1. Protein Tyrosine Kinase/RTK
    Neuronal Signaling
  2. TAM Receptor
    c-Met/HGFR
    Trk Receptor
  3. DS-1205b free base

DS-1205b free base 

Cat. No.: HY-114357A
Handling Instructions

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.

For research use only. We do not sell to patients.

DS-1205b free base Chemical Structure

DS-1205b free base Chemical Structure

CAS No. : 1855860-24-0

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Description

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo[1].

IC50 & Target[1]

AXL

1.3 nM (IC50)

MER

63 nM (IC50)

MET

104 nM (IC50)

TrkA

407 nM (IC50)

In Vitro

DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM)[1].
DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: NIH3T3-AXL cells
Concentration: 1, 10, 100, 1000, 10000 μM
Incubation Time: 2, 24 hours
Result: Completely inhibited the phosphorylation of AXL at concentrations above 10 nM.
Slightly inhibited the phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.
In Vivo

DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks[1]
Dosage: 3.1, 6.3, 13, 25, 50 mg/kg
Administration: P.o. twice daily for 5 days
Result: Inhibited tumor growth by 39-94%.
Reduced the phosphorylation of both AXL and AKT in tumors.
Molecular Weight

735.80

Formula

C₄₁H₄₂FN₅O₇

CAS No.

1855860-24-0

SMILES

O=C(C1=CN(CC2CCOCC2)C=C(C3=NC=C(C)C=C3)C1=O)NC4=CC=C(C5=CC(C6=CC=C(OC[[email protected]@H]7OCCOC7)C(OC)=C6)=CN=C5N)C(F)=C4

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

DS-1205bTAM Receptorc-Met/HGFRTrk ReceptorTyro3AxlMerTropomyosin related kinase receptorAXLkinaseMERMETTRKAmigrationtumorNIH3T3Inhibitorinhibitorinhibit

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DS-1205b free base
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HY-114357A
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