Senexin C
Based on 1 Customer Validation
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability.
For research use only. We do not sell to patients.
- Purity: 99.19%
- CAS No.: 2375554-02-0
- Formula: C28H27N5O
- Molecular Weight:449.55
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
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CDK8/CycC 3.6 nM (IC50) |
CDK19/CycC 2.9 nM (Kd) |
CDK8/CycC 1.4 nM (Kd) |
Senexin C (compound 20a) exhibits potent CDK8/19 inhibitory activity with high selectivity (IC50s of 56 and 108 nM for 293-NFκB-Luc and MV4-11-Luc cells, respectively)[1].
Senexin C (2 μM) shows potency in different kinase assays (IC50= 3.6 nM for CD8/CycC, Kd=1.4 nM for CD8/CycC, Kd=2.9 nM for CDK19/CycC)[1].
Senexin C (1 μM, 3 h) shows inhibition on CDK8/19 dependent cellular gene expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:293 cells
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Concentration:1 µM
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Incubation Time:3 h
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Result:Showed inhibition on CDK8/19 dependent cellular gene expression.
Senexin C (40 mg/kg; p.o.; twice daily for 4 weeks) suppresses the systemic growth of MV4-11 AML with good tolerability[1]. Pharmacokinetic Parameters of Senexin C in eight-week-old female Balb/c mice[1].
| parameters | iv (2.5 mg/kg) | po (100 mg/kg) | ||
| plasma | tumor | plasma | tumor | |
| C0 (μg/mL) | 503 | |||
| Kel (h-1) | 0.93 | 0.06 | 0.2 | 0.1 |
| T1/2 (h) | 0.75 | 12.1 | 3.53 | 7.27 |
| Tmax (h) | 0.58 | 12 | 12 | |
| Cmax (ng/mL or ng/g) | 488 | 144 | 5728 | |
| AUC0-24 h (ng x h/ml or ng x h/g) | 331 | 6408 | 2182 | 88,600 |
| F% | 16.5% | 34.6% | ||
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:eight-week-old female Balb/c mice ( CT26 tumor mode)[1]
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Dosage:2.5 mg/kg (10 mL/kg of 2.5 mg/mL Senexin C solution in 5% dextrose), 100 mg/kg (10 mL/kg of 10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle)
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Administration:2.5 mg/kg, i.v.; 100 mg/kg, p.o.
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Result:Showed good oral bioavailability.
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Animal Model:eight-week-old female NSG mice ( AML model)[1]
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Dosage:40 mg/kg
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Administration:p.o.; twice daily, 4 weeks
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Result:Suppressed the systemic growth of MV4-11 AML with good tolerability.
Chemical Information
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CAS No. 2375554-02-0
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Appearance Solid
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Molecular Weight 449.55
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Formula C28H27N5O
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Color Off-white to light yellow
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SMILES
N#CC1=CC=C2N=CC=C(NCCC3=CC=C4C=C(C(N5CCN(C)CC5)=O)C=CC4=C3)C2=C1
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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 : 33.33 mg/mL (74.14 mM; ultrasonic and warming and heat to 160°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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.56 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (276 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 | 2.2244 mL | 11.1222 mL | 22.2445 mL | 55.6112 mL |
| 5 mM | 0.4449 mL | 2.2244 mL | 4.4489 mL | 11.1222 mL | |
| 10 mM | 0.2224 mL | 1.1122 mL | 2.2244 mL | 5.5611 mL | |
| 15 mM | 0.1483 mL | 0.7415 mL | 1.4830 mL | 3.7074 mL | |
| 20 mM | 0.1112 mL | 0.5561 mL | 1.1122 mL | 2.7806 mL | |
| 25 mM | 0.0890 mL | 0.4449 mL | 0.8898 mL | 2.2244 mL | |
| 30 mM | 0.0741 mL | 0.3707 mL | 0.7415 mL | 1.8537 mL | |
| 40 mM | 0.0556 mL | 0.2781 mL | 0.5561 mL | 1.3903 mL | |
| 50 mM | 0.0445 mL | 0.2224 mL | 0.4449 mL | 1.1122 mL | |
| 60 mM | 0.0371 mL | 0.1854 mL | 0.3707 mL | 0.9269 mL |
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