Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  Pharmaceutical intermediates >  Heterocyclic compound >  Pyridine compound >  Ethylpyridine >  4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-

4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-

Basic information Safety Supplier Related

4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- Basic information

Product Name:
4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-
Synonyms:
  • 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-
  • CS-429
  • TGX-221; TGX 221
  • TGX-221, PI3K Inhibitor (±
  • TGX221; TGX221; TGX 221.
  • TGX 221
  • (+/-)-7-Methyl-2-(morpholin-4-yl)-9-(1-phenylaminoethyl)pyrido[1,2-a]pyrimidin-4-one
  • 7-methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one
CAS:
663619-89-4
MF:
C21H24N4O2
MW:
364.44
Product Categories:
  • Inhibitors
  • Akt
  • mTOR
  • PI3K
Mol File:
663619-89-4.mol
More
Less

4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- Chemical Properties

Melting point:
198-201oC
Boiling point:
557.3±60.0 °C(Predicted)
Density 
1.25±0.1 g/cm3(Predicted)
storage temp. 
Hygroscopic, Refrigerator, under inert atmosphere
solubility 
DMSO (Slightly), Methanol (Very Slightly)
pka
3.90±0.50(Predicted)
form 
Pale yellow solid.
color 
Off-White to Pale Yellow
More
Less

4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- Usage And Synthesis

Uses

TGX-221 is a potent, selective, and cell permeable inhibitor of Phosphatidylinositol 3-kinase (PI3K) p110β.

Definition

ChEBI: 9-(1-anilinoethyl)-7-methyl-2-(4-morpholinyl)-4-pyrido[1,2-a]pyrimidinone is a pyridopyrimidine.

General Description

A cell-permeable morpholino-pyrimidinone compound that acts as a reversible, ATP-competitive, selective, and highly potent inhibitor of PI 3-Kβ (IC50 = 0.005, 0.1, 5, and ≥3.5 μM for -β, -δ, -α and -γ isoforms, respectively) with little activity against a panel of 15 commonly studied protein kinases even at concentrations as high as 10.0 μM. An excellent tool for studying p110β-dependent responses both in cells in vitro and in animals in vivo.

Biological Activity

tgx-221 is a potent inhibitor of (phosphatidylinositol 3-kinases) pi3k which specifically inhibits pi3k -p110β isoform with ic50 value of 8.5 nm [1].in j774.2 macrophage cells, tgx-221 has been demonstrated to reduce insulin-induced phosphorylation of ser473 of protein kinase b (pkb). while in in cho-ir and 3t3-l1 cells, tgx-221 has no effect on pkb phosphprylation [1].

Biochem/physiol Actions

Cell permeable: yes

in vivo

tgx-221 significantly improved blood flow in fecl3-induced arterial thrombosis as well as increased tail and renal bleeding times in mice. in addition, tgx-221 has revealed to disrupt cfrs in a folts model of arterial thrombosis in male sprague-dawley rats [2].

storage

Store at -20°C

References

[1] chaussade c1, rewcastle gw, kendall jd, denny wa, cho k, gr nning lm, chong ml, anagnostou sh,jackson sp, daniele n, shepherd pr. evidence for functional redundancy of class ia pi3k isoforms in insulin signalling. biochem j. 2007 jun 15;404(3):449-58.
[2] bird je1, smith pl, bostwick js, shipkova p, schumacher wa. bleeding response induced by anti-thrombotic doses of a phosphoinositide 3-kinase (pi3k)-β inhibitor in mice. thromb res. 2011 jun;127(6):560-4.

4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Chembest Research Laboratories Limited
Tel
021-20908456
Email
sales@BioChemBest.com
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 17702719238
Email
sales@sun-shinechem.com
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Email
sales@trio-pharmatech.com (International market)
Xi’an chemsoar Medical Technology Co., ltd
Tel
029-86538357
More
Less

4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-(663619-89-4)Related Product Information