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DS-1205b free base

Katalog-Nr.GC62597

Die freie Base von DS-1205b ist ein potenter und selektiver Inhibitor der AXL-Kinase mit einem IC50-Wert von 1,3 nM. Die freie Base von DS-1205b hemmt auch MER, MET und TRKA mit IC50-Werten von 63, 104 bzw. 407 nM. Die freie Base von DS-1205b kann die Zellmigration in vitro und das Tumorwachstum in vivo hemmen.

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DS-1205b free base Chemische Struktur

Cas No.: 1855860-24-0

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10mM (in 1mL DMSO)
481,00 $
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1mg
131,00 $
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5 mg
297,00 $
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10 mg
446,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of DS-1205b free base

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].

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].

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

[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.

Chemical Properties of DS-1205b free base

Cas No. 1855860-24-0 SDF
Formula C41H42FN5O7 M.Wt 735.8
Löslichkeit DMSO : 50 mg/mL (67.95 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of DS-1205b free base

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.3591 mL 6.7953 mL 13.5906 mL
5 mM 0.2718 mL 1.3591 mL 2.7181 mL
10 mM 0.1359 mL 0.6795 mL 1.3591 mL
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In vivo Formulation Calculator (Clear solution) of DS-1205b free base

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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