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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >PI3K / Akt / mTOR >Akt inhibitors >A-674563

A-674563

A-674563 Structure
  • ₹0
  • Product name: A-674563
  • CAS: 552325-73-2
  • MF: C22H22N4O
  • MW: 358.44
  • EINECS:
  • MDL Number:MFCD11840461
  • Synonyms:A-674563;(alphaS)-alpha-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]benzeneethanamine;A-674563 /A674563;(2S)-1-(5-(3-methyl-1H-indazol-5-yl)pyridin-3-yloxy)-3-phenylpropan-2-amine;(alphaS)-alpha-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]benzeneethanamine A-674563;A-674563 (alphaS)-alpha-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]benzeneethanamine A-674563 /A674563;A-674563;A 674563; A674563;(S)-1-(5-(3-Methyl-1H-indazol-5-yl)pyridin-3-yloxy)-3-phenylpropan-2-amine
Manufacturer Product number Product description Packaging Price Updated Buy

Properties

Boiling point :624.4±55.0 °C(Predicted)
Density :1.229
storage temp. :Store at -20°C
solubility :insoluble in EtOH; ≥23.8 mg/mL in H2O; ≥4.9 mg/mL in DMSO
form :solid
pka :13.43±0.40(Predicted)
color :White to yellow

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 May cause respiratory irritation Specific target organ toxicity, single exposure;Respiratory tract irritation Category 3 Warning GHS hazard pictograms
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Description

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki = 11 nM for Akt1). It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families. A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4 μM. In vivo, 40 mg/kg/day A-674563 in combination with 15 mg/kg/day paclitaxel was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.

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