A-674563 hydrochloride

Name: A-674563 hydrochloride
Brand: SIGMA

≥98% (HPLC)

别名:

αS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-benzeneethanamine hydrochloride, (1S)-1-Benzyl-2-(5-(3-methyl-1H-indazol-5-yl)-pyridin-3-yloxy)-ethylamine hydrochloride, (2S)-1-(5-(3-methyl-1H-indazol-5-yl)pyridin-3-yloxy)-3-phenylpropan-2-amine hydrochloride, A 674563 hydrochloride, A674563 hydrochloride

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关于此项目

经验公式（希尔记法）:

C₂₂H₂₂N₄O · xHCl

分子量:

358.44 (free base basis)

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD11840461

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

desiccated

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属性

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H₂O: 2 mg/mL, clear

storage temp.

-10 to -25°C

SMILES string

[nH]1nc(c2c1ccc(c2)c3cncc(c3)OC[C@@H](N)Cc4ccccc4)C

InChI key

BPNUQXPIQBZCMR-IBGZPJMESA-N

说明

Biochem/physiol Actions

A-674563 is an orally available ATP-competitive pan-AKT (PKB, protein Kinase B) inhibitor (AKT1 Ki = 11 nM) with additional potency against PKA, Cdk2 GSK3β (IC50 = 1.4, 4.2,10 nM, respectively). A-674563 reduces the phosphorylation of cellular Akt substrates (0.1-10 μM; MiaPaCa-2) and enhances paclitaxel efficacy in a PC-3 xenograft model in mice in vivo (40 mg A-674563/kg via p.o. b.i.d. for 21 days, 15 mg paclitaxel/day on days 20, 24, 28).

Orally available ATP-competitive pan-AKT (PKB, protein Kinase B) inhibitor that enhances paclitaxel efficacy in a PC-3 xenograft model in mice in vivo.