Linperlisib (YY-20394) | PI3Kδ inhibitor | Probechem Biochemicals

Chemical Structure : Linperlisib

CAS No.: 1702816-75-8

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Linperlisib (YY-20394, YY20394)

货号: PC-23166Not For Human Use, Lab Use Only.

Linperlisib (YY-20394) is a potent, selective and orally active PI3Kδ inhibitor (IC50=4.6 nM), inhibitr PI3Kδ expressing human tumor cells growth both in vitro and in vivo.

规格	价格	库存
5 mg	￥1380	In stock
10 mg	￥2180	In stock
25 mg	￥3880	In stock
50 mg	￥5880	In stock
100 mg		Get quote

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生物&药学活性

Linperlisib (YY-20394) is a potent, selective and orally active PI3Kδ inhibitor (IC50=4.6 nM), inhibitr PI3Kδ expressing human tumor cells growth both in vitro and in vivo.
Linperlisib (YY-20394) is less activity against PI3Kγ giving a kinase inhibition profile that is more PI3Kδ-selective by nearly 2 orders of magnitude
Linperlisib (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.
Linperlisib (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.
Linperlisib (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.
Linperlisib (YY-20394) displayed significant anti-tumor efficacy in other syngeneic mouse tumor models tested including mouse colorectal cancer models MC-38 model in C57BL/c mice and CT26 model in BALB/c mice.

物理化学性质&存储条件

分子量	588.70
分子式	C28H37FN6O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[5-[6-fluoro-8-[[4-(1-hydroxy-1-methylethyl)-1-piperidinyl]methyl]-2-(4-morpholinyl)-4-quinazolinyl]-2-methoxy-3-pyridinyl]-methanesulfonamide

参考文献

1. Wang T, et al. Clin Cancer Res. 2023 Apr 14;29(8):1440-1449.

2. Jiang B, et al. J Hematol Oncol. 2021 Aug 23;14(1):130.

3. ZuSheng Xu, et al. Cancer Immunol Res (2016) 4 (11_Supplement): B048.

Linperlisib (YY-20394, YY20394)

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Linperlisib (YY-20394, YY20394)

生物&药学活性

物理化学性质&存储条件

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