XAV939A potent inhibitor of beta-catenin, TNKS1, and TNKS2

XAV939 (CAS 284028-89-3)

XAV939 | CAS 284028-89-3 is rated 5.0 out of 5 by 1.
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Synonym: 3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
Application: A potent inhibitor of beta-catenin, TNKS1, and TNKS2
CAS Number: 284028-89-3
Purity: ≥98%
Molecular Weight: 312.31
Molecular Formula: C14H11F3N2OS
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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XAV939 is a potent, small molecule inhibitor of tankyrase 1 (TNKS) (IC50 = 11 nM) and tankyrase 2 (IC50 = 4 nM). By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells. At concentrations as low as 0.3 μM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.


References

1. Smith, S., et al., 1998. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science (New York, N.Y.). 282(5393): 1484-7. PMID: 9822378
2. Huang, Shih-Min A., et al., 2009. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 461(7264): 614-20. PMID: 19759537

Physical State :
Solid
Solubility :
Soluble in 1:5 EtOH:PBS (pH 7.2) (~0.15 mg/ml), DMSO (~2 mg/ml), DMF (~5 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C.
Storage :
Store at -20° C
Melting Point :
207.14° C (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
Tankyrase 1: IC50 = 11 nM; Tankyrase 2: IC50 = 4 nM; Protein Wnt-3a: IC50 = 51 nM (human); Catenin beta-1: IC50 = 51 nM (human)
pK Values :
pKb: 7.10 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
Transport :
UN 2811, Class 6.1, Packing group III
PubChem CID :
2726824
MDL Number :
MFCD16879017
EC Number :
206-765-9
SMILES :
C1CSCC2=C1NC(=NC2=O)C3=CC=C(C=C3)C(F)(F)F

Download SDS (MSDS)

Certificate of Analysis

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XAV939  Product Citations

See how others have used XAV939. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 16 total

PMID: # 31116975  2019. Cell Rep. 27: 2281-2291.e5.

PMID: # 31586036  2019. J. Immunol.

PMID: # 29197497  Cheng, Y. et al. 2018. Life Sci. 192: 183-189.

PMID: # 30240284  2018. Epigenetics. 13: 1013-1026.

PMID: # 28750181  2018. Connect. Tissue Res. 59: 245-254.

PMID: # 29345284  Li, L. et al. 2018. Int. J. Oncol. 52: 473-484.

PMID: # 29934219  2018. Bioorg. Med. Chem. 26: 3953-3957.

PMID: # 27709831  2017. J. Cell. Mol. Med. 21: 568-578.

PMID: # 29088702  Hangauer, MJ. et al. 2017. Nature. 551: 247-250.

PMID: # 26940070  Yong, X. et al. 2016. Cancer letters. 374: 292-303.

Citations 1 to 10 of 16 total

What is the appearance of the compound?

Asked by: two2igm05
Thank your for your question. XAV939, sc-296704, is in white powder form.
Answered by: Chemical Support 4
Date published: 2017-03-03
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Rated 5 out of 5 by from An increase in Tankyrase 1/2 protein expression An increase in Tankyrase 1/2 protein expression was observed by WB in SW480 cells post treatment with XAV939. -SCBT QC
Date published: 2015-04-16
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