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A-674563 (hydrochloride)

A-674563 (hydrochloride)

中文名稱A-674563 (hydrochloride)
中文同義詞AKT1抑制劑(A-674563 HYDROCHLORIDE);化合物 A-674563 HYDROCHLORIDE;鹽酸鹽形式;(S)-1-((5-(3-甲基-1H-吲唑-5-基)吡啶-3-基)氧基)-3-苯基丙烷-2-胺鹽酸鹽;化合物A-674563 HCL,10 MM DMSO 溶液;A-674563 hydrochloride試劑;A-674563 hydrochloride試劑
英文名稱A-674563 (hydrochloride)
英文同義詞A-674563 (hydrochloride);A-674563 hydrochloride (A 674563 hydrochloride;(S)-1-((5-(3-Methyl-2H-indazol-5-yl)pyridin-3-yl)oxy)-3-phenylpropan-2-amine hydrochloride
CAS號2070009-66-2
分子式C22H23ClN4O
分子量394.9
EINECS號
相關(guān)類別細胞生物學(xué)試劑
Mol文件2070009-66-2.mol
結(jié)構(gòu)式A-674563 (hydrochloride) 結(jié)構(gòu)式

A-674563 (hydrochloride) 性質(zhì)

儲存條件-10 to -25°C
溶解度H2O: 2?mg/mL, clear
形態(tài)固體
顏色淺黃至卡其色
水溶解性H2O: 2mg/mL, clear
InChIKeyBPNUQXPIQBZCMR-IBGZPJMESA-N
SMILES[nH]1nc(c2c1ccc(c2)c3cncc(c3)OC[C@@H](N)Cc4ccccc4)C

A-674563 (hydrochloride) 用途與合成方法

A-674563 hydrochloride 是具有選擇性的高效 Akt1 抑制劑,其 Ki 值為 11 nM。

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

WGK GermanyWGK 3
存儲類別11 - 可燃固體

MSDS信息

更新日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/06/05HY-13254AA-674563 hydrochloride2070009-66-21 mg600元
2026/06/05HY-13254AA-674563 (hydrochloride)
A-674563 hydrochloride
2070009-66-25mg1400元

A-674563 (hydrochloride) 上下游產(chǎn)品信息

"A-674563 (hydrochloride)"相關(guān)產(chǎn)品信息
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