structure of 7-Methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline

7-Methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline

CAS No.: 1002304-34-8
M. Wt: 383.403
M. Fa: C22H17N5O2
InChI Key: HEAIZQNMNCHNFD-UHFFFAOYSA-N
Appearance: Off white solid

Names and Identifiers of 1002304-34-8

CAS Number

1002304-34-8

IUPAC Name

7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline

InChI

InChI=1S/C22H17N5O2/c1-28-16-7-8-17-19(13-16)23-12-11-20(17)29-14-22-25-24-21-10-9-18(26-27(21)22)15-5-3-2-4-6-15/h2-13H,14H2,1H3

InChIKey

HEAIZQNMNCHNFD-UHFFFAOYSA-N

Canonical SMILES

COC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5

UNII

Y2SR66P7VM

Physical and chemical properties of 1002304-34-8

Acidity coefficient

5.98±0.27(Predicted)

Density

1.3±0.1 g/cm3

Exact Mass

383.138214

Index of Refraction

1.696

LogP

4.02

Molecular Formula

C22H17N5O2

Molecular Weight

383.403

PSA

74.43000

Storage condition

-20℃

Solubility of 1002304-34-8

Solvent Dissolution Phenomenon Temperature Effect pH Effect
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Key Milestone of 1002304-34-8

Compound ID Name/Target Development Status Key Milestones
AMG 510 Sotorasib (KRAS G12C inhibitor) Approved (FDA approval in 2021) First clinical data published in 2018; Breakthrough Therapy Designation in 2020; Approved for NSCLC in 2021
AMG 232 MDM2 inhibitor Phase II clinical trials (terminated) First-in-human trial in 2016; Paused in 2018 due to toxicity/efficacy not meeting expectations
AMG 757 DLL3/CD3 bispecific antibody Phase II clinical trials (2024) Entered clinical trials in 2020; for small cell lung cancer

Interaction Studies of 1002304-34-8

Interaction studies involving AMG-208 have focused on its pharmacokinetics and potential drug-drug interactions. As a substrate for cytochrome P450 3A4 (CYP3A4), AMG-208 may interact with other drugs metabolized by this enzyme, necessitating careful monitoring when co-administered with such medications. Furthermore, studies have indicated that concurrent inhibition of both c-Met and vascular endothelial growth factor pathways can yield synergistic effects, enhancing therapeutic outcomes.

Biological Activity of 1002304-34-8

The biological activity of AMG-208 has been evaluated in various preclinical and clinical studies. It has demonstrated significant antitumor effects, particularly in prostate cancer models, where it induced apoptosis and suppressed tumor growth in xenograft studies. In a first-in-human clinical trial involving patients with advanced solid tumors, AMG-208 exhibited manageable toxicity profiles and showed evidence of antitumor activity, leading to complete and partial responses in some patients. The compound's ability to inhibit both c-Met and RON is believed to contribute to its efficacy against tumors that rely on these pathways for growth and metastasis.

Physical sample testing spectrum (NMR) of 1002304-34-8

Physical sample testing spectrum (NMR) of 1002304-34-8

Retrosynthesis analysis of 1002304-34-8

  • Route#1

    Cas:98-80-6
    Cas:1002304-34-8