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CCT-251921

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Purity:97.74%

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COA HPLC HNMR

CCT-251921

Catalog No. T14901Cas No. 1607837-31-9

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM].

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Pack Size	Price	Availability
1 mg	$87	In Stock
5 mg	$233	In Stock
10 mg	$342	In Stock
25 mg	$577	In Stock
50 mg	$827	In Stock
100 mg	$1,130	In Stock
1 mL x 10 mM (in DMSO)	$213	In Stock

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Product Introduction

Bioactivity

Description	CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM].
Targets&IC50	CDK19:2.6 nM (IC50), CDK8:2.3 nM (IC50)
In vitro	CCT-251921 exhibits limited activity across a panel of 55 receptors, ion channels, and enzymes at 1 μM, as well as a panel of 279 kinases, while showing weak inhibition of CYPs. It effectively inhibits basal WNT pathway activity in human cancer cell lines with constitutive activation of WNT pathway signaling, specifically in LS174T (β-catenin mutant), SW480, and Colo205 (APC mutant) cell lines, and PA-1 human teratocarcinoma cells, which depend on WNT ligand.
In vivo	CCT-251921 exhibits enhanced oral pharmacokinetics and pharmaceutical properties, maintaining inhibition of STAT1SER727 phosphorylation for over 6 hours post-dose. In an APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduced tumor weight in mice by 54.2% on day 15.

Chemical Properties

Molecular Weight	410.9
Formula	C21H23ClN6O
Cas No.	1607837-31-9

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 15 mg/mL (36.51 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4337 mL	12.1684 mL	24.3368 mL	121.6841 mL
5 mM	0.4867 mL	2.4337 mL	4.8674 mL	24.3368 mL
10 mM	0.2434 mL	1.2168 mL	2.4337 mL	12.1684 mL
20 mM	0.1217 mL	0.6084 mL	1.2168 mL	6.0842 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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Tech Support

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