Taselisib (GDC 0032)

Catalog No.S7103 Synonyms: RG7604

Taselisib (GDC 0032) Chemical Structure

Molecular Weight(MW): 460.53

Taselisib (GDC 0032) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

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Biological Activity

Description Taselisib (GDC 0032) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
Features A beta isoform-sparing PI3K inhibitor.
Targets
PI3Kδ [1]
(Cell-free assay)
PI3Kα [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
C2β [1]
(Cell-free assay)
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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MOLM16 cells NYnk[5l6WHKxbHnm[ZJifGmxbjDhd5NigQ>? M4ntZVczKGh? NVHZbGJ7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGxiVHn0[ZIuSmy3ZTDhd5NigQ>? NIrsWYQzOjd{N{[0NC=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cyclin D1 / Cyclin E / Cleaved PARP / p-AKT / pPRAS40 / p-mTOR / pp70S6K / BRCA1 / c-Myc ; 

PubMed: 27382432     


(C) Increased growth arrest and apoptosis when taselisib and letrozole are combined. Immunoblots from MCF7-ARO samples treated for 24 hours with 0.4 μM taselisib and/or 0.6 μM letrozole. (D) Taselisib and letrozole independently influence the expression of well-known ER target genes. Treatments are for 0.4 hrs with 0.6 μM taselisib and/or 0.1μM letrozole. Dotted lines for all viability data are indicative of CellTiterGlo counts at the beginning of drug treatment. Error bars indicate standard deviation around the mean.

27382432
Growth inhibition assay
Cell viability; 

PubMed: 27382432     


(A) Cell potency of taselisib and letrozole was determined in a 96-hour viability assay. (B) Taselisib combines well with letrozole in MCF7-ARO cells. The effect on viability of taselisib and letrozole as single agents is shown in the black and red lines, respectively. The combination effect of the two drugs is indicated with the blue line. 

27382432
In vivo GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t1/2 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). [1]

Protocol

Kinase Assay:[1]
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Characterization of Biochemical and Cellular Activity in Vitro:

Enzymatic activity of the class I PI3K isoforms is measured using a fluorescence polarization assay that monitors formation of the product 3,4,5-inositoltriphosphate molecule as it competes with fluorescently labeled PIP3 for binding to the GRP-1 pleckstrin homology domain protein. An increase in phosphatidyl inositide-3-phosphate product results in a decrease in fluorescence polarization signal as the labeled fluorophore is displaced from the GRP-1 protein binding site. Class I PI3K isoforms are expressed and purified as heterodimeric recombinant proteins. Tetramethylrhodamine-labeled PIP3 (TAMRA-PIP3), di-C8-PIP2, and PIP3 detection reagents are purchased from Echelon Biosciences. PI3Kα is assayed under initial rate conditions in the presence of 10 mM Tris (pH 7.5), 25 μM ATP, 9.75 μM PIP2, 5% glycerol, 4 mM MgCl2, 50 mM NaCl, 0.05% (v/v) Chaps, 1 mM dithiothreitol, and 2% (v/v) DMSO at 60 ng/mL. After assay for 30 min at 25 °C, reactions are terminated with a final concentration of 9 mM EDTA, 4.5 nM TAMRA-PIP3, and 4.2 μg/mL GRP-1 detector protein before reading fluorescence polarization on an Envision plate reader. IC50 values are calculated from the fit of the dose-response curves to a 4-parameter equation. Each reported value is an average of three experiments, and all have a standard deviation less than one geometric mean.
Animal Research:[1]
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  • Animal Models: MCF7-neo/Her2 xenograft model
  • Formulation: 0.5% methylcellulose with 0.2% Tween-80
  • Dosages: 1.4, 2.8, 5.8, 11.25, or 22.5 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 70 mg/mL warmed (151.99 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 460.53
Formula

C24H28N8O2

CAS No. 1282512-48-4
Storage powder
in solvent
Synonyms RG7604

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID