BAY-1082439
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C25H30N6O5
- MW: 494.54
Description
BAY-1082439 is an oral, highly selective and balanced PI3Kα/β inhibitor, with IC50 values of 4.9 nM and 15 nM for PI3Kα and PI3Kβ isoforms respectively, and >1000-fold selectivity against mTOR kinase. BAY-1082439 demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN. In vivo, it also showed clear advantages over the strong PI3Kα inhibitor BAY80-6946 (Copanlisib) in PTEN/PI3Kβ-driven tumor models. BAY-1082439 represents a new type of PI3K inhibitor with unique pharmacological and pharmacodynamic properties to be further explored.
More Information
| Parent CAS No. | 1375469-38-7 |
|---|---|
| Chemical Name | (R)-N-(8-(2-Hydroxy-3-morpholinopropoxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylnicotinamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12C3=NCCN3C(NC(=O)C3C(C)=NC=CC=3)=NC=1C(OC)=C(OC[C@H](O)CN1CCOCC1)C=C2 |&1:25,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C25H30N6O5/c1-16-18(4-3-7-26-16)24(33)29-25-28-21-19(23-27-8-9-31(23)25)5-6-20(22(21)34-2)36-15-17(32)14-30-10-12-35-13-11-30/h3-7,17,27,32H,8-15H2,1-2H3/t17-/m1/s1 |
| InChiKey | QJTLLKKDFGPDPF-QGZVFWFLSA-N |
| CID | 135905473 |
| Short Description | PI3Kα/β inhibitor |
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