RLY-2608
Highest phase reached
Phase 1
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 1
- Drug type
- Small molecule
- Drug name
- RLY-2608
- Molecular weight
- 608.91
- Structure (SMILES)
- N#Cc1c(-c2cc(NC(=O)c3cc(F)cc(C(F)(F)F)c3)c3c(c2)C(=O)N[C@H]3c2cc(F)ccc2Cl)ccc2ncnn12
- acc 602
- ACC-602
- c200825002 fp
- C200825002-FP
- rly 2608
- RLY 2608
- Rly-2608
- RLY-2608
- rly2608
- RLY2608
- rtx 1274076
- rtx 4076
- RTX-1274076
- RTX-4076
- zovegalisib
- Zovegalisib
- ZOVEGALISIB
- zovegalisib [INN]
- ZOVEGALISIB [USAN]
- zovegalisib inn
- zovegalisib usan
- CAS registry numbers
- 2733573-94-7
- ChEMBL ID
- CHEMBL6068523
- InChIKey
- VYWRYBZVVSPTQN-SANMLTNESA-N
- PubChem compound IDs
- 166822065
- FDA ingredient codes (UNII)
- LR5XLA3BPC
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- zovegalisib
- Type
- Synthetic organic
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- PIK3CA
- Protein identifier
- P42336
- Median affinity
- 7.32
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- PIK3CA
- Protein identifier
- P42336
- Median affinity
- 8.4
- Affinity units
- pIC50
- Condition identifier
- EFO_0009146
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 3
- Condition identifier
- MONDO_1040002
- Highest recorded phase
- 2
- Hydrogen bond acceptors
- 6
- Hydrogen bond donors
- 2
- Polar surface area
- 112.18
- Calculated partition coefficient (ALogP)
- 6.3
- Calculated partition coefficient (XLogP)
- 5.5
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 4
- Heavy atoms
- 43
- Molecular formula
- C29H14ClF5N6O2
- Monoisotopic mass
- 608.0786922
- Natural product
- No
- Recorded assays
- 59
- Active assays
- 4
Active assay types
- Confirmatory
Related records
Trials (3)
- A Phase 2 Study of Mutant-selective PI3Kα Inhibitor, RLY-2608, in Adults and Children With PIK3CA Related Overgrowth Spectrum and Malformations Driven by PIK3CA Mutation (The ReInspire Study)
- First-in-Human Study of Mutant-selective PI3Kα Inhibitor, RLY-2608, as a Single Agent in Patients With Advanced Solid Tumors and in Combination With Endocrine Therapy +/- a CDK4/6 or CDK4 Inhibitor in Patients With Advanced Solid Tumors or Advanced Breast Cancer
- Phase 3 Study of RLY-2608 + Fulvestrant vs Capivasertib + Fulvestrant as Treatment for Locally Advanced or Metastatic PIK3CA-mutant HR+/HER2- Breast Cancer