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CAY10763

Katalog-Nr.GC47061

A dual inhibitor of IDO1 and STAT3 activation

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CAY10763 Chemische Struktur

Cas No.: 2364458-49-9

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500 μg
111,00 $
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1 mg
213,00 $
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5 mg
836,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of CAY10763

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50 = 46 nM) and STAT3 activation.1 It binds to STAT3 (Kd = 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively.

1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

Chemical Properties of CAY10763

Cas No. 2364458-49-9 SDF
Canonical SMILES O=C(C1=C/2C=CC=C1)C(N[C@H](CC3=CC=CC=C3)C(NC4=CC(OC)=CC(OC)=C4)=O)=CC2=N/O
Formula C27H25N3O5 M.Wt 471.5
Löslichkeit DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml 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 CAY10763

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1209 mL 10.6045 mL 21.2089 mL
5 mM 0.4242 mL 2.1209 mL 4.2418 mL
10 mM 0.2121 mL 1.0604 mL 2.1209 mL
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In vivo Formulation Calculator (Clear solution) of CAY10763

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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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