Famlasertib
Based on 1 Customer Validation
Famlasertib is a potent, brain-penetrant MAP4K inhibitor with IC50s value of 0.3 nM, 23.7 nM, and 44.7 nM for HGK (MAP4K4), MLK3, and MLK1, respectively. Famlasertib shows motor neuron protection and anti-inflammatory properties. Famlasertib can be used for the study of amyotrophic lateral sclerosis (ALS).
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2375591-69-6
- Formula: C26H27ClN4O
- Molecular Weight:446.97
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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MAPK Compound Library
HY-L010
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CNS-Penetrant Compound Library
HY-L028
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Oxygen Sensing Compound Library
HY-L045
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Anti-Obesity Compound Library
HY-L087
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Highly Selective Inhibitors Library
HY-L158
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
All MAP4K Isoforms
More
Biological Activity
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MAP4K4 0.3 nM (IC50) |
MLK3 23.7 nM (IC50) |
MLK1 44.7 nM (IC50) |
Famlasertib (Prostetin/12k) rescues Cyclopiazonic acid (HY-N6771)-induced neurodegeneration with an EC50 of 0.1 μM in motor neuron survival assay[1].
Famlasertib significantly decreases TNFα secretion with an EC50 of ~0.47 μM, in Lipopolysaccharides (HY-D1056) (LPS)-stimulated microglia[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.
Chemical Information
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CAS No. 2375591-69-6
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Appearance Solid
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Molecular Weight 446.97
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Formula C26H27ClN4O
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Color White to off-white
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SMILES
OCCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(NC=C4C5=CC(Cl)=CC=C5)N=C3
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Synonyms
Prostetin/12k
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (223.73 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 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (11.19 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation
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Data Sheet (272 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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Handling Instructions (2659 KB)
References
[1]. Bos PH, et al. Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents. Cell Chem Biol. 2019 Dec 19;26(12):1703-1715.e37. [Content Brief]
[2]. Moreno R, et al. The emerging role of mixed lineage kinase 3 (MLK3) and its potential as a target for neurodegenerative diseases therapies. Eur J Med Chem. 2023 Sep 5;257:115511. [Content Brief]
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 | 2.2373 mL | 11.1864 mL | 22.3729 mL | 55.9322 mL |
| 5 mM | 0.4475 mL | 2.2373 mL | 4.4746 mL | 11.1864 mL | |
| 10 mM | 0.2237 mL | 1.1186 mL | 2.2373 mL | 5.5932 mL | |
| 15 mM | 0.1492 mL | 0.7458 mL | 1.4915 mL | 3.7288 mL | |
| 20 mM | 0.1119 mL | 0.5593 mL | 1.1186 mL | 2.7966 mL | |
| 25 mM | 0.0895 mL | 0.4475 mL | 0.8949 mL | 2.2373 mL | |
| 30 mM | 0.0746 mL | 0.3729 mL | 0.7458 mL | 1.8644 mL | |
| 40 mM | 0.0559 mL | 0.2797 mL | 0.5593 mL | 1.3983 mL | |
| 50 mM | 0.0447 mL | 0.2237 mL | 0.4475 mL | 1.1186 mL | |
| 60 mM | 0.0373 mL | 0.1864 mL | 0.3729 mL | 0.9322 mL | |
| 80 mM | 0.0280 mL | 0.1398 mL | 0.2797 mL | 0.6992 mL | |
| 100 mM | 0.0224 mL | 0.1119 mL | 0.2237 mL | 0.5593 mL |
Famlasertib Related Classifications
HY-168972 Related Classifications
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