Details
Stereochemistry | ACHIRAL |
Molecular Formula | C14H11F3N2OS |
Molecular Weight | 312.31 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)C1=CC=C(C=C1)C2=NC(=O)C3=C(CCSC3)N2
InChI
InChIKey=KLGQSVMIPOVQAX-UHFFFAOYSA-N
InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)
Molecular Formula | C14H11F3N2OS |
Molecular Weight | 312.31 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/19759537
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19759537
XAV-939 was discovered as a selectively inhibitor of Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition, regulates axin levels and does not affect CRE, NF-κB or TGF-β. Wnt/b-catenin pathway has been implicated in many cancers.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19759537
Curator's Comment: # Novartis Institutes for Biomedical Research
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL6164 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19759537 |
11.0 nM [IC50] | ||
Target ID: CHEMBL6154 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19759537 |
4.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28240680
SH-SY5Y cells, was inhibited by XAV939. XAV939 treatment led to the reduction of β-catenin within the cells, confirming its inhibitory effect of WNT. The inhibition of WNT signaling by XAV939 did not affect cell morphology, survival, and proliferation; however, the differentiation and sensitivity to anticancer drugs of human neuroblastoma cells were altered. The treatment of XAV939 resulted in the downregulation of mature neuronal markers, including β-tubulin III, PHOX2A, and PHOX2B, whereas neural progenitor markers (PAX6, TFAP2α, and SLUG) were upregulated.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 20:19:51 GMT 2023
by
admin
on
Sat Dec 16 20:19:51 GMT 2023
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Record UNII |
G2MY39VR77
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Record Status |
Validated (UNII)
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Record Version |
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-
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Created by
admin on Sat Dec 16 20:19:52 GMT 2023 , Edited by admin on Sat Dec 16 20:19:52 GMT 2023
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G2MY39VR77
Created by
admin on Sat Dec 16 20:19:52 GMT 2023 , Edited by admin on Sat Dec 16 20:19:52 GMT 2023
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |
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