Structure of LY2109761
CAS No.: 700874-71-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
LY2109761 demonstrates oral activity and selectivity as an inhibitor of TGF-β receptor type I/II, with Kis of 38 nM and 300 nM, respectively.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 700874-71-1 |
Formula : | C26H27N5O2 |
M.W : | 441.52 |
SMILES Code : | N1(CCOC2=CC=C3C(C4=C(CCC5)N5N=C4C6=NC=CC=C6)=CC=NC3=C2)CCOCC1 |
MDL No. : | MFCD12923354 |
InChI Key : | IHLVSLOZUHKNMQ-UHFFFAOYSA-N |
Pubchem ID : | 11655119 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
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In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Esophageal squamous cell carcinoma cells | 20 μM | 24 h | LY2109761 reduced DJ-1-induced metastasis of bystander ESCC cells | PMC9413943 |
U251 cells | 2 mg/ml | 24 h and 48 h | Inhibition of TGFβ pathway, weakening the interaction between RUNX1 and p-SMAD3/SUV39H1 | PMC6872557 |
N9 cells | 2 mg/ml | 24 h and 48 h | Inhibition of TGFβ pathway, weakening the interaction between RUNX1 and p-SMAD3/SUV39H1 | PMC6872557 |
CT26 cells | 10 μM | 25 h | LY2109761 inhibits TGF-β-mediated cell migration, invasion, and tumorigenicity | PMC2776056 |
CT26-Luc cells | 10 μM | 5 days | LY2109761 inhibits TGF-β-mediated cell migration, invasion, and tumorigenicity | PMC2776056 |
A549 cells | 2μM | 72 h | To evaluate the effect of LY2109761 on TGF-β or S1P-induced epithelial-mesenchymal transition (EMT). The results showed that LY2109761 reversed the morphological changes induced by TGF-β or S1P, inhibited the up-regulation of the mesenchymal marker CD90 and the down-regulation of the epithelial marker CD326. | PMC9306821 |
MC38 cells | 5 μM | 5 days | LY2109761 inhibited TGF-β-induced proliferation, migration, and invasion of MC38 cells. | PMC2831103 |
SW620 cells | 5 μM | 5 days | LY2109761 inhibited TGF-β-induced migration and invasion of SW620 cells. | PMC2831103 |
PANC-1 cells | 5 μM | 72 h | To evaluate the cytotoxicity of LY2109761 on PANC-1 cells, results showed that LY2109761 did not exhibit significant cytotoxicity at low concentrations, with only minor toxicity observed at 50 μM. | PMC7372733 |
Pancreatic stellate cells (PSCs) | 5 μM | 48 h | To evaluate the inhibitory effect of LY2109761 on type I collagen expression in pancreatic stellate cells (PSCs), results showed that LY2109761 significantly reduced type I collagen expression. | PMC7372733 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Nude mice | Pulmonary metastasis model | Intraperitoneal injection | 50 mg/kg | Once a week for 6 weeks | LY2109761 significantly suppressed the invasion of K150 cells and alleviated pulmonary metastasis | PMC9413943 |
Mice | PVR mouse model | Intraperitoneal injection | 10 mg/kg | Consecutive 14 days | To investigate the inhibitory effect of LY2109761 on fibrosis induced by FXa in PVR mouse model, results showed LY2109761 significantly alleviated FXa-induced fibrosis. | PMC8300057 |
Nude mice | Patient-derived xenograft (PDX) model | Tail vein injection | 50 mg/kg | Once every other day for 15 days | Inhibition of TGFβ pathway, reducing tumor growth and invasion | PMC6872557 |
Balb/c mice | Balb/c nude mice | Oral | 50 mg/kg | Twice daily for 23 days | LY2109761 reduces liver metastasis and prolongs survival | PMC2776056 |
BALB/c mice | Asthma-like disease model | Subcutaneous injection | 50 mg/kg | Single dose 15 minutes before | To evaluate the effect of LY2109761 on S1P-induced asthma-like features. The results showed that LY2109761 inhibited S1P-induced airway hyperresponsiveness (AHR), mucus hyperproduction, and pulmonary fibrosis, and reversed S1P-induced CD90 up-regulation and CD326 down-regulation. | PMC9306821 |
C57BL/6 mice | Colorectal cancer liver metastasis model | Oral | 50 mg/kg | Twice daily for 28 days | LY2109761 significantly inhibited the metastasis of colorectal cancer cells to the liver and prolonged the survival of mice. | PMC2831103 |
Mice | miR-424(322)/503 double-knockout mice | Oral | 50 mg/kg | Twice daily for 24 hours | To inhibit TGF-β signaling and observe its effect on mammary gland involution. Results showed that LY2109761 treatment inhibited involution, maintaining the structure of secretory acini and increasing epithelial density. | PMC4015488 |
Nude mice | Orthotopic pancreatic cancer model | Intravenous injection | 13.2 mg/kg | Every 5 days for a total of 6 injections | To evaluate the antitumor efficacy of LY2109761 in an orthotopic pancreatic cancer model, results showed that LY2109761 significantly inhibited tumor growth and reduced collagen expression and activation of PSCs in the tumor. | PMC7372733 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.32mL 2.26mL 1.13mL |
22.65mL 4.53mL 2.26mL |
Tags: LY2109761 | LY 2109761 | LY-2109761 | TGF-β Receptor | Autophagy | TGF-β receptor type 1 | SMAD signaling | Transforming growth factor beta receptors | fibrotic diseases | 700874-71-1
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