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CCT251545

Katalog-Nr.GC17606

CCT251545 ist ein oral bioverfÜgbarer und potenter Inhibitor der WNT-Signalgebung mit einem IC50 von 5 nM in 7dF3-Zellen. CCT251545 ist eine selektive chemische Sonde zur Erforschung der Rolle von CDK8 und CDK19 bei Erkrankungen des Menschen.

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CCT251545 Chemische Struktur

Cas No.: 1661839-45-7

Größe Preis Lagerbestand Menge
10mM (in 1mL DMSO)
117,00 $
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2mg
69,00 $
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5mg
126,00 $
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10mg
210,00 $
Auf Lager
50mg
630,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

APC mutant human colorectal cancer cell line (COLO205-F1756 clone 4)

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.035 μM

Applications

In COLO205-F1756 clone 4, CCT251545 potently inhibited WNT pathway activity, with the IC50 value of 0.035 μM. Moreover, CCT251545 did not affect endogenous levels of TCF1 or TCF4.

Animal experiment [1]:

Animal models

Mice bearing COLO205-F1756 clone 4 xenografts

Dosage form

70 mg/kg; p.o.; b.i.d., for 9 days

Applications

In mice bearing COLO205-F1756 clone 4 xenografts, CCT251545 (70 mg/kg; p.o.; b.i.d., for 9 days) substantially inhibited WNT signaling and reduced tumor weights by 37.5%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Mallinger A, Crumpler S, Pichowicz M, et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. J Med Chem, 2015, 58(4): 1717-1735.

Background

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM [1].

The WNT signaling network controls cellular functions such as proliferation and differentiation, and is a major regulator of mammalian development. WNT signaling is frequently deregulated in malignancy, especially in colon cancer, and plays an important role in the generation and maintenance of cancer stem cells [1].

CCT251545 is an orally bioavailable and potent WNT signaling inhibitor discovered through high-throughput cell-based screening. CCT251545 is also a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19. CCT251545 changed gene expression regulated by WNT pathway and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1 [2]. CCT251545 also inhibited GSK3α and -β with IC50 values of 0.462 and 0.690 μM. In APC mutant human colorectal cancer cell line (COLO205-F1756 clone 4), CCT251545 inhibited WNT pathway activity with IC50 value of 0.035 nM [1].

In both mouse and rat, CCT251545 exhibited moderate clearance with moderate to high oral bioavailability. In mice bearing COLO205-F1756 clone 4 tumor xenografts, CCT251545 (70 mg/kg po bid for 9 days) significantly inhibited WNT signaling and reduced tumor weights by 37.5% [1].

References:
[1].  Mallinger A, Crumpler S, Pichowicz M, et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. J Med Chem, 2015, 58(4): 1717-1735.
[2].  Dale T, Clarke PA, Esdar C, et al. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat Chem Biol, 2015, 11(12): 973-980.

Chemical Properties

Cas No. 1661839-45-7 SDF
Chemical Name 8-(3-chloro-5-(4-(1-methyl-1H-pyrazol-4-yl)phenyl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one
Canonical SMILES O=C(NCC1)C1(CC2)CCN2C3=C(C4=CC=C(C5=CN(C)N=C5)C=C4)C=NC=C3Cl
Formula C23H24ClN5O M.Wt 421.92
Löslichkeit ≥ 42.2mg/mL 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

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3701 mL 11.8506 mL 23.7012 mL
5 mM 0.474 mL 2.3701 mL 4.7402 mL
10 mM 0.237 mL 1.1851 mL 2.3701 mL
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Berechnen

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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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