2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Anaplastic lymphoma kinase (ALK) Apoptosis
  4. Neladalkib TFA

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.

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Neladalkib TFA Chemical Structure

Neladalkib TFA Chemical Structure

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5 mg USD 300 In-stock
10 mg USD 480 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Neladalkib TFA:

Neladalkib TFA Related Antibodies

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Description

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[1][2].

In Vitro

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.

Neladalkib TFA Related Antibodies

Apoptosis Analysis[2]

Cell Line: NCI-H3122
Concentration: 1, 10, 100 nM
Incubation Time: 24 H
Result: Increased annexin V and propidium iodide (PI) staining.

Cell Cycle Analysis[2]

Cell Line: NCI-H3122
Concentration: 1, 10, 100 nM
Incubation Time: 24 H
Result: Reduced S phase cells.
In Vivo

Neladalkib (0.06-1.5 mg/kg, orally, twice daily, days 0-28) TFA has antitumor activity in mice[2].

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.
Molecular Weight

566.94

Formula

C25H23ClF4N6O3
Appearance

Solid

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
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7639 mL 8.8193 mL 17.6385 mL
5 mM 0.3528 mL 1.7639 mL 3.5277 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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Neladalkib TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NeladalkibNVL-655NVL655NVL 655Anaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Ba/F3antitumorCLIP1-LTKInhibitorinhibitorinhibit

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