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Chemical Structure| 1356962-20-3 Chemical Structure| 1356962-20-3

Structure of AZD-3463
CAS No.: 1356962-20-3

Chemical Structure| 1356962-20-3

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

Synonyms: ALK/IGF1R inhibitor

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Product Details of AZD-3463

CAS No. :1356962-20-3
Formula : C24H25ClN6O
M.W : 448.95
SMILES Code : ClC1=CN=C(NC2=CC=C(N3CCC(N)CC3)C=C2OC)N=C1C4=CNC5=C4C=CC=C5
Synonyms :
ALK/IGF1R inhibitor
MDL No. :MFCD25976759

Safety of AZD-3463

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AZD-3463

RTK

Isoform Comparison

Biological Activity

Target
  • ALK

    ALK, Ki:0.75 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
BμMs 250 nM 5 days AZD3463 eliminated the DZNep-induced osteoclast differentiation and bone resorption function. PMC8193724
MDA-MB-231 1200 nM 24 and 48 hours AZD3463 significantly decreased the viability and proliferation of MDA-MB-231 cells. PMC8193724
A4573 20 nM 48 hours AZD3463 inhibits ALK and IGF-1R signaling pathways, enhancing the cytotoxicity of ST and vorinostat, further reducing cell growth PMC4646493
TC32 20 nM 48 hours AZD3463 inhibits ALK and IGF-1R signaling pathways, enhancing the cytotoxicity of ST and vorinostat, further reducing cell growth PMC4646493
MDA-MB-231BO cells 0.5, 2, 5, 10 nM 24 hours AZD3463 alleviated IGF-1-induced IGF-1R phosphorylation in a dose-dependent manner and suppressed the proliferation and migration of MDA-MB-231BO cells. PMC7186597

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice breast cancer bone metastasis model intraperitoneal injection 125 μg 5% Imiquimod cream Once daily for up to 7 days The combination of AZD3463 and DZNep reduced tumor volume and protected against bone loss. PMC8193724
nude mice orthotopic xenograft mouse models of NB intraperitoneal injection 125 mg/kg twice daily for 3 days assess the drug’s effect on inhibiting tumor growth in orthotopic xenograft mouse models of NB PMC4726162
nude mice breast cancer bone metastasis model intraperitoneal injection 25 mg/kg Single injection, 30 minutes before Jo2 injection AZD3463 significantly inhibited the progression of breast cancer bone metastasis, and its combination with zoledronic acid showed enhanced antitumor activity. PMC7186597

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.14mL

2.23mL

1.11mL

22.27mL

4.45mL

2.23mL

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