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PF-01367338

(CAS No:459868-92-9)
Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.
CAS No:459868-92-9
Molecular Weight(MW):421.36
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 459868-92-9
Molecular formula(MF) C19H18FN3O.H3Po4
Molecular Weight(MW): 421.36
Alias 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-azepino[5,4,3-cd]indol-6-one, phosphate (1:1);8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-pyrrolo[4,3,2- ef][2]benzazepin-6-one phosphate (1:1);rucaparib phosphate;
Solubility
In vitro DMSO 84 mg/mL (199.35 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
Biological Activity
Description Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.
Features The first PARP inhibitor used in clinical trials combined with temozolomide.
Targets
PARP [1]
(Cell-free assay)
1.4 nM(Ki)
In vitro

Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. [1] [2] The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. [3] Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells. [4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT-474 Function Assay 0.1/1/500/1000 nM inhibits PARP activity at starting concerntration of 500 nM 25128455
BT474 Growth Inhibition Assay 500 nM 10–15 d reduces cell growth in the four lines and significantly 25128455
SKBR3 Growth Inhibition Assay 500 nM 10–15 d reduces cell growth in the four lines and significantly 25128455
AU565 Growth Inhibition Assay 500 nM 10–15 d reduces cell growth in the four lines and significantly 25128455
EFM192A Growth Inhibition Assay 500 nM 10–15 d reduces cell growth in the four lines and significantly 25128455
MDA-MB-231 Function Assay 10/20/40 μM 24 h increases p-AKT levels in a dose-dependent manner 24420152
MDA-MB-231 Cell Viability Assay 0.1-40 μM 24 h IC50 = 17.77 μM 24420152
MDA-MB-231 Apoptosis Assay 10/20/40 μM 24 h induces apoptosis dose dependently 24420152
MDA-MB-231 Growth Inhibition Assay 10/20/40 μM 24 h blocks cell cycle progression in G2/M phase 24420152
H460 Growth Inhibition Assay 400 nM 24 h increases cellular radiosensitivity 24411611
A549  Growth Inhibition Assay 400 nM 24 h increases cellular radiosensitivity 24411611
DT40 Growth Inhibition Assay IC50=21 nM 24356813
DU145 Growth Inhibition Assay IC50=18 nM 24356813
COLO704 Growth Inhibition Assay IC50=2.52 ± 0.67 μM 23729402
OVMANAb Growth Inhibition Assay IC50=2.58 ± 0.38 μM 23729402
OV177 Growth Inhibition Assay IC50=2.78 ± 0.71 μM 23729402
OAW28 Growth Inhibition Assay IC50=3.61 ± 0.28 μM 23729402
OVSAHO Growth Inhibition Assay IC50=3.64 ± 0.33 μM 23729402
OVKATE Growth Inhibition Assay IC50=3.64 ± 1.79 μM 23729402
OVCAR3 Growth Inhibition Assay IC50=3.74 ± 0.40 μM 23729402
PEO14 Growth Inhibition Assay IC50=3.84 ± 0.76 μM 23729402
A2780 Growth Inhibition Assay IC50=3.94 ± 0.25 μM 23729402
OVTOKO Growth Inhibition Assay IC50=4.14 ± 1.53 μM 23729402
KURAMOCHIb Growth Inhibition Assay IC50=4.34 ± 0.29 μM 23729402
TOV21G Growth Inhibition Assay IC50=5.07 ± 1.30 μM 23729402
OVISE Growth Inhibition Assay IC50=5.68 ± 0.23 μM 23729402
KK Growth Inhibition Assay IC50=6.15 ± 1.42 μM 23729402
RMUGS Growth Inhibition Assay IC50=7.03 ± 1.83 μM 23729402
PEO6 Growth Inhibition Assay IC50=7.06 ± 0.74 μM 23729402
OVCA429 Growth Inhibition Assay IC50=8.29 ± 1.64 μM 23729402
OV167 Growth Inhibition Assay IC50=8.33 ± 1.18 μM 23729402
RMG1 Growth Inhibition Assay IC50=9.32 ± 2.36 μM 23729402
OVCAR5 Growth Inhibition Assay IC50=9.50 ± 2.59 μM 23729402
EFO21 Growth Inhibition Assay IC50=9.92 ± 1.87 μM 23729402
ES2 Growth Inhibition Assay IC50=10.12 ± 1.23 μM 23729402
Tyk-nu Growth Inhibition Assay IC50=10.20 ± 1.12 μM 23729402
CAOV3 Growth Inhibition Assay IC50=10.37 ± 0.87 μM 23729402
OV207 Growth Inhibition Assay IC50=12.27 ± 0.32 μM 23729402
HEY Growth Inhibition Assay IC50=13.01 ± 0.75 μM 23729402
DOV13 Growth Inhibition Assay IC50>15 μM 23729402
EFO27 Growth Inhibition Assay IC50>15 μM 23729402
HEY C2 Growth Inhibition Assay IC50>15 μM 23729402
KOC-7cc Growth Inhibition Assay IC50>15 μM 23729402
MCASb Growth Inhibition Assay IC50>15 μM 23729402
OAW42 Growth Inhibition Assay IC50>15 μM 23729402
OV2008 Growth Inhibition Assay IC50>15 μM 23729402
OV90 Growth Inhibition Assay IC50>15 μM 23729402
OVCA420b Growth Inhibition Assay IC50>15 μM 23729402
OVCA432 Growth Inhibition Assay IC50>15 μM 23729402
PEA2 Growth Inhibition Assay IC50>15 μM 23729402
SKOV3 Growth Inhibition Assay IC50>15 μM 23729402
TOV112D Growth Inhibition Assay 0-3 μM IC50>15 μM 23729402
C4-2 Growth Inhibition Assay 0-3 μM 14 d DMSO decreases colony number dose dependently 23565244
PC3 Growth Inhibition Assay 0-3 μM 14 d DMSO decreases colony number dose dependently 23565244
DU145 Growth Inhibition Assay 0-3 μM 14 d DMSO decreases colony number dose dependently 23565244
VCaP  Growth Inhibition Assay 0-3 μM 14 d DMSO decreases colony number dose dependently 23565244
LNCaP  Growth Inhibition Assay 0-3 μM 14 d DMSO decreases colony number dose dependently 23565244
MDA-MB-468 Cell Viability Assay IC50=9.7 μM 22678161
MDA-MB-231 Cell Viability Assay IC50=13 μM 22678161
Cal-51 Cell Viability Assay IC50=8.6 μM 22678161

... Click to View More Cell Line Experimental Data
In vivo Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. [4] Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. [5]
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