459868-92-9 Usage
Description
PF-01367338 is a potent PARP1 inhibitor with a Ki value of less than 5 nM. It has demonstrated cytotoxic effects on human cancer cells and xenograft tumors with mutated or epigenetically silenced BRCA1/2. PF-01367338 also exhibits antiproliferative effects in a significant number of ovarian cancer cell lines and has the ability to synergize with other anticancer agents, such as topotecan, carboplatin, doxorubicin, paclitaxel, and temozolomide. Additionally, it has been shown to ameliorate the cardiotoxicity of doxorubicin. PF-01367338 has been recently approved for human use by the FDA.
Uses
Used in Oncology:
PF-01367338 is used as a PARP inhibitor oncolytic agent for the treatment of human cancers, particularly those with mutated or epigenetically silenced BRCA1/2. Its ability to demonstrate cytotoxic effects on cancer cells and xenograft tumors, as well as its synergistic effects with other anticancer agents, makes it a promising candidate for cancer therapy.
Used in Cardiovascular Protection:
PF-01367338 is used to ameliorate the cardiotoxicity of doxorubicin, a widely used chemotherapeutic drug. Its ability to reduce the harmful side effects of doxorubicin on the heart makes it a valuable addition to cancer treatment regimens, improving patient outcomes and quality of life.
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
Check Digit Verification of cas no
The CAS Registry Mumber 459868-92-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,5,9,8,6 and 8 respectively; the second part has 2 digits, 9 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 459868-92:
(8*4)+(7*5)+(6*9)+(5*8)+(4*6)+(3*8)+(2*9)+(1*2)=229
229 % 10 = 9
So 459868-92-9 is a valid CAS Registry Number.
InChI:InChI=1/C19H18FN3O.H3O4P/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15;1-5(2,3)4/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24);(H3,1,2,3,4)
459868-92-9Relevant articles and documents
SALTS OF TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASES
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Page 13, (2008/06/13)
Pharmaceutically acceptable salts of compounds of the formula (I) below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegener
