GDC-0068
- Ipatasertib - RG7440
- Optical Purity: 99% d.e.
- Soluble in DMSO
- MF: C24H32ClN5O2
- MW: 458
Description
GDC-0068 is a potent, APT-competitive and orally available small molecule pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively, and with selectivity over more than other 200 screened kinases. It displays robust antitumor activity with activation of PI3K-Akt-mTOR pathway.
More Information
| Parent CAS No. | 1001264-89-6 |
|---|---|
| Chemical Name | (S)-2-(4-Chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12[C@H](C)C[C@@H](O)C=1N=CN=C2N1CCN(C(=O)[C@H](CNC(C)C)C2C=CC(Cl)=CC=2)CC1 |&1:1,4,17,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C24H32ClN5O2/c1-15(2)26-13-19(17-4-6-18(25)7-5-17)24(32)30-10-8-29(9-11-30)23-21-16(3)12-20(31)22(21)27-14-28-23/h4-7,14-16,19-20,26,31H,8-13H2,1-3H3/t16-,19-,20-/m1/s1 |
| InChiKey | GRZXWCHAXNAUHY-NSISKUIASA-N |
| CID | 24788740 |
| Short Description | Akt inhibitor |
References
- L Sun et al. Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis. 2018 Sep 5;9(9):911.
- JF Blake et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.
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