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)

製品番号: HY-15609 純度: 99.31%
COA 取扱説明書 Technical Support

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.

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AZD-3463

AZD-3463 構造式

CAS 番号 : 1356962-20-3

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 67 在庫あり
Solution
10 mM * 1 mL in DMSO USD 67 在庫あり
Solid
5 mg $61 在庫あり
10 mg $94 在庫あり
25 mg $183 在庫あり
50 mg $275 在庫あり
100 mg $495 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

AZD-3463 関連抗体

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製品説明

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].

Cellular Effect
Cell Line Type Value Description References
BaF3 IC50
131.5 nM
Compound: 17; AZD3463
Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay
[PMID: 33243531]
BaF3 IC50
74.4 nM
Compound: 17; AZD3463
Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay
[PMID: 33243531]
IMR-32 IC50
2.8 nM
Compound: 42; AZD3463
Cytotoxicity against human IMR32 cells
Cytotoxicity against human IMR32 cells
[PMID: 31419130]
PC-9 IC50
253 nM
Compound: AZD3463
Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
[PMID: 28287083]
PC-9 IC50
378.3 nM
Compound: AZD3463
Anticancer activity against human PC-9 cells harboring T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
Anticancer activity against human PC-9 cells harboring T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
[PMID: 28287083]
PC-9 IC50
622.4 nM
Compound: AZD3463
Anticancer activity against human PC-9 cells harboring C797S/T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
Anticancer activity against human PC-9 cells harboring C797S/T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay
[PMID: 28287083]
SH-SY5Y IC50
1.7 nM
Compound: 42; AZD3463
Cytotoxicity against human SH-SY5Y cells
Cytotoxicity against human SH-SY5Y cells
[PMID: 31419130]
体外実験

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 関連抗体

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.
体内実験

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.
分子量

448.95

分子式

C24H25ClN6O
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.2227 mL 1.1137 mL 2.2274 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.
純度とドキュメンテーション
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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