LY2157299 | CAS#700874-72-2 | MedKoo Biosciences

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MedKoo product information:

LY2157299

LY2157299 is a novel selective small molecule transforming growth factor beta receptor (TGF-βR) kinase inhibitor.

Current developer: Eli Lilly.

MedKoo Code#: 205520
Name: LY2157299
CAS#: 700874-72-2 Synonym: LY-2157299; LY2157299; 6-Quinolinecarboxamide, 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]- 　 IUPAC/Chemical name: 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide
Chemical structure	Theoretical analysis
	MedKoo Code#: 205520 Name: LY2157299 CAS#: 700874-72-2 Chemical Formula: C22H19N5O Exact Mass: 369.15896 Molecular Weight: 369.41916 Elemental Analysis: C, 71.53; H, 5.18; N, 18.96; O, 4.33
Availability and price: LY2157299 is in stock. 10 mg / $280.00 20 mg / $450.00 50 mg / $750.00 100 mg / $1,250.00 Multiple grams available at low prices. To inquire quotation and lead time or to ask questions, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

Information about this agent

LY2157299 is a novel selective small molecule transforming growth factor beta receptor (TGF-βR) kinase inhibitor. LY-2157299 could inhibit TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells. Furthermore, in vivo administration of LY-2157299 ameliorated anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure. Most importantly, treatment with LY-2157199 stimulated hematopoiesis from primary MDS bone marrow specimens. These studies demonstrate that reduction in SMAD7 is a novel molecular alteration in MDS that leads to ineffective hematopoiesis by activating of TGF-β signaling in hematopoietic cells. These studies also illustrate the therapeutic potential of TBRI inhibitors in MDS. (source: Cancer Res. 2011 Feb 1;71(3):955-63. Epub 2010 Dec 28.).

References

1: Bhattachar SN, Perkins EJ, Tan JS, Burns LJ. Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus,™ simulations to predict absorption. J Pharm Sci. 2011 Nov;100(11):4756-65. doi: 10.1002/jps.22669. Epub 2011 Jun 16. PubMed PMID: 21681753.

2: Bueno L, de Alwis DP, Pitou C, Yingling J, Lahn M, Glatt S, Trocóniz IF. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44(1):142-50. Epub 2007 Nov 26. PubMed PMID: 18039567.

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