STK17A/B-IN-1
STK17A/B-IN-1 (compound 9) is an orally active, potent, and selective STK17A/B inhibitor with an IC50 of 23 nM against STK17A. STK17A/B-IN-1 can be used for study of cancer.
For research use only. We do not sell to patients.
- CAS No.: 3002038-21-0
- Formula: C26H27N7O
- Molecular Weight:453.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
99.5 μM
Compound: 9
|
Antiproliferative activity against human HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo luminescence assay
Antiproliferative activity against human HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo luminescence assay
|
[PMID: 38894933] |
| HEL | IC50 |
2.31 μM
Compound: 9
|
Antiproliferative activity against human HEL cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo luminescence assay
Antiproliferative activity against human HEL cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo luminescence assay
|
[PMID: 38894933] |
| Kasumi 1 | IC50 |
7.67 μM
Compound: 9
|
Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo luminescence assay
Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo luminescence assay
|
[PMID: 38894933] |
| MOLM-13 | IC50 |
0.92 μM
Compound: 9
|
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo luminescence assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo luminescence assay
|
[PMID: 38894933] |
Chemical Information
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CAS No. 3002038-21-0
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Molecular Weight 453.54
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Formula C26H27N7O
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SMILES
O=C(C1=CC=C(NC2=NC=CC(C3=CC4=C(N=C(N5CCCC5)N=C4)C=C3)=N2)C=C1)NC(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : 100 mg/mL (220.49 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 6.25 mg/mL (13.78 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (13.78 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
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.
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2049 mL | 11.0244 mL | 22.0488 mL | 55.1219 mL |
| 5 mM | 0.4410 mL | 2.2049 mL | 4.4098 mL | 11.0244 mL | |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2049 mL | 5.5122 mL | |
| 15 mM | 0.1470 mL | 0.7350 mL | 1.4699 mL | 3.6748 mL | |
| 20 mM | 0.1102 mL | 0.5512 mL | 1.1024 mL | 2.7561 mL | |
| 25 mM | 0.0882 mL | 0.4410 mL | 0.8820 mL | 2.2049 mL | |
| 30 mM | 0.0735 mL | 0.3675 mL | 0.7350 mL | 1.8374 mL | |
| 40 mM | 0.0551 mL | 0.2756 mL | 0.5512 mL | 1.3780 mL | |
| 50 mM | 0.0441 mL | 0.2205 mL | 0.4410 mL | 1.1024 mL | |
| 60 mM | 0.0367 mL | 0.1837 mL | 0.3675 mL | 0.9187 mL | |
| 80 mM | 0.0276 mL | 0.1378 mL | 0.2756 mL | 0.6890 mL | |
| 100 mM | 0.0220 mL | 0.1102 mL | 0.2205 mL | 0.5512 mL |