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

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

Neladalkib Estructura química

No. CAS : 2739866-40-9

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Descripciòn

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 has an IC50 of 2.7 nM in Ba/F3 CLIP1-LTK cells[1].
Neladalkib 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) increases the activation of caspase 3/7 and reduces the S-phase cells in NCI-H3122[2].
Neladalkib (1-100 nM, 24 h) promotes apoptosis in NCI-H3122 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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) 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.
Ensayo clínico
Peso molecular

452.91

Fòrmula

C23H22ClFN6O

No. CAS
Appearance

Solid

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (220.79 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 2.2079 mL 11.0397 mL 22.0794 mL
5 mM 0.4416 mL 2.2079 mL 4.4159 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.90%

Referencias

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. 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 2.2079 mL 11.0397 mL 22.0794 mL 55.1986 mL
5 mM 0.4416 mL 2.2079 mL 4.4159 mL 11.0397 mL
10 mM 0.2208 mL 1.1040 mL 2.2079 mL 5.5199 mL
15 mM 0.1472 mL 0.7360 mL 1.4720 mL 3.6799 mL
20 mM 0.1104 mL 0.5520 mL 1.1040 mL 2.7599 mL
25 mM 0.0883 mL 0.4416 mL 0.8832 mL 2.2079 mL
30 mM 0.0736 mL 0.3680 mL 0.7360 mL 1.8400 mL
40 mM 0.0552 mL 0.2760 mL 0.5520 mL 1.3800 mL
50 mM 0.0442 mL 0.2208 mL 0.4416 mL 1.1040 mL
60 mM 0.0368 mL 0.1840 mL 0.3680 mL 0.9200 mL
80 mM 0.0276 mL 0.1380 mL 0.2760 mL 0.6900 mL
100 mM 0.0221 mL 0.1104 mL 0.2208 mL 0.5520 mL
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  • 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.

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Inquiry Information

Nombre del producto:
Neladalkib
Cat. No.:
HY-156467
Cantidad:
MCE Japan Authorized Agent: