WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 558250
CAS#: 1380672-07-0
Description: G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor. G007-LK displayed high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice. G007-LK was first discovered by Dr. Stefan Krauss's team.
MedKoo Cat#: 558250
Name: G007-LK
CAS#: 1380672-07-0
Chemical Formula: C25H16ClN7O3S
Exact Mass: 529.07239
Molecular Weight: 529.95764
Elemental Analysis: C, 56.66; H, 3.04; Cl, 6.69; N, 18.50; O, 9.06; S, 6.05
Synonym: G007LK; G007LK; G007 LK.
IUPAC/Chemical Name: (E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile
InChi Key: HIWVLHPKZNBSBE-OUKQBFOZSA-N
InChi Code: InChI=1S/C25H16ClN7O3S/c1-37(34,35)18-10-11-20(28-15-18)24-31-29-22(33(24)21-5-3-2-4-19(21)26)12-13-23-30-32-25(36-23)17-8-6-16(14-27)7-9-17/h2-13,15H,1H3/b13-12+
SMILES Code: N#CC1=CC=C(C2=NN=C(/C=C/C3=NN=C(C4=NC=C(S(=O)(C)=O)C=C4)N3C5=CC=CC=C5Cl)O2)C=C1
License information:
MedKoo licensed the G007-LK patent right from Oslo University, Norway. G007-LK was covered by WO2012076898, pending national/regional patent applications continued from PCT/GB2011/052441 (WO2012/076898).
1: Lau T, Chan E, Callow M, Waaler J, Boggs J, Blake RA, Magnuson S, Sambrone A, Schutten M, Firestein R, Machon O, Korinek V, Choo E, Diaz D, Merchant M, Polakis P, Holsworth DD, Krauss S, Costa M. A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth. Cancer Res. 2013 May 15;73(10):3132-44. doi: 10.1158/0008-5472.CAN-12-4562. Epub 2013 Mar 28. PubMed PMID: 23539443.