SLC-391
SLC-391 is an orally active AXL kinase inhibitor with an IC50 of 9.6 nM against AXL kinase. SLC-391 inhibits Gas6-induced AXL-dependent phosphorylation of Akt. SLC-391 inhibits SARS-CoV-2 infection, entry and replication in cells. SLC-391 suppresses cancer cell proliferation. SLC-391 inhibits tumor growth in mouse solid tumor xenograft models. SLC-391 can be used for the research of COVID-19, influenza virus infection, triple-negative breast cancer, chronic myeloid leukemia and non-small cell lung cancer.
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- CAS No.: 1783825-18-2
- 화학식: C19H23N7O
- 분자량:365.43
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
SLC-391 is a potent and specific AXL inhibitor (IC50 for AXL is 9.6 nM, while IC50 values for TYRO3 and MER are 42.3 nM and 63.5 nM, respectively). SLC-391 also exhibits good selectivity for TAM kinases compared to other tyrosine kinases[1].
SLC-391 (0-1 μM; 0-72 h) inhibits SARS-CoV-2 infection of Vero E6 cells in a dose-dependent manner[1].
SLC-391 (0-1.5 μM; 58 h) dose-dependently blocks the binding of SARS-CoV-2 spike protein to ACE2[1].
SLC-391 (0-10 μM, 4 days) protects RPMI2650 cells from cytopathic effects induced by human influenza virus, with an EC50 of 0.14 μM, a TC50 >10 μM, and a TI greater than 71.4[1].
SLC-391 (0.003-10 μM; 4 days) reduces human influenza virus yields in RPMI2650 cells in a concentration-dependent manner in vitro, with reductions of 952.9-fold, 74.9-fold, and 34.8-fold at concentrations of 10 μM, 0.4 μM, and 0.003 μM, respectively[1].
SLC-391 inhibits Gas6-induced AXL-dependent Akt phosphorylation in human non-small cell lung cancer A549 cells with an IC50 of 0.29 μM[1].
SLC-391 inhibits the proliferation of AXL-expressing 4T1 cells (IC50 1.05 μM) and K562 cells (IC50 3.45 μM)[1].
SLC-391 (1 μM) completely inhibits the anchorage-independent proliferation of human non-small cell lung cancer A549 cells[1].
SLC-391 (0.2 μM) inhibits the invasive ability of human non-small cell lung cancer A549 cells by approximately 75%[1].
SLC-391 increases the number of natural killer cells, elevates the M1/M2 macrophage polarization ratio, subsequently increases the CD8+ T cell/regulatory T cell ratio, and reduces the number of immunosuppressive myeloid cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vero E6 cells
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Concentration:0, 0.01, 0.1, 1 μM
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Incubation Time:0, 24, 72 h
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Result:Inhibited SARS-CoV-2 infection in a dose-dependent manner, as indicated by increased qPCR cycle counts.
Effectively inhibited viral infection at 0.01 μM for 24 hours.
Maintained a high degree of viral inhibition at 1 μM for up to 72 hours.
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Cell Line:RPMI2650 cells
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Concentration:0, 0.003, 0.02, 0.08, 0.4, 2, 10 μM
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Incubation Time:4 days
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Result:Exhibited cytoprotective effects against Flu A-induced cytopathic effects, with an EC50 of 0.14 μM.
Showed no significant cytotoxicity up to 10 μM, with a TC50 >10 μM, resulting in a therapeutic index above 71.4.
SLC-391 (50 mg/kg; oral administration) inhibited the growth of CT-26 tumors in mice by 37%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:50 mg/kg; 75 mg/kg
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Administration:p.o.; twice daily
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Result:Achieved 60% tumor growth inhibition (TGI).
Achieved 67% tumor growth inhibition (TGI).
Reduced levels of phosphorylated Akt in tumor xenograft samples by 41%.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1783825-18-2
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분자량 365.43
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화학식 C19H23N7O
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SMILES
NC1=C(C=C(C2=CN(C3CCNCC3)N=C2)C=N1)C4=NN=C(CC5CC5)O4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- SLC-391
- 1783825-18-2
- SLC391
- SLC 391
- TAM Receptor
- SARS-CoV
- Akt
- Gas6
- CHO-hACE2 cells
- severe acute respiratory syndrome (SARS)
- influenza virus
- SARS-CoV-2
- Vero E6 cells
- ACE2
- middle east respiratory syndrome (MERS)
- AXL kinase
- COVID-19
- triple-negative breast cancer
- chronic myeloid leukemia
- non-small cell lung cancer
- CD-1 mice
- Inhibitor
- inhibitor
- inhibit