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

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

Cat. No.: HY-10617C
Handling Instructions

Rucaparib (AG014699) tartrate 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 tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research.

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

Rucaparib tartrate Chemical Structure

Rucaparib tartrate Chemical Structure

CAS No. : 773059-22-6

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Description

Rucaparib (AG014699) tartrate 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 tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].

IC50 & Target[1]

PARP-1

1.4 nM (Ki)

PARP-2

 

PARP-3

 

In Vitro

Rucaparib (AG014699) tartrate is a possible N-demethylation metabolite of AG14644[1].
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) tartrate 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 tartrate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib tartrate 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 tartrate 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) tartrate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) tartrate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) tartrate esults 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) tartrate 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) tartrate has greatest antitumor effect with three complete regressions[2].
Rucaparib tartrate 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.

Molecular Weight

473.45

Formula

C23H24FN3O7

CAS No.
SMILES

FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1.OC([[email protected]](O)[[email protected]@H](O)C(O)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Rucaparib tartrate
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