Biological activity ABT-888

Oct 11,2019

Biological activity

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

In vitro

Veliparib (ABT-888) is a potential anti-cancer drug acting as a PARP inhibitor,which inhibits PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays,respectively.ABT-888 reduces clonogenic survival and inhibits DNA repair in H460 cells. ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells.

In vivo

ABT-888 inhibits PARP in B16F10 and 9L xenograft models, thus enhancing the anticancer activity of temozolomide. The Combined with other cytotoxic agents, ABT-888 shows strong antitumor effect in MX-1 xenograft model. ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg according to the the size of tumors in A375 and Colo829 xenograft models.

Features

ABT-888 enhances the effectiveness of common cancer treatments, such as radiation therapy and alkylating agents.

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Oct 11,2019Inhibitors

ABT-888

912445-05-7

ABT-888 manufacturers

  • Veliparib dihydrochloride
  • 912445-05-7 Veliparib dihydrochloride
  • $0.00/ kg
  • 2023-12-26
  • CAS:912445-05-7
  • Min. Order: 1kg
  • Purity: 99%, Single impurity<0.1
  • Supply Ability: 1 ton
  • ABT-888
  • 912445-05-7 ABT-888
  • $1.00 / 10g
  • 2022-12-29
  • CAS:912445-05-7
  • Min. Order: 10g
  • Purity: 99.5%
  • Supply Ability: 1000kg
  • ABT-888
  • 912445-05-7 ABT-888
  • $1.00 / 1KG
  • 2019-07-06
  • CAS:912445-05-7
  • Min. Order: 1KG
  • Purity: 98%
  • Supply Ability: 100KG