eCF506

• CAT Number: I006583
• CAS Number: 1914078-41-3
• Molecular Formula: C26H38N8O3
• Molecular Weight: 510.643
• Purity: ≥95%
• Synonyms: eCF506; eCF-506; eCF 506.;tert-butyl (4-(4-amino-1-(2-(4-(dimethylamino)piperidin-1-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl)carbamate
• Target: SRC inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term or -20 °C for long term
• InChI: InChI=1S/C26H38N8O3/c1-26(2,3)37-25(35)30-19-8-7-17(15-20(19)36-6)22-21-23(27)28-16-29-24(21)34(31-22)14-13-33-11-9-18(10-12-33)32(4)5/h7-8,15-16,18H,9-14H2,1-6H3,(H,30,35)(H2,27,28,29)
• InChIKey: GMPQGWXPDRNCBL-UHFFFAOYSA-N
• SMILES: COC1=CC(C2=NN(CCN3CCC(N(C)C)CC3)C4=NC=NC(N)=C42)=CC=C1NC(OC(C)(C)C)=O

eCF506 is the first, potent and selective SRC inhibitor that inhibits SRC at subnanomolar concentration (IC50 < 0.5 nM) with a 1000-fold selectivity over ABL. eCF506 exhibits excellent water solubility, an optimal DMPK profile and oral bioavailability, halts SRC-associated neuromast migration in zebrafish embryos without inducing life-threatening heart defects, and inhibits SRC phosphorylation in tumor xenografts in mice. eCF506 targets a molecule called Src tyrosine kinase that is required for breast cancer cells to grow and spread. eCF506 may be highly effective at blocking growth of breast cancer cells.

Reference

1:Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC, Brunton VG, Patton EE, Carragher NO, Unciti-Broceta A. Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59(10):4697-710. doi: 10.1021/acs.jmedchem.6b00065. Epub 2016 May 4. PubMed PMID: 27115835; PubMed Central PMCID: PMC4885109.