INE963
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.58%
- CAS No.: 2640567-43-5
- Formule: C19H26N6O2S
- Masse moléculaire:402.51
-
Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
Anti-Infection Compound Library
HY-L002
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Clinical Compound Library
HY-L026
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
Orally Active Compound Library
HY-L061
-
Anti-Blood Cancer Compound Library
HY-L079
-
Antiparasitic Compound library
HY-L082
-
Protein-protein Interaction Inhibitor Library
HY-L109
-
Heterocyclic Compound Library
HY-L138
-
Membrane Protein-targeted Compound Library
HY-L149
-
Cytokine Inhibitors Library
HY-L161
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Hematopathy Compound Library
HY-L171
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
Anti-Aging Compound Library Mini
HY-L034M
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
Voir tous les produits spécifiques à Isoform Parasite
More
Activité biologique
|
Plasmodium |
|
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] |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2640567-43-5
-
Appearance Solid
-
Masse moléculaire 402.51
-
Formule 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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
-
Fiche technique (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)
-
Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
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.
| 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 |
INE963 Related Classifications
HY-145964 Related Classifications
Powered by Bioz