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
Taselisib (GDC-0032), purity > 98%, is in stock. Same day shipping after order is received.
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
The following data is based on the product molecular weight 460.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.