DS-1205

SKU: orb1298349

Description

DS-1205 is a highly potent and selective AXL kinase inhibitor (IC50 = 1.3 nM), with additional activity against MER, MET, and TRKA kinases. This small molecule has demonstrated efficacy in suppressing cell migration in vitro and impeding tumor growth in animal models, supporting its research use in oncology and metastasis studies.

Research Area

Immunology & Inflammation, Signal Transduction

Key Properties

• CAS Number: 1855860-24-0
• MW: 735.8
• Purity: 99.75% (May vary between batches)
• Formula: C₄₁H₄₂FN₅O₇
• SMILES: COc1cc(ccc1OC[C@H]1COCCO1)-c1cnc(N)c(c1)-c1ccc(NC(=O)c2cn(CC3CCOCC3)cc(-c3ccc(C)cn3)c2=O)cc1F
• Target: c-Met/HGFR,TAM Receptor,AXL,Trk receptor
• Solubility: DMSO:45 mg/mL (61.16 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.72 mM)

Bioactivity

• Target IC50:
  MET:104 nM (IC50)|Axl:1.3 nM (IC50)|Mer:63 nM (IC50)|TrkA:407 nM (IC50)
• In Vivo:
  DS-1205 (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice.
• In Vitro:
  DS-1205 (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM). DS-1205 (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205 decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

c-Met/HGFR, DS 1205, DS1205, DS-1205, DS-1205b, AXL, Axl, Inhibitor, Mer, NIH3T3, MET, migration, kinase, inhibit, Tropomyosin related kinase receptor, TRKA, Trk Receptor, Tyro3, tumor, TAM Receptor, TAMReceptor

Compound Identifiers

PubChem CID

129110632