Testing Data
LY2157299, inhibitor
LY2157299
Purity
>99%
Synonyms
LY2157299; inhibitor
Purity/Purification
>99%
Solubility
Unknown
Formula
C22H19N5O
CAS Number
700874-72-2
Preparation and Storage
Store at -20 degree C for 2 years.
Testing Data
Testing Data
Related Product Information for LY2157299, inhibitor
LY2157299 is a novel selective small molecule transforming growth factor beta receptor (TGF-betaR) kinase inhibitor with IC50 of 86 nM and 2 nM for TbetaR1 and 2 nM, respectively. LY2157299 was well tolerated at both doses of 40 and 80 mg and no drug-related CTCAE Grade 3 or 4 toxicities were observed. Absorption of LY2157299 was rapid as determined by plasma concentrations at the first sampling time (0.5 hours). Daily oral administration of LY2157299 was safe and well tolerated at the two dose levels and the pharmacokinetic profile was consistent with the prediction derived from preclinical PK/PD model. As would be predicted for an inhibitor of TGF-beta signaling, LY2157299 blocked the phsophorylation of Smad2 but had no effect on fibroblast growth factor (FGF) or platelet-derived growth factor (PDGF) signaling. However, another study reported that LY2157299 induced angiogenesis and enhanced VEGF-and basic-fibroblast-growth-factor-induced angiogenesis in a Matrigel-plug assay, whereas adding an alpha5-integrin-neutralizing antibody to the Matrigel selectively inhibited this enhanced response. [1][2][3][4]
Product Categories/Family for LY2157299, inhibitor
References
[1] Bueno L et al. Eur J Cancer. 2008 Jan; 44(1):142-50. [2] Workman P. Future Oncol. 2005 Jun; 1(3):315-8. [3] http://aacrmeetingabstracts.org/cgi/content/abstract/2005/1/1463-a [4] Liu Z et al. J Cell Sci. 2009 Sep 15; 122(Pt 18):3294-302. The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
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Product Notes
The LY2157299 (Catalog #AAA8506596) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "LY2157299, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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