NVP-TNKS656  (Synonyms: TNKS656)

NVP-TNKS656 (GMP) is NVP-TNKS656 (HY-13990) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC₅₀ of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.

NVP-TNKS656 (30 or 100 mg/kg, p.o.) (GMP) exhibits good exposure and moderate oral bioavailability of 32% and 53%, respectively. Some slight overproportional increase in oral exposure is observed between 30 and 100 mg/kg with the dose normalized AUC for the 100 mg/kg dose being 2-fold higher than for the 30 mg/kg dose. Mice treated with NVP-TNKS656 (350 mg/kg, p.o.) show good plasma and tumor exposures corresponding to AUC_0-24h of 515 and 325 μM·h, respectively^[1].

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

494.58

C₂₇H₃₄N₄O₅

1419949-20-4

O=C(N(CC1CC1)CC2=NC3=C(COCC3)C(N2)=O)CN4CCC(C(C5=CC=C(OC)C=C5)=O)CC4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Shultz MD, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor. J Med Chem. 2013 Aug 22;56(16):6495-511.  [Content Brief]