NVP-TNKS656|TNKS2 inhibitor|DC Chemicals

Cas No.:	1419949-20-4
Chemical Name:	TNKS656; TNKS-656,TNKS 656
Synonyms:	TNKS656; TNKS-656,TNKS 656
SMILES:	C(N(CC1CC1)CC1NC(=O)C2COCCC=2N=1)(=O)CN1CCC(C(=O)C2=CC=C(OC)C=C2)CC1
Formula:	C₂₇H₃₄N₄O₅
M.Wt:	494.58
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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.

In Vitro:

NVP-TNKS656 (30 or 100 mg/kg, p.o.) 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 AUC0-24h of 515 and 325 μM·h, respectively[1].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC7533	wiki4	WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.
DC5150	Veliparib (ABT-888 hydrochloride)	Veliparib is a potent inhibitor of both PARP-1 and PARP-2 by [3H]NAD+ with Kis of 5.2 and 2.9 nmol/L, respectively.
DC8899	ABT888 (free base)	Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively.
DC7334	UPF 1069	UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM; ~27-fold selective against PARP1.
DC8464	Rucaparib(AG-014447)	Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM.
DC5151	Rucaparib phosphate (AG-14699, PF-01367338)	Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM with binding affinity to nine PARP domains. Phase 1/2.
DC7237	PJ34 HCl	PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
DC4110	AZD-2281 (Olaparib)	Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1 and PARP2 with IC50 of 5 nM and 1 nM, respectively.
DC8463	NVP-TNKS656	NVP-TNKS656(TNKS-656) is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2.
DC7935	NU1025	NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM).