TG 100572 Hydrochloride

SKU: orb1309010

Description

TG 100572 Hydrochloride is a potent multi-targeted kinase inhibitor with activity against key receptor tyrosine kinases (VEGFR1/2, FGFR1/2, PDGFRβ) and Src-family kinases (Lck, Src, Yes, etc.). Its inhibitory profile supports its use in preclinical research for investigating angiogenesis and oncogenic signaling pathways in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 867331-64-4
• MW: 512.43
• Purity: 98.00% (May vary between batches)
• Formula: C₂₆H₂₇Cl₂N₅O₂
• SMILES: Cl.Cc1cc(cc2nnc(Nc3ccc(OCCN4CCCC4)cc3)nc12)-c1cc(O)ccc1Cl
• Target: PDGFR,Src,VEGFR,FGFR
• Solubility: 10% DMSO+90% Saline:2 mg/mL (3.9 mM);DMSO:20 mg/mL (39.03 mM)

Bioactivity

• Target IC50:
  FGFR1:2 nM|PDGFRβ:13 nM|VEGFR2:7 nM|VEGFR1:2 nM|FGFR2:16 nM
• In Vivo:
  Systemic delivery of TG 100572 in a murine model of laser-induced choroidal neovascularization (CNV) significantly suppresses CNV, but is associated with weight loss indicative of systemic toxicity. TG 100572 (23.4 μM) reaches the choroid and sclera within 30 minutes (Tmax = 0.5 h), with relatively low levels in the retina. Due to its short half-life in ocular tissues, TG 100572 is administered topically at least t.i.d. to maintain appropriate eye levels. The maximum concentration achievable in formulations is 0.7% w/v.
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• In Vitro:
  apoptosis in rapidly proliferating, but not quiescent, endothelial cell cultures induced by TG 100572. TG 100572 is shown to inhibit hRMVEC cell proliferation(IC50 of 610±72 nM). TG 100572 has the therapeutic potential to inhibit VEGF function in ocular endothelial cells, a contributing factor to pathological angiogenesis in diseases such as AMD and PDR.
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Storage & Handling

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

Alternative Names

Src, PDGFR, PDGFRβ, Platelet-derived growth factor receptor, TG 100572, TG 100572 Hydrochloride, TG100572, TG-100572, TG100572 Hydrochloride, TG-100572 Hydrochloride, Vascular endothelial growth factor receptor, VEGFR, VEGFR1, VEGFR2, inhibit, Inhibitor, Fibroblast growth factor receptor, FGFR1, FGFR2, FGFR

Compound Identifiers

PubChem CID

24823567