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LY2157299

Cat. No. M1980
LY2157299 Structure
Size Price Availability Quantity
5mg USD 95 In stock
10mg USD 140 In stock
50mg USD 440 In stock
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Quality Control
Biological Activity

LY2157299 could inhibit TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells. Furthermore, administration of LY2157299 ameliorated anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure in vivo. LY2157299 also shows dose dependent potentiation of VEGF or bFGF induced cell proliferation in HUVEC. LY2157299 blocked the phsophorylation of Smad2 but had no effect on fibroblast growth factor (FGF) or platelet-derived growth factor (PDGF) signaling. In the in vitro VEGF-stimulated cord formation assay, LY2157299 potentiates angiogenesis. LY2157299 induces angiogenesis and enhances VEGF and basic-fibroblast-growth-factor-induced angiogenesis in a Matrigel-plug assay, whereas adding an alpha5-integrin-neutralizing antibody to the Matrigel selectively inhibits this enhanced response.

Protocol
Cell Experiment
Cell lines HCC cell
Preparation method HCC cells were incubated in serum-free medium overnight and treated with 5 ng/mL of TGF-β for 1 hour followed by the addition of 1 or 10 μM galunisertib for 5 and 24 hours. Concentrations were selected to be in the range of observed plasma exposure
Concentrations 1 or 10 µM
Incubation time 5 and 24 h
Animal Experiment
Animal models Sprague-Dawley male rats
Formulation 0.9% NaCl water
Dosages 75 mg/kg/day
Administration intragastrically 
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 369.42
Formula C22H19N5O
CAS Number 700874-72-2
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Universite Paris-Sud (2014). Figure 6. LY2157299 (Abmole Bioscience)
Method Flow cytometry
Cell Lines IGR-CaP1 and IGR-CaP1-R cells
Concentrations 25 μM
Incubation Time 72 h
Results "Our results show that the targeting of the TGFβ signaling pathway with LY2157299 in combination with Docetaxel induces cell death of the Docetaxel-resistant cells."
Rating
Source Universite Paris-Sud (2014). Figure 5. LY2157299 (Abmole Bioscience)
Method Clonogenicity assay
Cell Lines IGR-CaP1 and IGR-CaP1-R cells
Concentrations 25 μM
Incubation Time 72 h
Results Figure 5A shows that treatment of cells with 25μM of LY2157299 alone did not affect the survival of parental and resistant cells.
Rating
References

Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase.
Zhou L, et al. Cancer Res. 2011 Feb 1;71(3):955-63. PMID: 21189329.

Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice.
Bueno L, et al. Eur J Cancer. 2008 Jan;44(1):142-50. PMID: 18039567.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY2157299 supplier, TGF-beta, inhibitors

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