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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.