| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
CLK2 0.096 nM (Kd) CLK4 0.61 nM (Kd) CLK1 4.8 nM (Kd) CLK3 6.5 nM (Kd) DYRK1A 0.074 nM (Kd) DYRK1B 1.5 nM (Kd) DYRK2 32 nM (Kd)
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|---|---|
| ln Vitro |
In a dose-dependent manner, T025 (0-1000 nM; 72 hours) strongly reduces the proliferation of MDA-MB-468 cells[1]. Phosphorylation levels in MDA-MB-468 cells are decreased by T025 (0-1000 nM; 6 hours)[1].
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| ln Vivo |
T025 (50 mg/kg; po; 2, 4, 8 hours) suppresses the phosphorylation of CLK-dependent genes and causes exon skipping in a variety of genes in Balb/c nude mice (7 to 8 week old females)[1]. T025 (50 mg/kg; po; twice daily on two days per week, for three weeks) reduces the formation of tumors in MDA-MB-468 xenograft mice without affecting body weight in Balb/c nude mice (seven to eight week old females) [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MDA-MB-468 cells Tested Concentrations: 1, 10, 100 and 1000 nM Incubation Duration: 72 hrs (hours) Experimental Results: Resulted in concentration dependent growth inhibition. Western Blot Analysis[1] Cell Types: MDA-MB-468 cells Tested Concentrations: 0, 10, 30, 100, 300 and 1000 nM Incubation Duration: 6 hrs (hours) Experimental Results: diminished both pCLK2 and CLK2. |
| Animal Protocol |
Animal/Disease Models: Balb/c nude mice (7 to 8 week-old females)[1]
Doses: 50 mg/kg Route of Administration: Oral administration; 2, 4, 8 hrs (hours). Experimental Results: pCLK2 detected with immunohistochemistry and immunoblotting diminished, by a reduction in the RPS6KB1 exon 7 and BCLAF1 exon 11 percentage splice-in (PSI) values. Animal/Disease Models: Balb/c nude mice ( 7 to 8 week-old females)[1] Doses: 50 mg/kg Route of Administration: Oral administration; twice (two times) daily on 2 days per week, for 3 weeks. Experimental Results: Suppressed tumor growth and < 10% nadir body weight loss. |
| References |
[1]. Iwai K, et al. Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability. EMBO Mol Med. 2018 Jun;10(6):e8289.
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| Molecular Formula |
C21H18N8
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|---|---|
| Molecular Weight |
382.42
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| CAS # |
2407433-00-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
N1C=C(C2C=CC3C(=CC=CN=3)C=2)C2=C(N=C(NC)N=C12)NCC1N=CC=CN=1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 8.25 mg/mL (21.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (26.15 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6149 mL | 13.0746 mL | 26.1493 mL | |
| 5 mM | 0.5230 mL | 2.6149 mL | 5.2299 mL | |
| 10 mM | 0.2615 mL | 1.3075 mL | 2.6149 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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