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Staurosporine | CAS No: 62996-74-1 | GMP-certified suppliers
A medication that serves as a potent enzyme inhibitor used primarily in research on kinase-mediated signaling pathways relevant to oncology and pharmacological studies.
Therapeutic categories
AlkaloidsCarbazolesEnzyme InhibitorsHeterocyclic Compounds, Fused-RingIndole AlkaloidsIndoles
Generic name
Staurosporine
Molecule type
small molecule
CAS number
62996-74-1
DrugBank ID
DB02010
Approval status
Experimental drug
Product Snapshot
- Staurosporine is an experimental small molecule compound used primarily in research applications
- Its main therapeutic use is as a kinase inhibitor in oncology and cell biology studies
- Currently, Staurosporine does not have FDA or EMA approval for clinical use
Clinical Overview
Staurosporine (CAS Number 62996-74-1) is an indolocarbazole compound characterized by a polycyclic aromatic structure where an indole moiety is fused to a carbazole framework. It functions primarily as a potent inhibitor of protein kinase C (PKC). This inhibition results in enhanced cyclic AMP (cAMP)-mediated responses, as demonstrated in human neuroblastoma cells.
Although staurosporine is a well-recognized molecular tool for studying kinase-mediated signal transduction pathways, it currently holds an experimental status without any approved clinical indications. Its broad activity includes inhibition of various protein kinases beyond PKC, reflecting a wide-ranging influence on intracellular signaling events, which has limited direct therapeutic application due to a lack of selectivity and associated toxicity.
Mechanistically, staurosporine binds competitively to the ATP-binding site of protein kinases, thereby blocking phosphorylation events critical for cellular processes such as proliferation, differentiation, and apoptosis. Its kinase inhibition profile additionally includes effects on P-glycoprotein, positioning staurosporine within multiple drug categories including enzyme inhibitors and P-glycoprotein inhibitors.
Pharmacokinetic data are limited, but as a complex alkaloid, staurosporine is generally expected to have low aqueous solubility and variable absorption and distribution characteristics. Toxicity considerations are significant; staurosporine has been reported to induce cytotoxicity and apoptosis in various cell types, which constrains its applicability primarily to research settings.
Notable usage contexts for staurosporine concentrate on in vitro studies aimed at elucidating kinase function and signal transduction mechanisms rather than clinical therapy. It serves as an important biochemical probe in oncology research and pharmacological investigations.
From a sourcing and quality perspective, procurement of staurosporine as an active pharmaceutical ingredient requires rigorous analytical verification due to its complex structure and biological activity. Suppliers should provide detailed certificates of analysis confirming purity, structural integrity, and absence of impurities, consistent with regulatory standards for research-grade compounds. Stability data and appropriate storage conditions must also be established to maintain bioactivity during distribution and usage.
Although staurosporine is a well-recognized molecular tool for studying kinase-mediated signal transduction pathways, it currently holds an experimental status without any approved clinical indications. Its broad activity includes inhibition of various protein kinases beyond PKC, reflecting a wide-ranging influence on intracellular signaling events, which has limited direct therapeutic application due to a lack of selectivity and associated toxicity.
Mechanistically, staurosporine binds competitively to the ATP-binding site of protein kinases, thereby blocking phosphorylation events critical for cellular processes such as proliferation, differentiation, and apoptosis. Its kinase inhibition profile additionally includes effects on P-glycoprotein, positioning staurosporine within multiple drug categories including enzyme inhibitors and P-glycoprotein inhibitors.
Pharmacokinetic data are limited, but as a complex alkaloid, staurosporine is generally expected to have low aqueous solubility and variable absorption and distribution characteristics. Toxicity considerations are significant; staurosporine has been reported to induce cytotoxicity and apoptosis in various cell types, which constrains its applicability primarily to research settings.
Notable usage contexts for staurosporine concentrate on in vitro studies aimed at elucidating kinase function and signal transduction mechanisms rather than clinical therapy. It serves as an important biochemical probe in oncology research and pharmacological investigations.
From a sourcing and quality perspective, procurement of staurosporine as an active pharmaceutical ingredient requires rigorous analytical verification due to its complex structure and biological activity. Suppliers should provide detailed certificates of analysis confirming purity, structural integrity, and absence of impurities, consistent with regulatory standards for research-grade compounds. Stability data and appropriate storage conditions must also be established to maintain bioactivity during distribution and usage.
Identification & chemistry
| Generic name | Staurosporine |
|---|---|
| Molecule type | Small molecule |
| CAS | 62996-74-1 |
| UNII | H88EPA0A3N |
| DrugBank ID | DB02010 |
Pharmacology
Targets
| Target | Organism | Actions |
|---|---|---|
| Muscarinic acetylcholine receptor M1 | Humans | |
| Tyrosine-protein kinase Lck | Humans | |
| Serine/threonine-protein kinase pim-1 | Humans |
Formulation & handling
- Staurosporine is a small molecule with low aqueous solubility, requiring appropriate solubilization strategies for formulation.
- The compound’s moderate lipophilicity (LogP ~3.97) suggests potential challenges in oral bioavailability and necessity for careful excipient selection.
- As an experimental indolocarbazole derivative, stability under formulation conditions should be verified given its polycyclic aromatic structure.
