NVP-BGT226, PI3K/mTOR Dual Inhibitor
Overview | |
Catalog # | bs-66050c-2mg-solid |
Product Name | NVP-BGT226, PI3K/mTOR Dual Inhibitor |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 534.53 Formula: C28 H25 F3 N6 O2 CAS Number: 1245537-68-1 InChi Key: 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 Smiles: CN1C(=O)N(C2C1=CN=C1C=CC(=CC1=2)C1C=NC(=CC=1)OC)C1=CC=C(C=C1)N1CCNC(C1)C(F)(F)F Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid Power. Shelf Life: 1.0 years |
Description | NVP-BGT226 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. |