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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.58%
- No. CAS: 2640567-43-5
- Fòrmula: C19H26N6O2S
- Peso molecular:402.51
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Almacenamiento:
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]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
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Plasmodium |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | CC50 |
6.7 μM
Compound: 1; INE963
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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
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[PMID: 35229610] |
| K562 | CC50 |
6 μM
Compound: 1; INE963
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Cytotoxicity against human K562 cells assessed as inhibition of cell growth
Cytotoxicity against human K562 cells assessed as inhibition of cell growth
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[PMID: 35229610] |
| MT4 | CC50 |
4.9 μM
Compound: 1; INE963
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Cytotoxicity against human MT4 cells assessed as inhibition of cell growth
Cytotoxicity against human MT4 cells assessed as inhibition of cell growth
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[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.
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Animal Model:P. falciparum-infected mouse models[1]
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Dosage:30 mg/kg
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Administration:po, 4 doses
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Result:Caused 99% parasitemia reduction.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2640567-43-5
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Appearance Solid
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Peso molecular 402.51
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Fòrmula C19H26N6O2S
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Color White to off-white
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SMILES
OC1(CCN(CC1)C2=NN3C(S2)=NC=C3C4=C(OC)N=C(C(C)C)C=C4)CN
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureza y Documentación
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Ficha de datos (275 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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
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