4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐
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- CAS号:
- 1431697-86-7
- 英文名:
- AT 7867 dihydrochloride
- 英文别名:
- AT7867 hcl;AT7867 2HCl;AT 7867 dihydrochloride;AT-7867 dihydrochloride;AT7867 (dihydrochloride);AT-7867 DIHYDROCHLORIDE;AT 7867 DIHYDROCHLORIDE;4-(4-Chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine hydrochloride (1:2)
- 中文名:
- 4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐
- 中文别名:
- 化合物 T21624;AT7867 盐酸盐;4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐;AKT1/AKT2/AKT3和P70S6K/PKA抑制剂(AT7867 DIHYDROCHLORIDE)
- CBNumber:
- CB82666590
- 分子式:
- C20H21Cl2N3
- 分子量:
- 374.31
- MOL File:
- 1431697-86-7.mol
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4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐性质、用途与生产工艺
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
)
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Akt2
17 nM (IC
50
)
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Akt3
47 nM (IC
50
)
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PKA
20 nM (IC
50
)
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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
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上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-12059A | AT7867 dihydrochloride | | 1 mg | 545元 |
2024/04/30 | HY-12059A | 4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐 AT7867 dihydrochloride | 1431697-86-7 | 5mg | 1200元 |
4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐
生产厂家
1431697-86-7, 4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐 相关搜索:
- 细胞生物学试剂
- C20H22Cl3N3
- C20H20ClN32HCl
- 化合物 T21624
- AT7867 盐酸盐
- AKT1/AKT2/AKT3和P70S6K/PKA抑制剂(AT7867 DIHYDROCHLORIDE)
- 4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶二盐酸盐
- 1431697-86-7
- AT7867 hcl
- AT-7867 DIHYDROCHLORIDE;AT 7867 DIHYDROCHLORIDE
- AT7867 2HCl
- 4-(4-Chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine hydrochloride (1:2)
- AT-7867 dihydrochloride
- AT7867 (dihydrochloride)
- AT 7867 dihydrochloride