PKMYT1-IN-8
Based on 1 Customer Validation
PKMYT1-IN-8 (Compound 137) is the inhibitor for PKMYT1 with an IC50 of 9 nM. PKMYT1-IN-8 inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2with IC50s of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. PKMYT1-IN-8 inhibits the proliferation of cancer cell OVCAR3 with GI50 of 2.02 μM.
For research use only. We do not sell to patients.
- Purity: 99.31%
- CAS No.: 3065631-84-4
- Formula: C17H16F3N5O2
- Molecular Weight:379.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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PKMYT1 9 nM (IC50) |
Chemical Information
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CAS No. 3065631-84-4
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Appearance Solid
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Molecular Weight 379.34
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Formula C17H16F3N5O2
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Color White to off-white
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SMILES
CC1=NC(C(F)(F)F)=C2C(N(C3=C(C)C=CC(O)=C3C)C(N)=C2C(N)=O)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (131.81 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)
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: ≥ 2.5 mg/mL (6.59 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 (6.59 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.
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
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Data Sheet (281 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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Handling Instructions (2659 KB)
References
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 | 2.6362 mL | 13.1808 mL | 26.3616 mL | 65.9039 mL |
| 5 mM | 0.5272 mL | 2.6362 mL | 5.2723 mL | 13.1808 mL | |
| 10 mM | 0.2636 mL | 1.3181 mL | 2.6362 mL | 6.5904 mL | |
| 15 mM | 0.1757 mL | 0.8787 mL | 1.7574 mL | 4.3936 mL | |
| 20 mM | 0.1318 mL | 0.6590 mL | 1.3181 mL | 3.2952 mL | |
| 25 mM | 0.1054 mL | 0.5272 mL | 1.0545 mL | 2.6362 mL | |
| 30 mM | 0.0879 mL | 0.4394 mL | 0.8787 mL | 2.1968 mL | |
| 40 mM | 0.0659 mL | 0.3295 mL | 0.6590 mL | 1.6476 mL | |
| 50 mM | 0.0527 mL | 0.2636 mL | 0.5272 mL | 1.3181 mL | |
| 60 mM | 0.0439 mL | 0.2197 mL | 0.4394 mL | 1.0984 mL | |
| 80 mM | 0.0330 mL | 0.1648 mL | 0.3295 mL | 0.8238 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.6590 mL |