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BGT226 (maleate)

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].

Product Specifications

CAS Number

[1245537-68-1]

Product Name Alternative

NVP-BGT226 (maleate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; mTOR; PI3K

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/nvp-bgt226.html

Purity

99.92

Solubility

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

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

Molecular Formula

C32H29F3N6O6

Molecular Weight

650.60

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

MTOR; PI3Kα; PI3Kβ; PI3Kγ

Citation 01

Arch Pharm (Weinheim) . 2024 Sep;357 (9) :e2400066.|Front Pharmacol. 2020 Nov 11;11:580407.|Harvard Medical School LINCS LIBRARY|Research Square Print. 2023 Mar 9.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Molecules. 2020 Apr 23;25 (8) :1980.

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