A-674563 (hydrochloride)
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- CAS号:
- 2070009-66-2
- 英文名:
- A-674563 (hydrochloride)
- 英文别名:
- A-674563 (hydrochloride);A-674563 hydrochloride
(A 674563 hydrochloride
- 中文名:
- A-674563 (hydrochloride)
- 中文别名:
- 盐酸盐形式;化合物 A-674563 HYDROCHLORIDE;AKT1抑制剂(A-674563 HYDROCHLORIDE);(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
- CBNumber:
- CB23053858
- 分子式:
- C22H23ClN4O
- 分子量:
- 394.9
- MOL File:
- 2070009-66-2.mol
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A-674563 (hydrochloride)化学性质
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形态:
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Solid
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颜色:
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Light yellow to khaki
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A-674563 (hydrochloride)性质、用途与生产工艺
A-674563 hydrochloride 是具有选择性的高效 Akt1 抑制剂,其 Ki 值为 11 nM。
Akt1
11 nM (Ki)
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PKA
16 nM (Ki)
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CDK2
46 nM (Ki)
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GSK3β
110 nM (Ki)
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ERK2
260 nM (Ki)
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PKCδ
360 nM (Ki)
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RSK2
580 nM (Ki)
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MAPK-AP2
1.1 μM (Ki)
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PKCγ
1.2 μM (Ki)
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Chk1
2.6 μM (Ki)
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CK2
5.4 μM (Ki)
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SRC
13 μM (Ki)
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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.
A-674563 (hydrochloride)
上下游产品信息
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-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 |
A-674563 (hydrochloride)
生产厂家
2070009-66-2, A-674563 (hydrochloride) 相关搜索:
- 细胞生物学试剂
- (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
- 盐酸盐形式
- 化合物 A-674563 HYDROCHLORIDE
- AKT1抑制剂(A-674563 HYDROCHLORIDE)
- 2070009-66-2
- A-674563 hydrochloride
(A 674563 hydrochloride
- A-674563 (hydrochloride)