459868-92-9 Usage
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 academic research and scientific papers
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
