| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
TRK-IN-31 (compound 10o) (72 hours) exhibits potent antiproliferative activity, with IC50 values of 81.4 nM and 131.4 nM against Ba/F3-MPRIP-TRKAG667C and Ba/F3-MPRIP-TRKAG595R cells, respectively [1]. TRK-IN-31 (1-20 nM, 2 hours) significantly inhibits the TRK signaling pathway in Ba/F3-MPRIP-TRKA and MO-91 cells [1]. TRK-IN-31 (0.04-1 μM, 2 hours) significantly inhibits the TRKA G667C signaling pathway in cells, with particularly good results at 0.2 μM in Ba/F3-MPRIP-TRKAG667C cells [1]. TRK-IN-31 (1 μM, 1 h) exhibits extremely high selectivity for 92 kinases (S(10): 0.043), and shows significant inhibitory activity against TRKA/B/C and CSF1R, with inhibition rates of 97%-103% [1]. TRK-IN-31 has excellent binding ability to TRKAG595R, which can enhance its stability with proteins and reduce conformational fluctuations [1].
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|---|---|
| ln Vivo |
TRK-IN-31 (compound 10o) (25-150 mg/kg, orally, twice daily for 10 days) showed dose-dependent potent antitumor activity in the Ba/F3-MPRIP-TRKAG667C subcutaneous tumor mouse model and was well tolerated, with the highest dose reaching 150 mg/kg[1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Ba/F3-MPRIP-TRKA cells, MO-91 cells Tested Concentrations: 1, 5, 20 nM Incubation Duration: 2 hours Experimental Results: The TRK signaling pathway was significantly inhibited in both Ba/F3-MPRIP-TRKA and MO-91 cells. In Ba/F3-MPRIP-TRKA cells, a concentration of 5 nmol/L almost completely inhibited the activation of TRKA and its key downstream molecules PLCγ and Erk. |
| Animal Protocol |
Animal/Disease Models:Ba/F3-MPRIP-TRKAG667C cells (2 × 10⁶ cells/mouse)[1] were subcutaneously injected into the right abdomen of 4-6 week old female nude mice.
Doses: 25, 150 mg/kg. Route of Administration: After the tumor volume reached approximately 50 mm³, the drug was administered orally twice daily for 10 days. Experimental Results: Tumor growth was significantly delayed in a dose-dependent manner, with inhibition rates of 42.4% and 52.5% at doses of 25 mg/kg and 150 mg/kg, respectively. The drug was well tolerated, and no significant weight loss was observed at doses up to 150 mg/kg. |
| References |
| Molecular Formula |
C30H29F2N5O4
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|---|---|
| Molecular Weight |
561.58
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC1=CC=C(C=C1[C@@H]2N(C3=CNC(C(C(NC4=CC5=C(C=C4)OC(C(N6CCN(CC6)C)=O)=C5)=O)=C3)=O)CCC2)F
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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)
|
| 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 | 1.7807 mL | 8.9035 mL | 17.8069 mL | |
| 5 mM | 0.3561 mL | 1.7807 mL | 3.5614 mL | |
| 10 mM | 0.1781 mL | 0.8903 mL | 1.7807 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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