| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
LCB 03-0110 dihydrochloride targets multiple kinases including the Discoidin domain receptor (DDR) family (DDR1 and DDR2), the c-Src tyrosine kinase family (all eight Src family kinases with IC50 of 2-20 nM), as well as Btk and Syk. It is an ATP-competitive inhibitor that binds to the ATP-binding pocket of these kinases. The compound inhibits DDR2 activated tyrosine kinase activity with an IC50 of 6 nM and the nonactivated form with an IC50 of 145 nM.
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| ln Vitro |
LCB 03-0110 dihydrochloride exhibits potent in vitro activity against multiple kinase targets. It inhibits the activated tyrosine kinase activity of DDR2 with an IC50 of 6 nM and the nonactivated form of DDR2 with an IC50 of 145 nM. In cell-based assays, it suppresses collagen-induced autophosphorylation of DDR1 and DDR2 with IC50 values of 164 and 171 nM, respectively. It inhibits all eight Src family kinases with IC50 values ranging from 2 to 20 nM. The compound also suppresses the proliferation and migration of primary dermal fibroblasts induced by TGF-β1 and type I collagen (IC50=194 nM).
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| ln Vivo |
LCB 03-0110 dihydrochloride demonstrates in vivo activity in wound healing models, where it suppresses hypertrophic scar formation. The compound inhibits macrophage and fibroblast activation in vivo, as it inhibits LPS-induced macrophage activation and TGF-β1-induced fibroblast activation in vitro. In animal models of wound healing, LCB 03-0110 reduces scar formation, indicating its potential as an anti-fibrotic agent. Further studies are needed to fully characterize its in vivo efficacy in other disease models.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cell-based) assay for LCB 03-0110 dihydrochloride involves assessing its ATP-competitive inhibition of kinase activity. Kinase assays are performed using recombinant DDR2 (activated and nonactivated forms) and Src family kinases. The compound is incubated with the kinase, ATP, and a substrate peptide. Kinase activity is measured by detecting phosphorylated substrate using techniques such as radiometric or fluorescence-based assays. IC50 values are determined from dose-response curves.
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| Cell Assay |
The in vitro cell-based assay for LCB 03-0110 dihydrochloride involves treating cells with the compound and measuring downstream signaling and functional responses. In DDR1/2-expressing cells, collagen-induced autophosphorylation is assessed by Western blotting with phospho-specific antibodies (IC50=164 and 171 nM for DDR1 and DDR2). In primary dermal fibroblasts, TGF-β1 and type I collagen-induced proliferation and migration are measured (IC50=194 nM). In LPS-activated J774A.1 macrophage cells, the compound inhibits cell migration and the synthesis of nitric oxide, iNOS, COX2, and TNF-α.
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| Animal Protocol |
In vivo animal experiments for LCB 03-0110 dihydrochloride are conducted in wound healing models to evaluate its anti-scarring efficacy. Animals (typically mice or rats) are subjected to skin wounding, and the compound is administered topically or systemically. Wound healing is monitored over time, and scar formation is assessed histologically. The compound suppresses hypertrophic scar formation in these models. Additional studies may evaluate its effects on macrophage and fibroblast activation in vivo.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of LCB 03-0110 dihydrochloride are not extensively reported in the available literature. As a small molecule kinase inhibitor, it is expected to have moderate oral bioavailability and tissue distribution. The compound is typically formulated for in vivo administration using standard vehicles. Physicochemical properties include a molecular weight of 490.443 g/mol and a formula of C24H25Cl2N3O2S. Further pharmacokinetic studies are required to determine its half-life, clearance, and bioavailability.
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| Toxicity/Toxicokinetics |
Toxicological data for LCB 03-0110 dihydrochloride are not extensively documented. As a research compound, its safety profile is typically evaluated in standard cytotoxicity and acute toxicity assays. The compound is classified for research use only and is not intended for human therapeutic use. Comprehensive toxicological characterization would be required prior to any clinical development. References for its biological activity include Sun X, et al. J Pharmacol Exp Ther. 2012 Mar;340(3):510-9; Jung SH, et al. Br J Dermatol. 2013 Jan;168(1):112-9; and Kim BH, et al. Exp Dermatol. 2015 Jul;24(7):503-9.
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| References | |
| Additional Infomation |
LCB 03-0110 dihydrochloride (CAS 1962928-28-4) is a potent, ATP-competitive inhibitor of DDR family kinases, c-Src tyrosine kinase family, Btk, and Syk. It has a molecular weight of 490.443 g/mol and a formula of C24H25Cl2N3O2S. The compound is primarily used in research on fibrosis, scar formation, and inflammation. It is not approved for clinical use and is available only for research purposes. References: Sun X, et al. J Pharmacol Exp Ther. 2012; Jung SH, et al. Br J Dermatol. 2013; Kim BH, et al. Exp Dermatol. 2015.
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| Molecular Formula |
C24H25CL2N3O2S
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|---|---|
| Molecular Weight |
490.45
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| Exact Mass |
489.104
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| CAS # |
1962928-28-4
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| Related CAS # |
LCB 03-0110;1228102-01-9
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| PubChem CID |
121513872
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1COCCN1CC2=CC(=CC=C2)C3=CC4=NC=CC(=C4S3)NC5=CC(=CC=C5)O.Cl.Cl
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| InChi Key |
OEWGAUGZPPUIPF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23N3O2S.2ClH/c28-20-6-2-5-19(14-20)26-21-7-8-25-22-15-23(30-24(21)22)18-4-1-3-17(13-18)16-27-9-11-29-12-10-27;;/h1-8,13-15,28H,9-12,16H2,(H,25,26);2*1H
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| Chemical Name |
3-[[2-[3-(morpholin-4-ylmethyl)phenyl]thieno[3,2-b]pyridin-7-yl]amino]phenol;dihydrochloride
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0389 mL | 10.1947 mL | 20.3894 mL | |
| 5 mM | 0.4078 mL | 2.0389 mL | 4.0779 mL | |
| 10 mM | 0.2039 mL | 1.0195 mL | 2.0389 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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