TG 100801

SKU: orb1708359

Description

TG-100801 is a dual VEGFR2 and Src/YES kinase inhibitor investigated as a potential therapeutic for age-related macular degeneration (AMD). It has demonstrated efficacy in preclinical models, reducing choroidal neovascularization in vivo and inhibiting endothelial cell proliferation in vitro.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 867331-82-6
• MW: 580.08
• Purity: >99.99% (May vary between batches)
• Formula: C₃₃H₃₀ClN₅O₃
• SMILES: Cc1cc(cc2nnc(Nc3ccc(OCCN4CCCC4)cc3)nc12)-c1cc(OC(=O)c2ccccc2)ccc1Cl
• Target: PDGFR,Src,VEGFR,FGFR
• Solubility: DMSO:3 mg/mL (5.17 mM);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  PDGFRβ:13 nM|FGFR1:2 nM|VEGFR1:2 nM|FGFR2:16 nM|VEGFR2:7 nM
• In Vivo:
  TG 100801 is formed by derivatizing the phenol moiety in TG100572 to produce an ester, striking an optimal balance between stability (physical and chemical) and hydrolysis rate among the prodrugs examined. TG100801 does not exhibit meaningful kinase activity but exposure to esterases (abundant in mammalian tissues) rapidly releases active TG 100572. Mice receiving daily intraperitoneal injections of TG 100572 (5 mg/kg) display smaller CNV lesions compared to vehicle-injected mice.
  Read more...
• In Vitro:
  TG100801 is a locally administered prodrug that readily converts to active TG100572. TG100572 inhibits endothelial cell proliferation in vitro (ED50 = 610 ± 71 nM) and blocks the phosphorylation of extracellular signal-regulated kinase (ERK) induced by VEGF .
  Read more...

Storage & Handling

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

Alternative Names

TG 100801, TG 100572, TG100801, TG-100801, Src, PDGFRβ, Yes, VEGFR2, VEGFR1, FGFR1, FGFR2

Compound Identifiers

PubChem CID

11973736