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Voruciclib

Catalog No.GC45983

Voruciclib es un inhibidor de CDK selectivo y activo por vÍa oral con valores de Ki de 0,626 nM-9,1 nM. Voruciclib bloquea potentemente CDK9, el regulador transcripcional de MCL-1. Voruciclib reprime la expresiÓn de MCL-1 en mÚltiples modelos de linfoma difuso de células B grandes (DLBCL).

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Voruciclib Chemical Structure

Cas No.: 1000023-04-0

Tamaño Precio Disponibilidad Cantidad
1mg
121,00 $
Disponible
5mg
359,00 $
Disponible
10mg
660,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description of Voruciclib

Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).1 It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 μM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.

|1. Dey, J., Deckwerth, T.L., Kerwin, W.S., et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk diffuse large B-cell lymphoma to BCL2 inhibition. Sci. Rep. 7(1), 18007 (2017).

Chemical Properties of Voruciclib

Cas No. 1000023-04-0 SDF
Canonical SMILES O=C1C=C(C2=C(Cl)C=C(C(F)(F)F)C=C2)OC3=C1C(O)=CC(O)=C3[C@@]4([H])[C@H](CO)N(C)CC4
Formula C22H19ClF3NO5 M.Wt 469.8
Solubility Soluble in DMSO 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 Voruciclib

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1 mg 5 mg 10 mg
1 mM 2.1286 mL 10.6428 mL 21.2857 mL
5 mM 0.4257 mL 2.1286 mL 4.2571 mL
10 mM 0.2129 mL 1.0643 mL 2.1286 mL
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In vivo Formulation Calculator (Clear solution) of Voruciclib

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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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Average Rating: 5 ★★★★★ (Based on Reviews and 36 reference(s) in Google Scholar.)

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