1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. Rucaparib phosphate

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

Cat. No.: HY-10617 Purity: 99.67%
Handling Instructions

Rucaparib phosphate (AG-014699 phosphate) est un inhibiteur de PARP qui est oralement actif et puissant, avec un Ki de 1,4 nM pour PARP1 dans la essai cellule-gratuit. Rucaparib phosphate présente une affinité de liaison avec huit autres domaines PARP.

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.

For research use only. We do not sell to patients.

Rucaparib phosphate Chemical Structure

Rucaparib phosphate Chemical Structure

CAS No. : 459868-92-9

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10 mM * 1 mL in DMSO USD 92 In-stock
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10 mg USD 144 In-stock
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50 mg USD 300 In-stock
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100 mg USD 468 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Rucaparib phosphate:

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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].

IC50 & Target[1][2]

PARP-1

1.4 nM (Ki)

PARP-2

 

PARP-3

 

In Vitro

Rucaparib (AG014699) phosphate is a possible N-demethylation metabolite of AG14644[1].
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) phosphate is cytotoxic and has the LC50 being 5 μM in Capan-1 (BRCA2 mutant) cells and only 100 nM in MX-1 (BRCA1 mutant) cells[2].
The radio-sensitization by Rucaparib phosphate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib phosphate can target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions[5].
Rucaparib phosphate inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Rucaparib (AG014699) phosphate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) phosphate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) phosphate results in a 50% increase in the temozolomide-induced tumor growth delay[1].
Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) phosphate significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions[2].
Rucaparib (150 mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) phosphate has greatest antitumor effect with three complete regressions[2].
Rucaparib phosphate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CD-1 nude mice aged 10-12 weeks with Capan-1 cells[1]
Dosage: 10 mg/kg for i.p. or 50, 150 mg/kg for p.o.
Administration: IP or PO
Result: Significantly inhibited the growth of the tumor.
Clinical Trial
Molecular Weight

421.36

Formula

C₁₉H₂₁FN₃O₅P

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (78.32 mM)

H2O : 5 mg/mL (11.87 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

  • 2.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (5.15 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (5.15 mM); Clear solution

  • 5.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (5.15 mM); Clear solution

  • 6.

    Add each solvent one by one:  1% DMSO    99% saline

    Solubility: ≥ 0.5 mg/mL (1.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.76%

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