TGR-1202

• CAT Number: I001918
• CAS Number: 1532533-67-7
• Molecular Formula: C₃₁H₂₄F₃NO₃
• Molecular Weight: 571.56
• Purity: ≥95%
• Target: PI3Kdelta
• Solubility: 10mM in DMSO
• Storage: 3 years -20C powder
• Related CAS: 1532533-75-7 ( TGR-1202 sulfate)
• IC50: 22.2 nM
• InChI: InChI=1S/C31H24F3N5O3/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29/h4-16H,1-3H3,(H2,35,36,37)/t16-/m0/s1
• InChIKey: IUVCFHHAEHNCFT-INIZCTEOSA-N
• SMILES: C(C)OC1=C(C=C(C=C1)C2=NN(C3=C2C(=NC=N3)N)C(C)C4=C(C(=O)C5=C(O4)C=CC(=C5)F)C6=CC(=CC=C6)F)F

TGR-1202 (CAT: I001918) is a small molecule inhibitor that targets the enzyme phosphoinositide 3-kinase delta (PI3Kδ). PI3Kδ is involved in signaling pathways that regulate cell growth, survival, and immune function. TGR-1202 specifically inhibits PI3Kδ and has shown promising results in preclinical and clinical studies as a potential treatment for hematologic malignancies, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL). By selectively targeting PI3Kδ, TGR-1202 aims to disrupt the signaling pathways that contribute to cancer cell growth and survival. It is currently being evaluated in clinical trials to determine its safety and efficacy in various cancer indications.

Reference

1: Locatelli SL, Careddu G, Inghirami G, Castagna L, Sportelli P, Santoro A,
Carlo-Stella C. The novel PI3K-δ inhibitor TGR-1202 enhances Brentuximab
Vedotin-induced Hodgkin lymphoma cell death via mitotic arrest. Leukemia. 2016
Dec;30(12):2402-2405. doi: 10.1038/leu.2016.224. Epub 2016 Aug 8. PubMed PMID:
27499137.