Pladienolide B is a mRNA splicing inhibitor, exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B decreases splicing capacity up to 75% in vitro. Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B induces apoptosis. Pladienolide B directly targets splicesome-associated 130 (SAP130), inhibits splicing factor 3B subunit (SF3B1) and impairs U2 small nuclear ribonucleoprotein (U2 snRNP) interaction with pre-mRNA. Pladienolide B arrests cell cycle in G1 and G2/M phases. Pladienolide B displays antitumor activity against gastric cancer cells (IC50 values are 1.6-4.9 nM). Pladienolide B is cell permeable and active in vivo.
Pladienolides B can be dissolved in DMSO for in vitro use.
For in vivo study, pladienolides B were dissolved at appropriate concentrations in 3.5% DMSO and 6.5% Tween 80 in 5% glucose solution.
| Molecular Weight | 536.7 |
| Formula | C30H48O8 |
| CAS Number | 445493-23-2 |
| Solubility (25°C) | DMSO |
| Storage | -20°C, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Bowery. TiPS. GABAB receptors and their significance in mammalian pharmacology.
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