504907 Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem

504907
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Empirical FormulaCAS #
C₂₅H₁₆ClN₇O₃S 1380672-07-0

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      Description
      OverviewA cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50 = 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax ~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC50 >10 µM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50 >10 µM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation in vitro (200 nM) and tumor expansion in mice in vivo (20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number504907
      Brand Family Calbiochem®
      SynonymsTNKS1/2 Inhibitor VI, G007LK, Wnt Pathway Inhibitor XXI, 4-(5-((E)-2-(4-(2-Chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)ethenyl)-1,3,4-oxadiazol-2-yl)benzonitrile
      References
      ReferencesLau, T., et al. 2013. Cancer Res. 73, 3132.
      Voronkov, A., et al. 2013. J. Med. Chem. 56, 3012.
      Product Information
      CAS number1380672-07-0
      FormWhite powder
      Hill FormulaC₂₅H₁₆ClN₇O₃S
      Chemical formulaC₂₅H₁₆ClN₇O₃S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationTankyrase 1/2 Inhibitor VI, G007-LK, CAS 1380672-07-0, is a cell-permeable, potent and highly selective inhibitor of tankyrase (IC50 = 33 & 26 nM for TNKS1 and TNKS2, respectively).
      Biological Information
      Primary TargetTankyrase 1/2
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Lau, T., et al. 2013. Cancer Res. 73, 3132.
      Voronkov, A., et al. 2013. J. Med. Chem. 56, 3012.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision15-October-2013 JSW
      SynonymsTNKS1/2 Inhibitor VI, G007LK, Wnt Pathway Inhibitor XXI, 4-(5-((E)-2-(4-(2-Chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)ethenyl)-1,3,4-oxadiazol-2-yl)benzonitrile
      DescriptionA cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50 = 33 and 26 nM, respectively, in TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax ~300 and 600 nM, respectively). In addition to being more selective over PARP1/2 (IC50 >10 µM vs 116 nM/47 nM with XAV939) than the nicotinamide site-targeting XAV939 (Cat. No. 575545), G007-LK is also shown to display little or no inhibitory potency (IC50 >10 µM) toward 5 other PARP enzymes (PARP3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50 >10 µM). Wnt signaling inhibition upon G007-LK treatment in 11 APC (Adenomatous polyposis coli/deleted in polyposis 2.5/DP2.5) mutatant CRC (colorectal cancer) lines ranges from no effect to varying degrees of partial blockages that do not correlate with the observed CRC colony formation inhibitions.Two CRC lines, COLO-320DM & SW403, whose colony formation are affected by G007-LK in vitro (by 70% and 27%, respectively, at 200 nM in 7 to 13 d) are also inhibited by G007-LK for their tumor expansion in mice in vivo (by 47% and 42%, respectively, on d21; 20 mg/kg per daily i.p.), while G007-LK toxicity is observed at high dosages in mice (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.) due to small intestine damage as a result of on-target wnt signaling inhibition in normal tissue. Exhibits favorable pharmacokinetic properties in mice when administered via i.p. ( Plasma t1/2 ≥2.73 h; Cmax ≥2.358 µg/mL; 5 mg/kg) or p.o. ( Plasma t1/2 ≥2.8 h; Cmax ≥871 ng/mL; 5 mg/kg).
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1380672-07-0
      Chemical formulaC₂₅H₁₆ClN₇O₃S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (25 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesLau, T., et al. 2013. Cancer Res. 73, 3132.
      Voronkov, A., et al. 2013. J. Med. Chem. 56, 3012.