2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. Rucaparib hydrochloride

Rucaparib hydrochloride  (Synonyms: AG014699 hydrochloride; PF-01367338 hydrochloride)

Cat. No.: HY-10617B
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Rucaparib (AG014699) hydrochloride 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 hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research.

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Rucaparib hydrochloride Chemical Structure

Rucaparib hydrochloride Chemical Structure

CAS No. : 773059-19-1

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Rucaparib hydrochloride Related Antibodies

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Description

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

IC50 & Target

PARP-1

1.4 nM (Ki)

PARP-2

 

PARP-3

 

In Vitro

Rucaparib (AG014699) hydrochloride is a possible N-demethylation metabolite of AG14644[1].
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) hydrochloride 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 hydrochloride is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib hydrochloride 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 hydrochloride inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells[6].

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

Rucaparib hydrochloride Related Antibodies
In Vivo

Rucaparib (AG014699) hydrochloride and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) hydrochloride significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) hydrochloride 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) hydrochloride 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) hydrochloride has greatest antitumor effect with three complete regressions[2].
Rucaparib (1 mg/kg; i.p.; daily for 5d) hydrochloride enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts[6].

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

Animal Model: Female athymic nude mice, implanted SW620 colorectal tumor cells (1 × 107 cells per animal) s.c.[1]
Dosage: 0.1 mg/kg in combination with Temozolomide (p.o., 200 mg/kg), 0.05, 0.15, and 0.5 mg/kg in combination with Temozolomide (p.o., 68 mg/kg) or 10 mg/kg
Administration: IP, single dose for 0.1 mg/kg and 10 mg/kg, five daily doses for 0-0.5 mg/kg
Result: Significantly increased Temozolomide toxicity, showed outstanding chemosensitization potency and caused enhancement of Temozolomide-induced tumor growth delay.
Animal Model: CD-1 nude mice bearing established Capan-1 xenografts[2]
Dosage: 10 mg/kg or 50, 100 and 150 mg/kg
Administration: IP for 10 mg/kg; PO for 50, 100 and 150 mg/kg, single dose (Pharmacokinetics)
Result: Parent drug was detectable in the plasma only at 30 min after 10 mg/kg i.p and up to 4 h for 50–150 mg/kg p.o.. Was still detectable in most mice receiving oral rucaparib at 3 days. Does not easily cross the plasma membrane.
Animal Model: CD-1 nude mice bearing established Capan-1 xenografts[2]
Dosage: 10 mg/kg i.p. daily for 5 days per week for 6 weeks, 50 or 150 mg/kg p.o. daily × five weekly × six, 150 mg/kg p.o. once per week for 6 weeks or three times per week for 6 weeks, or 150 mg/kg p.o. daily for five days every 3 weeks
Administration: IP or PO
Result: 10 mg/kg i.p. significantly inhibited the growth of the tumor, daily oral administration at 150 mg/kg had an equivalent effect on tumor growth to 10 mg/kg i.p.. The schedule with the greatest antitumor effect was oral administration of 150 mg/kg on a once weekly schedule with three complete regressions.
Animal Model: CD-1 nude mice, NB1691 and SHSY5Y xenografts[6]
Dosage: 1 mg/kg
Administration: IP, daily for 5 d in combination with Temozolomide (orally daily ×5 at a dose of 68 mg/kg)
Result: Enhanced the antitumor activity of Temozolomide and indicated complete and sustained tumor regression.
Clinical Trial
Molecular Weight

359.83

Formula

C19H19ClFN3O
CAS No.
SMILES

FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Rucaparib hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rucaparib773059-19-1AG014699PF-01367338AG 014699AG-014699PF01367338PF 01367338PARPpoly ADP ribose polymeraseorallyPARP-1PARP-2PARP-3hexose-6-phosphate dehydrogenaseH6PDcastration-resistant prostate cancerCRPCInhibitorinhibitorinhibit

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