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LY2157299 (Galunisertib)

Cat. No. M1980
LY2157299 (Galunisertib) Structure
Synonym:

Galunisertib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 23  USD23 In stock
5mg USD 38  USD38 In stock
10mg USD 50  USD50 In stock
25mg USD 90  USD90 In stock
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Quality Control & Documentation
Biological Activity

LY2157299 (Galunisertib) 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.

Product Citations
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."
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.
Protocol (for reference only)
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 
Chemical Information
Molecular Weight 369.42
Formula C22H19N5O
CAS Number 700874-72-2
Solubility (25°C) DMSO 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Zhou L, et al. Cancer Res. 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.

[2] Bueno L, et al. Eur J Cancer. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice.

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Keywords: LY2157299 (Galunisertib), Galunisertib supplier, TGF-β Receptor, inhibitors, activators


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