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DS-1205

Catalog No. T9123 CAS 1855860-24-0

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

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DS-1205, CAS 1855860-24-0

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Purity: 98%

Biological Description

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Description	DS-1205 is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205 also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205 can inhibit cell migration in vitro and tumor growth in vivo[1].
Targets&IC50	TrkA:407 nM (IC50), Met:104 nM (IC50), Mer:63 nM (IC50), Axl:1.3 nM (IC50)
In vitro	DS-1205 (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM)[1]. 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)[1].
In vivo	DS-1205 (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice[1].

Molecular Weight	284.32
Formula	C14H16N6O
CAS No.	1855860-24-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 45 mg/mL (61.16 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Jimbo T, et, al. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019 Aug 27;10(50):5152-5167.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

DS-1205 1855860-24-0 Tyrosine Kinase/Adaptors TAM Receptor TRKA c-Met/HGFR migration Axl Tyro3 Trk Receptor MET DS 1205 Mer Tropomyosin related kinase receptor tumor DS1205 kinase inhibit Inhibitor DS-1205b NIH3T3 inhibitor

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