AZD8186
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C24H25F2N3O4
- MW: 457.47
Description
AZD8186 is a metabolically stable and pharmacologically excellent PI3Kβ/δ isoform-selective inhibitor. It is orally available, potent and selective. Enantiomerically pure AZD8186 inhibits PI3Kβ and PI3Kδ in cellular assays with IC50 values of 3 nM and 17 nM, respectively, highly selective over PI3Kα (IC50 = 752 nM). It has demonstrated a profound pharmacodynamics modulation of p-Akt in PTEN-deficient PC3 prostate tumor bearing mice after oral administration, and showed a complete inhibition of tumor growth in the mouse PTEN-deficient PC3 prostate tumor xenograft model.
More Information
| Parent CAS No. | 1627494-13-6 |
|---|---|
| Chemical Name | (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C(N[C@H](C)C2=CC(C(=O)N(C)C)=CC3C(=O)C=C(N4CCOCC4)OC2=3)=CC(F)=CC=1F |&1:3,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C24H25F2N3O4/c1-14(27-18-11-16(25)10-17(26)12-18)19-8-15(24(31)28(2)3)9-20-21(30)13-22(33-23(19)20)29-4-6-32-7-5-29/h8-14,27H,4-7H2,1-3H3/t14-/m1/s1 |
| InChiKey | LMJFJIDLEAWOQJ-CQSZACIVSA-N |
| CID | 52913813 |
| Short Description | PI3K p110β/δ inhibitor |
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