GDC-0032 (TASELISIB)

Description

Background Information:

GDC-0032 (Taselisib) is a cell permeable, orally bioavailable, and
next-generation β isoform-sparing pan PI3K inhibitor. Embedded with
unique features, GDC-0032 is a much more upgraded version of GDC-0941
(Pictilisib) in most pharmacological parameters. It potently and
selectively inhibits PI3Kα/δ/γ isoforms with IC50 values of 0.29 nM/0.12
nM/0.97nM, with reduced inhibitory potency against PI3Kβ (IC50 >8
nM, >30 fold less potent relative to the PI3Kα isoform). This
selectivity and isoform-biased profile has allowed for greater efficacy
in vivo at the maximum tolerated dose relative to a pan inhibitor in
representative PI3Kα (PIK3CA) mutant xenografts, and noticeably it
preferentially inhibited PIK3CA mutant cells relative to cells with
wild-type PI3K. It is currently in clinical evaluation.

Reference:

1. C. O. Ndubaku, 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.
2. S. Lopez, et al, Taselisib, a selective inhibitor of PIK3CA, is
highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous
carcinoma in vitro and in vivo. Gynecol Oncol. 2014
Nov;135(2):312-7*Made for reproducible, high quality research.

APIM050148: GDC-0032 (TASELISIB)

CAS No.: 1282512-48-4.
Molecular Formula: C₂₄H₂₈N₈O_2.
Molecular Weight: 460.5.
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.

Additional information

Ship from Country	USA
Size	10 mg, 100 mg, 200 mg, 50 mg

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