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SR7826 (SR-7826) is a novel and potent inhibitor of LIM kinase (LIMK) with anticancer activity. It has IC50 of 43 nM, and displays >100-fold selectivity over ROCK1 and ROCK2.
| ln Vitro |
Only Limk1 and STK16 were inhibited with ≥80% inhibition by SR7826 (compound 18b) at 1 μM in an investigation against a panel of 61 kinases. SR7826 is an efficient inhibitor of PC-3 cell migration and invasion. In A7r5 (IC50 = 470 nM) and PC-3 cells (IC50 < 1 µM), SR7826 (Compound 18b) suppresses cofilin phosphorylation [1]. SR7826 (1 μM) suppresses cofilin phosphorylation in prostate tissue and cultured stromal cells (WPMY-1) as well as prostatic strip contraction brought on by electric field stimulation. SR7826 fragments actin filaments and lowers viability in WPMY-1 cells [3].
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| ln Vivo |
Treatment with SR7826 (10 mg/kg; oral gavage; once daily; for 11 days; hAPPJ20 mice) significantly reduced cofilin Ser3 phosphorylation. SR7826 also dramatically increased apical and basal spine density in hAPPJ20 mice compared with mock-treated animals [2]. Plasma pharmacokinetic studies were performed in rats. After intravenous injection, PK characteristics of SR7826 (compound 18b; 1mg/kg), Cl is 5.2mL/min/kg, T1/2 is 2.2h, AUC is 8.4μM*h, Cmax is 7.7μM, and oral bioavailability in rats The concentration is 36% (orally; 2mg/kg) [1].
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| Animal Protocol |
Animal/Disease Models: hAPPJ20 mice (6 oral years) [2]
Doses: 10 mg/kg Route of Administration: po (oral gavage); one time/day; for 11 days Experimental Results: Dramatically diminished cofilin Ser3 (a LIMK1 substrate) Phosphorylation. |
| References |
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| Molecular Formula |
C22H21N5O2
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|---|---|
| Molecular Weight |
387.434444189072
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| Exact Mass |
387.169
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| CAS # |
1219728-20-7
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| PubChem CID |
45381385
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| Appearance |
White to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.738
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| LogP |
2.53
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
533
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WQAGVQVBDHOHRD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21N5O2/c1-15-13-23-21-19(15)20(24-14-25-21)16-7-9-17(10-8-16)26-22(29)27(11-12-28)18-5-3-2-4-6-18/h2-10,13-14,28H,11-12H2,1H3,(H,26,29)(H,23,24,25)
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| Chemical Name |
1-(2-hydroxyethyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]-1-phenylurea
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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 : ~100 mg/mL (~258.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.45 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.45 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 | 2.5811 mL | 12.9056 mL | 25.8111 mL | |
| 5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5811 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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