AZD-9574
Highest phase reached
Phase 1
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 1
- Drug type
- Small molecule
- Drug name
- AZD-9574
- Molecular weight
- 428.44
- Structure (SMILES)
- CNC(=O)c1ccc(N2CCN(Cc3ccc4nc(C)c(=O)[nH]c4c3F)CC2)c(F)n1
- azd 9574
- Azd-9574
- AZD-9574
- azd9574
- AZD9574
- palacaparib
- Palacaparib
- PALACAPARIB
- Palacaparib (AZD9574)
- palacaparib [INN]
- PALACAPARIB [USAN]
- palacaparib inn
- palacaparib usan
- CAS registry numbers
- 2756333-39-6
- ChEMBL ID
- CHEMBL5095223
- InChIKey
- WXRCLFFPZXJCLS-UHFFFAOYSA-N
- PubChem compound IDs
- 162524593
- FDA ingredient codes (UNII)
- 9UG32UQW48
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- palacaparib
- Type
- Synthetic organic
- Action type
- Inhibitor
- Target
- poly(ADP-ribose) polymerase 1
- Gene symbol
- poly(ADP-ribose) polymerase 1
- Action type
- Inhibitor
- Target
- poly(ADP-ribose) polymerase 2
- Gene symbol
- poly(ADP-ribose) polymerase 2
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- poly(ADP-ribose) polymerase 1
- Gene symbol
- PARP1
- Protein identifier
- P09874
- Median affinity
- 8.3
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- poly(ADP-ribose) polymerase 2
- Gene symbol
- PARP2
- Protein identifier
- Q9UGN5
- Median affinity
- 4.03
- Affinity units
- pIC50
Investigated indications
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0008170
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0008315
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0009831
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0021042
- Highest recorded phase
- 1
Trial references
- NCT05417594
- Hydrogen bond acceptors
- 6
- Hydrogen bond donors
- 2
- Polar surface area
- 94.22
- Calculated partition coefficient (ALogP)
- 1.59
- Calculated partition coefficient (XLogP)
- 1.2
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 4
- Heavy atoms
- 31
- Molecular formula
- C21H22F2N6O2
- Monoisotopic mass
- 428.17723029
- Natural product
- No
- Recorded assays
- 176
- Active assays
- 17
Active assay types
- Confirmatory
Distribution coefficient (LogD)
- Median
- 1.9
- Mean
- 1.9
- Minimum
- 1.9
- Maximum
- 1.9
- Unit
- unitless
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- LogD
Solubility
- Median
- 19,000
- Mean
- 19,000
- Minimum
- 19,000
- Maximum
- 19,000
- Unit
- nM
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Solubility
Oral bioavailability
- Median
- 91
- Mean
- 87.51
- Minimum
- 50
- Maximum
- 116
- Unit
- %
- Assays
- 5
- Standard deviation
- 23.9312
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Plasma protein binding
- Median
- 0.0685
- Mean
- 0.0685
- Minimum
- 0.04
- Maximum
- 0.097
- Unit
- fraction unbound
- Assays
- 2
- Standard deviation
- 0.0403051
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Fu
Related records
Trials (4)
- Phase I/IIa Study of AZD5335 as Monotherapy and Combination Therapy in Participants With Solid Tumors
- Phase Ib/II Platform Study of Multiple Anti-Cancer Agents in Participants With Metastatic Prostate Cancer
- Study of AZD0516 as Monotherapy and in Combination in Participants With Metastatic Prostate Cancer
- Study of AZD9574 as Monotherapy and in Combination With Anti-cancer Agents in Participants With Advanced Solid Malignancies
In development for (1)
- Cancer Phase 1