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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. |
Chemical Structure |
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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 |
SMILES Code |
CC(C)(N1N=CC(C2=CC=C3C4=NC(C5=NC(C)=NN5C(C)C)=CN4CCOC3=C2)=C1)C(N)=O |
Theoretical Analysis |
XingMo Cat#:XM176 Product Name:Taselisib (GDC0032) Synonyms:GDC0032; GDC0032; GDC 0032; RG7604; RG7604; RG 7604; Taselisib. CAS#:1282512-48-4 Chemical Formula:C24H28N8O2 Exact Mass:460.23352 Molecular Weight:460.53
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Technical Data |
Appearance: solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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 Condition: Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life:
>2 years if stored properly.
Drug Formulation:
This drug may be formulated in DMSO
Stock Solution Storage:
0 - 4℃ for short term (days to weeks), or -20℃ for long term (months). |
WARNING: This product is for research use only, not for human or veterinary use
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