ChemicalBook > CAS DataBase List > LY2109761

LY2109761

Description In vitro In vivo

Product Name: LY2109761
CAS No.: 700874-71-1
Chemical Name: LY2109761
Synonyms: CS-101;LY210976;LY2109761;LY2109761, >=98%;LY2109761 USP/EP/BP;LY2109761/LY-2109761;N-CYCLOPENTYL-Β-ALANINE;LY2109761, 10 mM in DMSO;N-CYCLOPENTYL-WEI -ALANINE;LY2109761, 98%, a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor
CBNumber: CB42596729
Molecular Formula: C26H27N5O2
Formula Weight: 441.52
MOL File: 700874-71-1.mol

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LY2109761 Property

Boiling point:: 640.9±55.0 °C(Predicted)
Density: 1.34
storage temp.: Store at -20°C
solubility: ≥22.1 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form: solid
pka: 6.27±0.10(Predicted)
color: White to yellow
InChI: InChI=1S/C26H27N5O2/c1-2-9-27-22(4-1)26-25(24-5-3-11-31(24)29-26)21-8-10-28-23-18-19(6-7-20(21)23)33-17-14-30-12-15-32-16-13-30/h1-2,4,6-10,18H,3,5,11-17H2
InChIKey: IHLVSLOZUHKNMQ-UHFFFAOYSA-N
SMILES: N1C2C(=CC=C(OCCN3CCOCC3)C=2)C(C2C(C3=NC=CC=C3)=NN3CCCC3=2)=CC=1

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Safety

HS Code: 29349990

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2051
Product name: LY2109761
Purity: ≥98% (HPLC)
Packaging: 5 mg
Price: $98.28
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML2051
Product name: LY2109761
Purity: ≥98% (HPLC)
Packaging: 25 mg
Price: $399
Updated: 2025/07/31

Cayman Chemical

Product number: 15409
Product name: LY2109761
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 15409
Product name: LY2109761
Purity: ≥98%
Packaging: 5mg
Price: $99
Updated: 2024/03/01

Cayman Chemical

Product number: 15409
Product name: LY2109761
Purity: ≥98%
Packaging: 10mg
Price: $176
Updated: 2024/03/01

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LY2109761 Chemical Properties,Usage,Production

Description

LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2.

In vitro

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.

In vivo

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.

Description

LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases (IC₅₀ = 69 nM). It has been used to study the role of TGF-β signaling in tumor cell migration and metastasis in pancreatic tumor cell lines where 5 μM of the compound completely disrupts Smad-2 phosphorylation, an immediate downstream target of the kinase activity. It can also suppress radiation-induced inflammatory cytokine signaling and proangiogenic genes, including ID1, in human primary fibrobalsts.

Uses

LY 2109761 is a novel transforming growth factor beta receptor type I and type II dual inhibitor that is potentially used to treat and suppress pancreatic cancer.

Synthesis

110-91-8

700874-75-5

700874-71-1

The general procedure for the synthesis of 4-(2-((4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl)oxy)ethyl)morpholine from morpholine and the compound (CAS: 700874-75-5) is as follows: 2-[4-(2-pyridin-2-yl-5,6-dihydro-4H- pyrrolo[1,2-b]pyrazol-3-yl)-quinolin-7-yloxy]-ethyl (87 mg, 0.19 mmol) was mixed with morpholine (1 mL) and the reaction was heated at 50 °C for 4 hours. Upon completion of the reaction, excess morpholine was removed by vacuum distillation. Subsequently, the product was separated by extraction using a solvent mixture of isopropanol and chloroform (1:3, v/v). The organic layer was washed with aqueous sodium chloride and dried with anhydrous sodium sulfate. Finally, the title compound (83 mg, 100% yield) was obtained in light yellow solid form by vacuum concentration. Mass spectrometry analysis showed MS ES+ m/e 442.0 ([M+1]+).

in vivo

LY2109761 (50 mg/kg, p.o.) greatly reduces the tumor volume and increases the median survival duration of the mice to 45.0 days. The mice treated with LY2109761 develop significantly fewer metastatic lesions and, in some of them, no metastatic lesion, as indicated by the GFP signal, can be identified in the abdomen^[1].
LY2109761 enhances radiation-induced tumor growth delay in a U87MG subcutaneous xenograft tumor model in BALB/c nude mice. LY2109761 increases survival in an orthotopical CSLC glioblastoma model and enhanced antitumor activity of radiation^[2].

References

[1]melisi d, ishiyama s, sclabas gm et al. ly2109761, a novel transforming growth factor beta receptor type i and type ii dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. mol cancer ther 2008; 7: 829-840.
[2]li hy, mcmillen wt, heap cr et al. optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type i receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type i inhibitor as antitumor agent. j med chem 2008; 51: 2302-2306.
[3]xu y, tabe y, jin l et al. tgf-beta receptor kinase inhibitor ly2109761 reverses the anti-apoptotic effects of tgf-beta1 in myelo-monocytic leukaemic cells co-cultured with stromal cells. br j haematol 2008; 142: 192-201.
[4]zhang m, kleber s, rohrich m et al. blockade of tgf-beta signaling by the tgfbetar-i kinase inhibitor ly2109761 enhances radiation response and prolongs survival in glioblastoma. cancer res 2011; 71: 7155-7167.
[5]flechsig p, dadrich m, bickelhaupt s et al. ly2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of tgf-beta and bmp-associated proinflammatory and proangiogenic signals. clin cancer res 2012; 18: 3616-3627.

LY2109761 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from LY2109761 manufacturers

Career Henan Chemical Co

Product: LY2109761 700874-71-1
Price: US $7.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 1000kg
Release date: 2020-01-13

700874-71-1, LY2109761Related Search:

LY 294002 Hydrochloride 1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE LY-404039 LY3143921 LY 2606368 LY 379268 LY-2940094 xav-939 SB 431542 GW788388 SB525334 PLX4032 LY 2157299

LY2109761/LY-2109761

LY2109761

Quinoline, 4-[5,6-dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-Morpholinyl)ethoxy]-

4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]quinoline

LY210976

4-[2-[4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl]oxyethyl]Morpholine

N-CYCLOPENTYL-WEI -ALANINE

N-CYCLOPENTYL-Β-ALANINE

LY2109761, 98%, a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor

7-(2-morpholinoethoxy)-4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline

4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]quinoline LY 2109761

LY2109761, >=98%

4-(2-(4-(2-(Pyridin-2-yl)-3a,4,5,6-tetrahydro-3H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yloxy)e

CS-101

LY2109761 USP/EP/BP

LY2109761, 10 mM in DMSO

700874-71-1

Inhibitors

Smad

TGF-beta