| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
CRT-0105950 targets LIMK1 and LIMK2 (LIM domain kinases). It acts as a potent inhibitor with IC50 values of 0.3 nM for LIMK1 and 1 nM for LIMK2. By inhibiting LIMK, it prevents the phosphorylation of cofilin, a key regulator of actin dynamics.
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| ln Vitro |
CRT-0105950 inhibits filamentous actin (cofilin) phosphorylation. It promotes α-tubulin acetylation in cells. It disrupts microtubule organization. It has an IC50 of 0.3 nM for LIMK1 and 1 nM for LIMK2.
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| ln Vivo |
CRT-0105950 can be used in the study of renal carcinoma. It has been studied for its potential in cancer research. It inhibits cofilin phosphorylation and promotes α-tubulin acetylation.
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| Enzyme Assay |
CRT-0105950 is evaluated in cell-free kinase assays using purified LIMK1 and LIMK2 enzymes. The compound is incubated with the kinase, ATP, and a substrate, and the inhibition of kinase activity is measured. IC50 values are determined to quantify the potency of LIMK inhibition.
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| Cell Assay |
CRT-0105950 is assessed in cell-based assays using cancer cell lines. Cells are treated with CRT-0105950, and cofilin phosphorylation is measured by Western blot analysis. α-tubulin acetylation is assessed using immunofluorescence microscopy. Microtubule organization is evaluated by visualizing the cytoskeleton.
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| Animal Protocol |
CRT-0105950 is administered in animal models to evaluate its effects on tumor growth and metastasis. It has been studied in models of renal carcinoma. Efficacy is assessed by measuring tumor growth inhibition and biomarkers of LIMK inhibition.
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| ADME/Pharmacokinetics |
CRT-0105950 has a molecular weight of 393.89 and a molecular formula of C21H16ClN3OS. It has a CAS number of 1661845-86-8. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CRT-0105950. The compound is for research use only and is not intended for human therapeutic use. It is a potent LIMK inhibitor used in cancer research.
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| References | |
| Additional Infomation |
CRT-0105950 is a potent LIMK1/2 inhibitor. It is also known as CRT0105950. It can be used in the study of renal carcinoma. It is not approved for clinical use.
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| Molecular Formula |
C21H16CLN3OS
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|---|---|
| Molecular Weight |
393.88
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| Exact Mass |
393.07
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| CAS # |
1661845-86-8
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| PubChem CID |
117918970
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
556.6±60.0 °C at 760 mmHg
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| Flash Point |
290.4±32.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.695
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| LogP |
4.37
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
476
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(C=C1)C2=C(C=CN=C2)C3=CN=C(S3)NC4=CC=C(C=C4)O)Cl
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| InChi Key |
QYDBOFPHPMYWDO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H16ClN3OS/c1-13-2-7-16(19(22)10-13)18-11-23-9-8-17(18)20-12-24-21(27-20)25-14-3-5-15(26)6-4-14/h2-12,26H,1H3,(H,24,25)
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| Chemical Name |
4-[[5-[3-(2-chloro-4-methylphenyl)pyridin-4-yl]-1,3-thiazol-2-yl]amino]phenol
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| Synonyms |
CRT0105950 CRT 0105950 CRT-0105950
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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 : ~250 mg/mL (~634.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5388 mL | 12.6942 mL | 25.3884 mL | |
| 5 mM | 0.5078 mL | 2.5388 mL | 5.0777 mL | |
| 10 mM | 0.2539 mL | 1.2694 mL | 2.5388 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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