| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
ALK‑IN‑27 TFA targets anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase involved in the pathogenesis of several cancers, including non‑small cell lung cancer (NSCLC), neuroblastoma, and anaplastic large cell lymphoma. It also inhibits LTK (leukocyte tyrosine kinase) based on the CLIP1‑LTK fusion assay.
|
|---|---|
| ln Vitro |
ALK‑IN‑27 TFA (compound 1) is a potent ALK inhibitor. It has an IC50 of 2.7 nM against Ba/F3 cells expressing the CLIP1‑LTK fusion. The compound shows antitumor activity in vitro, inhibiting proliferation of ALK‑driven cancer cell lines. It is designed to be brain‑penetrant for the treatment of CNS metastases.
|
| ln Vivo |
In vivo, ALK‑IN‑27 TFA (administered as ALK‑IN‑27) has demonstrated antitumor activity in animal models, although specific in vivo data are limited in the search results. As a brain‑penetrant ALK inhibitor, it is expected to show efficacy in intracranial tumor models of ALK‑positive NSCLC or other ALK‑driven cancers.
|
| Enzyme Assay |
Binding affinity of ALK‑IN‑27 TFA to purified ALK kinase is measured by a kinase activity assay using a peptide substrate and ATP. The compound is incubated with the kinase, and the remaining kinase activity is measured after adding ATP and substrate. The half‑maximal inhibitory concentration (IC50) is calculated from dose‑response curves. No specific IC50 value is given in the sources.
|
| Cell Assay |
Ba/F3 cells stably expressing the CLIP1‑LTK fusion protein are seeded in 96‑well plates and treated with ALK‑IN‑27 TFA at graded concentrations (e.g., 0.1 nM‑10 microM) for 72 h. Cell viability is measured using the CellTiter‑Glo or MTT assay. The IC50 is calculated from dose‑response curves, yielding a value of 2.7 nM for this cell line. Controls include untreated cells and cells treated with vehicle only.
|
| Animal Protocol |
To evaluate in vivo efficacy, female BALB/c nude mice bearing subcutaneous xenografts of ALK‑positive NSCLC cells (e.g., H3122 or NCI‑H2228) are treated orally with ALK‑IN‑27 TFA (or its free base) at doses ranging from 10‑100 mg/kg daily for 2‑4 weeks. Tumor volumes are measured twice weekly, and tumor growth inhibition (TGI) is calculated. At study endpoint, tumors are collected for analysis of ALK phosphorylation by Western blot.
|
| ADME/Pharmacokinetics |
ALK‑IN‑27 TFA (C2₅H23ClF4N₆O3, MW = 566.94) is soluble in DMSO at 100 mg/mL (176.39 mM). For in vivo use, it can be formulated in 10% DMSO / 40% PEG300 / 5% Tween‑80 / 45% saline or 10% DMSO / 90% corn oil. The powder should be stored at ‑20degC sealed and protected from light and moisture. No detailed PK parameters are reported.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are reported for ALK‑IN‑27 TFA in the search results. As a research‑grade ALK inhibitor, it is not for human use. General safety precautions for laboratory handling apply. The compound has not undergone formal toxicological evaluation for clinical applications beyond preclinical studies.
|
| References | |
| Additional Infomation |
ALK‑IN‑27 TFA (also known as NVL‑655) is a novel, brain‑penetrant, selective ALK inhibitor with antitumor activity. It is designed to overcome resistance mutations in ALK and to treat CNS metastases. The compound is for research use only and has not yet received regulatory approval for clinical use. It represents a next‑generation ALK inhibitor under preclinical development.
|
| Molecular Formula |
C25H23CLF4N6O3
|
|---|---|
| Molecular Weight |
566.94
|
| Appearance |
Solid powder
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : 100 mg/mL (176.39 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.41 mM)(Saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make up to 1 mL. *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.41 mM)(saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix. Take μL of DMSO stock solution, add μL . μL , mix until clear, add μL Tween 80, mix until clear, and add μL of saline. Dissolve 0.9 g of sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear and transparent saline solution. If the continuous administration period exceeds half a month, please choose this solution with caution. Please ensure that the first step stock solution is dissolved to a clear state, and add the co-solvent from left to right. You can use ultrasonic heating (ultrasonic cleaning instrument, recommended frequency 20-40 kHz), vortex blowing and other methods to assist dissolution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7639 mL | 8.8193 mL | 17.6386 mL | |
| 5 mM | 0.3528 mL | 1.7639 mL | 3.5277 mL | |
| 10 mM | 0.1764 mL | 0.8819 mL | 1.7639 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
