- A-443654
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- $2.00 / 100KG
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2025-10-13
- CAS:552325-16-3
- Min. Order: 0.1KG
- Purity: 99%
- Supply Ability: g-kg-tons
- A-443654
-
- $1.00 / 1KG
-
2019-09-02
- CAS:552325-16-3
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1lg; 2kg; 5kg; 10kg; 100kg
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| | A-443654 Basic information |
| Product Name: | A-443654 | | Synonyms: | A-443654;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;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)-;inhibit,A443654,A-443654,Inhibitor,PKB,Akt,A 443654,Protein kinase B;A-443654, 10 mM in DMSO | | CAS: | 552325-16-3 | | MF: | C24H23N5O | | MW: | 397.47 | | EINECS: | | | Product Categories: | Akt;mTOR;PI3K | | Mol File: | 552325-16-3.mol |  |
| | A-443654 Chemical Properties |
| 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 |
| | A-443654 Usage And Synthesis |
| 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 |
| | A-443654 Preparation Products And Raw materials |
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