ChemicalBook > CAS DataBase List > TG 100572 (Hydrochloride)

TG 100572 (Hydrochloride)

Product Name
TG 100572 (Hydrochloride)
CAS No.
867331-64-4
Chemical Name
TG 100572 (Hydrochloride)
Synonyms
TG 100572 HCl;TG 100572 (Hydrochloride);TG100572 HYDROCHLORIDE;TG-100572 HYDROCHLORIDE;4-chloro-3-[5-methyl-3-[4-(2-pyrrolidin-1-ylethoxy)anilino]-1,2,4-benzotriazin-7-yl]phenol;4-Chloro-3-[5-methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-1,2,4-benzotriazin-7-yl]phenol monohydrochloride;Vascular endothelial growth factor receptor,FGFR,TG100572,PDGFR,Inhibitor,TG 100572 Hydrochloride,TG 100572,VEGFR,Platelet-derived growth factor receptor,inhibit,Fibroblast growth factor receptor,TG-100572,Src
CBNumber
CB42628473
Molecular Formula
C26H27Cl2N5O2
Formula Weight
512.44
MOL File
867331-64-4.mol
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TG 100572 (Hydrochloride) Property

storage temp. 
Store at -20°C
solubility 
DMSO: ≥ 44 mg/mL (85.87 mM)
form 
Powder
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0784
Product name
TG100572Hydrochloride
Purity
99.58%
Packaging
1mg
Price
$132
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611444
Product name
TG 100572 hydrochloride
Packaging
5mg
Price
$368.9
Updated
2021/12/16
ChemScene
Product number
CS-0784
Product name
TG100572Hydrochloride
Purity
99.58%
Packaging
10mg
Price
$456
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611444
Product name
TG 100572 hydrochloride
Packaging
10mg
Price
$615.4
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
HCH0316531
Product name
4-CHLORO-3-[5-METHYL-3-[[4-[2-(1-PYRROLIDINYL)ETHOXY]PHENYL]AMINO]-1,2,4-BENZOTRIAZIN-7-YL]PHENOL HYDROCHLORIDE
Purity
95.00%
Packaging
1G
Price
$771.89
Updated
2021/12/16
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TG 100572 (Hydrochloride) Chemical Properties,Usage,Production

Description

TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

in vitro

In Vitro:TG 100572 shows sub-nanomolar activity against the Src family as well as RTK such as VEGFR1 and R2, FGFR1 and R2, and PDGFRβ. TG 100572 inhibits vascular endothelial cell proliferation (ED50=610±71 nM) and blocks VEGF-induced phosphorylation of extracellular signal-regulated kinase. TG 100572 induces apoptosis in rapidly proliferating, but not quiescent, endothelial cell cultures[1]. TG 100572 is shown to inhibit hRMVEC cell proliferation, with an IC50 of 610±72 nM. This suggests that 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[2].

in vivo

In Vivo:Systemic delivery of TG 100572 in a murine model of laser-induced choroidal neovascularization (CNV) causes significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity[1]. A concentration of 23.4 μM (Cmax) of TG 100572 is reached in 30 min (Tmax)=0.5 h) in the choroid and the sclera. However, the levels of TG 100572 in the retina are relatively low. The half-life of TG 100572 in ocular tissues is very short; hence, the compound is administered topically minimum t.i.d. to maintain appropriate drug levels in the eye. The maximum concentration one can achieve in formulations using TG 100572 is 0.7% w/v[2].

References

References:[1]. Doukas J, et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. J Cell Physiol. 2008 Jul;216(1):29-37. [2]. Palanki MS, et al. Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. J Med Chem. 2008 Mar 27;51(6):1546-59.

TG 100572 (Hydrochloride) Preparation Products And Raw materials

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Preparation Products

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TG 100572 (Hydrochloride) Suppliers

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867331-64-4, TG 100572 (Hydrochloride)Related Search:


  • TG 100572 (Hydrochloride)
  • TG 100572 HCl
  • 4-Chloro-3-[5-methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-1,2,4-benzotriazin-7-yl]phenol monohydrochloride
  • TG100572 HYDROCHLORIDE;TG-100572 HYDROCHLORIDE
  • 4-chloro-3-[5-methyl-3-[4-(2-pyrrolidin-1-ylethoxy)anilino]-1,2,4-benzotriazin-7-yl]phenol
  • Vascular endothelial growth factor receptor,FGFR,TG100572,PDGFR,Inhibitor,TG 100572 Hydrochloride,TG 100572,VEGFR,Platelet-derived growth factor receptor,inhibit,Fibroblast growth factor receptor,TG-100572,Src
  • 867331-64-4
  • C26H26ClN5O2HCl
  • C26H27Cl2N5O2