CDK8/19-IN-51

SKU: orb1704639

Description

CDK8/19-IN-51 is a potent and orally bioavailable dual inhibitor of CDK8 and CDK19, exhibiting low nanomolar IC50 values. It demonstrates anticancer activity in research models, particularly in studies focusing on colorectal and gastric cancers, and is utilized in both in vitro and in vivo experimental settings.

Research Area

Cell Biology

Key Properties

• CAS Number: 1860885-61-5
• MW: 414.46
• Purity: >99.99% (May vary between batches)
• Formula: C₂₃H₂₂N₆O₂
• SMILES: O=C(C1=NC2=C(C=NC(N)=C2C=C1)C3=CC=C(C=C3)C=4C=NN(C4)C)N5CC(OC)C5
• Target: CDK
• Solubility: DMSO:8 mg/mL (19.3 mM)

Bioactivity

• Target IC50:
  CDK19:5.6 nM|CDK8:5.1 nM|7dF3:7.2 nM|p-STAT1727:17.9 nM
• In Vivo:
  In in vivo pharmacokinetic (PK) studies in mice and rats, CDK8/19-IN-51 exhibited moderate in vivo clearance and volume of distribution (Vd) but showed low bioavailability in mice. In an SW620 human colorectal carcinoma xenograft model, oral administration of CDK8/19-IN-51 (5 mg/kg) inhibited phospho-STAT1^Ser727 in a time-dependent manner. CDK8/19-IN-51 serves as an advanced chemical tool for further investigation of the efficacy, safety, and tolerability of dual CDK8/19 inhibitors .
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• In Vitro:
  In SW620 human colorectal carcinoma cells harboring an activating APC mutation, CDK8/19-IN-51 inhibited phospho-STAT1^Ser727 with an IC50 of 17.9 nM, which serves as a biomarker of CDK8 inhibition .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CCT251545 analogue, Compound 51, CCT-251545 analogue, Compound 51

Compound Identifiers

PubChem CID

118660867