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Rucaparib

Cat. No. M4931
Rucaparib Structure
Size Price Availability Quantity
5mg USD 88 In stock
10mg USD 150 In stock
50mg USD 460 In stock
100mg USD 720 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells.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.

Product Citations
Customer Product Validations & Biological Datas
Source Invest New Drugs (2018). Figure 5. Rucaparib (AbMole BioScience)
Method intraperitoneally
Cell Lines female BALB/c nude mice
Concentrations 8 mg/kg
Incubation Time 4 weeks
Results The tumor volume in the rucaparib treatment group was less than that in the control group (P<0.05), indicating that rucaparib inhibited tumor growth
Source Invest New Drugs (2018). Figure 4. Rucaparib (AbMole BioScience)
Method Immunofluorescence
Cell Lines Hela and Siha cells
Concentrations 10 μmol/L
Incubation Time 24 hours
Results Compared with the radiotherapy group, the overall expression of DNA damage markers decreased slowly in the combined group, implying that rucaparib can block IR-induced DNA DSB repair, and enhance the sensitivity to radiotherapy by cervical cancer cells.
Source Invest New Drugs (2018). Figure 3. Rucaparib (AbMole BioScience)
Method Clonogenic assay
Cell Lines Hela and Siha cells
Concentrations 0, 1, 5, or 10 μmol/L
Incubation Time 24 hours
Results The clonogenic assay showed that rucaparib combined with radiotherapy inhibited the ability of cervical cancer cells to form colonies, with the effect exacerbated with an increasing drug concentration
Source Invest New Drugs (2018). Figure 2. Rucaparib (AbMole BioScience)
Method Flow cytometry
Cell Lines Hela and Siha cells
Concentrations 0, 1, 5, 10, 20, 40, or 80 umol/L
Incubation Time 48 h
Results At rucaparib concentrations of 0 μM, 20 μM, and 40 μM, the proportions of Hela cells in the G2/M phase were 25.11%, 31.11%, and 35.78%, respectively; while the proportions of Siha cells in the G2/M phase were 16.09%, 26.71%, and 32.22%, respectively
Source Invest New Drugs (2018). Figure 1. Rucaparib (AbMole BioScience)
Method CCK-8 assay
Cell Lines Hela and Siha cells
Concentrations 20 μM, 40 μM
Incubation Time 72 h
Results CCK-8 results showed that the viability of cells decreased significantly as the concentration of rucaparib gradually increased
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 323.36
Formula C19H18FN3O
CAS Number 283173-50-2
Purity >98%
Solubility DMSO > 80 mg/ml; Water <1 mg/ml
Storage at -20°C
References

Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial.
Thomas HD,et.al. Mol Cancer Ther. 2007 Mar;6(3). PMID: 17363489.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Rucaparib supplier, inhibitors

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