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Taselisib

Catalog No. T1999   CAS 1282512-48-4
Synonyms: RG-7604, GDC-0032

Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Taselisib Chemical Structure
Taselisib, CAS 1282512-48-4
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 61.00
10 mg In stock $ 93.00
25 mg In stock $ 159.00
50 mg In stock $ 207.00
100 mg In stock $ 369.00
200 mg In stock $ 549.00
500 mg In stock $ 885.00
1 mL * 10 mM (in DMSO) In stock $ 61.00
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Purity: 99.62%
Purity: 99.46%
Purity: 98.92%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity.
Targets&IC50 PI3Kγ:0.97 nM(Ki), PI3Kα:0.29 nM(Ki), PI3Kβ:9.1 nM(Ki), PI3Kδ:0.12 nM(Ki), C2β:292 nM
Kinase Assay 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.
Cell Research 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.
Synonyms RG-7604, GDC-0032
Molecular Weight 460.53
Formula C24H28N8O2
CAS No. 1282512-48-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 70 mg/mL (151.99 mM), warmed

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Ndubaku CO, et al. J Med Chem, 2013, 56(11), 4597-4610.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Reprogramming Compound Library Bioactive Compound Library ReFRAME Related Library Target-Focused Phenotypic Screening Library Anti-Metabolism Disease Compound Library Anti-Cancer Compound Library Neural Regeneration Compound Library

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Keywords

Taselisib 1282512-48-4 Metabolism PI3K/Akt/mTOR signaling PI3K Carbonic Anhydrase RG7604 inhibit RG-7604 Inhibitor GDC0032 Phosphoinositide 3-kinase GDC 0032 RG 7604 GDC-0032 inhibitor

 

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