| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
LCB03-0110 targets multiple kinases through ATP-competitive binding. Its primary targets include the discoidin domain receptor (DDR) family (DDR1 and DDR2) and the c-Src family of tyrosine kinases. The compound also potently inhibits spleen tyrosine kinase (Syk), Bruton's tyrosine kinase (Btk), and vascular endothelial growth factor receptor 2 (VEGFR-2). Additionally, it inhibits c-Src kinase with an IC₅₀ of 1.3 nM and shows activity against the nonactivated form of DDR2 with an IC₅₀ of 145 nM. By targeting these kinases, LCB03-0110 simultaneously suppresses multiple pathways involved in inflammation, fibrosis, angiogenesis, and neurodegeneration. It also inhibits VEGFR-2 and JAK/STAT3 signaling in primary cultured human endothelial cells and cancer cells.
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| ln Vitro |
LCB 03-0110 Transcription factor β1 and type I collagen-induced proliferation and migration of primary cutaneous fibroblasts [1].
In vitro, LCB03-0110 suppresses the proliferation and migration of primary dermal fibroblasts induced by transforming growth factor β1 (TGF-β1) and type I collagen. This activity correlates with the inhibition of enhanced expression of α-smooth muscle actin and activation of Akt1 and focal adhesion kinase (FAK). In J774A.1 macrophage cells activated by lipopolysaccharide (LPS), LCB03-0110 inhibits cell migration and the synthesis of nitric oxide (NO), inducible nitric-oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and tumor necrosis factor-α (TNF-α). Furthermore, an in vitro kinase assay and molecular modeling revealed that LCB03-0110 inhibits VEGFR-2, c-SRC, and TIE-2 kinase activity via preferential binding at the ATP-binding site. |
| ln Vivo |
In rabbit ear wounds, LCB 03-0110 can lessen the development of hypertrophic scars and stop the buildup of myofibroblasts and macrophages in wounds [1].
In vivo, topical application of LCB03-0110 to full excisional wounds on rabbit ears suppresses the accumulation of myofibroblast and macrophage cells in the healing wound and reduces hypertrophic scar formation after wound closing, without delaying the wound closing process. The compound also lessens the development of hypertrophic scars and stops the buildup of myofibroblasts and macrophages in wounds. Additionally, LCB03-0110 has demonstrated anti-inflammatory effects in both HCE-2 cells and other models. It has been shown to prevent allergic contact dermatitis in mice via topical administration. |
| Enzyme Assay |
In vitro kinase assays for LCB03-0110 typically involve the use of purified recombinant kinase enzymes. The compound is incubated with the target kinase, a peptide substrate, and ATP at varying concentrations in a suitable buffer system. Kinase activity is measured by quantifying substrate phosphorylation using techniques such as radiometric detection (e.g., ³³P-ATP incorporation), fluorescence polarization, or ELISA-based detection. IC₅₀ values are determined from dose-response curves. For DDR2 inhibition, the nonactivated form of the enzyme is used. Molecular modeling studies are often performed to confirm binding at the ATP-binding site.
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| Cell Assay |
Cellular assays for LCB03-0110 are performed using primary dermal fibroblasts to assess proliferation and migration in response to TGF-β1 and type I collagen stimulation. J774A.1 macrophage cells activated by LPS are used to evaluate inhibition of cell migration, NO production, iNOS, COX-2, and TNF-α synthesis. Primary cultured human endothelial cells and cancer cells are used to assess inhibition of VEGFR-2 and JAK/STAT3 signaling. Cells are treated with the compound at various concentrations, and endpoints are measured by Western blotting (for protein expression), ELISA (for cytokine levels), and functional assays (for migration and proliferation).
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| Animal Protocol |
In vivo animal models for LCB03-0110 include the rabbit ear full excisional wound model to evaluate scar formation. In this model, full-thickness excisional wounds are created on rabbit ears, and the compound is applied topically. Wound healing is monitored over time, and tissue samples are collected for histopathological analysis to assess myofibroblast and macrophage accumulation, as well as hypertrophic scar formation. The compound has also been studied in a mouse model of allergic contact dermatitis, where it was administered topically. Efficacy is assessed by measuring inflammatory responses and skin lesion severity.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LCB03-0110 include a molecular weight of 417.5 g/mol and a molecular formula of C₂₄H₂₃N₃O₂S. The compound is soluble in DMSO at 45 mg/mL. It is supplied as a solid powder with a purity of >98%. Storage conditions: powder at -20°C for up to one year; if dissolved in non-DMSO solvent, aliquots should be stored at -80°C for up to 6 months. Direct profiling studies have examined the pharmacokinetics of LCB03-0110, showing differential levels of brain penetration. Detailed PK parameters such as half-life, bioavailability, and volume of distribution are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
The compound is labeled as harmful if swallowed and very toxic to aquatic life with long-lasting effects. Safety precautions include washing skin thoroughly after handling and not eating, drinking, or smoking when using the product. As a research compound, its full safety profile would need to be established through comprehensive preclinical toxicity assessments. The compound is supplied for research use only and is not for human consumption. Standard laboratory safety practices should be followed when handling this compound.
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| References | |
| Additional Infomation |
Inhibits discoid domain receptor family tyrosine kinases; structure can be found in the first article.
LCB03-0110 is also known as LCB 03-0110, LCB030110, and LCB-03-0110. It is a thienopyridine derivative that functions as a potent pan-DDR/c-Src family tyrosine kinase inhibitor. The compound has demonstrated efficacy in suppressing scar formation by inhibiting fibroblast and macrophage activation. It is used in research applications studying fibrosis, inflammation, angiogenesis, and neurodegeneration. Its multi-kinase inhibition profile makes it a valuable tool for investigating the roles of DDR, Src, Syk, Btk, and VEGFR-2 in various pathological processes. The compound is for research use only. |
| Molecular Formula |
C24H23N3O2S
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|---|---|
| Molecular Weight |
417.523324251175
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| Exact Mass |
417.151
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| CAS # |
1228102-01-9
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| Related CAS # |
LCB 03-0110 dihydrochloride;1962928-28-4
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| PubChem CID |
71577234
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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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
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| InChi Key |
ZCWXCBKGPJOAFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23N3O2S/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)
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| Chemical Name |
3-[[2-[3-(morpholin-4-ylmethyl)phenyl]thieno[3,2-b]pyridin-7-yl]amino]phenol
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| Synonyms |
LCB03 0110; LCB030110; LCB03-0110
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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 | 2.3951 mL | 11.9755 mL | 23.9509 mL | |
| 5 mM | 0.4790 mL | 2.3951 mL | 4.7902 mL | |
| 10 mM | 0.2395 mL | 1.1975 mL | 2.3951 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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