1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    mTOR
    Autophagy
  3. BGT226 maleate

BGT226 maleate (Synonyms: NVP-BGT226 (maleate))

Cat. No.: HY-13334 Purity: 99.76%
Handling Instructions

BGT226 maleate (NVP-BGT226 maleate) 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.

For research use only. We do not sell to patients.

BGT226 maleate Chemical Structure

BGT226 maleate Chemical Structure

CAS No. : 1245537-68-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 186 In-stock
Estimated Time of Arrival: December 31
5 mg USD 130 In-stock
Estimated Time of Arrival: December 31
10 mg USD 230 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1248 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 2 publication(s) in Google Scholar

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Description

BGT226 maleate (NVP-BGT226 maleate) 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)

PI3Kγ

38 nM (IC50)

PI3Kβ

63 nM (IC50)

mTOR

 

Autophagy

 

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].

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 hour
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].

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.
Clinical Trial
Molecular Weight

650.60

Formula

C₃₂H₂₉F₃N₆O₆

CAS No.

1245537-68-1

SMILES

COC1=CC=C(C=N1)C2=CC=C(C3=C2)N=CC(N4C)=C3N(C4=O)C5=CC=C(C(C(F)(F)F)=C5)N6CCNCC6.OC(/C=C\C(O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 42.86 mg/mL (65.88 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5370 mL 7.6852 mL 15.3704 mL
5 mM 0.3074 mL 1.5370 mL 3.0741 mL
10 mM 0.1537 mL 0.7685 mL 1.5370 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.84 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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BGT226 maleate
Cat. No.:
HY-13334
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