iRucaparib-AP6

iRucaparib-AP6 is a highly efficient and specific PARP1 degrader based on Rucaparib by using thePROTAC approach. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1.

Product information

CAS Number: 2410557-00-3

Molecular Weight: 886.96

Formula: C46H55FN6O11

Chemical Name: 2-(2,6-dioxopiperidin-3-yl)-4-[23-(4-{6-fluoro-9-oxo-3,10-diazatricyclo[6.4.1.0⁴,¹³]trideca-1,4(13),5,7-tetraen-2-yl}phenyl)-22-methyl-4,7,10,13,16,19-hexaoxa-1,22-diazatricosan-1-yl]-2,3-dihydro-1H-isoindole-1,3-dione

Smiles: CN(CC1C=CC(=CC=1)C1NC2C=C(F)C=C3C=2C=1CCNC3=O)CCOCCOCCOCCOCCOCCOCCNC1=CC=CC2C(=O)N(C3CCC(=O)NC3=O)C(=O)C1=2

InChiKey: YHMDCINUVWULST-UHFFFAOYSA-N

InChi: InChI=1S/C46H55FN6O11/c1-52(29-30-5-7-31(8-6-30)42-33-11-12-49-43(55)35-27-32(47)28-37(50-42)40(33)35)14-16-60-18-20-62-22-24-64-26-25-63-23-21-61-19-17-59-15-13-48-36-4-2-3-34-41(36)46(58)53(45(34)57)38-9-10-39(54)51-44(38)56/h2-8,27-28,38,48,50H,9-26,29H2,1H3,(H,49,55)(H,51,54,56)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (56.37 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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 = 92%). iRucaparib-AP6 (0-20 μM; 24 hours) induces degradation of PARP1 at low concentrations.

Products are for research use only. Not for human use.