2. Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  3. IGF-1R Anaplastic lymphoma kinase (ALK) Autophagy Apoptosis
  4. AZD-3463

AZD-3463  (Synonyms: ALK/IGF1R inhibitor)

Cat. No.: HY-15609 Purity: 99.58%
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AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells.

For research use only. We do not sell to patients.

AZD-3463 Chemical Structure

AZD-3463 Chemical Structure

CAS No. : 1356962-20-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 67 In-stock
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10 mg USD 94 In-stock
50 mg USD 275 In-stock
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Based on 1 publication(s) in Google Scholar

AZD-3463 Related Antibodies

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Description

AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells[1][2][3].

In Vitro

AZD-3463 (0-50 µM; 72 h) suppresses the viability and proliferation of both wild type and mutant ALK NB cells[1].
AZD-3463 (10 µM; 0-4 h) effectively inhibits ALK-mediated PI3K/AKT/mTOR signaling and induces apoptosis and autophagy in NB cells[1].
AZD-3463 (0-100 nM; 4 h) inhibits FLT3-ITD-mediated activation of AKT, ERK1/2 and p38 in a dose-dependent manner in MOLM-13 and MV4-11 cells[2].

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

AZD-3463 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: IMR-32, NGP, NB-19, SH-SY5Y, SK-N-AS and LA-N-6 cells
Concentration: 0-50 µM
Incubation Time: 72 h
Result: Inhibited IMR-32, NGP, NB-19, SH-SY5Y, SK-N-AS and LA-N-6 cells with IC50 values of 2.802, 14.55, 11.94, 1.745, 21.34 and 16.49 µM, respectively.

Cell Autophagy Assay[1]

Cell Line: IMR-32, NGP , SH-SY5Y and SK-N-AS cells
Concentration: 10 µM
Incubation Time: 0-4 h
Result: Potently inhibited or totally abolished the phosphorylation of Akt Ser473 and RPS6 Thr235/236.
Induced cleavage of the autophagy marker LC3 A/BΙΙ within four hours.

Apoptosis Analysis[2]

Cell Line: MOLM-13 and MV4-11 cells
Concentration: 0-100 nM
Incubation Time: 4 h (pretreat)
Result: Selectively inhibited FLT3-ITD but not ligand-induced wild-type FLT3.
In Vivo

AZD3463 (15 mg/kg; i.p.; once daily for 2 days) inhibits tumor growth in different orthotopic NB xenograft mouse models[1].

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

Animal Model: 5 to 6-week-old female athymic Ncr nude mice (SH-SY5Y and NGP xenograft tumors bearing mice)[1].
Dosage: 15 mg/kg
Administration: Intraperitoneal injection; once daily for 2 days
Result: Showed anti-tumor efficacy in both ALK WT and F1174L mutant orthotropic xenograft mouse models of NB.
Molecular Weight

448.95

Formula

C24H25ClN6O
CAS No.
Appearance

Solid

Color

Light green to green

SMILES

ClC(C=NC(NC1=C(OC)C=C(N2CCC(N)CC2)C=C1)=N3)=C3C4=CNC5=C4C=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (44.55 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 2.2274 mL 11.1371 mL 22.2742 mL
5 mM 0.4455 mL 2.2274 mL 4.4548 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

Mass
=
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 mg/mL (4.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
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).
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

Purity: 99.58%

COA (253 KB) LCMS (95 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2274 mL 11.1371 mL 22.2742 mL 55.6855 mL
5 mM 0.4455 mL 2.2274 mL 4.4548 mL 11.1371 mL
10 mM 0.2227 mL 1.1137 mL 2.2274 mL 5.5685 mL
15 mM 0.1485 mL 0.7425 mL 1.4849 mL 3.7124 mL
20 mM 0.1114 mL 0.5569 mL 1.1137 mL 2.7843 mL
25 mM 0.0891 mL 0.4455 mL 0.8910 mL 2.2274 mL
30 mM 0.0742 mL 0.3712 mL 0.7425 mL 1.8562 mL
40 mM 0.0557 mL 0.2784 mL 0.5569 mL 1.3921 mL
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AZD-3463 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:

AZD-34631356962-20-3ALK/IGF1R inhibitorAZD3463AZD 3463IGF-1RAnaplastic lymphoma kinase (ALK)AutophagyApoptosisInsulin-like growth factor-1 receptorAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246neuroblastomaALKreceptortyrosinekinasePI3K/AKT/mTOR. pathwaycrizotinibresistanceInhibitorinhibitorinhibit

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