| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
TrkA 3.3 nM (IC50) TrkB 6.4 nM (IC50) TrkC 4.3 nM (IC50) TRKAG667C 9.4 nM (IC50) FLT3 1.3 nM (IC50) RET 9.9 nM (IC50) VEGFR2 71.1 nM (IC50)
|
|---|---|
| ln Vitro |
At 1 μM, TRK II-IN-1 (compound 12d) exhibits nearly 70% inhibition against Kit, CSF1R, DDR1, and DDR2, and over 90% kinase inhibition against VEGFR2, RET, and FLT3[1]. Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB, and Ba/F3-ETV6-TRKC cells are inhibited by TRK II-IN-1 (72 h), with IC50s of 26.1, 44.7, and 15.7 nM, respectively[1]. A panel of Ba/F3 cells that have been stably transformed with wild type, xDFG, and solvent-front (SF) mutant TRK fusion proteins has its proliferation suppressed by TRK II-IN-1 (72 h), with IC50s ranging from 2.6 to 143.3 nM[1]. Apoptosis is induced in Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells by TRK II -IN-1 (0.4-500 nM; 48 h)[1]. In Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells, TRK II-IN-1 (0.4-500 nM; 24 h) stops cell cycle progression in the G0/G1 phase[1]. The phosphorylation of TRKA, TRKAG667C kinases, and their downstream AKT, ERK, and PLCγ1 is suppressed in a dose-dependent manner by TRK II-IN-1 (0.8-500 nM; 6 h)[1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions Tested Tested Concentrations: 0.4, 2 , 10, 50 nM for Ba/F3-CD74-TRKA cells; 4, 20, 100, 500 nM for Ba/F3-CD74-TRKAG667C cells Incubation Duration: 48 hrs (hours) Experimental Results: Notable apoptotic cells (18.74% in 100 nM and 35.65 % in 500 nM) were observed in Ba/F3-CD74-TRKA cells. Induced Ba/F3-CD74-TRKAG667C cell apoptosis with 11.22% and 56.25% at the concentration of 10 nM and 50 nM, respectively. Cell Cycle Analysis[1] Cell Types: Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions Tested Tested Concentrations: 0.4, 2, 10, 50 nM for Ba/F3-CD74-TRKA cells; 4, 20, 100, 500 nM for Ba/F3- CD74-TRKAG667C cells Incubation Duration: 24 hrs (hours) Experimental Results: Arrested cell cycle progression in the G0/G1 phase. Western Blot Analysis[1] Cell Types: Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions Tested Tested Concentrations: 0.8, 4, 20, 100, 500 nM Incubation Duration: 6 hrs (hours) Experimental Results: Inhibited the activation of TRKA and downst |
| References |
[1]. Xiang S, et, al. Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114899.
|
| Molecular Formula |
C29H31F3N8O
|
|---|---|
| Molecular Weight |
564.60
|
| CAS # |
2904690-41-9
|
| 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 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 | 1.7712 mL | 8.8558 mL | 17.7117 mL | |
| 5 mM | 0.3542 mL | 1.7712 mL | 3.5423 mL | |
| 10 mM | 0.1771 mL | 0.8856 mL | 1.7712 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
