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Diazepinomicin

Chemical Structure : Diazepinomicin

CAS No.: 733035-26-2

Diazepinomicin (TLN 4601;ECO-4601)

Catalog No.: PC-62205Not For Human Use, Lab Use Only.

Diazepinomicin (TLN 4601, ECO-4601) is a brain penetrant inhibitor of Ras-RAF-MAPK pathway post Ras prenylation and prior to MEK activation, binds the central and/or peripheral benzodiazepine receptors (PBR, TSPO).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Diazepinomicin (TLN 4601, ECO-4601) is a brain penetrant inhibitor of Ras-RAF-MAPK pathway post Ras prenylation and prior to MEK activation, binds the central and/or peripheral benzodiazepine receptors (PBR, TSPO); prevents EGF-induced phosphorylation of Raf-1, MEK, and ERK1/2; reduces Ras-GTP levels and induces apoptosis; shows antitumor activity and decreases tumor Raf-1 protein levels in MIA PaCa-2 tumor-bearing mice.

Brain Cancer

Phase 2 Discontinued

Physicochemical Properties

M.Wt 462.58
Formula C28H34N2O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4,6,8-trihydroxy-10-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one

References

1. Campbell PM, et al. J Mol Signal. 2010 Nov 2;5:18.

2. Quah SY, et al. Pharmacol Ther. 2016 Jun;162:35-57.

3. Boufaied N, et al. Anticancer Drugs. 2010 Jun;21(5):543-52.

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