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

BGT226 maleate  (Synonyms: NVP-BGT226 maleate)

Cat. No.: HY-13334 Purity: 99.87%
COA Handling Instructions

BGT226 (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
Solution
10 mM * 1 mL in DMSO USD 205 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 205 In-stock
Solid
1 mg USD 68 In-stock
5 mg USD 143 In-stock
10 mg USD 253 In-stock
50 mg USD 990 In-stock
100 mg USD 1373 In-stock
200 mg   Get quote  
500 mg   Get quote  

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

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of BGT226 maleate:

BGT226 maleate Related Antibodies

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BGT226 (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

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].

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

BGT226 maleate Related Antibodies

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].

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.
Clinical Trial
Molecular Weight

650.60

Appearance

Solid

Formula

C32H29F3N6O6
CAS No.
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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (96.07 mM; ultrasonic and warming and heat to 60°C)

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    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (3.84 mM); Suspended solution; Need ultrasonic

  • 3.

    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 available by MCE.
Purity & Documentation

Purity: 99.87%

COA (253 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References
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BGT226 maleate Related Classifications

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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  • Dilution Calculator

The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

BGT2261245537-68-1NVP-BGT226BGT 226BGT-226PI3KmTORAutophagyApoptosisPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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