NVP-BGT226, CAS No. 1245537-68-1, is a novel dual PI3K/mTOR inhibitor with an IC50 ~1 nM. In cellular assays it could produce nearly complete inhibition of PI3K signaling at low nanomolar (<50 nM) concentrations. Flow cytometric analysis revealed an accumulation of cells in the G0–G1 phase with a concomitant loss in the S-phase. TUNEL assay and the analysis of Caspase 3/7 and PARP indicated that BGT226 induced cancer cell death through an apoptosis independent pathway. BGT226 induced autophagy as indicated by the aggregation and upregulation of the microtubule-associated protein light chain 3B-II, and p62 degradation. It is in the phase I/II clinical trials for the treatment of advanced solid tumors.

Product information

CAS Number: 1245537-68-1

Molecular Weight: 534.53

Formula: C28H25F3N6O2

Chemical Name: 8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(3-(trifluoromethyl)piperazin-1-yl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one

Smiles: CN1C(=O)N(C2=C1C=NC1=CC=C(C=C12)C1=CN=C(C=C1)OC)C1=CC=C(C=C1)N1CCNC(C1)C(F)(F)F

InChiKey: OZZKIDQZIPMFBM-UHFFFAOYSA-N

InChi: InChI=1S/C28H25F3N6O2/c1-35-23-15-33-22-9-3-17(18-4-10-25(39-2)34-14-18)13-21(22)26(23)37(27(35)38)20-7-5-19(6-8-20)36-12-11-32-24(16-36)28(29,30)31/h3-10,13-15,24,32H,11-12,16H2,1-2H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

BGT226 was used at 0.2 µM concentration in cellular assays to investigate its effects on the PI3K/AKT signaling pathways.

In Vivo:

BGT226 was dissolved in 90% NMP/10% PEG300 and orally dosed at 5mg/Kg once a day.

References:

1. 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. (2011) Clin Cancer Res. 17(22):7116-26.
2. Baumann P, et al. Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. (2012) Anticancer Drugs. 23(1):131-8.
3. Sanchez CG, et al. Preclinical modeling of combined phosphatidylinositol-3-kinase inhibition with endocrine therapy for estrogen receptor-positive breast cancer. (2011) Breast Cancer Res. 13(2):R21
4. Fokas E, et al. NVP-BEZ235 and NVP-BGT226, dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitors, enhance tumor and endothelial cell radiosensitivity. (2012) Radiat Oncol. 7:48

Products are for research use only. Not for human use.