| Description | Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity. |
| In vitro | GDC-0032与氟维司群联用,增强氟维司群活性,导致肿瘤消退和肿瘤生长延迟（91％肿瘤生长抑制（TGI））.此外,GDC-0032与他莫昔芬联用,增强他莫昔芬在体内的效力,GDC-0032的肿瘤生长抑制率为102％.GDC-0032药代动力学大约与剂量成比例并且与时间无关,平均t1/2为40小时. |
| In vivo | 临床前期数据表明,GDC-0032具有增加PI3Kα同种型（PIK3CA）突变体和HER2扩增的癌细胞系的活性。GDC-0032抑制MCF7-neo/HER2 细胞增殖,IC50为2.5 nM。GDC-0032是I类PI3Kα,δ和γ同种型的口服生物可利用的,有效的和选择性的抑制剂,相对于PI3Kα同种型,其对PI3Kβ同种型抑制率低30倍。 |
| Cell experiments | GDC-0032 is dissolved in DMSO. Cells are seeded in replicates of 6 in 96-well plates with 500 to 5,000 cells/well overnight and then treated with GDC-0032. After 4 days, the media are removed and the cells are fixed with 4% glutaraldehyde for 30 minutes. Fixed cells are stained with 0.1% crystal violet for 2 minutes, then washed, and dissolved in 10% acetic acid. |
| Target activity | PI3Kγ:0.97 nM(Ki), PI3Kα:0.29 nM(Ki), PI3Kβ:9.1 nM(Ki), PI3Kδ:0.12 nM(Ki), C2β:292 nM |
| Synonyms | RG-7604, GDC-0032 |
| molecular weight | 460.53 |
| Molecular formula | C24H28N8O2 |
| CAS | 1282512-48-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 40 mg/mL (86.86 mM), Heating is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Ndubaku CO, et al. J Med Chem, 2013, 56(11), 4597-4610. |
| Citations | 1. Huang Q, Ru Y, Luo Y, et al.Identification of a targeted ACSL4 inhibitor to treat ferroptosis-related diseases.Science Advances.2024, 10(13): eadk1200. |