网站主页 > 化工产品目录 > 生物化工 > 抑制剂 > PI3K/Akt/mTOR抑制剂(PI3K/Akt/mTOR) > PI3K 抑制剂 > (S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮

(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮

(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮 更多供应商
公司名称:上海波以尔化工有限公司  
联系电话:86-21-50180596
产品介绍:中文名称:(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮
英文名称:(S)-1-4-2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno3,2-dpyrimidin-6-ylmethylpiperazin-1-yl-2-hydroxypropan-1-one
CAS:1032754-93-0
公司名称:百灵威科技有限公司  
联系电话:400-666-7788 +86-10-82848833
产品介绍:英文名称:GDC-0980
CAS:1032754-93-0
包装信息:0.5Mg,1Mg,200Mg,50Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称:上海佰世凯化学科技有限公司  
联系电话:+86(0)21-20908456
产品介绍:英文名称:GDC-0980 (RG7422)
CAS:1032754-93-0
备注:C13709
公司名称:武汉永璨生物科技有限公司  
联系电话:0086-27-5925 3327; QQ:40199614
产品介绍:英文名称:GDC-0980
CAS:1032754-93-0
纯度:98% 包装信息:1g,5g,10g,50g 备注:only used for research
公司名称:VDM Biochemicals   
联系电话:0330-2528181
产品介绍:英文名称:GDC 0980
CAS:1032754-93-0
纯度:>=99%
最新发布供应信息
GDC-0980_ChemScene, LLC
2016/6/18 9:20:44
GDC0980_-
2012/8/16 13:27:51
(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮
生物活性 体外研究 体内研究 特征
中文名称:(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮
中文同义词:(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮;RG7422;GDC-0980 (RG7422);GNE 390; GDC 0980; RG 7422
英文名称:(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one
英文同义词:(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one;GNE 390;GDC-0980;(S)-1-(4-((2-(2-aMinopyriMidin-5-yl)-7-Methyl-4-Morpholinothieno[3,2-d]pyriMidin-6-yl)Methyl)piperazin-1-yl)-2-hydroxypropan-1-one;GDC-0980 (RG7422);Apitolisib;Apitolisib (GDC-0980, RG7422);(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one GNE 390 GDC0980(RG7422)
CAS号:1032754-93-0
分子式:C23H30N8O3S
分子量:498.61
EINECS号:
相关类别:An inhibitor of Class I PI3 kinase and mTOR kinase.;PI3K/Akt/mTOR;小分子抑制剂;Inhibitors;小分子抑制剂,天然产物;Akt;mTOR;PI3K
Mol文件:1032754-93-0.mol
(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮
(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮 性质
密度 1.399
(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮 用途与合成方法
生物活性GDC-0980 (RG7422)是一种有效的,I型PI3K抑制剂,作用于PI3Kα/β/δ/γ,IC50分别为5 nM/27 nM/7 nM/14 nM,也抑制mTOR,Ki为17 nM,高选择性作用于其他PIKK家族激酶。Phase 2。
体外研究GDC-0980 shows the potent and selective inhibitory activities against class I PI3K and mTOR kinase versus a large panel of kinases with Ki of 17 nM for mTOR and IC50 of 5 nM, 27 nM, 7 nM, and 14 nM for PI3Kα, β, δ, and γ, respectively. In vitro, GDC-0980 significantly inhibits cell proliferation in PC3 and MCF7 cells with IC50 of 307 nM and 255 nM, respectively. A recent study shows that GDC-0980 reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200 nM 50%), <500 nM 100%), breast (IC50 <200 nM 37%, <500 nM 78%) and NSCLC lines (IC50 <200 nM 29%, <500 nM 88%) and less potency in pancreatic (IC50 <200 nM 13%, <500 nM 67%) and melanoma cell lines (IC50 <200 nM 0%, <500 nM 33%).
体内研究In both PC-3 and MCF-7 neo/HER2 xenograft models, GDC-0980 at a dose of 1 mg/kg, exhibits significant antitumor activity by causing tumor growth delay. Furthermore, GDC-0980 results in tumor stasis or regressions at the maximum tolerated dose of 7.5 mg/kg. In mice, intravenous GDC-0980 administration at 1 mg/kg leads to low clearance (Clp: 9.2 mL/min/kg, Vss: 1.7 L/kg). While, oral administration at 5 mg/kg in 80% PEG400 and at 50 mg/kg as a crystalline suspension in 0.5% methylcellulose/0.2% Tween-80 also results in favorable pharmacokinetic parameters.
特征GDC-0980 (RG7422) is a potent, selective, and orally available inhibitor of PI3Kα, β, δ, γ and mTOR.
安全信息
"(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮" 相关产品信息
BKM120 (NVP-BKM120, Buparlisib) MK-2206 2HCl GDC0068,RG7440 (2S)-N1-[4-甲基-5-[2-(2,2,2-三氟-1,1-二甲基乙基)-4-吡啶基]-2-噻唑基]-1,2-吡咯烷二甲酰胺 Pictilisib (GDC-0941) BEZ235 (NVP-BEZ235, Dactolisib)