| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
TRK-IN-34 (compound 5c) exhibits good metabolic stability in human liver microsomes with a half-life of up to 153.1 minutes [1]. TRK-IN-34 (3 days) effectively inhibits the proliferation of Ba/F3 cells expressing wild-type or mutant TRKA fusion proteins. Its IC50 values for CD74-NTRK1-WT, CD74-NTRK1-G595R and CD74-NTRK1-G667C are 3 nM, 6 nM and 17 nM, respectively [1]. After 6 hours of treatment, TRK-IN-34 (1.23-300 nM; 6 hours) dose-dependently inhibits the phosphorylation of TRKA and its downstream signaling proteins PLCγ1 and ERK in Ba/F3 cells expressing wild-type or mutant TRKA fusion proteins [1]. TRK-IN-34 effectively inhibits wild-type and mutant TRK kinases in cell-free enzyme activity assays. For key drug-resistant mutants, such as TRKAG595R, TRKAG667C, TRKCG623R and TRKAF589L, their IC50 values are 0.75 nM, 0.96 nM, 0.73 nM and 0.44 nM, respectively[1].
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| ln Vivo |
TRK-IN-34 (compound 5c) (30-60 mg/kg; orally; twice daily; 2 weeks) showed potent dose-dependent antitumor efficacy in Ba/F3-LMNA-TRKAG667C xenograft mice, with a TGI of 91% at 30 mg/kg and 115% at 60 mg/kg, and partial regression in 4/6 animals [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Ba/F3-CD74-NTRK1-WT, Ba/F3-CD74-NTRK1-G595R and Ba/F3-CD74-NTRK1-G667C cells Test concentrations: 1.23, 3.7, 11.1, 33.3, 100 nM (Ba/F3-CD74-NTRK1-WT and Ba/F3-CD74-NTRK1-G595R cells); 3.7, 11, 33, 100, 300 nM (Ba/F3-CD74-NTRK1-G667C cells) Incubation Duration: 6 hours Experimental Results: In all three Ba/F3 cell lines (wild type, G595R, G595R, G667C ... In the mutant (G667C mutant), phosphorylation of TRKA, PLCγ1, and ERK was reduced in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models:Ba/F3-LMNA-TRKAG667C xenograft [1]
Doses: 30 mg/kg; 60 mg/kg Route of Administration: Oral; twice daily; 2 weeks Experimental Results: The tumor growth inhibition rate (TGI) reached 91% at a dose of 30 mg/kg. The TGI reached 115% at a dose of 60 mg/kg, and partial tumor regression was observed in 4 out of 6 animals. |
| References |
| Molecular Formula |
C19H16F4N6O
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|---|---|
| Molecular Weight |
420.36
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| CAS # |
2489327-91-3
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
FC1=CC=C(OCC(F)(F)F)C([C@@H](C)NC2=NC3=C(C4=CNN=C4)C=NN3C=C2)=C1
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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 | 2.3789 mL | 11.8946 mL | 23.7891 mL | |
| 5 mM | 0.4758 mL | 2.3789 mL | 4.7578 mL | |
| 10 mM | 0.2379 mL | 1.1895 mL | 2.3789 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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