| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
The strongest inhibitory kinase is CLK1 (IC50: 2 nM). With the exception of CLK1, only two kinases have IC50 values less than 100 nM: CLK2 (IC50: 31 nM) and CLK4 (IC50: 8 nM). DYRK1A has the strongest off-target of all the kinases. It was also investigated whether CLK1-IN-1 could cause autophagy in human ovarian cancer cell lines, BNL CL.2 and SKOV-3. A clear dose dependence was observed in the impact of CLK1-IN-1 on yellow LC3 spots, with the maximum effect observed at a dose of 10 μM. Additionally, compared to cells treated with DMSO, the number of red LC3 puncta (mRFP signal 35 only) increased in cells treated with CLK1-IN-1, indicating the formation of autolysosomes. Crucially, CLK1-IN-1 promotes SQSTM1/p62 degradation and raises the ratio of red to yellow LC3 dots, both of which show that autophagic flux is induced by CLK1-IN-1 [1].
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| ln Vivo |
When exposed to APAP, the liver is severely injured; however, when treated with CLK1-IN-1 (ip, 30 mg/kg), the liver is significantly protected. The two labeling enzymes were returned to normal levels after therapy with CLK1-IN-1, according to the results [1]. This was achieved by dramatically lowering blood ALT and AST levels.
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| References |
| Molecular Formula |
C24H16FN5O
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|---|---|
| Molecular Weight |
409.415147781372
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| Exact Mass |
409.133
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| CAS # |
2123491-32-5
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| PubChem CID |
129318964
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| Appearance |
White to off-white solid powder
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| LogP |
4.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
631
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1C=CC(=CC=1)[C@H](C)N1C2C(=CN=C3C=CC(C4C=CC5=C(C=4)N=CO5)=CC=23)N=N1
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| InChi Key |
BHKVSOQUPYXVRZ-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C24H16FN5O/c1-14(15-2-6-18(25)7-3-15)30-24-19-10-16(4-8-20(19)26-12-22(24)28-29-30)17-5-9-23-21(11-17)27-13-31-23/h2-14H,1H3/t14-/m0/s1
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| Chemical Name |
5-[1-[(1S)-1-(4-fluorophenyl)ethyl]triazolo[4,5-c]quinolin-8-yl]-1,3-benzoxazole
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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 : ~25 mg/mL (~61.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4425 mL | 12.2124 mL | 24.4248 mL | |
| 5 mM | 0.4885 mL | 2.4425 mL | 4.8850 mL | |
| 10 mM | 0.2442 mL | 1.2212 mL | 2.4425 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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