Linperlisib (YY-20394)

InvivoChem Cat #:V5059CAS #:1702816-75-8Purity >=98%

Description: Linperlisib (YY-20394; PI3Kdelta-IN-2)is a novel, potent, orally bioavailable, and highly selective PI3Kdelta inhibitor that was being investigated in a phase I trial for patients with relapse or refractory B-cell malignancies. YY-20394 was developed with specific selectivity against PI3Kdelta and inhibited PI3Kdelta expressing human tumor cells growth both in vitro and in vivo. In addition, YY-20394 significantly inhibited primary tumor growth in immune-competent mice with 4T1 and CT26 tumors, as well as 4T1 lung metastasis with dose dependency. The anti-tumor efficacy of YY-20394 was largely mediated by T cells. More importantly, YY-20394 synergistically enhanced the anti-tumor efficacy of anti-PD-L1 antibody in CT26 model and achieved long-term immune memory which is specific for CT26 tumors, but not for unrelated A20 tumors. In vitro mechanistic studies showed YY-20394 significantly inhibited T cell differentiation into Treg both in mouse splenocyte and in human primary CD4+ T cells, and was especially potent inhibiting their IL-10 secretion in vitro. Analyses of tumors treated with YY-20394 reviewed that YY-20394 decreased the percentage of Treg in the tumor infiltrating leukocytes, as well as IL-10 secretion. It also showed some effects on the myeloid populations in the tumors. These data suggest the YY-20394, a novel PI3Kdelta inhibitor, represents a promising and safe immune modulator and shows great potential as a cancer immuno-therapeutics.

References: https://cancerres.aacrjournals.org/content/77/13_Supplement/5675

-20C for 3 years in powder form

Synonym: YY-20394; YY 20394; YY20394
Chemical Name: Methanesulfonamide, N-(5-(6-fluoro-8-((4-(1-hydroxy-1-methylethyl)-1-piperidinyl)methyl)-2-(4-morpholinyl)-4-quinazolinyl)-2-methoxy-3-pyridinyl)-
InChi Key: NVWKNQGHVMMAJW-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H37FN6O5S/c1-28(2, 36)20-5-7-34(8-6-20)17-19-13-21(29)15-22-24(31-27(32-25(19)22)35-9-11-40-12-10-35)18-14-23(33-41(4, 37)38)26(39-3)30-16-18/h13-16, 20, 33, 36H, 5-12, 17H2, 1-4H3
SMILES Code: CS(=O)(NC1=CC(C2=C3C=C(F)C=C(CN4CCC(C(C)(O)C)CC4)C3=NC(N5CCOCC5)=N2)=CN=C1OC)=O