Apoptolidin Chemical Properties

Melting point:

128-130°

alpha 

21D -5.2° (c = 1.0 in methanol)

Boiling point:

1108.9±65.0 °C(Predicted)

Density 

1.25±0.1 g/cm3(Predicted)

Flash point:

87℃

storage temp. 

-20°C

solubility 

Soluble in DMSO, DMF, ethanol, or methanol.

pka

11.71±0.70(Predicted)

form 

DMSO solution

color 

White

biological source

Amycolatopsis sp.

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO, DMF, ethanol or methanol may be stored at -20°C for up to 3 months.

Safety Information

RIDADR 

NA 1993 / PGIII

WGK Germany 

2

Apoptolidin Usage And Synthesis

Description

Apoptolidin (194874-06-1) is a powerful inducer of apoptosis in a variety of cancer cell lines.1?Is believed to act via inhibition of F0F1-ATPase2?but correlation studies indicate that a second mechanism may be the actual mode of action3.? Cell permeable.

Uses

Apoptolidin, originally isolated from a Nocardiopsis sp., induces apoptotic cell death in rat glial cells transformed with the adenovirus E1A oncogene (IC50 = 11 ng/ml). Apoptolidin is among the most selective cytotoxic agents tested by the NCI in human cancer cell lines. Although the apoptotic activity of apoptolidin correlates with F0F1-ATPase inhibition, recent evidence suggests the existence of a secondary biological target or more complex mode of action.

References

1) Kim et al. (1997), Apoptolidin, a new apoptosis inducer in transformed cells from Nocardiopsis sp.; J. Antibiot. (Tokyo), 50 628 2) Salomon et al. (2001), Apoptolidin, a selective cytotoxic agent, is an inhibitor of F0F1-ATPase; Chem. Biol., 8 71 3) Wender et al. (2006), Correlation of F0F1-ATPase inhibition and antiproliferative activity of apoptolidin analogues; Org. Lett., 8 589

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