Products for Research Use Only

GDC-0032

CAT: 0013-GTR19163929-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19163929-01Size:1 g
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Description
GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. (In Vitro) :Taselisib (GDC-0032) (100 nM) inhibits AKT/mTOR signaling in PIK3CA mutant cell lines but not in cells with loss or mutation of PTEN; Taselisib (GDC-0032) enhances radiation-induced apoptosis and inhibits growth in head and neck cancer cell lines that are sensitive to its single-agent activiy. Taselisib (GDC-0032) enhances the effects of MEK1/2 inhibition on both BRAFV600E/PTENNull human melanoma cells autochthonous mouse melanomas. (In Vivo) :Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; Taselisib (GDC-0032) and radiation is more effective than either treatment alone in nude mice implanted with subcutaneous Cal-33 xenografts. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.) .
CAS Number
1282512-48-4
Product Name Alternative
?Taselisib
Purity
>98% (HPLC)
Solubility
Ethanol: 7 mg/mL warmed (15.19 mM) ; DMSO: 70 mg/mL warmed (151.99 mM)
Smiles
CC (C) (N1N=CC (C2=CC=C3C4=NC (C5=NC (C) =NN5C (C) C) =CN4CCOC3=C2) =C1) C (N) =O
Molecular Formula
C24H28N8O2
Molecular Weight
460.53
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2- (4- (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