Pladienolide B

Modify Date: 2025-08-25 18:13:08

Pladienolide B Structure
Pladienolide B structure
Common Name Pladienolide B
CAS Number 445493-23-2 Molecular Weight 536.697
Density 1.1±0.1 g/cm3 Boiling Point 673.8±55.0 °C at 760 mmHg
Molecular Formula C30H48O8 Melting Point N/A
MSDS N/A Flash Point 209.6±25.0 °C

 Use of Pladienolide B


Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis[1][2][3].

 Names

Name pladienolide B
Synonym More Synonyms

 Pladienolide B Biological Activity

Description Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis[1][2][3].
Related Catalog
In Vitro Pladienolide B (0.1-2 nM; 24-72 hours) inhibits human cervical carcinoma cells viability[3]. Pladienolide B (0.1-2 nM; 24-48 hours) reduces SF3b1 expression in human cervical carcinoma cells[3]. Pladienolide B induces (0.1-2 nM; 24 hours) cell cycle arrest and apoptosis[3]. Cell Viability Assay[3] Cell Line: HeLa cells Concentration: 0.1, 0.5, 1, 1.5, 2 nM Incubation Time: 24, 48, 72 hours Result: Significantly decreased cell viability, and the decrease was concentration- and time-dependent. Apoptosis Analysis[3] Cell Line: HeLa cells Concentration: 0.1, 0.5, and 2 nM Incubation Time: 24 hours Result: The apoptotic cells were highly induced at 24 hours. RT-PCR[3] Cell Line: HeLa cells Concentration: 0.1, 0.5, and 2 nM Incubation Time: 24, 48 hours Result: Induced a time- and concentration-dependent decrease in cellular SF3b1 proteins.
In Vivo Pladienolide B (2.5-10 mg/kg; i.v.; daily for 5 days) has strong antitumor activities[4]. Animal Model: Female or male BALB/c nu/nu mice (7 weeks of age) (PC-3, OVCAR-3, DU-145, WiDr, and HCT-116, BSY-1 xenografts)[4] Dosage: 2.5, 5, and 10 mg/kg Administration: I.v.; daily for 5 days Result: Showed strong growth inhibitory or regressive activities against these xenografts.
References

[1]. Effenberger KA, et al. Coherence between cellular responses and in vitro splicing inhibition for the anti-tumor drug pladienolide B and its analogs. J Biol Chem. 2014 Jan 24;289(4):1938-47.

[2]. Aouida M, et al. CRISPR/Cas9-mediated target validation of the splicing inhibitor Pladienolide B. Biochim Open. 2016 Feb 24;3:72-75.

[3]. Zhang Q, et al. Inhibition of SF3b1 by pladienolide B evokes cycle arrest, apoptosis induction and p73 splicing in human cervical carcinoma cells. Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):1273-1280.

[4]. Mizui Y, et al. Pladienolides, new substances from culture of Streptomyces platensis Mer-11107. III. In vitro and in vivo antitumor activities. J Antibiot (Tokyo). 2004 Mar;57(3):188-96.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 673.8±55.0 °C at 760 mmHg
Molecular Formula C30H48O8
Molecular Weight 536.697
Flash Point 209.6±25.0 °C
Exact Mass 536.334900
LogP 3.34
Vapour Pressure 0.0±4.7 mmHg at 25°C
Index of Refraction 1.533
Storage condition -20°C

 Synonyms

pladienolide B
Oxacyclododec-9-en-2-one, 8-(acetyloxy)-4,7-dihydroxy-12-[(1E,3E,5S)-6-[(2R,3R)-3-[(1R,2S)-2-hydroxy-1-methylbutyl]oxiranyl]-1,5-dimethyl-1,3-hexadien-1-yl]-7,11-dimethyl-, (4R,7R,8S,9E,11S,12S)-
(2S,3S,4E,6S,7R,10R)-7,10-Dihydroxy-2-[(2E,4E,6S)-7-{(2R,3R)-3-[(2R,3S)-3-hydroxy-2-pentanyl]-2-oxiranyl}-6-methyl-2,4-heptadien-2-yl]-3,7-dimethyl-12-oxooxacyclododec-4-en-6-yl acetate
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