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| | PF-01367338 Basic information |
| | PF-01367338 Chemical Properties |
| Melting point | >173°C (dec.) | | storage temp. | Sealed in dry,Room Temperature | | solubility | Soluble in DMSO (up to 25 mg/ml). | | form | Yellow solid. | | color | Yellow | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| | PF-01367338 Usage And Synthesis |
| Description | Rucaparib phosphate (459868-92-9) is a potent (Ki<5 nM) PARP1 inhibitor.1?Cytotoxic to human cancer cells or xenograft tumors with mutated or epigenetically silenced BRCA1/2.2?Demonstrates antiproliferative effects in 26 out of 39 ovarian cancer cell lines.3?Synergizes with other anticancer agents such as topotecan, carboplatin, doxorubicin, paclitaxel,3 and temozolomide.4?Ameliorates the cardiotoxicity of doxorubicin.5?Recently approved for human use by the FDA. | | Uses | PARP inhibitor oncolytic | | References | 1) Thomas?et al.?(2007),?Preclinical selection of a n novel poly(ADP-ribose) polymerase inhibitor for clinical trial; Mol. Cancer Ther.,?6?945
2) Drew?et al.?(2011),?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
3) Ihnen?et al.?(2013),?Therapeutic potential of the poly(ADP-ribose) polymerase inhibitor rucaparib for the treatment of sporadic human ovarian cancer; Mol. Cancer Ther.,?12?1002
4) Plummer?et al.?(2013),?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
5) Ali?et al.?(2011),?The clinically active PARP inhibitor AG014699 ameliorates cardiotoxicity but does not enhance the efficacy of doxorubicin, despite improving tumor perfusion and radiation response in mice; Mol. Cancer Ther.,?10?2320 |
| | PF-01367338 Preparation Products And Raw materials |
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