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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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CAS No.: 2494082-34-5
Formule: C₁₅H₉F₅N₂O₃
Masse moléculaire:360.24

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

PTG-0861 Chemical Structure

CAS No.: 2494082-34-5

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

HDAC6

5.92 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform HDAC :

Cellular Effect

Cell Line	Type	Value	Description	References
Fibroblast	IC₅₀	11.5 μM Compound: 54; PTG-0861	Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Fibroblast	IC₅₀	14.6 μM Compound: 54; PTG-0861	Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
HUVEC	IC₅₀	10.3 μM Compound: 54; PTG-0861	Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
MM1.S	IC₅₀	1.9 μM Compound: 54; PTG-0861	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	[PMID: 32615502]
MV4-11	IC₅₀	1.85 μM Compound: 1	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	[PMID: 34101461]
MV4-11	IC₅₀	1.85 μM Compound: 54; PTG-0861	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	[PMID: 32615502]
RPMI-8226	IC₅₀	4.94 μM Compound: 54; PTG-0861	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	[PMID: 32615502]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.1-5 μM
Incubation Time:

6 hours
Result:

Induced the accumulation of acetylated a-tubulin expression at 500 nM.

Immunofluorescence^[1]

Cell Line:

HeLa cells
Concentration:

0-2 μM
Incubation Time:

6 hours
Result:

Increased levels of acetylated a-tubulin at 0.1 μM.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0-4 μM
Incubation Time:

18 hours
Result:

Induced about 18% cells late apoptosis at 4 μM while at low dose 0.25 μM only about 5%.

Cell Cytotoxicity Assay^[1]

Cell Line:

Hematological cancer cell lines MV4-11, MM.1S, and RPMI 8226
Concentration:

1.24-4.94 μM
Incubation Time:

72 hours
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.

Cell Line:
Concentration:
Incubation Time:

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

In Vivo

PTG-0861 (compound 54) (oral administration, 20 mg/kg, everyday, 5 days) has no effect on weight and no obvious toxicity in CD1 mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CD1 mice^[1]
Dosage:

20 mg/kg
Administration:

Oral administration; everyday; 5 days
Result:

No weight loss in mice and no obvious toxicity.

Animal Model:

Male CD1 mice^[1]
Dosage:

20 mg/kg
Administration:

Intraperitoneal injection; once
Result:

The pharmacokinetic parameters of PTG-0861 in vivo

Parameter PTG-0861

half-life 0.25 h

C_max 526 ng/mL

AUC_last 190 h∗ng/mL

AUC_inf 219 h∗ng/mL

AUC Extr(%) 0.324

MRT(h) 0.350

AUC/D(h∗mg/mL) 9.5

Chemical Information

CAS No. 2494082-34-5
Masse moléculaire 360.24
Formule C₁₅H₉F₅N₂O₃
SMILES

O=C(NCC1=CC=C(C(NO)=O)C=C1)C2=C(F)C(F)=C(F)C(F)=C2F
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Justyna M Gawel，et al. PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia. Eur J Med Chem. 2020 Sep 1;201:112411. [Content Brief]

Calculators

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Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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Parameter	PTG-0861
half-life	0.25 h
C_max	526 ng/mL
AUC_last	190 h∗ng/mL
AUC_inf	219 h∗ng/mL
AUC Extr(%)	0.324
MRT(h)	0.350
AUC/D(h∗mg/mL)	9.5