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Rucaparib (phosphate)

$92$884

Products Details

Product Description

– Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].

Web ID

– HY-10617

Storage Temperature

– 4°C (Powder, sealed storage, away from moisture)

Shipping

– Room Temperature

Applications

– Cancer-programmed cell death

Molecular Formula

– C19H21FN3O5P

Citations

– Analyst. 2018 May 29;143(11):2501-2507.|Biochem Biophys Res Commun. 28 September 2021.|J Mol Med (Berl). 2019 Aug;97(8):1183-1193.|Patent. US20200078369A1|Patent. US20200129476A1|Sens Actuators B Chem. 2018 Nov 10; 273:1047-1053. |Sens Actuators B Chem. 2018, 259: 565-572.|Aging. 2021 Jan 20;13(3):4242-4257.|Am J Cancer Res. 2020 Aug 1;10(8):2649-2676.|bioRxiv. 2023 Feb 6.|bioRxiv. 2023 Feb 7.|BMC Cancer. 2022 Mar 23;22(1):312.|Clin Cancer Res. 2017 Feb 15;23(4):1001-1011. |DNA Repair (Amst). 2019 Jan;73:64-70.|FASEB J. 2022 Jul;36(7):e22418.|Front Oncol. 2021 Jul 9;11:681441.|Gene. 2020 Oct 30;759:145000.|Genes Dis. 2023 Apr 12.|Int J Mol Sci. 2020 Feb 11;21(4):1185.|JCI Insight. 2023 Nov 8;8(21):e165268.|Nat Methods. 2023 Jul 20.|Patent. US20180263995A1.|Patent. US20180362972A1.|Research Square Print. September 20th, 2022.|Research Square Print. September 22nd, 2022.|Sci Adv. 2022 Feb 18;8(7):eabl9794.|Sci Transl Med. 2021 May 26;13(595):eabe8226.|Talanta. 2018 Apr 1;180:127-132.|Theranostics. 2020 Jul 25;10(21):9477-9494.

References

– [1]Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14(2):237-246.|[2]Jianneng Li, et al. Hexose-6-phosphate dehydrogenase blockade reverses prostate cancer drug resistance in xenograft models by glucocorticoid inactivation. Sci Transl Med. 2021 May 26;13(595):eabe8226.|[3]J Murray, et al. Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules. Br J Cancer. 2014 Apr 15;110(8):1977-84.|[4]Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264.|[5]Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.|[6]Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956.

CAS Number

– 459868-92-9

Molecular Weight

– 421.36

Compound Purity

– 99.76

SMILES

– O=P(O)(O)O.FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1

Clinical Information

– Launched

Research Area

– Cancer

Solubility

– DMSO : ≥ 33 mg/mL|H2O : 5 mg/mL (ultrasonic;warming;heat to 60°C)

Target

– PARP

Isoform

– PARP1;PARP2;PARP3

Pathway

– Cell Cycle/DNA Damage;Epigenetics

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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