Rucaparib (Synonyms: AG014699; PF-01367338)

Name: Rucaparib
Brand: MedChemExpress
SKU: HY-10617A
Rating: 5.0 (38 reviews)

Cat. No.: HY-10617A Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

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Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research.

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

Rucaparib Chemical Structure

CAS No. : 283173-50-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 92	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 38 publication(s) in Google Scholar

Other Forms of Rucaparib:

38 Publications Citing Use of MCE Rucaparib

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•Related Screening Libraries:

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View All PARP Isoform Specific Products:

View All Isoforms

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

PARP-1

1.4 nM (Ki)

PARP-2

PARP-3

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	32.21 μM Compound: 2; AG014699	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 34656898]
DLD-1	IC₅₀	0.027 μM Compound: 2	Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days	[PMID: 34570508]
GBM	EC₅₀	> 100000 nM Compound: Rucaparib	Cytotoxicity against human patient derived GBM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst staining based assay Cytotoxicity against human patient derived GBM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst staining based assay	[PMID: 32527552]
GBM	EC₅₀	> 100000 nM Compound: Rucaparib	Synergistic cytotoxicity against human patient derived GBM cells assessed as reduction in cell viability measured after 48 hrs in presence of temozolomide by Hoechst staining based assay Synergistic cytotoxicity against human patient derived GBM cells assessed as reduction in cell viability measured after 48 hrs in presence of temozolomide by Hoechst staining based assay	[PMID: 32527552]
GBM	IC₅₀	2262 nM Compound: Rucaparib	Synergistic antiproliferative activity against human patient derived GBM cells assessed as reduction in cell proliferation measured after 48 hrs in presence of temozolomide by Edu incorporation assay Synergistic antiproliferative activity against human patient derived GBM cells assessed as reduction in cell proliferation measured after 48 hrs in presence of temozolomide by Edu incorporation assay	[PMID: 32527552]
GBM	IC₅₀	53443 nM Compound: Rucaparib	Antiproliferative activity against human patient derived GBM cells assessed as reduction in cell proliferation measured after 48 hrs by Edu incorporation assay Antiproliferative activity against human patient derived GBM cells assessed as reduction in cell proliferation measured after 48 hrs by Edu incorporation assay	[PMID: 32527552]
HT-22	IC₅₀	57 μM Compound: 53	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
LoVo	GI₅₀	144 nM Compound: 4; AG014699	Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay	[PMID: 26652717]
LoVo	EC₅₀	4.69 nM Compound: 4; AG014699	Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay	[PMID: 26652717]
MCF7	CC₅₀	19.47 μM Compound: AG014699	Anticancer activity against human MCF7 cells after 96 hrs by MTT assay Anticancer activity against human MCF7 cells after 96 hrs by MTT assay	[PMID: 26342868]
MCF7	IC₅₀	6.61 μM Compound: 2; AG014699	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 34656898]
MDA-MB-231	IC₅₀	39 μM Compound: Ruc; Rib	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay	[PMID: 35707158]
MDA-MB-436	CC₅₀	3 μM Compound: AG014699	Anticancer activity against human BRCA1-deficient MDA-MB-436 cells after 96 hrs by MTT assay Anticancer activity against human BRCA1-deficient MDA-MB-436 cells after 96 hrs by MTT assay	[PMID: 26342868]
MX1	IC₅₀	6.51 μM Compound: 2; AG014699	Antiproliferative activity against human BRCA mutant MX1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human BRCA mutant MX1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 34656898]
OVCAR-3	IC₅₀	3.31 μM Compound: Rucaparib	Antiproliferative activity against human OVCAR3 cells after 24 hrs by MTT assay Antiproliferative activity against human OVCAR3 cells after 24 hrs by MTT assay	[PMID: 29456106]
U-87MG ATCC	IC₅₀	20 μM Compound: Ruc; Rib	Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay	[PMID: 35707158]

In Vitro

Rucaparib (AG014699) is a possible N-demethylation metabolite of AG14644^[1].
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) 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 is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib 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 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.

In Vivo

Rucaparib (AG014699) and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) 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) 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) has greatest antitumor effect with three complete regressions^[2].
Rucaparib 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 CD-1 nude mice aged 10-12 weeks with Capan-1 cells^[2]
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

323.36

Formula

C₁₉H₁₈FN₃O

CAS No.

283173-50-2

Appearance

Solid

Color

Off-white to yellow

SMILES

FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1

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 : 25 mg/mL (77.31 mM; ultrasonic and adjust pH to 4 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0925 mL	15.4626 mL	30.9253 mL
5 mM	0.6185 mL	3.0925 mL	6.1851 mL
10 mM	0.3093 mL	1.5463 mL	3.0925 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (248 KB) HNMR (257 KB) RP-HPLC (242 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956. [Content Brief]

[2]. J Murray, et al. Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules. Br J Cancer. 2014 Apr 15;110(8):1977-84. [Content Brief]

[3]. Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249. [Content Brief]

[4]. Jianneng Li, et al. Hexose-6-phosphate dehydrogenase blockade reverses prostate cancer drug resistance in xenograft models by glucocorticoid inactivation. Sci Transl Med. 2021 May 26;13(595):eabe8226. [Content Brief]

[5]. Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264. [Content Brief]

[6]. Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14(2):237-246. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0925 mL	15.4626 mL	30.9253 mL	77.3132 mL
	5 mM	0.6185 mL	3.0925 mL	6.1851 mL	15.4626 mL
	10 mM	0.3093 mL	1.5463 mL	3.0925 mL	7.7313 mL
	15 mM	0.2062 mL	1.0308 mL	2.0617 mL	5.1542 mL
	20 mM	0.1546 mL	0.7731 mL	1.5463 mL	3.8657 mL
	25 mM	0.1237 mL	0.6185 mL	1.2370 mL	3.0925 mL
	30 mM	0.1031 mL	0.5154 mL	1.0308 mL	2.5771 mL
	40 mM	0.0773 mL	0.3866 mL	0.7731 mL	1.9328 mL
	50 mM	0.0619 mL	0.3093 mL	0.6185 mL	1.5463 mL
	60 mM	0.0515 mL	0.2577 mL	0.5154 mL	1.2886 mL

Rucaparib Related Classifications

Help & FAQs

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Rucaparib (Synonyms: AG014699; PF-01367338)

Customer Review

Other Forms of Rucaparib:

38 Publications Citing Use of MCE Rucaparib

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•Related Small Molecules:

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View All PARP Isoform Specific Products:

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References

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Complete Stock Solution Preparation Table

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Rucaparib (Synonyms: AG014699; PF-01367338)

Customer Review

Other Forms of Rucaparib:

Rucaparib Related Antibodies

38 Publications Citing Use of MCE Rucaparib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PARP Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Rucaparib Related Antibodies

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Complete Stock Solution Preparation Table

Rucaparib Related Classifications

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