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ChemicalBook--->CAS DataBase List--->867334-05-2

867334-05-2

867334-05-2 Structure

867334-05-2 Structure
IdentificationBack Directory
[Name]

Phenol, 4-chloro-3-[5-Methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]aMino]-1,2,4-benzotriazin-7-yl]-
[CAS]

867334-05-2
[Synonyms]

TG 100572
TG100572;TG-100572
4-Chloro-3-[5-methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-1,2,4-benzotriazin-7-yl]phenol
4-Chloro-3-(5-methyl-3-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)benzo[e][1,2,4]triazin-7-yl)phenol
Phenol, 4-chloro-3-[5-Methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]aMino]-1,2,4-benzotriazin-7-yl]-
[Molecular Formula]

C26H26ClN5O2
[MDL Number]

MFCD16877427
[MOL File]

867334-05-2.mol
[Molecular Weight]

475.97
Chemical PropertiesBack Directory
[Boiling point ]

683.5±65.0 °C(Predicted)
[density ]

1.331±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO: ≥ 150 mg/mL (315.15 mM)
[form ]

Powder
[pka]

8.82±0.18(Predicted)
Hazard InformationBack Directory
[Uses]

TG 100572 is a Src kinase inhibitor.
[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].

[IC 50]

VEGFR1: 2 nM (IC50); VEGFR2: 7 nM (IC50); FGFR1: 2 nM (IC50); FGFR2: 16 nM (IC50); PDGFRβ: 13 nM (IC50)
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