WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 202895
Description: TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit.TGX221 selectively inhibits renal cell carcinoma cells with both VHL and SETD2 mutations and links multiple pathways. TGX221 blocks xenograft tumor growth of prostate cancer in nude mice. TGX221 is a selective inhibitor for ccRCC with both VHL and SETD2 mutations. TGX221 also targeted cancer cells with CDKN2A and PTEN mutations. TGX221 also exhibited significant selectivity in inhibiting cell motility and tumourigenesis of ccRCC cells with VHL and SETD2 mutations. TGX221 is a novel inhibitor with high selectivity for ccRCC with VHL and SETD2 mutations.
MedKoo Cat#: 202895
Chemical Formula: C21H24N4O2
Exact Mass: 364.18993
Molecular Weight: 364.44
Elemental Analysis: C, 69.21; H, 6.64; N, 15.37; O, 8.78
Synonym: TGX221; TGX221; TGX 221.
IUPAC/Chemical Name: 7-methyl-2-morpholino-9-(1-(phenylamino)ethyl)-4H-pyrido[1,2-a]pyrimidin-4-one
InChi Key: CPRAGQJXBLMUEL-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H24N4O2/c1-15-12-18(16(2)22-17-6-4-3-5-7-17)21-23-19(13-20(26)25(21)14-15)24-8-10-27-11-9-24/h3-7,12-14,16,22H,8-11H2,1-2H3
SMILES Code: O=C1C=C(N2CCOCC2)N=C3N1C=C(C)C=C3C(NC4=CC=CC=C4)C
TGX-221 is a LY294002 (structure shown below) analogue, able to inhibit selectively the PI3Kβ isoform in vitro. The observed inhibition of platelet-ECC interaction and platelet activation by tirofiban contributes to explain the mechanism of "platelet anaesthesia". TGX-221 represents a promising alternative to GP IIb/IIIa blockade and should be further investigated for use during ECC in vivo. see http://www.ncbi.nlm.nih.gov/pubmed/18327411.
1: Feng C, Sun Y, Ding G, Wu Z, Jiang H, Wang L, Ding Q, Wen H. PI3Kβ inhibitor TGX221 selectively inhibits renal cell carcinoma cells with both VHL and SETD2 mutations and links multiple pathways. Sci Rep. 2015 Apr 8;5:9465. doi: 10.1038/srep09465. PubMed PMID: 25853938.
2: Chen R, Zhao Y, Huang Y, Yang Q, Zeng X, Jiang W, Liu J, Thrasher JB, Forrest ML, Li B. Nanomicellar TGX221 blocks xenograft tumor growth of prostate cancer in nude mice. Prostate. 2015 May;75(6):593-602. doi: 10.1002/pros.22941. Epub 2015 Jan 25. PubMed PMID: 25620467; PubMed Central PMCID: PMC4376584.
3: Ukhanov K, Corey EA, Ache BW. Phosphoinositide 3-kinase dependent inhibition as a broad basis for opponent coding in Mammalian olfactory receptor neurons. PLoS One. 2013 Apr 9;8(4):e61553. doi: 10.1371/journal.pone.0061553. Print 2013. PubMed PMID: 23585911; PubMed Central PMCID: PMC3621990.
4: Moir LM, Trian T, Ge Q, Shepherd PR, Burgess JK, Oliver BG, Black JL. Phosphatidylinositol 3-kinase isoform-specific effects in airway mesenchymal cell function. J Pharmacol Exp Ther. 2011 May;337(2):557-66. doi: 10.1124/jpet.110.173583. Epub 2011 Feb 24. PubMed PMID: 21349933.
5: Lu XY, Ciraolo E, Stefenia R, Chen GQ, Zhang Y, Hirsch E. Sustained release of PI3K inhibitor from PHA nanoparticles and in vitro growth inhibition of cancer cell lines. Appl Microbiol Biotechnol. 2011 Mar;89(5):1423-33. doi: 10.1007/s00253-011-3101-1. Epub 2011 Feb 1. PubMed PMID: 21286711.
6: Sturgeon SA, Jones C, Angus JA, Wright CE. Advantages of a selective beta-isoform phosphoinositide 3-kinase antagonist, an anti-thrombotic agent devoid of other cardiovascular actions in the rat. Eur J Pharmacol. 2008 Jun 10;587(1-3):209-15. doi: 10.1016/j.ejphar.2008.03.017. Epub 2008 Mar 29. PubMed PMID: 18455722.
(Last Updated: 4/20/2016)