| Company Name: |
Haoyuan Chemexpress Co., Ltd.
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021-58950125 |
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info@chemexpress.com |
| Products Intro: |
Product Name:TG 100572 (Hydrochloride)
CAS:867331-64-4
Purity:>98% Package:1100RMB/1mg
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Email: |
eric_feng1954@126.com |
| Products Intro: |
Product Name:TG 100572 (Hydrochloride)
CAS:867331-64-4
Purity:95% -98%HPLC Package:1GR;10GR;50GR;100GR;250GR;500GR;1KG;5KG;10KG;100KG
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TG 100572 (Hydrochloride) manufacturers
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| | TG 100572 (Hydrochloride) Basic information |
| Product Name: | TG 100572 (Hydrochloride) | | Synonyms: | 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 | | CAS: | 867331-64-4 | | MF: | C26H27Cl2N5O2 | | MW: | 512.44 | | EINECS: | | | Product Categories: | | | Mol File: | 867331-64-4.mol |  |
| | TG 100572 (Hydrochloride) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: ≥ 44 mg/mL (85.87 mM) | | form | Powder | | color | Pink to red |
| | TG 100572 (Hydrochloride) Usage And Synthesis |
| 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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