LY-2109761(LY2109761)|TGF-β receptor inhibitor|DC Chemicals

Cas No.:	700874-71-1
Chemical Name:	7-(2-morpholinoethoxy)-4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline
Synonyms:	LY 2109761; LY2109761
SMILES:	N12N=C(C(C3=C4C=CC(OCCN5CCOCC5)=CC4=NC=C3)=C1CCC2)C6=NC=CC=C6
Formula:	C₂₆H₂₇N₅O₂
M.Wt:	441.52
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

LY2109761 treatment induces a dose-dependent low-anchorage growth inhibition of L3.6pl/GLT cells, leading to ~33% or 73% inhibition at 2 μM and 20 μM, respectively, which can be strongly enhanced when combined with gemcitabine in combination index value of 0.36581. Blocking TβRI/II kinase activity with LY2109761 (5 μM) completely suppresses both the basal and TGF-β1-stimulated migration and invasion of L3.6pl/GLT cells, significantly enhances the detachment-induced apoptosis by 26% at 8 hours treatment, and completely suppresses TGF-β–induced Smad2 phosphorylation. LY2109761 treatment at 1 nM is sufficient to significantly block the migration and invasion but not adhesion of hepatocellular carcinoma cells by increasing E-cadherin expression. LY2109761 pretreatment enhances radiosensitivity of glioblastoma cells via TGF-β signaling blockage. LY2109761 (10 μM) reduces the self-renewal and proliferation of GBM-derived cancer stem–like cells (CSLC), which can be significantly enhanced when combined with radiation. Administration of LY2109761 (50 mg/kg) alone or in combination with gemcitabine (25 mg/kg) significantly reduces the tumor volume by ~70% and ~90%, respectively, prolongs the survival with the median survival duration of 45.0 days and 77.5 days, respectively, and reduces spontaneous abdominal metastases in the L3.6pl/GLT Xenograft mice model. In consistent with the in vitro effect, administration of LY2109761 alone or in combination with radiation, markedly inhibits tumor growth in the orthotopical CSLC glioblastoma model by 43.4% and 76.3%, respectively, decreases tumor invasion and tumor microvessel density, and significantly enhances radiation-induced tumor growth delay in the U87MG xenograft mice model. For the detailed information of LY-2109761, the solubility of LY-2109761 in water, the solubility of LY-2109761 in DMSO, the solubility of LY-2109761 in PBS buffer, the animal experiment (test) of LY-2109761, the cell expriment (test) of LY-2109761, the in vivo, in vitro and clinical trial test of LY-2109761, the EC50, IC50,and Affinity of LY-2109761, Please contact DC Chemicals.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
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DC41892	pm26TGF-β1 peptide	pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
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DC41013	ALK2-IN-4 succinate	ALK2-IN-4 succinate is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
DC29096	LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)	LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
DC28553	TGFBR1-IN-1	TGFBR1-IN-1 is an ALK5 inhibitor extracted from patent WO2018004290A1, Compound 33, has an IC50 of 10-100 nM.
DC7189	LY-2109761	LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.