WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205746
Description: Taselisib, also known as GDC0032 or RG7606, is a selective, potent, orally bioavailable inhibitor of PI3Ka with a Ki = 0.2nM, and with reduced inhibitory activity against PI3Kβ. This selectivity profile, and excellent pharmacokinetic and pharmaceutical properties, allowed for greater efficacy in vivo at the maximum tolerated dose relative to a pan Class I PI3K inhibitor in PIK3CA mutant xenografts. Notably, GDC-0032 preferentially inhibited PIK3CA mutant cells relative to cells with wild-type PI3K. GDC-0032 potently inhibits signal transduction downstream of PI3K and induces apoptosis at low concentrations in breast cancer cell lines and xenograft models that harbor PIK3CA mutations.
MedKoo Cat#: 205746
Name: Taselisib (GDC0032)
Chemical Formula: C24H28N8O2
Exact Mass: 460.23352
Molecular Weight: 460.53
Elemental Analysis: C, 62.59; H, 6.13; N, 24.33; O, 6.95
Synonym: GDC0032, GDC0032, GDC 0032, RG7604, RG7604, RG 7604, Taselisib
IUPAC/Chemical Name: 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
InChi Key: BEUQXVWXFDOSAQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H28N8O2/c1-14(2)32-22(27-15(3)29-32)19-13-30-8-9-34-20-10-16(6-7-18(20)21(30)28-19)17-11-26-31(12-17)24(4,5)23(25)33/h6-7,10-14H,8-9H2,1-5H3,(H2,25,33)
SMILES Code: CC(C)(N1N=CC(C2=CC=C3C4=NC(C5=NC(C)=NN5C(C)C)=CN4CCOC3=C2)=C1)C(N)=O
1: Lopez S, Schwab CL, Cocco E, Bellone S, Bonazzoli E, English DP, Schwartz PE, Rutherford T, Angioli R, Santin AD. 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 Aug 26. pii: S0090-8258(14)01277-3. doi: 10.1016/j.ygyno.2014.08.024. [Epub ahead of print] PubMed PMID: 25172762.