Taselisib free base · Synonyms: GDC-0032 | RG-7604

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ…

For research use only. Not for human or veterinary use.

Target PI3K

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Taselisib structure

CAS No.: 1282512-48-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 698.00	BP-02499-500mg	In stock	Get quote
1 g	USD 1,278.00	BP-02499-1g	In stock	Get quote
5 g	USD 3,998.00	BP-02499-5g	In stock	Get quote

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Description

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

Biological activity

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. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM. The combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI for GDC-0032). GDC-0032 is currently in a phase I clinical trial.

Identifiers

SMILES: CC(C)N1N=C(C)N=C1C1=CN2CCOC3=CC(=CC=C3C2=N1)C1=CN(N=C1)C(C)(C)C(N)=O
InChIKey: BEUQXVWXFDOSAQ-UHFFFAOYSA-N

Specifications

MW (average): 460.5315
Formula: C₂₄H₂₈N₈O₂
CAS No.: 1282512-48-4
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 6 months

Solubility

Soluble in DMSO;H2O

Documents

References

[1]. Zachary S. Zumsteg, et al. Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations. Clin Cancer Res. 2016 Apr 15; 22(8): 2009–2019.

[2]. Marian M. Deuker, et al. PI3′-Kinase Inhibition Forestalls the Onset of MEK1/2 Inhibitor Resistance in BRAF-Mutated Melanoma. Cancer Discov. 2015 Feb; 5(2): 143–153.

[3]. Ndubaku CO, et al. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610.

Same target

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Same research area

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