AZD-3463

ALK/IGF1R inhibitor CAS# 1356962-20-3

AZD-3463

Catalog No. BCC3907----Order now to get a substantial discount!

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AZD-3463: 5mg $69 In Stock
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Chemical structure

AZD-3463

3D structure

Chemical Properties of AZD-3463

Cas No. 1356962-20-3 SDF Download SDF
PubChem ID 56599293 Appearance Powder
Formula C24H25ClN6O M.Wt 448.95
Type of Compound N/A Storage Desiccate at -20°C
Synonyms ALK/IGF1R inhibitor
Solubility DMSO : 20 mg/mL (44.55 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name N-[4-(4-aminopiperidin-1-yl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine
SMILES COC1=C(C=CC(=C1)N2CCC(CC2)N)NC3=NC=C(C(=N3)C4=CNC5=CC=CC=C54)Cl
Standard InChIKey GCYIGMXOIWJGBU-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H25ClN6O/c1-32-22-12-16(31-10-8-15(26)9-11-31)6-7-21(22)29-24-28-14-19(25)23(30-24)18-13-27-20-5-3-2-4-17(18)20/h2-7,12-15,27H,8-11,26H2,1H3,(H,28,29,30)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of AZD-3463

DescriptionAZD3463 is a novel orally bioavailable inhibitor of ALK with a Ki value of 0.75 nM.
TargetsALK    
IC500.75 nM(Ki)     

AZD-3463 Dilution Calculator

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AZD-3463 Molarity Calculator

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Preparing Stock Solutions of AZD-3463

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2274 mL 11.1371 mL 22.2742 mL 44.5484 mL 55.6855 mL
5 mM 0.4455 mL 2.2274 mL 4.4548 mL 8.9097 mL 11.1371 mL
10 mM 0.2227 mL 1.1137 mL 2.2274 mL 4.4548 mL 5.5685 mL
50 mM 0.0445 mL 0.2227 mL 0.4455 mL 0.891 mL 1.1137 mL
100 mM 0.0223 mL 0.1114 mL 0.2227 mL 0.4455 mL 0.5569 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on AZD-3463

Target: ALK, IGF1R

IC50: 0.75 nM(Ki)

AZD3463 is a novel orally bioavailable ALK/IGF1R inhibitor with Ki value of 0.75 nM. ALK expression is largely restricted to neurons and upregulated in neuroblastoma. Activated ALK has been shown to promote cell survival and growth. High ALK expression or mutations in the ALK gene correlates with adverse outcomes in neuroblastoma. Therefore, ALK receptor tyrosine kinase is an important therapeutic target for drug development against neuroblastoma [1].

In vitro: AZD3463 (5, 10, 20, and 50 μM) effectively inhibited the proliferation of neuroblastoma cell lines with wild type ALK (WT) and ALK activating mutations (F1174L and D1091N) via targeting the ALK-mediated PI3K/AKT/mTOR pathway and ultimately induced apoptosis and autophagy in vitro. Moreover, AZD3463 (1 μM) significantly enhanced the cytotoxic effects of doxorubicin (1 μM) on neuroblastoma cells [1]. AZD3463 simultaneously inhibited STAT3 and AKT to augment the cytotoxic effects of temozolomide and further reduce cell growth [2].

In vivo: AZD3463 (15 mg/kg, i.p. injection) showed significant therapeutic efficacy on the growth of the neuroblastoma tumors with WT and F1174L oncogenic mutant ALK in orthotopic xenograft mouse models [1].

References:
1.  Wang Y, Wang L, Guan S, Cao W, Wang H, Chen Z, et al. Novel ALK inhibitor AZD3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. Sci Rep. 2016;6:19423.
2.  Sampson VB, Vetter NS, Kamara DF, Collier AB, Gresh RC, Kolb EA. Vorinostat Enhances Cytotoxicity of SN-38 and Temozolomide in Ewing Sarcoma Cells and Activates STAT3/AKT/MAPK Pathways. PLoS One. 2015;10(11):e0142704.

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Description

AZD-3463 is an ALK/IGF1R inhibitor which overcomes multiple mechanisms of acquired resistance to crizotinib.

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