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  1. PI3K/Akt/mTOR Anti-infection
  2. PI4K Reverse Transcriptase
  3. BF738735

BF738735 是一種磷脂酰肌醇 4-激酶 IIIβ (PI4KIIIβ) 抑制劑,IC50 為 5.7 nM。

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BF738735 Chemical Structure

BF738735 Chemical Structure

CAS No. : 1436383-95-7

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥1320
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1 mg ¥419
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5 mg ¥1200
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10 mg ¥2100
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25 mg ¥4700
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查看 PI4K 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC50 of 5.7 nM.

IC50 & Target[1]

PI4KIIIβ

5.7 nM (IC50)

PI4KIIIα

1.7 μM (IC50)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa EC50
31 nM
Compound: 5, BF738735
Antienteroviral activity against Human rhinovirus 14 infected in human HeLa cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
Antienteroviral activity against Human rhinovirus 14 infected in human HeLa cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
[PMID: 24900715]
HeLa CC50
61000 nM
Compound: 5, BF738735
Cytotoxicity against human HeLa cells after 2 to 3 days by MTS assay
Cytotoxicity against human HeLa cells after 2 to 3 days by MTS assay
[PMID: 24900715]
RD EC50
11 nM
Compound: 5, BF738735
Antienteroviral activity against Enterovirus 71 infected in human RD cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
Antienteroviral activity against Enterovirus 71 infected in human RD cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
[PMID: 24900715]
Vero EC50
13 nM
Compound: 5, BF738735
Antienteroviral activity against poliovirus 2 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
Antienteroviral activity against poliovirus 2 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
[PMID: 24900715]
Vero EC50
15 nM
Compound: 5, BF738735
Antienteroviral activity against Coxsackievirus B3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
Antienteroviral activity against Coxsackievirus B3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
[PMID: 24900715]
Vero EC50
19 nM
Compound: 5, BF738735
Antienteroviral activity against poliovirus 1 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
Antienteroviral activity against poliovirus 1 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
[PMID: 24900715]
Vero EC50
21 nM
Compound: 5, BF738735
Antienteroviral activity against Coxsackievirus A9 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
Antienteroviral activity against Coxsackievirus A9 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
[PMID: 24900715]
Vero EC50
5 nM
Compound: 5, BF738735
Antienteroviral activity against poliovirus 3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
Antienteroviral activity against poliovirus 3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay
[PMID: 24900715]
體外研究
(In Vitro)

BF738735 在體外強烈抑制 PI4KIIIβ 活性,IC50 值為 5.7 nM。BF738735 也會損害 PI4KIIIα,但僅在約 300 倍的濃度下 (IC50 值為 1.7 μM)。此外,還分析了 BF738735 對一組 150 種細胞激酶的活性,包括濃度為 10 μM 的 13 種脂質(zhì)激酶。對于所有激酶,抑制小于 10%,表明 BF738735 在體外特異性抑制 PI4KIIIβ。BF738735 表現(xiàn)出廣譜的抗病毒活性,因為它抑制所有測試的腸道病毒和鼻病毒,50% 有效濃度范圍在 4 到 71 nM 之間。BF738735 有效抑制所有測試的病毒,EC50 值范圍在 4 到 71 nM 之間。BF738735 的細胞毒性與 EC50 值平行測定,使用相同培養(yǎng)條件 3 至 4 天,CC50 值范圍為 11 至 65 μM,但細胞毒性較低,導(dǎo)致高選擇性指數(shù)。低濃度的 BF738735 將熒光素酶的量減少到 GuaHCl 處理的水平,表明 BF738735 阻斷了病毒 RNA 的復(fù)制。BF738735 在此測定中的 EC50 值為 77 nM,這與在柯薩奇病毒血清型 B3 (CVB3) 的多循環(huán)測定中觀察到的抑制作用相當(dāng)[1] 。

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

體內(nèi)研究
(In Vivo)

BF738735 被循環(huán)中具有良好抗病毒血漿水平的標本很好地耐受,觀察到 25 mg/kg 的完全抑制和 5 mg/kg 劑量的部分抑制[2]。

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

分子量

426.46

Formula

C21H19FN4O3S

CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
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)
細胞實驗: 

DMSO 中的溶解度 : 125 mg/mL (293.11 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3449 mL 11.7244 mL 23.4489 mL
5 mM 0.4690 mL 2.3449 mL 4.6898 mL
查看完整儲備液配制表

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

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.88 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

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

    Solubility: ≥ 2.08 mg/mL (4.88 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。
動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動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 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲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: 99.10%

參考文獻
Kinase Assay
[1]

The PI4K in vitro activity assay is performed. Briefly, recombinant PI4KIIIβ or PI4KIIIα and their substrate, phosphatidylinositol (PI)-phosphatidylserine (PS), are diluted in buffer containing Triton X-100. The reaction is started by addition of a mixture of ATP and 0.25 μCi of [γ-33P]ATP. After 75 to 90 min of incubation at 30°C, the reaction is terminated by addition of phosphoric acid. The incorporated radioactivity is measured by using a TopCount NXT microplate scintillation counter. Data are converted to the percent inhibition relative to controls[1].

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

Cell Assay
[1]

Buffalo green monkey (BGM) kidney cells, HeLa R19 cells, and HeLa Rh cells are grown at 37°C, 5% CO2 in minimal essential medium (MEM) supplemented with 10% fetal bovine serum, penicillin, and streptomycin. The assays to determine the 50% effective concentration (EC50) and 50% cytotoxic concentration (CC50) of BF738735 are performed. Briefly, cells are infected with 100 CCID50 for 2 h, after which the virus is removed and serial dilutions of BF738735 (0.01, 0.033, 0.1, 0.33, 1, 3.33, 10, 33.33 and 100 μM) are added. For determination of the CC50, serial dilutions of BF738735 are added to the cells. Following 3 to 4 days of incubation, the medium is replaced with CellTiter 96 AQueous One solution reagent. Optical densities at 490 nm are corrected for background absorbance, which is determined from wells that lack cells. The resulting values for untreated cells are set to 100%[1].

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

Animal Administration
[2]

Mice[2]
BF738735 is used to study the bioavailability and antiviral effect in vivo. BF738735 is administrated in mice, 1 mg/kg intravenously or 5 mg/kg orally to treat coxsackievirus serotype B4 (CVB4) induced pancreatitis.

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

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1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 2.3449 mL 11.7244 mL 23.4489 mL 58.6221 mL
5 mM 0.4690 mL 2.3449 mL 4.6898 mL 11.7244 mL
10 mM 0.2345 mL 1.1724 mL 2.3449 mL 5.8622 mL
15 mM 0.1563 mL 0.7816 mL 1.5633 mL 3.9081 mL
20 mM 0.1172 mL 0.5862 mL 1.1724 mL 2.9311 mL
25 mM 0.0938 mL 0.4690 mL 0.9380 mL 2.3449 mL
30 mM 0.0782 mL 0.3908 mL 0.7816 mL 1.9541 mL
40 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4656 mL
50 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1724 mL
60 mM 0.0391 mL 0.1954 mL 0.3908 mL 0.9770 mL
80 mM 0.0293 mL 0.1466 mL 0.2931 mL 0.7328 mL
100 mM 0.0234 mL 0.1172 mL 0.2345 mL 0.5862 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:
BF738735
目錄號:
HY-U00426
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