Art. -Nr.: HY-13334A

BGT226

(Synonyms: NVP-BGT226)

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

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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Reinheit: 99.85%
CAS. Nr.: 915020-55-2
Formel: C₂₈H₂₅F₃N₆O₂
Molecular Weight:534.53

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BGT226 Chemical Structure

CAS. Nr.: 915020-55-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PI3Kα

4 nM (IC₅₀)

PI3Kβ

63 nM (IC₅₀)

PI3Kγ

38 nM (IC₅₀)

mTOR

Autophagy

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

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]

In Vitro

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.

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.

In Vivo

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.

Chemical Information

CAS. Nr. 915020-55-2
Appearance Solid
Molecular Weight 534.53
Formel C₂₈H₂₅F₃N₆O₂
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
Synonyms

NVP-BGT226
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (6)

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11:11:580407. PMID: 33343350
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Arch Pharm (Weinheim)

Discovery of potent CSK inhibitors through integrated virtual screening and molecular dynamic simulation. [Abstract]

2024 Sep;357(9):e2400066. PMID: 38809025
Res Sq

A first-in-class precision antibody conjugate targeting EGFR, mTOR, and PI3K to treat head and neck cancers. [Abstract]

2026 May 14:rs.3.rs-9655840. PMID: 42183362
Research Square Print

2023 Mar 9.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann Oncol. 2012 Sep;23(9):2399-408. [Content Brief]

[2]. Chang KY, et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res. 2011 Nov 15;17(22):7116-26. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

BGT226

6 Cited Publications

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BGT226

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Publications Citing Use of MedChemExpress (MCE) BGT226

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BGT226 Related Classifications

HY-13334A Related Classifications