Art. -Nr.: HY-145964

INE963

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INE963 is a potent and fast-acting blood-stage antimalarial agent, with an EC₅₀s of 3-6 nM. INE963 is potential for single-dose cures in uncomplicated malaria.

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Reinheit: 99.58%
CAS. Nr.: 2640567-43-5
Formel: C₁₉H₂₆N₆O₂S
Molecular Weight:402.51

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

INE963 Chemical Structure

CAS. Nr.: 2640567-43-5

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

INE963 is a potent and fast-acting blood-stage antimalarial agent, with an EC₅₀s of 3-6 nM. INE963 is potential for single-dose cures in uncomplicated malaria^[1].

IC₅₀ & Target

Plasmodium

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	CC₅₀	6.7 μM Compound: 1; INE963	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 35229610]
K562	CC₅₀	6 μM Compound: 1; INE963	Cytotoxicity against human K562 cells assessed as inhibition of cell growth Cytotoxicity against human K562 cells assessed as inhibition of cell growth	[PMID: 35229610]
MT4	CC₅₀	4.9 μM Compound: 1; INE963	Cytotoxicity against human MT4 cells assessed as inhibition of cell growth Cytotoxicity against human MT4 cells assessed as inhibition of cell growth	[PMID: 35229610]

In Vitro

INE963 inhibits Plasmodium falciparum Pf 3D7 blood stage with EC₅₀ of 3-6 nM. INE963 inhibits P. falciparum and P. vivax Brazilian isolates with EC₅₀s of 2 nM and 3 nM. INE963 inhibits P. falciparum Uganda isolates with EC₅₀ of 0.4 nM^[1].
INE963 inhibits human kinase Haspin, FLT3 with IC₅₀s of 5.5 μM and 3.6 μM. INE963 exhibits cytotoxicity in cells HepG2, K562, MT4 with CC₅₀s of 6.7 μM, 6.0 μM and 4.9 μM, respectively^[1].

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

In Vivo

INE963 (30 mg/kg, po, 4 doses) exhibits anti-malarial activity in P. falciparum-infected mouse models^[1].

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

Animal Model:

P. falciparum-infected mouse models^[1]
Dosage:

30 mg/kg
Administration:

po, 4 doses
Result:

Caused 99% parasitemia reduction.

Clinical Trial

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

Chemical Information

CAS. Nr. 2640567-43-5
Appearance Solid
Molecular Weight 402.51
Formel C₁₉H₂₆N₆O₂S
Color White to off-white
SMILES

OC1(CCN(CC1)C2=NN3C(S2)=NC=C3C4=C(OC)N=C(C(C)C)C=C4)CN
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (248.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.4844 mL

12.4221 mL

24.8441 mL

5 mM

0.4969 mL

2.4844 mL

4.9688 mL

10 mM

0.2484 mL

1.2422 mL

2.4844 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 (protect from light). 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 (6.21 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 (6.21 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 (6.21 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 (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Taft BR, et, al. Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria. J Med Chem. 2022 Mar 10;65(5):3798-3813. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4844 mL	12.4221 mL	24.8441 mL	62.1103 mL
	5 mM	0.4969 mL	2.4844 mL	4.9688 mL	12.4221 mL
	10 mM	0.2484 mL	1.2422 mL	2.4844 mL	6.2110 mL
	15 mM	0.1656 mL	0.8281 mL	1.6563 mL	4.1407 mL
	20 mM	0.1242 mL	0.6211 mL	1.2422 mL	3.1055 mL
	25 mM	0.0994 mL	0.4969 mL	0.9938 mL	2.4844 mL
	30 mM	0.0828 mL	0.4141 mL	0.8281 mL	2.0703 mL
	40 mM	0.0621 mL	0.3106 mL	0.6211 mL	1.5528 mL
	50 mM	0.0497 mL	0.2484 mL	0.4969 mL	1.2422 mL
	60 mM	0.0414 mL	0.2070 mL	0.4141 mL	1.0352 mL
	80 mM	0.0311 mL	0.1553 mL	0.3106 mL	0.7764 mL
	100 mM	0.0248 mL	0.1242 mL	0.2484 mL	0.6211 mL

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INE963

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Antiparasitic Compound library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

INE963

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Antiparasitic Compound library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

INE963 Related Classifications

HY-145964 Related Classifications