G007-LK is specific tankyrase 1/2 inhibitor.G007-LK (66) 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 had good oral availability in mice and about a three-hour half-life when administered intravenously, suggesting the compound was sufficiently stable to be a drug candidate.
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Name | G007-LK |
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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 |
Synonyms | G007LK,G007 LK. |
Molecular Formula | C25H16ClN7O3S |
Molecular Weight | 529.96 |
Smile | ClC1=C(C=CC=C1)N1C(=NN=C1C1=NC=C(C=C1)S(=O)(=O)C)/C=C/C1=NN=C(O1)C1=CC=C(C#N)C=C1 |
InChiKey | HIWVLHPKZNBSBE-OUKQBFOZSA-N |
InChi | 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+ |
CAS Number | 1380672-07-0 |
Related CAS |
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Formulation | crystalline solid |
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Purity | >98% by HPLC |
Storage | -20ºC for 2 years |
Solubility | 5mg/ml in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
HS Code |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |