GDC-0032
- Catalog NO.:A855667
- CAS No. : 1282512-48-4
- Molecular Formula:C24H28N8O2
- Molecular Weight: 460.53
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Product Details
CAS Number | 1282512-48-4 | Appearance | Off-white powder |
Catalog Number | A855667 | MDL Number | MFCD28167893 |
Molecular Formula | C24H28N8O2 | Molecular Weight | 460.53 |
Boiling Point | 783.3±70.0°C at 760 mmHg | Melting Point | |
Flash Point | Density | ||
Synonyms | Taselisib;RG7604;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 | ||
Storage Condition | Store in a tightly closed container,in a cool and dry place |
Safety
GHS Pictogram | |||
Signal Word | Warning | UN Number | |
Hazard Statements | H302-H315-H319-H335 | Class | |
Precautionary Statements | P261-P305+P351+P338 | Packing Group |
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. |