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CCT251545 analogue, Compound 51

Catalog No. T22633 CAS T22633

CCT251545 analog is a potent and selective CDK8/19 inhibitor (IC50: 5.1 nM and 5.6 nM, respectively). Mediator complex-associated kinases CDK8 and CDK19 are involved in the regulation of multiple transcription pathways. CDK8 plays as an oncogene in gastric and colorectal cancers through the activation of WNT signaling.

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CCT251545 analogue, Compound 51 Chemical Structure

CCT251545 analogue, Compound 51, CAS T22633

Pack Size	Availability	Price/USD	Quantity
5 mg	Inquiry	$ 329.00
25 mg	Inquiry	$ 1,120.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	CCT251545 analog is a potent and selective CDK8/19 inhibitor (IC50: 5.1 nM and 5.6 nM, respectively). Mediator complex-associated kinases CDK8 and CDK19 are involved in the regulation of multiple transcription pathways. CDK8 plays as an oncogene in gastric and colorectal cancers through the activation of WNT signaling.
In vitro	In SW620 human colorectal carcinoma cells harbouring activating APC-mutation, Compound 51 inhibited phospho-STAT1SER727 ( IC50 :17.9 nM). It is a biomarker of CDK8 inhibition [1].
In vivo	In vivo mouse and rat PK experiments, The compound demonstrated medium in vivo clearance and Vd but low bioavailability in mice. In an SW620 colorectal carcinoma human tumor xenograft model, Compound 51 (5 mg/kg p.o. dose) inhibited phospho-STAT1SER727 in a time-dependent way. Compound 51 is an advanced chemical tool to further explore the efficacy, safety, and tolerability of dual CDK8/19 ligands [1].

Molecular Weight	414.46
Formula	C23H22N6O2
CAS No.	T22633

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: > 20.7 mg/mL, Heating is recommended.

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CCT251545 analogue, Compound 51 T22633 Others CCT-251545 analogue, Compound 51 inhibitor inhibit

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