Neladalkib TFA
Based on 1 Customer Validation
Neladalkib TFA is the TFA salt form of Neladalkib (HY-156467). Neladalkib (NVL-655) is an oral ALK inhibitor, the IC50 for Neladalkib in inhibiting ALK is 2.8 nM. Neladalkib promotes cell apoptosis and has anti-tumor activity.
For research use only. We do not sell to patients.
- Purity: 99.70%
- Formula: C25H23ClF4N6O3
- Molecular Weight:566.94
-
Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Biological Activity
Neladalkib TFA has an IC50 of 2.7 nM in Ba/F3 CLIP1-LTK cells[1].
Neladalkib TFA has a strong inhibitory effect on ALKT1151insT, ALKT1151M, ALKL1152R, ALKC1156Y, ALKI1171N, ALKI1171S, ALKI1171T, ALKF1174L, ALKF1174S, ALKV1180L, ALKL1198F, ALKG1202R, ALKD1203N, ALKS1206R, and ALKR1275Q (IC50 = 0.9-6.8 nmol/L), while it has a weaker inhibitory effect on ALKG1196M, ALKG1269A, and ALKG1269S (IC50 = 11-79 nmol/L)[2].
Neladalkib (1-100 nM, 24 h) TFA increases the activation of caspase 3/7 and reduces the S-phase cells in NCI-H3122[2].
Neladalkib (1-100 nM, 24 h) TFA promotes apoptosis in NCI-H3122 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:ALK-driven tumor xenografts in mice[2]
-
Dosage:0.06, 0.2, 0.5, 1.5 mg/kg
-
Administration:Oral
-
Result:Inhibited tumor proliferation.
Chemical Information
-
Appearance Solid
-
Molecular Weight 566.94
-
Formula C25H23ClF4N6O3
-
Color White to off-white
-
SMILES
CCN1C2=C(C(Cl)=N1)CC3=CN(C)N=C3C4=CC=C(F)C=C4[C@H](OC5=C(N)N=CC2=C5)C.OC(C(F)(F)F)=O
-
Synonyms
NVL-655 TFA
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (176.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7639 mL | 8.8193 mL | 17.6386 mL | 44.0964 mL |
| 5 mM | 0.3528 mL | 1.7639 mL | 3.5277 mL | 8.8193 mL | |
| 10 mM | 0.1764 mL | 0.8819 mL | 1.7639 mL | 4.4096 mL | |
| 15 mM | 0.1176 mL | 0.5880 mL | 1.1759 mL | 2.9398 mL | |
| 20 mM | 0.0882 mL | 0.4410 mL | 0.8819 mL | 2.2048 mL | |
| 25 mM | 0.0706 mL | 0.3528 mL | 0.7055 mL | 1.7639 mL | |
| 30 mM | 0.0588 mL | 0.2940 mL | 0.5880 mL | 1.4699 mL | |
| 40 mM | 0.0441 mL | 0.2205 mL | 0.4410 mL | 1.1024 mL | |
| 50 mM | 0.0353 mL | 0.1764 mL | 0.3528 mL | 0.8819 mL | |
| 60 mM | 0.0294 mL | 0.1470 mL | 0.2940 mL | 0.7349 mL | |
| 80 mM | 0.0220 mL | 0.1102 mL | 0.2205 mL | 0.5512 mL | |
| 100 mM | 0.0176 mL | 0.0882 mL | 0.1764 mL | 0.4410 mL |