4SC-205

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205804

CAS#: NONE

Description: 4SC-205 is a small-molecule inhibitor of the human kinesin-related motor protein Eg5 with potential antineoplastic activity. Eg5 kinesin-related motor protein inhibitor 4SC-205 selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and cell death. The ATP-dependent Eg5 kinesin-related motor protein (also known as KIF11 or kinesin spindle protein-5) is a plus-end directed kinesin motor protein essential for the regulation of spindle dynamics, including assembly and maintenance, during mitosis.


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4SC-205 is not in stock. This product may be available through custom synthesis when its structure is available.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205804
Name: 4SC-205
CAS#: NONE
Chemical Formula:
Exact Mass:
Molecular Weight:
Elemental Analysis:


Synonym: 4SC205; 4SC 205; 4SC-205

IUPAC/Chemical Name: NONE


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

4SC-205 is an oral small-molecule inhibitor of the human kinesin spindle protein Eg5, which is of crucial importance for proper cell division (mitosis). Mitosis inhibitors, such as taxol, are used as the first-line therapy in numerous cancers. As opposed to taxol, which is neurotoxic, 4SC- 205 does not directly affect microtubules, but only the kinesin Eg5 which is only present during cell division. This compound is in the Phase I AEGIS study in patients with solid tumours or malignant lymphoma in order to evaluate its safety, tolerability, pharmacokinetics and pharmacodynamics. Currently, 4SC-205 is the only oral Eg5 kinesin inhibitor in clinical development.  Eg5 interacts with microtubules, a component of the mitosis mechanism, and mediates the segregation of the two spindle poles resulting in the correct distribution of the chromosomes to the daughter cells. Allosteric inhibition of Eg5 by 4SC- 205 leads to cell cycle arrest in mitosis and subsequent programmed cell death (apoptosis). Mitosis is the fundamental process required for cell division and tissue proliferation. The mitotic spindle apparatus has for decades been a primary target for the development of anti-mitotic drugs such as taxanes and vinca alkaloids, which are broadly used in cancer therapies as single chemotherapeutic agents or in combination. In preclinical tests, 4SC-205 has proven to be a particularly efficacious inhibitor of tumour cell proliferation of various cancer origins, both in vitro and in vivo.  (source: http://www.4sc.de/product-pipeline/clinical/4SC-205).   
 
 
 


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