955977-50-1
中文名稱
N/A
英文名稱
PI-3065
CAS
955977-50-1
分子式
C27H31FN6OS
分子量
506.638
MOL 文件
955977-50-1.mol
更新日期
2024/12/10 12:46:01
955977-50-1 結(jié)構(gòu)式
基本信息
中文別名
4-(6-((4-(環(huán)丙基甲基)哌嗪-1-基)甲基)-2-(5-氟-1H-吲哚-4-基)噻吩并[3,2-D]嘧啶-4-基)嗎啉6-[[4-(環(huán)丙基甲基)-1-哌嗪基]甲基]-2-(5-氟-1H-吲哚-4-基)-4-(4-嗎啉基)噻吩并[3,2-D]嘧啶
英文別名
129556PI-306
PI-3065
CS-1274
PI-3065, >=98%
PI-3065|PI3065
PI-3065 USP/EP/BP
4-(6-((4-(Cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyri
6-((4-(cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)-4-morpholinothieno[3,2-d]pyrimidine
6-(4-CyclopropylMethyl-piperazin-1-ylMethyl)-2-(5-fluoro-1H-indol-4-yl)-4-Morpholin-4-yl-thieno[3,2-d]pyriMidine
所屬類別
生物化工：PI3K 抑制劑物理化學(xué)性質(zhì)
密度1.372±0.06 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,Store in freezer, under -20°C
溶解度≥22.7 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
酸度系數(shù)(pKa)14.80±0.30(Predicted)
形態(tài)固體
顏色White to off-white
CAS 數(shù)據(jù)庫(kù)955977-50-1
常見(jiàn)問(wèn)題列表
生物活性
PI-3065是一種選擇性p110δ抑制劑，IC50為15 nM,選擇性比其他PI3K家族成員高出70多倍。體外研究
PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ.體內(nèi)研究
In mouse model, PI-3065 (75 mg/kg, p.o.) also suppresses 4T1 tumor growth and metastasis via inactivation of p110δ. In the LSL.KrasG12D/+; p53R172H/+; PdxCretg/+ (or KPC) model of pancreatic ductal adenocarcinoma, PI-3065 prolongs survival and reduces the incidence of macroscopic metastases and other disease-associated pathologies.靶點(diǎn)
|
p110α 910 nM (IC 50 ) |
p110β 600 nM (IC 50 ) |
p110δ 5 nM (IC 50 ) |