1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP

Rucaparib phosphate (Synonyms: AG-014699 phosphate; PF-01367338 phosphate)

Cat. No.: HY-10617 Purity: 99.71%
Data Sheet SDS Handling Instructions

Rucaparib (phosphate) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, and also shows binding affinity to eight other PARP domains.

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Rucaparib phosphate Chemical Structure

Rucaparib phosphate Chemical Structure

CAS No. : 459868-92-9

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10 mM * 1 mL in DMSO $77 In-stock
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Other Forms of Rucaparib phosphate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Rucaparib (phosphate) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, and also shows binding affinity to eight other PARP domains.

IC50 & Target

Ki: 1.4 nM (PARP1)

In Vitro

Rucaparib is the most potent PARP inhibitor in enzyme assays (Ki, 1.4 nM), and a possible N-demethylation metabolite of AG14644[1]. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions[2]. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells[3].

In Vivo

Rucaparib and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay[1]. Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy[3]. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts[4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00457470 Pfizer Diabetes Mellitus|Diabetic Retinopathy June 2007 Phase 2
NCT00664781 Cancer Research UK brca1 Mutation Carrier|brca2 Mutation Carrier|Breast Cancer|Ovarian Cancer December 2007 Phase 2
NCT00457470 Pfizer Diabetes Mellitus|Diabetic Retinopathy June 2007 Phase 2
NCT00664781 Cancer Research UK brca1 Mutation Carrier|brca2 Mutation Carrier|Breast Cancer|Ovarian Cancer December 2007 Phase 2
NCT01009190 Clovis Oncology, Inc. Advanced Solid Tumors February 2010 Phase 1
NCT02986100 Clovis Oncology, Inc. Solid Tumor November 2016 Phase 1
NCT02855944 Clovis Oncology, Inc.|Foundation Medicine Ovarian Cancer|Epithelial Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer September 2016 Phase 3
NCT02952534 Clovis Oncology, Inc.|Foundation Medicine Metastatic Castration Resistant Prostate Cancer November 2016 Phase 2
NCT01482715 Clovis Oncology, Inc.|Foundation Medicine Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer|Advanced Solid Tumor With Evidence of Germline or Somatic BRCA November 2011 Phase 1|Phase 2
NCT02042378 Clovis Oncology, Inc. Pancreatic Cancer|Pancreatic Ductal Adenocarcinoma April 2014 Phase 2
NCT03101280 Hoffmann-La Roche Gynecologic Neoplasms May 4, 2017 Phase 1
NCT01891344 Clovis Oncology, Inc.|Foundation Medicine Ovarian Cancer|Epithelial Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer September 2013 Phase 2
NCT02505048 UNICANCER|Clovis Oncology, Inc.|Fondation ARC Metastatic Breast Cancer March 2016 Phase 2
NCT01968213 Clovis Oncology, Inc.|Foundation Medicine|Myriad Genetics, Inc. Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Cancer January 2014 Phase 3
NCT02975934 Clovis Oncology, Inc.|Foundation Medicine Metastatic Castration Resistant Prostate Cancer January 2017 Phase 3
NCT02740712 Clovis Oncology, Inc. Neoplasms March 2016 Phase 1
NCT03140670 Abramson Cancer Center of the University of Pennsylvania Pancreatic Cancer May 1, 2017 Phase 2
NCT01074970 Hoosier Cancer Research Network|Clovis Oncology, Inc. Breast Cancer February 2010 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.3733 mL 11.8663 mL 23.7327 mL
5 mM 0.4747 mL 2.3733 mL 4.7465 mL
10 mM 0.2373 mL 1.1866 mL 2.3733 mL
Kinase Assay
[1]

Inhibition of PARP activity in 5×103 D283Med cells is measured using various concentrations of Rucaparib (0-1 μM), compared with DMSO-only. Maximally stimulated PARP activity is measured in samples of permeabilised cells by immunologica. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Medulloblastoma cell lines are seeded in 96-well plates at a density of 1×103, 3×103 and 3×103, respectively. At 24 hours (D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4 μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4 μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rucaparib is formulated in saline.

A single dose of temozolomide is administrated p.o. as a suspension in saline at 200 mg/kg either alone or in combination with a single i.p. administration of PARP inhibitor administered at 0.1 [Rucaparib and MS-AG14644 (equivalent to 0.078 mg/kg free AG14644 only)], 1.0, and 10 mg/kg (for the mesylate salts equivalent to 0.79 and 7.9 mg/kg free AG14451 and AG14452 and 0.78 and 7.8 free AG14531 and AG14644). Control animals are treated with either normal saline p.o. and i.p or normal saline p.o and PARP inhibitor 10 mg/kg i.p. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

421.36

Formula

C₁₉H₂₁FN₃O₅P

CAS No.

459868-92-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 33 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.71%

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Product Name:
Rucaparib phosphate
Cat. No.:
HY-10617
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