2126737-28-6
中文名稱
化合物 SB02024
英文名稱
4-[(3R)-3-methylmorpholin-4-yl]-6-[(2R)-2-(trifluoro
methyl)piperidin-1-yl]-1,2-dihydropyridin-2-one
CAS
2126737-28-6
分子式
C16H22F3N3O2
分子量
345.36
MOL 文件
2126737-28-6.mol
2126737-28-6 結(jié)構(gòu)式
基本信息
中文別名
化合物 SB02024 英文別名
4-[(3R)-3-methylmorpholin-4-yl]-6-[(2R)-2-(trifluoro
methyl)piperidin-1-yl]-1,2-dihydropyridin-2-one物理化學性質(zhì)
沸點432.2±45.0 °C(Predicted)
密度1.288±0.06 g/cm3(Predicted)
溶解度Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml
酸度系數(shù)(pKa)10.99±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
應(yīng)用領(lǐng)域
用途一
SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity to Sunitinib and Erlotinib and that Vps34 is a promising therapeutic target for combination strategies in breast cancer.