| Identification | Back Directory | [Name]
A-443654 | [CAS]
552325-16-3 | [Synonyms]
A-443654
A-443654;A443654
(2S)-1-(1H-indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan-2-amine
1H-Indole-3-ethanamine, α-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-, (αS)-
1H-Indole-3-ethanaMine, a-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]Methyl]-, (aS)-
(alphaS)-alpha-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-(S)-1H-indole-3-ethanamine | [Molecular Formula]
C24H23N5O | [MDL Number]
MFCD11840663 | [MOL File]
552325-16-3.mol | [Molecular Weight]
397.47 |
| Chemical Properties | Back Directory | [Boiling point ]
722℃ | [density ]
1.307 | [Fp ]
390℃ | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥19.85 mg/mL in DMSO; ≥44.3 mg/mL in EtOH | [form ]
solid | [pka]
13.43±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM)[1]. | [Definition]
ChEBI: (2S)-1-(1H-indol-3-yl)-3-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-2-propanamine is a member of indoles. | [in vivo]
A-443654 (7.5 mg/kg/d, s.c.) inhibits tumor growth in the 3T3-Akt1 flank tumor model. A-443654 (50 mg/kg, s.c.) induces apoptosis in 3T3-Akt1 flank tumors. A-443654 (30 mg/kg, s.c.) leads to increased levels of phosphorylated Akt1 in MiaPaCa-2 tumors[1]. | [target]
Akt1 | [IC 50]
Akt1: 160 pM (Ki); Akt2: 160 pM (Ki); Akt3: 160 pM (Ki); PKA: 6.3 nM (Ki); RSK2: 11 nM (Ki); PKCγ: 24 nM (Ki); CDK2: 24 nM (Ki); PKCδ: 33 nM (Ki); GSK3β: 41 nM (Ki); ERK2: 340 nM (Ki); cKIT: 1.2 μM (Ki); Chk1: 2.3 μM (Ki); CK2: 2.4 μM (Ki); SRC: 2.6 μM (Ki); KDR: 3.1 μM (Ki); MAPK-AP2: 3.3 μM (Ki); Flt1: 3.6 μM (Ki) | [References]
[1] Luo Y, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005 Jun;4(6):977-86. DOI:10.1158/1535-7163.MCT-05-0005
[2] Zheng J, et al. Rapamycin sensitizes Akt inhibition in malignant human breast epithelial cells. Cancer Lett. 2010 Oct 1;296(1):74-87. DOI:10.1016/j.canlet.2010.03.018
[3] Gallia GL, et al. Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells. Mol Cancer Ther. 2009 Feb;8(2):386-93. DOI:10.1158/1535-7163.MCT-08-0680
[4] Zhao Y, et al. Estrogen receptor alpha and beta regulate actin polymerization and spatial memory through an SRC-1/mTORC2-dependent pathway in the hippocampus of female mice. J Steroid Biochem Mol Biol. 2017 Nov;174:96-113. DOI:10.1016/j.jsbmb.2017.08.003 |
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| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Shaanxi Dideu Medichem Co. Ltd
|
| Telephone: |
+86-29-87569266 +86-17392581500 |
| Website: |
https://www.chemicalbook.com/manufacturer/shaanxi-dideu-medichem-220/ |
|