基本属性 生物活性靶点体外研究体内研究 用途与合成方法 4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐 价格(试剂级) 供应商 供应信息
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4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐

4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐

英文名称:AT 7867 dihydrochloride
CAS号:1431697-86-7
分子式:C20H21Cl2N3
分子量:374.31
EINECS号:
Mol文件:1431697-86-7.mol
4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐 结构式

4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐 性质

储存条件 Store at -20°C
溶解度 溶于二甲基亚砜
形态 粉末
颜色 白色至米白色

4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐 用途与合成方法

AT7867 dihydrochloride 是一种 ATP 竞争性的 Akt1/Akt2/Akt3 和 p70S6K/PKA 抑制剂,IC50 分别为 32 nM/17 nM/47 nM 和 85 nM/20 nM。

Akt1

32 nM (IC 50 )

Akt2

17 nM (IC 50 )

Akt3

47 nM (IC 50 )

PKA

20 nM (IC 50 )

The inhibition of AKT2 by AT7867 is shown to be ATP-competitive with a K i of 18nM. AT7867 also displays potent activity against the structurally related AGC kinases p70S6K and PKA, but shows a clear window of selectivity against kinases from other kinase sub-families. In vitro growth inhibition studies show that AT7867 blocks proliferation in a number of human cancer cell lines. AT7867 appears to be most potent at inhibiting proliferation in MES-SA uterine, MDA-MB-468 and MCF-7 breast, and HCT116 and HT29 colon lines (IC 50 values range from 0.9-3 μM), and least effective in the two prostate lines tested (IC 50 values range from 10-12 μM) .

Following oral administration at 20 mg/kg, the elimination of AT7867 from plasma appears to be similar to that observed after i.v. administration. Plasma levels of AT7867 remain above 0.5 μM for at least 6 hours following an oral dose of 20 mg/kg. Assuming linear pharmacokinetics following i.v. administration, the bioavailability by the oral route is calculated to be 44%. In vivo pharmacodynamic (PD) biomarker studies are therefore performed with this model. Following pharmacokinetic and tolerability studies, doses of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) are administered to athymic mice bearing MES-SA tumors and the phosphorylation status of GSK3β and S6RP in tumors is monitored over time. Clear inhibition of phosphorylation of the two markers of pathway activity is seen at 2 and 6 hours following treatment with AT7867. By 24 hours, total levels of both GSK3β and S6RP are greatly reduced.

4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-11-08 HY-12059A 1 mg 545
2024-11-08 HY-12059A 4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐 1431697-86-7 5mg 1200

4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐供应商 更多

苏州亚科科技股份有限公司
联系电话:0512-87182056 18013166090
产品介绍:
中文名称:AT7867 盐酸盐
英文名称:AT7867 dihydrochloride
CAS:1431697-86-7
纯度:98%
包装信息:10g;50g;1kg;5Kg;25kg;
南京百鑫德诺生物科技有限公司
联系电话:025-58849295 18951903616;
产品介绍:
英文名称:AT7867 2HCl
CAS:1431697-86-7
纯度:0.98
包装信息:1mg;5mg;10mg;25mg;50mg;100mg
备注:试剂
上海楼岚生物科技有限公司
联系电话:021-52996696,15000506266 15000506266
产品介绍:
英文名称:AT7867 hcl
CAS:1431697-86-7
纯度:98% HPLC
包装信息:5mg,10mg,50mg,100mg,1g,5g
上海源溪生物科技有限公司
联系电话:021-58447131 13564518121
产品介绍:
英文名称:AT7867 (dihydrochloride)
CAS:1431697-86-7
纯度:98% HPLC
包装信息:100mg,250mg,1g
ChemeGen 中国
联系电话: 18818260767
产品介绍:
英文名称:AT7867 dihydrochloride
CAS:1431697-86-7
纯度:98%
包装信息:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
备注:品牌:ChemeGen

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