Description
Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
Product information
CAS Number: 37318-06-2
Molecular Weight: 1025.27
Formula: C54H88O18
Chemical Name: 8,16-bis(4-{4-[(4,5-dihydroxy-6-methyloxan-2-yl)oxy]-5-ethyl-2-hydroxy-6-methyloxan-2-yl}-3-hydroxypentan-2-yl)-7,15-dimethyl-1,9-dioxacyclohexadeca-3,5,11,13-tetraene-2,10-dione
Smiles: CC1C=CC=CC(=O)OC(C(C)C(O)C(C)C2(O)CC(OC3CC(O)C(O)C(C)O3)C(CC)C(C)O2)C(C)C=CC=CC(=O)OC1C(C)C(O)C(C)C1(O)CC(OC2CC(O)C(O)C(C)O2)C(CC)C(C)O1
InChiKey: OSERMIPXNLXAPD-BQVJCPSSSA-N
InChi: InChI=1S/C54H88O18/c1-13-37-33(9)71-53(63,25-41(37)67-45-23-39(55)49(61)35(11)65-45)31(7)47(59)29(5)51-27(3)19-15-17-22-44(58)70-52(28(4)20-16-18-21-43(57)69-51)30(6)48(60)32(8)54(64)26-42(38(14-2)34(10)72-54)68-46-24-40(56)50(62)36(12)66-46/h15-22,27-42,45-52,55-56,59-64H,13-14,23-26H2,1-12H3/b19-15-,20-16-,21-18-,22-17-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Elaiophylin-mediated autophagy inhibition and lysosomal dysfunction affect ovarian cancer cell survival during hypoxia. Exposure to Elaiophylin (0.025-0.5 μM; 24 hours) causes a significant increase in ovarian cancer SKOV3 cell death in hypoxia conditions. In both the SKOV3 and A2780 cell lines, Elaiophylin (0.25, 0.5, 0.75 μM; 24 hours) treatment leads to significant activation of cleaved CASP9/caspase-9 and PARP1 and downregulation of BIRC5/survivin in a concentration-dependent manner.
In Vivo:
Treatment with 2 mg/kg Elaiophylin (given i.p. every 2 days for 21 days; in BALB/C athymic mice) significantly suppresses ovarian cancer SKOV3 cells growth compared with DMSO treatment, resulting in a 72% decrease in the average daily tumor growth rate compared with DMSO treatment . Lower doses of Elaiophylin as a single agent exert significant antitumor activity, while higher doses lead to intestinal toxicity. Administration of a lower dose (2 mg/kg) of Elaiophylin as a single agent achieves a significant antitumor effect without toxicity in an orthotopic ovarian cancer model with metastasis. Toxic reactions are observed only in the 8 mg/kg group.
Products are for research use only. Not for human use.
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