2. PI3K/Akt/mTOR Autophagy
  3. PI3K mTOR Autophagy
  4. BGT226

BGT226  (Synonyms: NVP-BGT226)

製品番号: HY-13334A 純度: 99.85%
COA 取扱説明書 Technical Support

BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.

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BGT226

BGT226 構造式

CAS 番号 : 915020-55-2

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 141 在庫あり
Solution
10 mM * 1 mL in DMSO USD 141 在庫あり
Solid
5 mg $120 在庫あり
10 mg $195 在庫あり
25 mg $400 在庫あり
50 mg $650 在庫あり
100 mg $990 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of BGT226:

BGT226 関連抗体

Top Publications Citing Use of Products

PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

mTOR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
mTOR mTORC1 mTORC2

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells[1][2].

IC50 & Target[1]

PI3Kα

4 nM (IC50)

PI3Kβ

63 nM (IC50)

PI3Kγ

38 nM (IC50)

mTOR

 

Autophagy

 

Cellular Effect
Cell Line Type Value Description References
Hep 3B2 IC50
1.22 μM
Compound: Chemical probe: NVP-BGT226
Cytotoxicity against human Hep3B cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human Hep3B cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 26003166]
HepG2 IC50
1.35 μM
Compound: Chemical probe: NVP-BGT226
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 26003166]
KB IC50
7.4 nM
Compound: BGT226; 2
Anticancer activity against human KB cells assessed as growth inhibition
Anticancer activity against human KB cells assessed as growth inhibition
[PMID: 34894440]
Mahlavu IC50
0.55 μM
Compound: Chemical probe: NVP-BGT226
Cytotoxicity against human Mahlavu cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human Mahlavu cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 26003166]
SCC-4 IC50
7.4 nM
Compound: BGT226; 2
Anticancer activity against human SCC-4 cells assessed as growth inhibition
Anticancer activity against human SCC-4 cells assessed as growth inhibition
[PMID: 34894440]
SNU-449 IC50
0.51 μM
Compound: Chemical probe: NVP-BGT226
Cytotoxicity against human SNU-449 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human SNU-449 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 26003166]
SNU-475 IC50
1.01 μM
Compound: Chemical probe: NVP-BGT226
Cytotoxicity against human SNU-475 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human SNU-475 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 26003166]
体外実験

BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 and Rapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively[2].
The expression levels of p-mTOR Ser2481 are decreased in BGT226-treated cell lines (200 nM; 24 hours) and both p-AKT Ser473 and p-mTOR Ser2448 are also decreased in BGT226-treated cell lines[2].

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

BGT226 関連抗体

Cell Viability Assay[2]

Cell Line: FaDu cells; OECM1 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time:
Result: Inhibited FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively.

Western Blot Analysis[2]

Cell Line: FaDu cells; OECM1 cells
Concentration: 200 nM
Incubation Time: 24 hours
Result: p-mTOR Ser2481 expression levels decreased, and both p-AKT Ser473 and p-mTOR Ser2448 expression levels also decreased.
体内実験

BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the tumor growth on day 21 compared with control[2].

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

Animal Model: Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model[2]
Dosage: 2.5 and 5 mg/kg
Administration: Oral administration; 21 days
Result: Caused 34.7% and 76.1% reduction of the tumor growth.
分子量

534.53

分子式

C28H25F3N6O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C2=CC=C(N3CCNCC3)C(C(F)(F)F)=C2)N(C)C4=C1C5=CC(C6=CC=C(OC)N=C6)=CC=C5N=C4
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 10 mg/mL (18.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8708 mL 9.3540 mL 18.7080 mL
5 mM 0.3742 mL 1.8708 mL 3.7416 mL
10 mM 0.1871 mL 0.9354 mL 1.8708 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (1.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1 mg/mL (1.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.85%

COA (260 KB) HNMR (263 KB) LCMS (93 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8708 mL 9.3540 mL 18.7080 mL 46.7701 mL
5 mM 0.3742 mL 1.8708 mL 3.7416 mL 9.3540 mL
10 mM 0.1871 mL 0.9354 mL 1.8708 mL 4.6770 mL
15 mM 0.1247 mL 0.6236 mL 1.2472 mL 3.1180 mL
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BGT226 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

BGT226915020-55-2NVP-BGT226BGT 226BGT-226PI3KmTORAutophagyPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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