Home Tools

Rucaparib hydrochloride

Catalog No. T61335 CAS 773059-19-1

Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Rucaparib hydrochloride Chemical Structure

Rucaparib hydrochloride, CAS 773059-19-1

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 2,140.00
50 mg	6-8 weeks	$ 2,785.00
100 mg	6-8 weeks	$ 3,520.00

Bulk Inquiry

This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].
In vitro	Rucaparib (AG014699) hydrochloride, a potential N-demethylation metabolite of AG14644, exhibits cytotoxicity with an LC50 of 5 μM in Capan-1 (BRCA2 mutant) cells and 100 nM in MX-1 (BRCA1 mutant) cells after 24-hour exposure at concentrations ranging from 0.1 to 100 μM. Its mechanism of enhancing radio-sensitivity involves the inhibition of NF-κB activation downstream, independent of single-strand break (SSB) repair inhibition, allowing it to target NF-κB activated by DNA damage and counteract the toxicity linked with classical NF-κB inhibitors, without affecting essential inflammatory functions. Additionally, Rucaparib inhibits PARP-1 activity by 97.1% at a 1 μM concentration in permeabilised D283Med cells, showcasing its potent inhibitory effect on this enzyme.
In vivo	Rucaparib (AG014699) hydrochloride, in combination with Temozolomide, significantly enhances Temozolomide toxicity, increases Temozolomide-induced body weight loss, and results in a significant increase in tumor growth delay. At a dosage of 1 mg/kg, it markedly inhibits tumor growth, achieving a 50% increase in Temozolomide-induced tumor growth delay in specific models. Furthermore, when administered at varying doses (10 mg/kg intraperitoneally (i.p.) or 50, 150 mg/kg orally (p.o.); daily for five days per week for six weeks), Rucaparib hydrochloride significantly restricts the growth of tumors, producing one complete and two partial regressions. Remarkably, a regimen of 150 mg/kg, p.o., once or three times a week for six weeks, shows the most significant antitumor effect with three complete regressions noted. In addition, a daily 1 mg/kg i.p. dosage of Rucaparib hydrochloride, when combined with Temozolomide, substantially enhances antitumor activity, indicating complete and sustained tumor regression in specific xenografts. In varying animal models, including female athymic nude mice with SW620 colorectal tumor cells and CD-1 nude mice with established Capan-1 xenografts, Rucaparib administrations have demonstrated a consistent ability to sensitize tumors to Temozolomide, significantly inhibit tumor growth, and are detectable in plasma post-administration, highlighting its chemosensitization potency and effectiveness in enhancing Temozolomide-induced tumor growth delay.

Molecular Weight	359.83
Formula	C19H19ClFN3O
CAS No.	773059-19-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Rucaparib hydrochloride 773059-19-1 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.