Art. -Nr.: HY-13731

PPI-2458

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PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.67%
CAS. Nr.: 431077-35-9
Formel: C₂₂H₃₆N₂O₆
Molecular Weight:424.53

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PPI-2458 Chemical Structure

CAS. Nr.: 431077-35-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research^[1]^[2].

Alle MetAP Isoform-spezifische Produkte anzeigen :

In Vitro

PPI-2458 potently inhibits HUVEC proliferation with a GI₅₀ of 0.2 nM and a maximum inhibition of >95% at 1 nM^[1].
PPI-2458 (0-100 nM, 6 days) inhibits proliferation and MetAP-2 in SU-DHL-16 cells^[2].

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

Cell Proliferation Assay^[2]

Cell Line:

SU-DHL-16 cells
Concentration:

0, 0.01, 0.1, 1, 10, and 100 nM
Incubation Time:

6 days
Result:

Inhibited SU-DHL-16 proliferation in a dose-dependent fashion with maximum inhibition of 60% achieved at the highest concentration (100 nmol/L) and GI₅₀ at 1.9 nmol/L.

In Vivo

PPI-2458 (0-50 mg/kg, Orally, qod) reverses joint swelling and inflammation in the PG-PS (25 mg/kg, i.p.)-induced arthritis model^[1].
PPI-2458 (0-3 mg/kg, Nasogastric intubation, qod) shows a decrease in germinal center lymphocytes in experimentally naive cynomolgus monkeys^[2].
PPI-2458 (0-100 mg/kg, Orally, qod) significantly suppresses tumor growth in a dose-dependent manner in severe combined immunodeficient mice with SR tumor xenografts ^[2].

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

Animal Model:

Female Lewis rats (101–121 g, PG-PS (25 mg/kg, i.p.)-induced arthritis model)^[1]
Dosage:

0.25, 1, 5, and 50 mg/kg
Administration:

Orally (po), started at day 15 after the chronic destructive phase of the disease was established and terminated on day 31
Result:

Significantly and dose-dependently attenuated the chronic inflammatory response. Markedly attenuated paw swelling in a dose-dependent manner with maximal protection at an orally administered dose of 50 mg/kg at day 31.

Animal Model:

Forty-two experimentally naive cynomolgus monkeys^[2]
Dosage:

0.1 mg/kg (three males and three females), 0.3 mg/kg (three males and three females), 1.0 mg/kg (five males and five females), and 3.0 mg/kg (five males and five females)
Administration:

Nasogastric intubation every other day (QOD) for 13 days (total of seven treatments)
Result:

Exhibited a marked decrease in germinal center lymphocytes.

Animal Model:

60 female Fox Chase severe combined immunodeficient mice (SR lymphoma cells were injected s.c. above the right hind leg)^[2]
Dosage:

10, 30, or 100 mg/kg
Administration:

oral gavage, QOD
Result:

Significantly suppressed tumor growth in a dose-dependent manner. PPI-2458 administered at 100 mg/kg produced the greatest degree of tumor growth inhibition, which was 57% (P < 0.001) at the end of the study.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 431077-35-9
Appearance Solid
Molecular Weight 424.53
Formel C₂₂H₃₆N₂O₆
Color White to off-white
SMILES

O=C(O[C@H](CC1)[C@@H](OC)[C@H]([C@@]2(C)O[C@@H]2C/C=C(C)\C)[C@]31CO3)N[C@@H](C(N)=O)C(C)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (235.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3555 mL

11.7777 mL

23.5555 mL

5 mM

0.4711 mL

2.3555 mL

4.7111 mL

10 mM

0.2356 mL

1.1778 mL

2.3555 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

Verweise

[1]. Bernier SG, et al. A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis. Proc Natl Acad Sci U S A. 2004 Jul 20;101(29):10768-73. [Content Brief]

[2]. Cooper AC, et al. A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo. Clin Cancer Res. 2006 Apr 15;12(8):2583-90. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3555 mL	11.7777 mL	23.5555 mL	58.8887 mL
	5 mM	0.4711 mL	2.3555 mL	4.7111 mL	11.7777 mL
	10 mM	0.2356 mL	1.1778 mL	2.3555 mL	5.8889 mL
	15 mM	0.1570 mL	0.7852 mL	1.5704 mL	3.9259 mL
	20 mM	0.1178 mL	0.5889 mL	1.1778 mL	2.9444 mL
	25 mM	0.0942 mL	0.4711 mL	0.9422 mL	2.3555 mL
	30 mM	0.0785 mL	0.3926 mL	0.7852 mL	1.9630 mL
	40 mM	0.0589 mL	0.2944 mL	0.5889 mL	1.4722 mL
	50 mM	0.0471 mL	0.2356 mL	0.4711 mL	1.1778 mL
	60 mM	0.0393 mL	0.1963 mL	0.3926 mL	0.9815 mL
	80 mM	0.0294 mL	0.1472 mL	0.2944 mL	0.7361 mL
	100 mM	0.0236 mL	0.1178 mL	0.2356 mL	0.5889 mL

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PPI-2458

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Metabolic Enzyme Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle MetAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PPI-2458

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Metabolic Enzyme Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle MetAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PPI-2458 Related Classifications

HY-13731 Related Classifications