LY2157299 Inhibitor CAS No. 700874-72-2

Cat. No.	Name	Size	Price
KI1407	LY2157299	5 mg	$272
	LY2157299	10 mg	$432
	LY2157299	50 mg	$1232
	LY2157299	200 mg	$3632

Chemical Characteristic

Product Name	LY2157299
Synonyms	Galunisertib
CAS No.	700874-72-2
Molecular Weight	369.42
Formula	C₂₂H₁₉N₅O
Chemical Name	4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide
Smiles	n1ccc(c2cc(ccc12)C(=O)N)c1c2n(nc1c1cccc(n1)C)CCC2
Chemical Structure

Biological activities

LY2157299 is a new type I receptor transforming growth factor-β (TGF-β) antagonist with an IC50 of 56 nM.^[1] LY-2157299 effectively inhibits the increased TGF-β signaling due to SMAD7 reduction. LY-2157299 can inhibit TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells. Furthermore, in vivo administration of LY-2157299 ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure. Most importantly, treatment with LY-2157199 stimulates hematopoiesis from primary myelodysplastic syndromes (MDS) bone marrow specimens. ^[2] In vivo, LY-2157299 induces angiogenesis and enhances VEGF and basic-fibroblast-growth-factor-induced angiogenesis in a matrigel-plug assay, whereas adding an α5-integrinneutralizing antibody to the matrigel selectively inhibits this enhanced response. ^[3]

Protocols

In vitro: LY-2157299 is diluted in DMSO as 20 mM of stock solution and kept at -20°C until use. ^[2]

References

[1] Bueno L, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-β kinase antagonist, in mice. Eur J Cancer. 2008, 44(1): 142-150. [2] Zhou L, et al. Reduced SMAD7 leads to overactivation of TGF-β signaling in MDS that can be reversed by a specific inhibitor of TGF-β receptor I kinase. Cancer Res. 2011, 71(3): 955-963. [3] Liu Z, et al. VEGF and inhibitors of TGFβ type-I receptor kinase synergistically promote blood-vessel formation by inducing α5-integrin expression. J Cell Sci. 2009, 122(Pt 18): 3294-3302.

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