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2070009-66-2

中文名稱 A-674563 (hydrochloride)
英文名稱 A-674563 (hydrochloride)
CAS 2070009-66-2
分子式 C??H??ClN?O
分子量 394.9
MOL 文件 2070009-66-2.mol
更新日期 2024/11/15 18:20:28
2070009-66-2 結(jié)構(gòu)式 2070009-66-2 結(jié)構(gòu)式

基本信息

中文別名
AKT1抑制劑(A-674563 HYDROCHLORIDE)
英文別名
A-674563 (hydrochloride)
A-674563 hydrochloride (A 674563 hydrochloride

物理化學(xué)性質(zhì)

形態(tài)Solid
顏色Light yellow to khaki

常見(jiàn)問(wèn)題列表

生物活性
A-674563 hydrochloride 是具有選擇性的高效 Akt1 抑制劑,其 Ki 值為 11 nM。
靶點(diǎn)

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)

體外研究

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.

體內(nèi)研究

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.

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