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

Tankyrase 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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: TNKS1/2 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

Primary Target: Tankyrase 1/2
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1380672-07-0C₂₅H₁₆ClN₇O₃S

Products

Catalog NumberPackaging Qty/Pack
5.04907.0001 Glass bottle 10 mg
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
Global Trade Item Number
Catalog Number GTIN
5.04907.0001 04055977263657

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 Protect from light
+2°C to +8°C
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.