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

BF738735 是一种磷脂酰肌醇 4-激酶 IIIβ (PI4KIIIβ) 抑制剂，IC50 为 5.7 nM。

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BF738735 Chemical Structure

BF738735 Chemical Structure

CAS No. : 1436383-95-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1320
In-stock
1 mg ￥419
In-stock
5 mg ￥1200
In-stock
10 mg ￥2100
In-stock
25 mg ￥4700
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

BF738735 相关抗体

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PI4KIIIβ PI4KIIIα PI4K PI4KII

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

PI4KIIIβ

5.7 nM (IC50)

PI4KIIIα

1.7 μM (IC50)

体外研究
(In Vitro)

BF738735 (Compound 1) strongly inhibits PI4KIIIβ activity in vitro, with an IC50 of 5.7 nM. BF738735 also impairs PI4KIIIα, but only at an ~300-fold-higher concentration (IC50 of 1.7 μM). In addition, the activity of BF738735 is analyzed on a set of 150 cellular kinases, including 13 lipid kinases at a concentration of 10 μM. For all kinases, the inhibition is less than 10%, indicating that BF738735 specifically inhibits PI4KIIIβ in vitro. BF738735 exhibits a broad spectrum of antiviral activity, as it inhibits all tested species of enteroviruses and rhinoviruses, with 50% effective concentrations ranging between 4 and 71 nM. BF738735 potently inhibits all viruses tested, with EC50s ranging between 4 and 71 nM. The cytotoxicity of BF738735, determined in parallel with the EC50 and using the same culture conditions for 3 to 4 days, is low, with CC50 values ranging from 11 to 65 μM, resulting in high selectivity indices. Low concentrations of BF738735 reduce the amount of luciferase to GuaHCl-treated levels, suggesting that the BF738735 blocks viral RNA replication. The EC50 of BF738735 in this assay is 77 nM, which is comparable to the inhibition observed in the multicycle assay for coxsackievirus serotype B3 (CVB3)[1].

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

BF738735 相关抗体:
体内研究
(In Vivo)

BF738735 is well tolerated by specimens with good plasma levels of the antiviral in circulation and a complete inhibition with 25 mg/kg and some inhibition with 5 mg/kg dose is observed[2].

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

426.46

Formula

C21H19FN4O3S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (293.11 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.88 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.88 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.10%

COA (196 KB) RP-HPLC (244 KB)

产品使用指南 (1538 KB)
参考文献
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.
参考文献

BF738735 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 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.

Keywords:

BF7387351436383-95-7BF 738735BF-738735PI4KReverse TranscriptasePhosphatidylinositol 4 kinasesPI4 kinasesInhibitorinhibitorinhibit

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