Art. -Nr.: HY-119307

Apratastat

(Synonyms: TMI-005)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC). Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Reinheit: 99.28%
CAS. Nr.: 287405-51-0
Formel: C₁₇H₂₂N₂O₆S₂
Molecular Weight:414.50

Speicherung:

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

Apratastat Chemical Structure

CAS. Nr.: 287405-51-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC)^[1]^[2]. Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

MMP

Alle MMP Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Apratastat (10 μM, 24 hours) inhibits expression of pro-inflammatory cytokines TNF-α and IL-6 in lung tissue samples^[3].
Apratastat (10 μM, 24 hours) reduces ADAM17 activity and MCAM release in HUVEC^[4].

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

Western Blot Analysis^[4]

Cell Line:

HUVEC (human umbilical vein endothelial cells)
Concentration:

10 μM
Incubation Time:

24 hours
Result:

Significantly inhibited ADAM17 at the protein level.

Real Time qPCR^[3]

Cell Line:

Lung tissue samples
Concentration:

10 μM
Incubation Time:

24 hours
Result:

Significantly reduced mRNA levels of TNF-α and IL-6.

In Vivo

Apratastat (10 mg/kg, i.p., administered twice at 4 and 16 hours post-induction) alleviats lung inflammation induced by Poly(I ) (HY-119307) and SARS-CoV-2 RBD-S protein in C57BL/6 mice^[3].
Apratastat (10 mg/kg, p.o., once daily for 14 days) exhibits anti-tumor and anti-angiogenic activity in the MC38 xenograft C57BL/6 mouse model^[4].

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

Animal Model:

Poly(I ) (HY-107202) and SARS-CoV-2 RBD-S protein-induced lung inflammation model in C57BL/6 mice^[3]
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection (i.p.), administered twice at 4 and 16 hours post-surgery
Result:

Significantly reduced neutrophil and macrophage numbers in lung tissue, improved lung tissue morphology.

Animal Model:

MC38 colorectal cancer cell xenograft model in C57BL/6 mice^[4]
Dosage:

10 mg/kg
Administration:

Oral gavage (p.o.), once daily for 14 days
Result:

Significantly inhibited tumor growth, reduced tumor angiogenesis and lymphangiogenesis.

Clinical Trial

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

Chemical Information

CAS. Nr. 287405-51-0
Appearance Solid
Molecular Weight 414.50
Formel C₁₇H₂₂N₂O₆S₂
Color White to off-white
SMILES

CC1(C)[C@H](C(NO)=O)N(S(=O)(C2=CC=C(OCC#CCO)C=C2)=O)CCS1
Synonyms

TMI-005
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

Publications (4)

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Journal Impact Factor

Signal Transduct Target Ther

Targeting a disintegrin and metalloprotease (ADAM) 17-CD122 axis enhances CD8+ T cell effector differentiation and anti-tumor immunity. [Abstract]

2024 Jun 26;9(1):152. PMID: 38918390
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
bioRxiv

Omicron Spike confers enhanced infectivity and interferon resistance to SARS-CoV-2 in human nasal tissue. [Abstract]

2023 Oct 12:2023.05.06.539698. PMID: 37425811

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (241.25 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

2.4125 mL

12.0627 mL

24.1255 mL

5 mM

0.4825 mL

2.4125 mL

4.8251 mL

10 mM

0.2413 mL

1.2063 mL

2.4125 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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Shu C, et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J Clin Pharmacol. 2011 Apr;51(4):472-81. [Content Brief]

[2]. Ieguchi K, et al. Savior or not: ADAM17 inhibitors overcome radiotherapy-resistance in non-small cell lung cancer. J Thorac Dis. 2016 Aug;8(8):E813-5. [Content Brief]

[3]. Lartey NL, et al. ADAM17/MMP inhibition prevents neutrophilia and lung injury in a mouse model of COVID-19. J Leukoc Biol. 2022 Jun;111(6):1147-1158. [Content Brief]

[4]. Stalin J, et al. Targeting of the NOX1/ADAM17 Enzymatic Complex Regulates Soluble MCAM-Dependent Pro-Tumorigenic Activity in Colorectal Cancer. Biomedicines. 2023 Nov 30;11(12):3185. [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	2.4125 mL	12.0627 mL	24.1255 mL	60.3136 mL
	5 mM	0.4825 mL	2.4125 mL	4.8251 mL	12.0627 mL
	10 mM	0.2413 mL	1.2063 mL	2.4125 mL	6.0314 mL
	15 mM	0.1608 mL	0.8042 mL	1.6084 mL	4.0209 mL
	20 mM	0.1206 mL	0.6031 mL	1.2063 mL	3.0157 mL
	25 mM	0.0965 mL	0.4825 mL	0.9650 mL	2.4125 mL
	30 mM	0.0804 mL	0.4021 mL	0.8042 mL	2.0105 mL
	40 mM	0.0603 mL	0.3016 mL	0.6031 mL	1.5078 mL
	50 mM	0.0483 mL	0.2413 mL	0.4825 mL	1.2063 mL
	60 mM	0.0402 mL	0.2010 mL	0.4021 mL	1.0052 mL
	80 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7539 mL
	100 mM	0.0241 mL	0.1206 mL	0.2413 mL	0.6031 mL

Keywords

Apratastat

4 Cited Publications

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Apratastat

Differentiation Inducing Compound Library

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Anti-Cancer Compound Library

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Publications Citing Use of MedChemExpress (MCE) Apratastat

Alle MMP Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Apratastat Related Classifications

HY-119307 Related Classifications