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530196 Pladienolide B, Streptomyces sp. - CAS 445493-23-2 - Calbiochem

A cell-permeable inhibitor of mRNA splicing that directly target the splicesome-associated protein 130 and impair U2 small nuclear ribonucleoprotein (U2 snRNP) interaction with pre-mRNA.

Pladienolide B, Streptomyces sp. - CAS 445493-23-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (2S,3S,6S,7R,10R,E)-7,10-dihydroxy-2-((S,2E,4E)-7-((2R,3R)-3-((2R,3S)-3-hydroxypentan-2-yl), Pla-B

Primary Target: SAP130, splicing factor SF3b subunit 3
530196
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
445493-23-2C₃₀H₄₈O₈
Description
OverviewA cell-permeable, antitumor macrolide that acts as a time- and dose-dependent inhibitor of mRNA splicing. Shown to directly target the splicesome-associated protein 130 (SAP130, splicing factor SF3b subunit 3) and impair U2 small nuclear ribonucleoprotein (U2 snRNP) interaction with pre-mRNA causing unspliced or incompletely spliced pre-mRNA accumulation and altered gene expression. Exhibits potent anti-proliferative effect on WiDr and DLD1 colon cancer cell lines (IC50 = 500 pM and 8.5 nM, respectively) and is reported to down-regulate hypoxia-induced VEGF gene expression (IC50 = 1.8 nM in U251 cells). Blocks cell cycle by arresting progression at both G1 and G2/M phases. However, it does not affect the proliferation of resistant type of WiDr and DLD1 cells bearing R1074H mutation in SF3B1 gene. Inhibits tumor growth in WiDr tumor bearing nude mice and in a BSY-1 xenograft murine model (~5 – 10 mg/kg/day).
Catalogue Number530196
Brand Family Calbiochem®
Synonyms(2S,3S,6S,7R,10R,E)-7,10-dihydroxy-2-((S,2E,4E)-7-((2R,3R)-3-((2R,3S)-3-hydroxypentan-2-yl), Pla-B
References
ReferencesYokoi, A., et al. 2011. FEBS J. 278, 4870.
O'Brien, K., et al. 2008. J. Biol. Chem. 283, 33147.
Kotake, Y., et al. 2007. Nat. Chem. Biol. 9, 570.
Mizui, T., et al. 2004. J. Antibiot. 57, 188.
Sakai, T., et al. 2004. J. Antibiot. 57, 180.
Sakai, T., et al. 2004. J. Antibiot. 57, 173.
Product Information
CAS number445493-23-2
FormWhite solid
Hill FormulaC₃₀H₄₈O₈
Chemical formulaC₃₀H₄₈O₈
Quality LevelMQ100
Applications
Biological Information
Primary TargetSAP130, splicing factor SF3b subunit 3
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
530196 0

Documentation

Pladienolide B, Streptomyces sp. - CAS 445493-23-2 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Yokoi, A., et al. 2011. FEBS J. 278, 4870.
O'Brien, K., et al. 2008. J. Biol. Chem. 283, 33147.
Kotake, Y., et al. 2007. Nat. Chem. Biol. 9, 570.
Mizui, T., et al. 2004. J. Antibiot. 57, 188.
Sakai, T., et al. 2004. J. Antibiot. 57, 180.
Sakai, T., et al. 2004. J. Antibiot. 57, 173.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision18-April-2014 JSW
Synonyms(2S,3S,6S,7R,10R,E)-7,10-dihydroxy-2-((S,2E,4E)-7-((2R,3R)-3-((2R,3S)-3-hydroxypentan-2-yl), Pla-B
DescriptionA cell-permeable, antitumor macrolide that acts as a time- and dose-dependent inhibitor of mRNA splicing. Shown to directly target the splicesome-associated protein 130 (SAP130, splicing factor SF3b subunit 3) and impair U2 small nuclear ribonucleoprotein (U2 snRNP) interaction with pre-mRNA causing unspliced or incompletely spliced pre-mRNA accumulation and altered gene expression. Exhibits potent anti-proliferative effect on WiDr and DLD1 colon cancer cell lines (IC50 = 500 pM and 8.5 nM, respectively) and is reported to down-regulate hypoxia-induced VEGF gene expression (IC50 = 1.8 nM in U251 cells). Blocks cell cycle by arresting progression at both G1 and G2/M phases. However, it does not affect the proliferation of resistant type of WiDr and DLD1 cells bearing R1074H mutation in SF3B1 gene. Inhibits tumor growth in WiDr tumor bearing nude mice and in a BSY-1 xenograft murine model (~5 – 10 mg/kg/day).
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number445493-23-2
Chemical formulaC₃₀H₄₈O₈
Purity≥95% by HPLC
SolubilityDMSO (20 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesYokoi, A., et al. 2011. FEBS J. 278, 4870.
O'Brien, K., et al. 2008. J. Biol. Chem. 283, 33147.
Kotake, Y., et al. 2007. Nat. Chem. Biol. 9, 570.
Mizui, T., et al. 2004. J. Antibiot. 57, 188.
Sakai, T., et al. 2004. J. Antibiot. 57, 180.
Sakai, T., et al. 2004. J. Antibiot. 57, 173.