LY2157299 --- TGFŒ≤ Inhibitor

Overview
Catalog #	bs-60064c-5mg-solid
Product Name	LY2157299 --- TGFŒ≤ Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 369.42 Formula: C22 H19 N5 O CAS Number: 700874-72-2 InChi Key: IVRXNBXKWIJUQB-UHFFFAOYSA-N InChi: InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28) Smiles: CC1=CC=CC(=N1)C1=NN2CCCC2=C1C1=CC=NC2=CC=C(C=C12)C(N)=O Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	LY2157299 is a novel potent and selective TGFβ receptor type I and type II (TβRI/II) inhibitor with IC50 of 86 nM and 2 nM, respectively. LY2157299 could inhibit the TGFβ induced Smad2 phosphorylation in HUVEC cells, promote VEGF induced HUVEC cell migration, and show dose dependent potentiation of VEGF or bFGF induced cell proliferation. It can also inhibit TGFβ–mediated Smad2 activation and hematopoietic suppression in primary hematopoietic stem cells in a dose-dependent manner. LY2157199 treatment stimulates hematopoiesis from primary MDS bone marrow specimens. In vivo administration of LY-2157299 ameliorated anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure. Oral administration of LY2157299 at 75 mg/kg/day displays significant antitumor activity against both Calu6 and MX1 xenografts in mice. LY2157299 in combination with lomustine (CCNU) more effectively blocks Smad phosphorylation than either agent alone, and significantly enhances the efficacy of lomustine in U87MG and CRL-2611 human glioblastoma xenografts. Currently LY2157299 is in phase I/II clinical trials for the treatment of glioma, HCC, and pancreatic cancer.