LDC4297

SKU: orb1223294

Description

LDC4297, also known as LCD044297, is a potent and selective CDK7 inhibitor. LDC4297 exerts broad-spectrum antiviral activity. LDC4297 inhibits CDK7 in vitro in the nano-picomolar range. CDK7 inhibitor LDC4297 is a promising candidate for further antiviral drug development, possibly offering new options for a comprehensive approach to antiviral therapy.(In Vitro):LDC4297 (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC50 value of 24.5 nM.LDC4297 (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI50 value of 4.5 μM.LDC4297 (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation.LDC4297 (0-10 μM; 7 d) shows broad antiviral activities to HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7) and Influenza A virus with EC50 values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13 and 0.99 μM, respectively.(In Vivo):LDC4297 (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses.

Key Properties

• CAS Number: 1453834-21-3
• MW: 432.52
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₈N₈O
• SMILES: CC(C)C(C=NN12)=C1N=C(OC3CNCCC3)N=C2NCC4=CC=CC=C4N5N=CC=C5
• Target: EGFR
• Solubility: DMSO : ≥ 60 mg/mL; 138.72 mM

Bioactivity

• In Vivo:
  LDC4297 (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses. Animal model: CD1 mice. Dosage: 100 mg/kg. Administration: Oral gavage; 100 mg/kg once. Result: Showed a half-life of 1.6 h, and the time to a mean peak plasma concentration of 1, 297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.
• In Vitro:
  LDC4297 (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC50 value of 24.5 nM. LDC4297 (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI50 value of 4.5 μM. LDC4297 (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation. LDC4297 (0-10 μM; 7 d) shows broad antiviral activities to HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7) and Influenza A virus with EC50 values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13 and 0.99 μM, respectively. Western blot analysis. Cell line: Primary cultures of fibroblasts derived from human (HFF) with virus infection. Concentration: 20 μM. Incubation time: 12, 24, 48 and 96 hours. Result: Showed inhibitory effect towards viral protein synthesis at the stage of immediate early (IE) gene expression and the drug-mediated reduction of IE1p72 levels partially recovered over time. Exerted an inhibitory effect on human cytomegalovirus (HCMV) induced an up-regulation of protein expression or protein phosphorylation, and reduced Rb expression in the uninfected control cells at 24 h.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LDC4297 | LDC-4297 | LDC 4297 | LCD044297

Quick Database Links

Gene Symbol

EGFR