HTH-01-091 TFA
Based on 1 Customer Validation
HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research.
For research use only. We do not sell to patients.
- Purity: 98.01%
- Formula: C28H29Cl2F3N4O4
- Molecular Weight:613.46
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
IC50: 10.5 nM (MELK), 41.8 nM (DYRK3), 42.5 nM (RIPK2), 60.6 nM (PIM1), 108.6 nM (smMLCK), 632 nM (mTOR), 962 nM (PIK3CA), 1230 nM (CDK7), 1740 nM (GSK3A)[1]
HTH-01-091 (1 μM) TFA selectively inhibits 4% of the kinases over 90%[1].
HTH-01-091 (0-10 μM, 1 h) TFA is cell permeable and causes MELK degradation[1].
HTH-01-091 (0-10 μM, 3 day) TFA exhibits minor antiproliferative effects in breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells
-
Concentration:0, 0.001, 0.01, 0.1, 1.0, and 10 μM
-
Incubation Time:3 day
-
Result:Showed antiproliferative activities in a panel of breast cancer cell lines, including MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells, with IC50 values of 4.00 μM, 6.16 μM, 8.80 μM, >10 μM, 8.75 μM, and 3.87 μM, respectively.
-
Cell Line:MDA-MB-468 cells
-
Concentration:0, 0.1, 1.0, and 10 μM
-
Incubation Time:1 h
-
Result:Reduced MELK protein levels in MDA-MB-468 cells; Dose-dependently decreased MELK pull-down by streptavidin beads, demonstrating that the compound is cell permeable and binds to MELK in an ATP-competitive fashion. Had no effect on ERK1/2 pull-down, showing no binding affinity of HTH-01-091 to ERK1/2.
Chemical Information
-
Appearance Solid
-
Molecular Weight 613.46
-
Formula C28H29Cl2F3N4O4
-
Color Light yellow to yellow
-
SMILES
O=C1N([C@H]2CC[C@H](CN(C)C)CC2)C3=C(CN1)C=NC4=CC=C(C5=CC(Cl)=C(O)C(Cl)=C5)C=C34.OC(C(F)(F)F)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (163.01 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: ≥ 2.5 mg/mL (4.08 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 (4.08 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.
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
-
Data Sheet (274 KB)
-
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)
- Portuguese - PT (251 KB)
-
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 | 1.6301 mL | 8.1505 mL | 16.3010 mL | 40.7525 mL |
| 5 mM | 0.3260 mL | 1.6301 mL | 3.2602 mL | 8.1505 mL | |
| 10 mM | 0.1630 mL | 0.8150 mL | 1.6301 mL | 4.0752 mL | |
| 15 mM | 0.1087 mL | 0.5434 mL | 1.0867 mL | 2.7168 mL | |
| 20 mM | 0.0815 mL | 0.4075 mL | 0.8150 mL | 2.0376 mL | |
| 25 mM | 0.0652 mL | 0.3260 mL | 0.6520 mL | 1.6301 mL | |
| 30 mM | 0.0543 mL | 0.2717 mL | 0.5434 mL | 1.3584 mL | |
| 40 mM | 0.0408 mL | 0.2038 mL | 0.4075 mL | 1.0188 mL | |
| 50 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8150 mL | |
| 60 mM | 0.0272 mL | 0.1358 mL | 0.2717 mL | 0.6792 mL | |
| 80 mM | 0.0204 mL | 0.1019 mL | 0.2038 mL | 0.5094 mL | |
| 100 mM | 0.0163 mL | 0.0815 mL | 0.1630 mL | 0.4075 mL |
Powered by Bioz