A-674563 (hydrochloride)
中文名称 | A-674563 (hydrochloride) |
---|---|
中文同义词 | AKT1抑制剂(A-674563 HYDROCHLORIDE);化合物 A-674563 HYDROCHLORIDE;盐酸盐形式;(S)-1-((5-(3-甲基-1H-吲唑-5-基)吡啶-3-基)氧基)-3-苯基丙烷-2-胺盐酸盐 |
英文名称 | A-674563 (hydrochloride) |
英文同义词 | A-674563 (hydrochloride);A-674563 hydrochloride (A 674563 hydrochloride |
CAS号 | 2070009-66-2 |
分子式 | C22H23ClN4O |
分子量 | 394.9 |
EINECS号 | |
相关类别 | 细胞生物学试剂 |
Mol文件 | 2070009-66-2.mol |
结构式 |
A-674563 (hydrochloride) 性质
Akt1 11 nM (Ki) |
PKA 16 nM (Ki) |
CDK2 46 nM (Ki) |
GSK3β 110 nM (Ki) |
ERK2 260 nM (Ki) |
PKCδ 360 nM (Ki) |
RSK2 580 nM (Ki) |
MAPK-AP2 1.1 μM (Ki) |
PKCγ 1.2 μM (Ki) |
Chk1 2.6 μM (Ki) |
CK2 5.4 μM (Ki) |
SRC 13 μM (Ki) |
A-674563 slows proliferation of tumor cells with an EC 50 of 0.4 μM. A563 (0-10 µM) significantly decreases GSK3 and MDM2 phosphorylation in STS cells. A563 shows inhibitory effect on all STS cell lines, with IC 50 values at 48 hours ranging from 0.22±0.034 µM (SW684) to 0.35 ±0.06 µM (SKLMS1). A563 induces G2 cell cycle arrest and apoptosis in STS cells. A563 (1 µM/12 hr) upregulates the expression of GADD45A independent of p53. A-674563 (10-1000 nM) is anti-proliferative and cytotoxic in cultured human melanoma cells, induces melanoma cell apoptotic death, inhibited by caspase inhibitors, and inhibits melanoma cells via Akt-dependent and -independent mechanisms. A-674563 is cytotoxic and anti-proliferative when added to U937 and AmL progenitor cells, activates caspase-3/9 and apoptosis in U937 and AmL progenitor cells, and manipulates other signalings in AmL cells whiling blocking Akt.
A-674563 (40 mg/kg/d, p.o.) shows no significant monotherapy activity, but the efficacy of the combination therapy (A-674563+paclitaxel) is significantly improved in the PC-3 prostate cancer xenograft model. A-674563 (20, 100 mg/kg) increases plasma insulin in an oral glucose tolerance test. A563 (20 mg/kg/bid; p.o.) exhibits slow tumor growth and a significant difference in tumor volume without significant weight loss of mice. A563-treated tumors express increased levels of GADD45α and decreased levels of PCNA (a nuclear marker for proliferation). Additionally, TUNEL assay staining levels (marker for apoptosis) increase in the A563-treated specimens. A-674563 (25, 100 mg/kg, lavage daily) potently inhibits A375 xenograft growth in mice. A-674563 (15, 40 mg/kg) injection inhibits U937 xenograft in vivo growth, and improves mice survival.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-13254A | A-674563 hydrochloride | 1 mg | 600元 | |
2024/04/30 | HY-13254A | A-674563 (hydrochloride) A-674563 hydrochloride | 2070009-66-2 | 5mg | 1400元 |