4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-
Synonym(s):(±)-7-Methyl-2-(morpholin-4-yl)-9-(1-phenylaminoethyl)-pyrido[1,2-a]-pyrimidin-4-one, PI 3-K Inhibitor VI;PI 3-Kβ Inhibitor VI, TGX-221 - CAS 663619-89-4 - Calbiochem
- CAS NO.:663619-89-4
- Empirical Formula: C21H24N4O2
- Molecular Weight: 364.44
- MDL number: MFCD11113209
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-06 15:28:16
What is 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-?
The Uses of 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-
TGX-221 is a potent, selective, and cell permeable inhibitor of Phosphatidylinositol 3-kinase (PI3K) p110β.
What are the applications of Application
PI 3-Kβ Inhibitor VI, TGX-221 is a reversible ATP-competitive inhibitor of PI 3-kinase β
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.
Properties of 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-
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) |
form | Pale yellow solid. |
pka | 3.90±0.50(Predicted) |
color | Off-White to Pale Yellow |
Safety information for 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-
Computed Descriptors for 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-
New Products
ALUMINIUM IODIDE 100 GM BUFFER CAPSULE PH 7.0 - 10 CAP BUFFER SOLUTION PH 9.5 (BORATE) EZEE BLUE GEL STAINER BORAX CARMINE (GRENACHERS ALCOHOLIC) POTASSIUM IODATE - IODIDE SOLN 0.1 N Dabigatran Acyl-O3-D-Glucuronide Trifluoroacetic Acid Salt Isofolic Acid Dabigatran 2-O-acylglucuronide metabolite Dabigatran Acyl-?-D- glucuronide Trifluroacetic Acid Erythromycin EP Impurity A Desloratidine Related Compound ARelated products of tetrahydrofuran
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