RK-582

• Description:

  RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model[1].

• UNSPSC:

  12352005

• Target:

  PARP

• Type:

  Reference compound

• Related Pathways:

  Cell Cycle/DNA Damage; Epigenetics

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/rk-582.html

• Purity:

  98.05

• Solubility:

  DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles:

  O=C(N1C)C2(CCN(C(NC3=C4CCCN3C)=NC4=O)CC2)C(C1=CC(N(C[C@@H]5C)C[C@H](O5)C)=C6)=C6F

• Molecular Formula:

  C27H35FN6O3

• Molecular Weight:

  510.60

• References & Citations:

  [1]Shirai F et al. Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer. J Med Chem. 2020 Apr 23;63 (8) :4183-4204.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 1

• CAS Number:

  [2171388-28-4]