| Identification | Back Directory | [Name]
A-674563 (hydrochloride) | [CAS]
2070009-66-2 | [Synonyms]
A-674563 (hydrochloride)
A-674563 hydrochloride
(A 674563 hydrochloride | [Molecular Formula]
C??H??ClN?O | [MDL Number]
MFCD18711680 | [MOL File]
2070009-66-2.mol | [Molecular Weight]
394.9 |
| Chemical Properties | Back Directory | [storage temp. ]
-10 to -25°C | [solubility ]
H2O: 2 mg/mL, clear | [form ]
Solid | [color ]
Light yellow to khaki | [Water Solubility ]
H2O: 2mg/mL, clear | [InChIKey]
BPNUQXPIQBZCMR-IBGZPJMESA-N | [SMILES]
[nH]1nc(c2c1ccc(c2)c3cncc(c3)OC[C@@H](N)Cc4ccccc4)C |
| Hazard Information | Back Directory | [Uses]
A-674563 Hydrochloride is a potent, orally available Akt1 inhibitor. | [Biological Activity]
A-674563 is an orally available ATP-competitive pan-AKT (PKBprotein Kinase B) inhibitor (AKT1 Ki = 11 nM) with additional potency against PKACdk2 GSK3β (IC50 = 1.44.2,10 nMrespectively). 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 days15 mg paclitaxel/day on days 202428). | [in vivo]
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[1]. 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[2]. A-674563 (25, 100 mg/kg, lavage daily) potently inhibits A375 xenograft growth in mice[3]. A-674563 (15, 40 mg/kg) injection inhibits U937 xenograft in vivo growth, and improves mice survival[4]. | [IC 50]
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) |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|