| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
LMTK3[1]
LMTK3-IN-1 targets lemur tyrosine kinase 3 (LMTK3), an oncogenic kinase. As an ATP-competitive inhibitor, it binds to the ATP-binding pocket of LMTK3. It promotes the degradation of LMTK3 through the ubiquitin-proteasome pathway, effectively suppressing its oncogenic activity. This dual mechanism of inhibition and degradation makes it a valuable tool for studying LMTK3-driven cancer progression. |
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| ln Vitro |
In vitro, LMTK3-IN-1 (10-20 μM) induces apoptosis in breast cancer (BC) cell lines. It exhibits significant anticancer effects across various cancer cell lines. Its activity is assessed using cell-based assays that measure cell viability, proliferation, and apoptosis in LMTK3-expressing cancer cells.
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| ln Vivo |
In vivo, LMTK3-IN-1 demonstrates strong efficacy in breast cancer (BC) mouse models. This demonstrates its antitumor activity in a preclinical model of breast cancer. Its ability to degrade LMTK3 and suppress its oncogenic activity contributes to its in vivo efficacy.
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| Enzyme Assay |
Cell-free assays for LMTK3-IN-1 typically involve measuring its binding affinity to LMTK3 using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). The Kd value of 2.5 μM is determined using these techniques. Additionally, kinase activity assays are used to confirm its ATP-competitive inhibition.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of LMTK3-IN-1. Breast cancer cell lines are treated with the compound. Cell viability and proliferation are measured to assess the compound's anti-proliferative effects. LMTK3 protein levels are measured to confirm degradation via the ubiquitin-proteasome pathway. Apoptosis assays are used to evaluate the compound's effects.
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| Animal Protocol |
In vivo animal experiments typically involve xenograft models of breast cancer. Mice bearing these tumors are administered LMTK3-IN-1. Tumor growth is monitored over time to assess the compound's efficacy. These studies are essential for demonstrating the in vivo antitumor activity of the compound.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of LMTK3-IN-1 are typical of a small molecule inhibitor. Its molecular weight is 356.30. While detailed PK parameters are not widely published, its properties suggest it is designed to have favorable drug-like characteristics to support efficacy in vivo.
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| Toxicity/Toxicokinetics |
The toxicity profile of LMTK3-IN-1 is not extensively documented but is likely to be similar to other kinase inhibitors. Common adverse effects may include fatigue and gastrointestinal disturbances. Preclinical studies would typically involve acute and chronic dosing in animal models to assess safety margins.
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| References | |
| Additional Infomation |
LMTK3-IN-1 is a research compound that targets LMTK3, an oncogenic kinase. It acts as an ATP-competitive inhibitor and promotes the degradation of LMTK3 via the ubiquitin-proteasome pathway. It is a valuable tool for studying LMTK3-driven cancer progression and for developing targeted therapy strategies. The compound is not approved for therapeutic use.
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| Molecular Formula |
C18H11F3N4O
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|---|---|
| Molecular Weight |
356.301353693008
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| Exact Mass |
356.088
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| CAS # |
2764850-23-7
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| PubChem CID |
138454301
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
472
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1=CC=CC(C2=CN=C3C=CC(C4=CC=NC=C4)=NN23)=C1)C(F)(F)F
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| InChi Key |
SFBZOJORTROAIE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H11F3N4O/c19-18(20,21)26-14-3-1-2-13(10-14)16-11-23-17-5-4-15(24-25(16)17)12-6-8-22-9-7-12/h1-11H
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| Chemical Name |
6-pyridin-4-yl-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazine
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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 | 2.8066 mL | 14.0331 mL | 28.0662 mL | |
| 5 mM | 0.5613 mL | 2.8066 mL | 5.6132 mL | |
| 10 mM | 0.2807 mL | 1.4033 mL | 2.8066 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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