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532384 PI3K Inhibitor, HS-173 - Calbiochem

532384
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1276110-06-5C₂₁H₁₈N₄O₄S

Products

Catalogue NumberPackaging Qty/Pack
5.32384.0001 Sklená flaša 10 mg
Description
OverviewA cell permeable imidazopyridine-carboxylate derived compound that acts as a potent and selective inhibitor of phosphatidylinositol 3-kinase a (PI3Ka; IC50 = 800 pM). Blocks the proliferation of several cancer cells (IC50 = 600 nM; 1.5 µM, and 7.8 µM for T47D, SK-BR3, and MCF-7 cells, respectively). Suppresses the growth and proliferation of hepatic stellate cells (HSC-T6 and LX-2 cells) and induces cell cycle arrest at G2/M phase in a dose and time-dependent manner. Induces apoptosis in HSC-T6 cells (~5 µM) as evidenced by morphological changes, activation of caspase-3, reduction in Bcl-2 levels, and loss of mitochondrial transmembrane potential. Exhibits anti-fibrolytic activity and diminishes the expression of profibrotic mediators, such as fibronectin and vimentin (~ 1 µM) and weakens the severity of hepatic damage in a murine model of carbon tetrachloride-induced fibrosis and reduces the phosphorylation of Akt and p70S6 kinase (10 mg/kg, p.o., 6d/week for 1 month).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number532384
Brand Family Calbiochem®
SynonymsPI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
References
ReferencesSon, M.K., et al. 2013. Sci. Rep. 3, 3470.
Lee, H., et al. 2013. Onc. Rep. 30, 863.
Kim, O., et al. 2011. J. Med. Chem. 54, 2455.
Product Information
CAS number1276110-06-5
FormLight beige powder
Hill FormulaC₂₁H₁₈N₄O₄S
Chemical formulaC₂₁H₁₈N₄O₄S
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetPI3Ka
Primary Target IC<sub>50</sub>800 pM
Purity≥96% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
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
5.32384.0001 04055977287226

Documentation

PI3K Inhibitor, HS-173 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Son, M.K., et al. 2013. Sci. Rep. 3, 3470.
Lee, H., et al. 2013. Onc. Rep. 30, 863.
Kim, O., et al. 2011. J. Med. Chem. 54, 2455.

Technical Info

Title
White Paper: Further considerations of antibody validation and usage.
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.

Revision27-February-2015 JSW
SynonymsPI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
DescriptionA cell permeable imidazopyridine-carboxylate derived compound that acts as a potent and selective inhibitor of phosphatidylinositol 3-kinase a (PI3Ka; IC50 = 800 pM). Blocks the proliferation of several cancer cells (IC50 = 600 nM; 1.5 µM, and 7.8 µM for T47D, SK-BR3, and MCF-7 cells, respectively). Suppresses the growth and proliferation of hepatic stellate cells (HSC-T6 and LX-2 cells) and induces cell cycle arrest at G2/M phase in a dose and time-dependent manner. Induces apoptosis in HSC-T6 cells (~5 µM) as evidenced by morphological changes, activation of caspase-3, reduction in Bcl-2 levels, and loss of mitochondrial transmembrane potential. Exhibits anti-fibrolytic activity and diminishes the expression of profibrotic mediators, such as fibronectin and vimentin (~ 1 µM) and weakens the severity of hepatic damage in a murine model of carbon tetrachloride-induced fibrosis and reduces the phosphorylation of Akt and p70S6 kinase (10 mg/kg, p.o., 6d/week for 1 month).
FormLight beige powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1276110-06-5
Chemical formulaC₂₁H₁₈N₄O₄S
Purity≥96% by HPLC
SolubilityDMSO (50 mg/ml)
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
ReferencesSon, M.K., et al. 2013. Sci. Rep. 3, 3470.
Lee, H., et al. 2013. Onc. Rep. 30, 863.
Kim, O., et al. 2011. J. Med. Chem. 54, 2455.