2. PROTAC Cell Cycle/DNA Damage Epigenetics
  3. PROTACs PARP
  4. iRucaparib-AP6

iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1.

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

iRucaparib-AP6 Chemical Structure

iRucaparib-AP6 Chemical Structure

CAS No. : 2410557-00-3

Size Price Stock Quantity
1 mg USD 550 In-stock
5 mg USD 1650 In-stock
10 mg USD 2850 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

iRucaparib-AP6 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE iRucaparib-AP6

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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

iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1[1].

IC50 & Target

PARP1

82 nM (DC50)

Cellular Effect
Cell Line Type Value Description References
CAPAN-1 IC50
0.95 μM
Compound: 3; iRucaparib-AP6
Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay
Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay
[PMID: 32924477]
MDA-MB-436 IC50
0.71 μM
Compound: 3; iRucaparib-AP6
Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay
Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay
[PMID: 32924477]
In Vitro

iRucaparib-AP6 (0-10 μM; 24 hours) decreases PARP-1 level in a dose dependent manner, exhibits a half-maximal degrading concentration (DC50) of 82 nM (Dmax is 92%)[1].
iRucaparib-AP6 (0-20 μM; 24 hours) induces degradation of PARP1 at low concentrations[1].

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

iRucaparib-AP6 Related Antibodies

Cell Viability Assay[1]

Cell Line: Primary rat neonatal cardiomyocyte cells
Concentration: 0.001 μM; 0.01 μM; 0.1 μM; 1 μM; 10 μM
Incubation Time: 24 hours
Result: Decreased PARP-1 level in primary rat neonatal cardiomyocyte cells.

Western Blot Analysis[1]

Cell Line: Primary rat neonatal cardiomyocyte cells
Concentration: 0.05 μM; 0.1 μM; 0.2 μM; 0.5 μM; 1 μM; 2 μM; 5 μM;10 μM; 20 μM
Incubation Time: 24 hours
Result: Induced robust PARP1 degradation at concentrations as low as 50 nM.
Molecular Weight

886.96

Formula

C46H55FN6O11
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCC1)C2=CC(F)=CC3=C2C1=C(C4=CC=C(C=C4)CN(CCOCCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C7CCC(NC7=O)=O)=O)=C5C6=O)C)N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (56.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1274 mL 5.6372 mL 11.2745 mL
5 mM 0.2255 mL 1.1274 mL 2.2549 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 (stored under nitrogen). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (2.82 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.27%

SDS (252 KB)

COA (245 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1274 mL 5.6372 mL 11.2745 mL 28.1862 mL
5 mM 0.2255 mL 1.1274 mL 2.2549 mL 5.6372 mL
10 mM 0.1127 mL 0.5637 mL 1.1274 mL 2.8186 mL
15 mM 0.0752 mL 0.3758 mL 0.7516 mL 1.8791 mL
20 mM 0.0564 mL 0.2819 mL 0.5637 mL 1.4093 mL
25 mM 0.0451 mL 0.2255 mL 0.4510 mL 1.1274 mL
30 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9395 mL
40 mM 0.0282 mL 0.1409 mL 0.2819 mL 0.7047 mL
50 mM 0.0225 mL 0.1127 mL 0.2255 mL 0.5637 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

iRucaparib-AP6 Related Classifications

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:

iRucaparib-AP62410557-00-3PROTACsPARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
iRucaparib-AP6
Cat. No.:
HY-130644
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.