PTG-0861
PTG-0861 is a selective histone deacetylase 6 (HDAC6) inhibitor with the IC50 value of 5.92 nM. PTG-0861 induces apoptosis and can be used in the study of acute myeloid leukemia, multiple myeloma and other hematological cancers.
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- No. CAS: 2494082-34-5
- Fòrmula: C15H9F5N2O3
- Peso molecular:360.24
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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HDAC6 5.92 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Fibroblast | IC50 |
11.5 μM
Compound: 54; PTG-0861
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Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
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[PMID: 32615502] |
| Fibroblast | IC50 |
14.6 μM
Compound: 54; PTG-0861
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Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
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[PMID: 32615502] |
| HUVEC | IC50 |
10.3 μM
Compound: 54; PTG-0861
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Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
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[PMID: 32615502] |
| MM1.S | IC50 |
1.9 μM
Compound: 54; PTG-0861
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Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
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[PMID: 32615502] |
| MV4-11 | IC50 |
1.85 μM
Compound: 1
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Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
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[PMID: 34101461] |
| MV4-11 | IC50 |
1.85 μM
Compound: 54; PTG-0861
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Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
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[PMID: 32615502] |
| RPMI-8226 | IC50 |
4.94 μM
Compound: 54; PTG-0861
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Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
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[PMID: 32615502] |
PTG-0861 (compound 54) (0.1-5 μM, 6 hours) stimulates the expression of acetylated a-tubulin and has inhibitory activity against HDAC6 with the IC50 value of 0.59 μM[1].
PTG-0861 (compound 54) (0-4 μM, 18 hours) can induce apoptosis in a dose-dependent manner and has some cytotoxic effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:0.1-5 μM
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Incubation Time:6 hours
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Result:Induced the accumulation of acetylated a-tubulin expression at 500 nM.
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Cell Line:HeLa cells
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Concentration:0-2 μM
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Incubation Time:6 hours
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Result:Increased levels of acetylated a-tubulin at 0.1 μM.
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Cell Line:MV4-11 cells
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Concentration:0-4 μM
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Incubation Time:18 hours
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Result:Induced about 18% cells late apoptosis at 4 μM while at low dose 0.25 μM only about 5%.
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Cell Line:Hematological cancer cell lines MV4-11, MM.1S, and RPMI 8226
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Concentration:1.24-4.94 μM
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Incubation Time:72 hours
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Result:Showed cytotoxic effects on MV4-11, MM.1S, and RPMI 8226 with the IC50 value of 1.85 μM，1.9 μM，4.94 μM, respectively.
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Cell Line:
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Concentration:
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Incubation Time:
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Result:Result: The pharmacokinetic parameters of PTG-0861 in vitro
Parameter PTG-0861 Percent Remaining (%) 0 min 100.00 Percent Remaining (%) 30 min 96.41 Percent Remaining (%) 60 min 97.98 Percent Remaining (%) 120 min 97.08 T1/2 (min) ∞ T1/2 (min) 50.85 ± 3.37 CLint (mL/min/106 cells) 27.32 ± 1.81 -Log Pe 5.66 ± 0.02 Papp (A-B) (10 6, cm/s) 1.33 ± 0.03 Papp (B-A) (10 6, cm/s) 0.94 ± 0.13 Efflux Ratio 0.71 ± 0.08
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 mice[1]
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Dosage:20 mg/kg
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Administration:Oral administration; everyday; 5 days
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Result:No weight loss in mice and no obvious toxicity.
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Animal Model:Male CD1 mice[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection; once
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Result:The pharmacokinetic parameters of PTG-0861 in vivo
Parameter PTG-0861 half-life 0.25 h Cmax 526 ng/mL AUClast 190 h∗ng/mL AUCinf 219 h∗ng/mL AUC Extr(%) 0.324 MRT(h) 0.350 AUC/D(h∗mg/mL) 9.5
Chemical Information
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No. CAS 2494082-34-5
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Peso molecular 360.24
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Fòrmula C15H9F5N2O3
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SMILES
O=C(NCC1=CC=C(C(NO)=O)C=C1)C2=C(F)C(F)=C(F)C(F)=C2F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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