CXCR6 antagonist 1
CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin (HY-15371)-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 2579689-85-1
- Formula: C27H30F3N3O4S
- Molecular Weight:549.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CXCR6 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-HEP1 | IC50 |
2.1 μM
Compound: 81
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Inhibition of CXCR6-mediated cell invasion in human SKHEP1 cells after 72 hrs by transwell assay
Inhibition of CXCR6-mediated cell invasion in human SKHEP1 cells after 72 hrs by transwell assay
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[PMID: 31882297] |
CXCR6 antagonist 1 potently inhibits CXCL16-induced β-arrestin recruitment in CXCR6-expressing DiscoveRx cells, with an IC50 of 40 nM[1].
CXCR6 antagonist 1 inhibits Forskolin (HY-15371)-induced cAMP signaling pathway in CXCR6-expressing DiscoveRx cells, with an IC50 of 540 nM[1].
CXCR6 antagonist 1 (72 h) inhibits the migration of hepatocellular carcinoma cell line SK-HEP-1 in a dose-dependent manner, with an IC50 of 2.1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (female)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; daily; Day 4 to Day 30
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Result:Reduced mean excised tumor weight to 59 ± 9 mg (30 mg/kg dose) and 55 ± 24 mg (60 mg/kg dose), with both doses showing significant reduction relative to vehicle control (P < 0.05).
Achieved tumor growth inhibition comparable to positive control cyclophosphamide.
Caused no deaths, behavioral phenotypes, or distinct body weight differences relative to control.
Chemical Information
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CAS No. 2579689-85-1
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Molecular Weight 549.61
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Formula C27H30F3N3O4S
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SMILES
C(N1[C@@]2(C[C@H](NC(=O)C3=CC(OC)=C(OC)C(OC)=C3)C[C@]1(CCC2)[H])[H])C4=NC=5C(S4)=CC=CC5C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CXCR6 antagonist 1 Related Classifications
HY-133151 Related Classifications
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