Taselisib (GDC 0032) - 10mM in DMSO, high purity , CAS No.1282512-48-4

Item Number

T421136

• Synonyms: Phenyl chloroformate [UN2746] [Poison] | Taselisib | DB12108 | 1282512-48-4 | Caswell No. 215B | A-dimethyl-1H-pyrazole-1-acetamide | A, | EX-A1581 | HY-13898 | NCGC00387039-02 | SCHEMBL1485247 | Q4272672 | Taselisib (USAN/INN) | UNII-L08J2O299M | BG1662
• Specifications & Purity: Moligand™, 10mM in DMSO
• Biochemical and Physiological Mechanisms: Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with K_i of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targetingPI3Kα/δ/γwithKiof 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

Targets

PI3Kδ (Cell-free assay); PI3Kα (Cell-free assay); PI3Kγ (Cell-free assay); PI3Kβ (Cell-free assay); C2β (Cell-free assay) 14554,0.12 nM(Ki); 0.29 nM(Ki); 0.97 nM(Ki); 9.1 nM(Ki); 292 nM

In vitro

GDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ isoforms, with 30 fold less inhibition of the PI3K β isoform relative to the PI3Kα isoform. Preclinical data show that GDC-0032 has increased activity against PI3Kα isoform (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM.

In vivo

GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t_1/2 of 40 hours. The combination of GDC-0032 enhances activity of fulvestrant resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI for GDC-0032).

Cell Research(from reference)

Cell lines：MCF7-neo/HER2 Cells 

Incubation Time：3 and 4 days