BKI-1369
Based on 1 Customer Validation
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.37%
- No. CAS: 1951431-22-3
- Fòrmula: C23H27N7O
- Peso molecular:417.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Help & FAQs
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Actividad biológica
IC50: 1.52 μM (hERG)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | IC50 |
>100 μM
Compound: BKI1369
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Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| HCT-116 | IC50 |
>55.2 μM
Compound: BKI1369
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| HepG2 | GI50 |
>10 μM
Compound: 17
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Growth inhibition of human HepG2 cells after 48 hrs by Alamar blue assay
Growth inhibition of human HepG2 cells after 48 hrs by Alamar blue assay
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[PMID: 27309760] |
| HL-60 | IC50 |
>100 μM
Compound: BKI1369
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Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| K562 | IC50 |
>100 μM
Compound: BKI1369
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Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| LN-229 | IC50 |
45.2 μM
Compound: BKI1369
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Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| NCI-H460 | IC50 |
>100 μM
Compound: BKI1369
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Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
| Z-138 | IC50 |
30.4 μM
Compound: BKI1369
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Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
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[PMID: 32835918] |
Chemical Information
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No. CAS 1951431-22-3
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Appearance Solid
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Peso molecular 417.51
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Fòrmula C23H27N7O
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Color White to off-white
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SMILES
NC1=C2C(N(CC3CCN(C)CC3)N=C2C4=CC=C5N=C(OCC)C=CC5=C4)=NC=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (119.76 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. 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. 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: ≥ 5 mg/mL (11.98 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
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 (272 KB)
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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)
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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. 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 | 2.3952 mL | 11.9758 mL | 23.9515 mL | 59.8788 mL |
| 5 mM | 0.4790 mL | 2.3952 mL | 4.7903 mL | 11.9758 mL | |
| 10 mM | 0.2395 mL | 1.1976 mL | 2.3952 mL | 5.9879 mL | |
| 15 mM | 0.1597 mL | 0.7984 mL | 1.5968 mL | 3.9919 mL | |
| 20 mM | 0.1198 mL | 0.5988 mL | 1.1976 mL | 2.9939 mL | |
| 25 mM | 0.0958 mL | 0.4790 mL | 0.9581 mL | 2.3952 mL | |
| 30 mM | 0.0798 mL | 0.3992 mL | 0.7984 mL | 1.9960 mL | |
| 40 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4970 mL | |
| 50 mM | 0.0479 mL | 0.2395 mL | 0.4790 mL | 1.1976 mL | |
| 60 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9980 mL | |
| 80 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7485 mL | |
| 100 mM | 0.0240 mL | 0.1198 mL | 0.2395 mL | 0.5988 mL |
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