Rucaparib, Free Base (AG-14447, CAS 283173-50-2), >99%

LC Laboratories' Product Number R-6300 - Rucaparib, Free Base (AG-14447, CAS 283173-50-2), >99% - for research use only. Rucaparib, also known as AG014699, is a potent PARP1 inhibitor with a Ki of 1.4 nM. This research compound is the free base form of rucaparib. We also offer the rucaparib, phosphate salt form; please see Rucaparib, Phosphate Salt, Cat. No. R-6399. The phosphate salt form of rucaparib is used for some or all rucaparib formulations for use in humans. Rucaparib inhibited the growth of human cancer cells or xenograft tumors with mutated or epigenetically silenced BRCA1/2. Rucaparib enhanced the cytotoxic effects of temozolomide and topotecan in childhood neuroblastoma. Rucaparib radiosensitized prostate cancer cells to low dose rate radiation applied over a longer period of time that resulted in enhanced DNA damage. Antiproliferative effects of rucaparib were demonstrated in 26 of 39 (67%) ovarian cancer cell lines and were not restricted to cell lines with BRCA1/2 mutations. Drug interactions with rucaparib were shown to be synergistic for topotecan, synergistic or additive for carboplatin, doxorubicin or paclitaxel, and additive for gemcitabine. Increased vessel perfusion by rucaparib may contribute to chemopotentiation in vivo. A phase 1 clinical trial demonstrated that the combination of rucaparib and temozolomide was well tolerated. PARP inhibition was shown at all doses. Combination treatment with rucaparib and temozolomide increased progression-free survival over historical controls in patients with metastatic melanoma. This rucaparib product is the free base, whose CAS number is given above. The CAS number of the phosphate salt form is 459868-92-9.

• Supplier: LC Laboratories
• Product #: R-6300
• Sku #: R-6300_5mg