4SC-203 is a multikinase inhibitor with potential antineoplastic activity. Multikinase inhibitor 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs). This may result in the inhibition of angiogenesis and cell proliferation in tumor cells in which these kinases are upregulated. FLT3 (FLK2), a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias (AML). VEGFRs, tyrosine kinase receptors, are overexpressed in a variety of tumor cell types and play key roles in angiogenesis.

MedKoo Cat#: 205802 Name: 4SC-203 CAS#: 895533-09-2 Chemical Formula: C33H38N8O4S Exact Mass: 642.27367 Molecular Weight: 642.77 Elemental Analysis: C, 61.66; H, 5.96; N, 17.43; O, 9.96; S, 4.99

Synonym: 4SC203; 4SC-203; 4SC 203; SC71710; SC-71710; SC 71710.

IUPAC/Chemical Name: 1-(2-methoxy-5-methylphenyl)-3-(6-((6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinazolin-4-yl)amino)benzo[d]thiazol-2-yl)urea

InChi Key: MAFACRSJGNJHCF-UHFFFAOYSA-N

InChi Code: InChI=1S/C33H38N8O4S/c1-21-6-9-27(43-3)26(16-21)37-32(42)39-33-38-24-8-7-22(17-30(24)46-33)36-31-23-18-28(44-4)29(19-25(23)34-20-35-31)45-15-5-10-41-13-11-40(2)12-14-41/h6-9,16-20H,5,10-15H2,1-4H3,(H,34,35,36)(H2,37,38,39,42)

SMILES Code: O=C(NC1=NC2=CC=C(NC3=C4C=C(OC)C(OCCCN5CCN(C)CC5)=CC4=NC=N3)C=C2S1)NC6=CC(C)=CC=C6OC

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-203 is a novel multi-target kinase inhibitor. In preclinical testing the compound has shown unique and strong selectivity against a set of kinases including FLT3, FLT3 mutants and VEGF-receptors. FLT3 is involved in the growth and maturation of normal blood cells. With the inhibition of VEGF receptor tyrosine kinases, 4SC-203 may also inhibit angiogenic processes – i.e. the formation of vascular structures that provide nutrition for tumours enabling them to grow rapidly – and could therefore also be applicable in solid cancer types. 4SC-203 was jointly developed with ProQinase GmbH, a company based in Freiburg, Germany. The molecule has successfully completed a randomised, double-blind, placebocontrolled Phase I study in healthy volunteers which demonstrated the safety, tolerability and pharmacokinetics of this intravenously delivered compound. (source: http://www.4sc.de/product-pipeline/clinical/4SC-203).         

References

 

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