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 > PKI-402

PKI-402

PKI-402 更多供应商
公司名称: 上海波以尔化工有限公司  
联系电话:
产品介绍: 英文名称:PKI-402
CAS:1173204-81-3
公司名称: 上海佰世凯化学科技有限公司  
联系电话: 021-20908456
产品介绍: 英文名称:PKI 402
CAS:1173204-81-3
备注:C14733
公司名称: 上海景颜化工科技有限公司  
联系电话: 13817811078
产品介绍: 英文名称:PKI-402
纯度:98%
公司名称: VDM Biochemicals   
联系电话: 0330-2528181
产品介绍: 英文名称:PKI402
CAS:1173204-81-3
纯度:>=98%
公司名称: 济南精合医药科技有限公司  
联系电话: +86 (531) 88811783
产品介绍: 英文名称:PKI-402
CAS:1173204-81-3
纯度:99% 包装信息:5Mg, 10Mg, 20Mg, 50Mg 备注:细胞信号通路抑制剂
最新发布供应信息
PI3K/mTOR双重抑制剂(PKI-402)
价格:询价
上海泽叶生物科技有限公司
2022/08/09 13:37:17
PKI-402
价格:¥1500mg
南京百鑫德诺生物科技有限公司
2020/03/30 13:12:37
PKI-402
生物活性体外研究体内研究靶点 MSDS 用途与合成方法 PKI-402价格(试剂级) 上下游产品信息
中文名称:PKI-402
中文同义词:1-[4-[3-乙基-7-(吗啉-4-基)-3H-[1,2,3]三唑并[4,5-D]嘧啶-5-基]苯基]-3-[4-[(4-甲基哌嗪-1-基)羰基]苯基]脲;PI3K/MTOR双重抑制剂(PKI-402)
英文名称:PKI-402
英文同义词:1-(4-(3-ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(1-methylpiperazine-4-carbonyl)phenyl)urea;1-(4-(3-ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(4-methylpiperazine-1-carbonyl)phenyl)urea;PKI-402;PKI402;1-(4-(3-Ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(4-methylpiper;PKI-402;1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea;CS-167;Urea, N-[4-[3-ethyl-7-(4-morpholinyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-yl]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-
CAS号:1173204-81-3
分子式:C29H34N10O3
分子量:570.65
EINECS号:
相关类别:信号转导通路激酶抑制剂;细胞生物学试剂;PI3K/Akt/mTOR;Akt;mTOR;PI3K
Mol文件:1173204-81-3.mol
PKI-402
PKI-402 性质
沸点 670.6±55.0 °C(Predicted)
密度 1.43
酸度系数(pKa)13.80±0.70(Predicted)
PKI-402 用途与合成方法
生物活性PKI-402是一种有效的,pan-PI3K/mTOR双重抑制剂,靶向作用于PI3Kα/β/γ/δ和mTOR,IC50分别为2 nM/7 nM/16 nM/14 nM和3 nM,也有效作用于PI3Kα突变型E545K和H1047R。
体外研究Equivalent to the IC50 for wild-type PI3Kα, PKI-402 inhibits E545K and H1047R PI3Kα mutants with IC50 of 3 nM. In a panel of 236 human protein kinases, PKI-402 only displays inhibitory activity against C-Raf and B-Raf with IC50 of 7 μM, and displays little activity against all other kinases with IC50 of > 10 μM. PKI-402 inhibits the growth of human tumor cell lines with IC50 of 6-349 nM. Consistently, PKI-402 inhibits phosphorylation of PI3K and mTOR effector proteins, particularly phosphorylated Akt (p-Akt) at T308 and S473 with IC50 of <10 nM and <30 nM, respectively. PKI-402 inhibits both p70S6K and 4EBP1 phosphorylation with IC50 of <10 nM. PKI-402 inhibits Akt phosphorylation of PRAS40 at T246 with IC50 of <30 nM, and inhibits Akt phosphorylation of ENOS at S1177 and GSK3α/GSK3β at S9/S21 with IC50 of <10 nM. In MDAMB-361, a breast tumor line with mutant PI3K-α (E545K) and elevated levels of Her2 receptor, PKI-402 treatment induces cleaved poly(ADP-ribose) polymerase (PARP), a marker for apoptosis. Less than 10% of MDAMB-361 cells exposed to PKI-402 at 0.3 μM (or higher) for 24 hours remain viable.
体内研究Single dose of PKI-402 (100 mg/kg) suppresses Akt phosphorylation (at T308) and induces cleaved PARP in MDA-MB-361 tumors. In normal tissue (heart and lung), PKI-402 (100 mg/kg) has minimal effect on p-Akt, with no detectable cleaved PARP. Consistently, PKI-402 at 100 mg/kg (daily for 5 days, one round) reduces initial tumor volume of 260 mm3 to 129 mm3 and prevents tumor regrowth for 70 days in MDA-MB-361. PKI-402 significantly inhibits the growth of A549 tumors in nude mice at 25 mg/kg and 50 mg/kg. PKI-402 at 100 mg/kg (daily for 5 days, one round) causes significant (P < 0.01) reduction in tumor growth of U87MG.
靶点

PI3Kα

2 nM (IC 50 )

PI3Kα-H1047R

3 nM (IC 50 )

PI3Kα-E545K

3 nM (IC 50 )

PI3Kβ

7 nM (IC 50 )

PI3Kδ

14 nM (IC 50 )

PI3Kγ

16 nM (IC 50 )

mTOR

3 nM (IC 50 )

安全信息
PKI-402 价格(试剂级)
更新日期产品编号产品名称CAS编号包装价格
2022/07/01HY-10683PKI-4021173204-81-35mg1534元
2022/07/01HY-10683PKI-4021173204-81-310mg2558元
"PKI-402" 相关产品信息()
NVP-BEZ235 依维莫司 硼替佐米 MK-22062HCl IPI-145 Apitolisib(GDC-0980,RG7422)