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Technical Data
| Formula | C26H27N5O2 |
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| Molecular Weight | 441.52 | CAS No. | 700874-71-1 | |
| Solubility (25°C)* | In vitro | DMSO | 9 mg/mL (20.38 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| 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. LY2109761 blocks autophagy and induces apoptosis. | ||||
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| 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 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. [1] 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. [2] 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. [3] |
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| In vivo | Administration of LY2109761 (50 mg/kg) alone or in combination 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. [1] 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. [3] |
Protocol (from reference)
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References
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Customer Product Validation
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Data from [Data independently produced by Invest Ophthalmol Vis Sci, 2014, 55(3), 1770-9]
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Data from [Data independently produced by Toxicology, 2014, 326C, 9-17]
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Data from [PLoS One, 2013, 8(12), e83521]
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Data from [Data independently produced by , , Mol Cell Proteomics, 2016, 15(3):1017-31]
Selleck's LY2109761 has been cited by 135 publications
| PALB2-mutated human mammary cells display a broad spectrum of morphological and functional abnormalities induced by increased TGFβ signaling [ Cell Mol Life Sci, 2024, 81(1):173] | PubMed: 38597967 |
| PALB2-mutated human mammary cells display a broad spectrum of morphological and functional abnormalities induced by increased TGFβ signaling [ Cell Mol Life Sci, 2024, 81(1):173] | PubMed: 38597967 |
| Serum-Induced Proliferation of Human Cardiac Stem Cells Is Modulated via TGFβRI/II and SMAD2/3 [ Int J Mol Sci, 2024, 25(2)959] | PubMed: 38256034 |
| Oxyberberine sensitizes liver cancer cells to sorafenib via inhibiting NOTCH1-USP7-c-Myc pathway [ Hepatol Commun, 2024, 8(4)e0405] | PubMed: 38573832 |
| Connexin 43 controls metastatic behavior in triple negative breast cancer through TGFβ1-Smad3-intergin αV signaling axis Based on optical image diagnosis [ SLAS Technol, 2024, 29(5):100190] | PubMed: 39299505 |
| TGF-β signaling promotes cervical cancer metastasis via CDR1as [ Mol Cancer, 2023, 22(1):66] | PubMed: 37004067 |
| Bromodomain-containing protein 4 activates androgen receptor transcription and promotes ovarian fibrosis in PCOS [ Cell Rep, 2023, 42(9):113090] | PubMed: 37669164 |
| Investigating the Role of TGF-β Signaling Pathways in Human Corneal Endothelial Cell Primary Culture [ Cells, 2023, 12(12)1624] | PubMed: 37371094 |
| FUT1-mediated terminal fucosylation acts as a new target to attenuate renal fibrosis [ Mol Med, 2023, 29(1):55] | PubMed: 37085770 |
| FUT1-mediated terminal fucosylation acts as a new target to attenuate renal fibrosis [ Mol Med, 2023, 29(1):55] | PubMed: 37085770 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.