counting
Cytostatic activity against human CEM/0 cells after 72 hrs by cell counting
[PMID: 21892829]
CCRF-CEM IC50
0.13 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of dipyridamole
Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of dipyridamole
[PMID: 21892829]
CCRF-CEM IC50
0.26 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of NBMPR
Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of NBMPR
[PMID: 21892829]
CCRF-CEM IC50
0.31 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against thymidine-kinase deficient human CEM cells after 72 hrs by cell counting
Cytostatic activity against thymidine-kinase deficient human CEM cells after 72 hrs by cell counting
[PMID: 21892829]
CCRF-CEM IC50
0.6 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against ENT1 transporter-deficient human CEM cells after 72 hrs by cell counting
Cytostatic activity against ENT1 transporter-deficient human CEM cells after 72 hrs by cell counting
[PMID: 21892829]
HeLa IC50
0.065 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against human HeLa cells after 72 hrs by cell counting
Cytostatic activity against human HeLa cells after 72 hrs by cell counting
[PMID: 21892829]
HeLa IC50
2.5 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against thymidine-kinase deficient human HeLa cells after 72 hrs by cell counting
Cytostatic activity against thymidine-kinase deficient human HeLa cells after 72 hrs by cell counting
[PMID: 21892829]
L1210 IC50
0.025 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against Mycoplasma hyorhinis-infected mouse L1210 cells after 48 hrs by cell counting
Cytostatic activity against Mycoplasma hyorhinis-infected mouse L1210 cells after 48 hrs by cell counting
[PMID: 21892829]
L1210 IC50
0.045 μM
Compound: 7m, diastereomeric mixture
Cytostatic activity against thymidine-kinase deficient mouse L1210 cells after 48 hrs by cell counting
Cytostatic activity against thymidine-kinase deficient mouse L1210 cells after 48 hrs by cell counting
[PMID: 21892829]
體外研究
(In Vitro)

Fosifloxuridine nafalbenamide 誘導(dǎo)損傷相關(guān)分子模式 (DAMPs) 的釋放,增加細(xì)胞表面鈣網(wǎng)蛋白 (CRT) 的表達(dá),并伴隨核核高遷移率族蛋白 1 (HMGB1) 的丟失[1]。

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

體內(nèi)研究
(In Vivo)

Fosifloxuridine nafalbenamide 在 HT-29 裸鼠異種移植模型中表現(xiàn)出抗癌活性[2]

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

Clinical Trial
分子量

613.53

Formula

C29H29FN3O9P

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 : 100 mg/mL (162.99 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 1.6299 mL 8.1496 mL 16.2991 mL
5 mM 0.3260 mL 1.6299 mL 3.2598 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 (4.07 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 (4.07 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
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 1.6299 mL 8.1496 mL 16.2991 mL 40.7478 mL
5 mM 0.3260 mL 1.6299 mL 3.2598 mL 8.1496 mL
10 mM 0.1630 mL 0.8150 mL 1.6299 mL 4.0748 mL
15 mM 0.1087 mL 0.5433 mL 1.0866 mL 2.7165 mL
20 mM 0.0815 mL 0.4075 mL 0.8150 mL 2.0374 mL
25 mM 0.0652 mL 0.3260 mL 0.6520 mL 1.6299 mL
30 mM 0.0543 mL 0.2717 mL 0.5433 mL 1.3583 mL
40 mM 0.0407 mL 0.2037 mL 0.4075 mL 1.0187 mL
50 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8150 mL
60 mM 0.0272 mL 0.1358 mL 0.2717 mL 0.6791 mL
80 mM 0.0204 mL 0.1019 mL 0.2037 mL 0.5093 mL
100 mM 0.0163 mL 0.0815 mL 0.1630 mL 0.4075 mL
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產(chǎn)品名稱:
Fosifloxuridine nafalbenamide
目錄號(hào):
HY-109115
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