NVP-TNKS656 Inhibitor CAS No. 1419949-20-4

Cat. No.	Name	Size	Price	Add Cart
KI3540	NVP-TNKS656	5 mg	$660

Chemical Characteristic

Product Name	NVP-TNKS656
Synonyms	TNKS656; TNKS-656
CAS No.	1419949-20-4
Molecular Weight	494.58
Formula	C₂₇H₃₄N₄O₅
Chemical Name	N-(cyclopropylmethyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)-N-((4-oxo-3,5,7,8-tetrahydro-4H-pyrano[4,3-d]pyrimidin-2-yl)methyl)acetamide
Smiles	C(=O)(CN1CCC(CC1)C(=O)c1ccc(cc1)OC)N(Cc1nc2c(c(=O)[nH]1)COCC2)CC1CC1
Chemical Structure
Documents	HNMR LCMS

Biological activities

NVP-TNKS656 is a potent tankyrase inhibitor.^[1] NVP-TNKS656 is an orally active antagonist of Wnt pathway activity. In vitro, NVP-TNKS656 inhibits tankyrase with an IC50 of 3.5 nM. In vivo, NVP-TNKS656 modulates Wnt/beta-catenin signaling, cohorts of MMTV-Wnt1 tumor bearing mice. NVP-TNKS656-treated tumors show a stabilization of Axin1 protein and a corresponding 70??0% reduction in the Wnt/beta-catenin target gene Axin2 mRNA level compared to vehicle control animals. In addition, NVP-TNKS656 has highly favorable physicochemical properties, and high lipophilic efficiency.^[1] After oral administration in Sprague??awley rats, NVP-TNKS656 shows good overall exposure and bioavailability (F = 46%) and an initial rapid phase of absorption followed by a second peak at 6 hours postdose. After iv administration, NVP-TNKS656 again displays good exposure and low clearance (12 mL/min/kg), in line with the low in vitro clearance prediction in rat liver microsomes (ER = 0.24).^[2]

Protocols

In vitro, NVP-TNKS656 is dissolved in DMSO.^[1]

References

[1] Shultz MD, et al. Identification of NVP-TNKS656: The Use of Structure??fficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor. Journal of medicinal chemistry, 2013, 56(16): 6495-6511. [2] Valerie S, et al. Poly(ADP-ribose): novel functions for an old molecule. Nature Reviews Molecular Cell Biology, 2006, 7 (7), 517-528\

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