LY364947 - CAS 396129-53-6
Catalog number:
396129-53-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Targets:
TGF-β Receptor
Description:
LY364947 is a selective inhibitor of TGF-β type-I receptor with potential anticancer activity. LY364947 inhibits TGF-β-dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3).
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Synonyms:
LY364947; LY-364947; LY 364947; HTS 466284.
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1.Validated RP-HPLC method for the simultaneous analysis of gemcitabine and LY-364947 in liposomal formulations.
Bansal SS1, Celia C, Ferrati S, Zabre E, Ferrari M, Palapattu G, Grattoni A. Curr Drug Targets. 2013 Aug;14(9):1061-9.
Combined use of gemcitabine (Gem) and LY-364947 (LY), a TGF-β1 receptor inhibitor, has shown promise for the treatment of fibrotic pancreatic cancer, by reducing collagen production and improving tumor drug penetration. The preparation and optimization of novel Gem and LY formulations, including co-encapsulation in liposomes, require a validated method for the simultaneous quantification of both drugs, a method that had yet to be developed. Here we demonstrate an RP-HPLC protocol for the simultaneous detection of Gem and LY at 266 and 228 nm with retention times of 3.37 and 11.34 mins, respectively. The method, which uses a C18 column and a KH2PO4 (10 mM)-methanol mobile phase, was validated for linearity, precision, accuracy, limits of detection, and robustness. Co-loaded liposomes with both Gem and LY (Gem/LY liposomes) were developed to investigate the protocol applicability to pharmacokinetic analysis and formulation characterization.
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CAS 396129-53-6 LY364947

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