Senexin C

SKU: orb1687341

Description

Senexin C is a potent and selective CDK8/19 inhibitor with oral bioavailability, demonstrating improved metabolic stability and potency over Senexin B. It exhibits anticancer activity by inhibiting the proliferation of MV4-11 leukemia cells in vitro, supporting its investigation in oncology research.

Research Area

Cell Biology

Key Properties

• CAS Number: 2375554-02-0
• MW: 449.55
• Purity: 98.06% (May vary between batches)
• Formula: C₂₈H₂₇N₅O
• SMILES: N#CC=1C=CC2=NC=CC(NCCC=3C=CC4=CC(=CC=C4C3)C(=O)N5CCN(C)CC5)=C2C1
• Target: CDK
• Solubility: DMSO:20 mg/mL (44.49 mM);10% DMSO+90% Saline:2 mg/mL (4.45 mM)

Bioactivity

• Target IC50:
  CDK8-CyclinC:3.6 nM|CDK8-CyclinC:1.4 nM (Kd)|CDK8-CyclinC:2.9 nM (Kd)
• In Vivo:
  Tumor-bearing mice（CT26 tumor mode） received Senexin C via intravenous injection at 2.5 mg/kg or orally at 100 mg/kg, and compound concentrations in blood and tumors were measured by LC-MS/MS. The results indicated that Senexin C exhibits favorable tumor PK characteristics and low toxicity.
• In Vitro:
  Senexin C exhibits high selectivity for CDK8 and CDK19, with similar Kd values of 55 nM and 44 nM respectively for ATP analog binding, while showing much higher Kd values for the other three non-target kinases (HASPIN: 1000 nM; MAP4K2: 940 nM; MYO3B: > 30,000 nM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK19, CDK8

Compound Identifiers

PubChem CID

146403432