R-6399 Rucaparib, Phosphate Salt, >99%

Synonyms : [AG-14699] [AG014699] [PF01367338]

Related Terms : [Rubraca]

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  • 5 mg
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  • 51
  • 43
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  • 10 mg
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  • 64
  • 13,000
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  • 25 mg
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  • 129
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  • 50 mg
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  • 161
  • 135
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  • 100 mg
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  • 259
  • 219
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  • 200 mg
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  • 440
  • 371
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  • 300 mg
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  • 580
  • 490
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  • M.W. 421.36
  • C19H18FN3O•H3PO4
  • [459868-92-9]

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  • Rucaparib, also known as AG014699, is a potent PARP1 inhibitor with a Ki of 1.4 nM. Thomas H.D., et al. "Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial." Mol. Cancer Ther. 6: 945-956 (2007).
  • This research compound is the phosphate salt form of rucaparib. We also plan to offer the rucaparib, free base form; please see Rucaparib, Free Base, Cat. No. [R-6300]. The free base form will be added to our website as soon as the first lot is ready. 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. Drew Y., et al. "Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2." J. Natl. Cancer Inst. 103: 334-346 (2011).
  • Rucaparib enhanced the cytotoxic effects of temozolomide and topotecan in childhood neuroblastoma. Daniel R.A., et al. "Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma." Clin. Cancer Res. 15: 1241-1249 (2009).
  • Rucaparib radiosensitized prostate cancer cells to low dose rate radiation applied over a longer period of time that resulted in enhanced DNA damage. Chatterjee P., et al. "PARP inhibition sensitizes to low dose-rate radiation TMPRSS2-ERG fusion gene-expressing and PTEN-deficient prostate cancer cells." PLoS One 8: e60408 (2013).
  • 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. Ihnen M., et al. "Therapeutic Potential of the Poly(ADP-ribose) Polymerase Inhibitor Rucaparib for the Treatment of Sporadic Human Ovarian Cancer." Mol. Cancer Ther. 12: 1002-1015 (2013).
  • Increased vessel perfusion by rucaparib may contribute to chemopotentiation in vivo. Ali M., et al. "Vasoactivity of AG014699, a clinically active small molecule inhibitor of poly(ADP-ribose) polymerase: a contributory factor to chemopotentiation in vivo?" Clin. Cancer Res. 15: 6106-6112 (2009).
  • A phase 1 clinical trial demonstrated that the combination of rucaparib and temozolomide was well tolerated. PARP inhibition was shown at all doses. Plummer R., et al. "Phase I study of the poly(ADP-ribose) polymerase inhibitor, AG014699, in combination with temozolomide in patients with advanced solid tumors." Clin. Cancer Res. 14: 7917-7923 (2008).
  • Combination treatment with rucaparib and temozolomide increased progression-free survival over historical controls in patients with metastatic melanoma. Plummer R., et al. "A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation." Cancer Chemother. Pharmacol. 71: 1191-1199 (2013).
  • This rucaparib product is the phosphate salt, whose CAS number is given above. The CAS number of free base form is 283173-50-2.
  • Another CAS number previously assigned to Rucaparib, Phosphate Salt, namely 917828-48-9, has been deleted by CAS and is no longer in use.
  • Rucaparib (as the camsylate salt) is the active ingredient in the drug product sold under the trade name Rubraca®.  This drug is currently approved in a least one country for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer.  NOTE: THE RUCAPARIB PHOSPHATE SOLD BY LC LABORATORIES FOR RESEARCH IS NOT RUBRACA®, AND IS NOT FOR HUMAN USE.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.