DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Rizavasertib
CAS 552325-16-3
MF C24H23N5O MW397.5 g/mol
(2S)-1-(1H-indol-3-yl)-3-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]propan-2-amine
(2S)-1-(1H-indol-3-yl)-3-{[5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl]oxy}propan-2-amine
serine/threonine kinase inhibitor, A-443654, A 443654, A443654, Q4UG565ZYH
Rizavasertib was a drug candidate originally developed by Abbott (now AbbVie).[1][2][3][4] It is a pan akt Inhibitor.[5] It is now used as an akt inhibitor tool compound.[6]
Rizavasertib (also known by its developmental code A-443654) is a potent, small-molecule pan-Akt (protein kinase B) inhibitor originally developed by Abbott Laboratories (now AbbVie). It acts as a highly effective research tool compound used to investigate cellular signaling pathways, particularly in oncology and tumor cell biology
- Mechanism of Action: It is an ATP-competitive inhibitor that targets all three Akt isoforms (Akt1, Akt2, and Akt3) with equal intracellular potency, showing an inhibition constant (\(\text{K}_{i}\)) of 160 pM.
Key Biological & Research Effects
- Pathway Modulation: It induces a rapid, paradoxical phosphorylation of Akt at the Ser-473 residue, occurring independently of mTORC1 inhibition.
- Mitotic Regulation: The compound interferes with normal cell division (mitotic progression) by regulating the expression of Aurora A kinase.
- Oncology Models: In preclinical testing, it has demonstrated an ability to prolong survival in animal models of intracranial glioma and shows potential therapeutic relevance against both primary and drug-resistant T-cell acute lymphoblastic leukemia (T-ALL).
Current Status
Rizavasertib’s highest global development status remains Preclinical. It is not approved for human use or clinical medical treatment and is sold exclusively by chemical suppliers like MedChemExpress as an analytical reference standard or reagent for qualitative, quantitative, and methodological research (such as HPLC, GC, and mass spectrometry).
PAT
US20030199511 and literature Bioorganic & Medicinal Chemistry 2006, 14, 6832–6846, a method for preparing A-443654 is disclosed,
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2003051366&_cid=P11-MTGMSN-41566-1
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=US40155124&_cid=P11-MTGN0W-48129-1
SIMILAR
EXAMPLE 191
(1R)-1-(1H-Indol-3-ylmethyl)-2-[5-(3-methyl-1H-indazol-5-yl)-pyridin-3-yloxy]-ethylamine
PAT
CN104610229
https://patentscope.wipo.int/search/en/detail.jsf?docId=CN133679262&_cid=P11-MTGNFX-58461-1
Example 4: Preparation of Compound 6
| Compound 5 (104 g, 178.9 mmol) and methanol (620 ml, 6V) were added to a 1 L three-necked flask. A 4M HCl/ethyl acetate (130 ml) solution was added dropwise at a temperature below 25 °C. The reaction was allowed to proceed overnight. The reaction was monitored by TLC until the starting material was completely reacted. The mixture was concentrated and drained to dryness using an oil pump to obtain 104 g of crude product. Water (900 ml) and ethyl acetate (1350 ml) were added, and the mixture was stirred until the system was clear. The mixture was allowed to stand, and the organic layer was separated. The aqueous phase was extracted once again with ethyl acetate (500 ml). The organic phases were combined, and water (180 ml) was added. Most of the ethyl acetate was concentrated until solid began to precipitate. The mixture was cooled in an ice bath, stirred, and allowed to crystallize for 30 min. The mixture was filtered, and the filter cake was dried to obtain a white solid (57.9 g, yield 86%, purity 98.3%). |
| 1H NMR(CD 3 OD,500MHz):δppm 8.45(s,1H),8.25(brs,1H),7.98(s,1H),7.61(m,4H),7.37(s,1H),7.16(s,1H),7.10(m,1H),7.00(m,1H),4.18(m,1H),4.03(m,1H),3.56(m,1H),3.10(m,1H),3.00(m,1H),2.62(s,3H)；ESI/MS:m/z＝398(M+H)+. |
Pat
- Kinase inhibitorsPublication Number:US-6831175-B2Priority Date:2001-12-13Grant Date:2004-12-14
- 3- (Phenyl-alkoxy) -5- (phenyl) -pyridine derivatives and related compounds as kinase inhibitors for cancer treatmentPublication Number:JP-2005516927-APriority Date:2001-12-13
- Methods of treating muscular wasting diseases using NF-KB activation inhibitorsPublication Number:US-9173920-B2Priority Date:2006-03-15Grant Date:2015-11-03
- Kinase inhibitorsPublication Number:US-2003187026-A1Priority Date:2001-12-13
- 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancerPublication Number:CA-2470214-A1Priority Date:2001-12-13
- Kinase inhibitorsPublication Number:US-2003199511-A1Priority Date:2001-12-13
- 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancerPublication Number:WO-03051366-A2Priority Date:2001-12-13
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References
- “Research programme: protein kinase inhibitors – AbbVie”. AdisInsight. Springer Nature Switzerland AG.
- Luo Y, Shoemaker AR, Liu X, Woods KW, Thomas SA, de Jong R, et al. (June 2005). “Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo”. Molecular Cancer Therapeutics. 4 (6): 977–986. doi:10.1158/1535-7163.MCT-05-0005. PMID 15956255.
- Gandelman M, Dansithong W, Kales SC, Paul S, Maag G, Aoyama E, et al. (October 2021). “The AKT modulator A-443654 reduces α-synuclein expression and normalizes ER stress and autophagy”. The Journal of Biological Chemistry. 297 (4) 101191. doi:10.1016/j.jbc.2021.101191. PMC 8482485. PMID 34520759.
- Ming J, Jin S, Liu Z, Yang K, Shi M, Niu Y (October 2025). “Imidacloprid contributes to bladder cancer progression: preliminary evidence based on network toxicology, machine learning and molecular docking”. BMC Pharmacology & Toxicology. 26 (1) 180. doi:10.1186/s40360-025-01016-9. PMC 12577002. PMID 41168844.
- Crowell JA, Steele VE, Fay JR (August 2007). “Targeting the AKT protein kinase for cancer chemoprevention”. Molecular Cancer Therapeutics. 6 (8): 2139–2148. doi:10.1158/1535-7163.MCT-07-0120. PMID 17699713.
- Garcia-Echeverria C, Sellers WR (September 2008). “Drug discovery approaches targeting the PI3K/Akt pathway in cancer”. Oncogene. 27 (41): 5511–5526. doi:10.1038/onc.2008.246. PMID 18794885.
 | |
| Clinical data | |
|---|---|
| Other names | A-443654 |
| Identifiers | |
| IUPAC name | |
| CAS Number | 552325-16-3 |
| PubChem CID | 10172943 |
| IUPHAR/BPS | 8204 |
| DrugBank | DB08073 |
| ChemSpider | 8348448 |
| UNII | Q4UG565ZYH |
| ChEBI | CHEBI:91351 |
| ChEMBL | ChEMBL379300 |
| PDB ligand | L20 (PDBe, RCSB PDB) |
| CompTox Dashboard (EPA) | DTXSID20436347  |
| Chemical and physical data | |
| Formula | C24H23N5O |
| Molar mass | 397.482 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
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#rizavasertib, #anax labs, #serine/threonine kinase inhibitor, #A-443654, #A 443654, #A443654, #Q4UG565ZYH
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