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TG100801

Product Name
TG100801
CAS No.
867331-82-6
Chemical Name
TG100801
Synonyms
TG100801;TG100801;TG-100801;4-Chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-amino)benzo[e][1,2,4]triazin-7-y;4-Chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-amino)benzo[e][1,2,4]triazin-7-yl)p;4-Chloro-3-(5-methyl-3-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)benzo[e][1,2,4]triazin-7-yl)phenyl benzoate;4-Chloro-3-[5-methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-1,2,4-benzotriazin-7-yl]phenol 1-benzoate;Phenol, 4-chloro-3-[5-Methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]aMino]-1,2,4-benzotriazin-7-yl]-, 1-benzoate
CBNumber
CB22583019
Molecular Formula
C33H30ClN5O3
Formula Weight
580.08
MOL File
867331-82-6.mol
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TG100801 Property

Boiling point:
747.9±70.0 °C(Predicted)
Density 
1.310
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Powder
pka
9.59±0.20(Predicted)
color 
Brown to reddish brown
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0785
Product name
TG100801
Purity
98.60%
Packaging
5mg
Price
$264
Updated
2021/12/16
ApexBio Technology
Product number
A3870
Product name
TG100801
Packaging
5mg
Price
$322
Updated
2021/12/16
ChemScene
Product number
CS-0785
Product name
TG100801
Purity
98.60%
Packaging
10mg
Price
$456
Updated
2021/12/16
ApexBio Technology
Product number
A3870
Product name
TG100801
Packaging
10mg
Price
$557
Updated
2021/12/16
Matrix Scientific
Product number
098186
Product name
4-Chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-amino)benzo[e][1,2,4]triazin-7-yl)phenyl benzoate
Purity
95+%
Packaging
250mg
Price
$742
Updated
2021/12/16
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TG100801 Chemical Properties,Usage,Production

Uses

TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 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.

Biological Activity

tg100801 is a multi-kinases inhibitor. it is a pro-drug version of tg100572. [1]tg100572 inhibits several growth factor receptors in addition to src family kinases. tg100801 significantly inhibited laser-induced cnv in mice, and suppressed fluorescein leakage from the vasculature and retinal thickening measured by optical coherence tomography in a rat model or retinal vein occlusion. tg100801 may play as a new topically applied treatment approach for ocular neovascularization and retinal edema. the highest concentration of tg100801 was found at the front of the rat eye (conjunctiva and cornea). [1]

in vivo

TG 100801 exhibits excellent ocular pharmacokinetics and poor systemic circulation and shows good efficacy in the laser induced choroidal neovascularization model. 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[1]. TG 100801 nor TG100572 are detectable in plasma following topical delivery of TG 100801, and adverse safety signals (such as weight loss) are not observed even with prolonged dosing schedules. Topical TG 100801 significantly suppresses laser-induced choroidal neovascularlization in mice, and reduces fluorescein leakage from the vasculature and retinal thickening measured by optical coherence tomography in a rat model or retinal vein occlusion.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[2].

target

VEGFR1

IC 50

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

References

1. doukas j, mahesh s, umeda n 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.

TG100801 Preparation Products And Raw materials

Raw materials

Preparation Products

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TG100801 Suppliers

China 50 United States 5 Global 55
Nanjing JinruiJiuAn Biotechnology Co., Ltd.
Tel
025-58196018 800028039
Fax
025-83453306
Email
sales@fartop.net
Country
China
ProdList
2229
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
SPIRO PHARMA
Tel
Fax
-
Email
eric_feng1954@126.com
Country
China
ProdList
9248
Advantage
55
Guangzhou QiYun Biotechnology Co., Ltd.
Tel
020-61288194 61288195
Fax
020-61288700
Email
505721671@qq.com
Country
China
ProdList
3866
Advantage
58
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
Amatek Scientific Co. Ltd.
Tel
0512-56316828
Fax
0512-56316826
Email
info@amateksci.com
Country
China
ProdList
28774
Advantage
58
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
Henan Alfachem Co.,Ltd.
Tel
0371-55051623 18137891487
Fax
QQ：2853979817
Email
3983243027@qq.com
Country
China
ProdList
9985
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32470
Advantage
58

867331-82-6, TG100801Related Search:


  • TG100801
  • Phenol, 4-chloro-3-[5-Methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]aMino]-1,2,4-benzotriazin-7-yl]-, 1-benzoate
  • 4-Chloro-3-[5-methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-1,2,4-benzotriazin-7-yl]phenol 1-benzoate
  • 4-Chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-amino)benzo[e][1,2,4]triazin-7-yl)p
  • 4-Chloro-3-(5-methyl-3-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)benzo[e][1,2,4]triazin-7-yl)phenyl benzoate
  • 4-Chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-amino)benzo[e][1,2,4]triazin-7-y
  • TG100801;TG-100801
  • 867331-82-6
  • C33H30ClN5O3