Rucaparib Camsylate, Inhibitor

Rucaparib Camsylate

Cat. Num. AAA5755489

• Synonyms: Rucaparib Camsylate; inhibitor

• Form/Format: Solid. Powder

• Solubility: DMSO: 82.33mg/mL (148.17mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C29H34FN3O5S
• SMILES: CC1(C)[C@@H]2CC[C@@]1(CS(O)(=O)=O)C(=O)C2.CNCc1ccc(cc1)-c1[nH]c2cc(F)cc3C(=O)NCCc1c23
• CAS Number: 1859053-21-6
• Target & IC50: PARP-1: ic50 1.4nM (ki)
• In Vitro: Rucaparib is not toxic but obviously enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Rucaparib and AG14584 obviously (P <0.05) increase temozolomide toxicity. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib (1mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy [1][3][4].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Rucaparib Camsylate, inhibitor

Rucaparib Camsylate is a PARP inhibitor (PARP1,Ki of 1.4nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.

Product Categories/Family for Rucaparib Camsylate, inhibitor

Chromatin/Epigenetic; DNA Damage/DNA Repair

References

Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956.
Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956.
Hunter JE, et al. NF-kappaB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264.
Hunter JE, et al. NF-kappaB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264.
Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br J Cancer, 2010, 103(10), 1588-1596.
Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br J Cancer, 2010, 103(10), 1588-1596.
Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.
Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.