[CAS NO. 1225037-39-7] Bimiralisib (PQR309)
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PRODUCTS SPECIFICATIONS [1225037-39-7]
Store
Catalog
SLK-S8738
Brand
Selleck
CAS
1225037-39-7
DESCRIPTION [1225037-39-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 411.38 |
| Molecular Formula | C17H20F3N7O2 |
| SMILES | NC1=NC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C(C(F)(F)F)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
Bimiralisib (PQR309) is a novel brain-penetrant dual inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.
Targets
In vitro
PQR309 shows in vitro activity with a median IC50 value of 233 nmol/L (95% CI, 174-324 nmol/L) in most of the tesed lymphoma cell lines (increasing doses, 72 hours). The arrest in proliferation is mainly due to cell cycle arrest with a block in G1 rather than to apoptosis, limited to only 2/7 cell lines. PQR309 is more active in B-cell lymphoma cell lines (DLBCL, MCL, CLL, and SMZL) than in the T-cell derived ALCL. PQR309 inhibits PI3K/mTOR signaling in lymphoma cell lines. It has in vitro and in vivo antilymphoma activity as single agent and in combination.
References
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