N-CYCLOPENTYL-Β-ALANINE
LY2109761
CAS: 700874-71-1
Molecular Formula: C26H27N5O2
N-CYCLOPENTYL-Β-ALANINE - Names and Identifiers
N-CYCLOPENTYL-Β-ALANINE - Physico-chemical Properties
| Molecular Formula | C26H27N5O2 |
| Molar Mass | 441.52 |
| Density | 1.34 |
| Boling Point | 640.9±55.0 °C(Predicted) |
| Solubility | DMSO 2 mg/mL (4.52 mM);Water <1 mg/mL (<1 mM);Ethanol <1 mg/mL (<1 mM) |
| pKa | 6.27±0.10(Predicted) |
| Storage Condition | -20℃ |
| Use | A small molecule inhibitor of the TGF-β receptor type 1/type II kinases. |
| In vitro study | LY2109761 treatment of FG/GLT or L3.6pl/GLT monolayer cell growth has no anti-proliferation effect, but significantly inhibits the low adherent growth of L3.6pl/GLT cells, and this effect is dose-dependent, at 2 μm and 20 μm, the inhibition was ~ 33% and 73%, respectively, and the combination with Gemcitabine strongly enhanced this effect. LY2109761(5 μm) blocked the activity of tβri/II kinase, completely inhibited the migration and invasion of L3.6pl/GLT cells stimulated by basal type and TGF-β1, and significantly enhanced the apoptosis induced by detachment, after 8 hours of treatment, apoptosis reached 26%, and the phosphorylation of Smad2 induced by TGF-β was completely inhibited. 1 nM LY2109761 significantly blocked migration and invasion by increasing E-cadherin expression without inhibiting adhesion of HCC cells. LY2109761 pretreated glioblastoma cells to enhance radiosensitivity by blocking TGF-β signaling. LY2109761(10 μm) acts on GBM-derived cancer stem-like cells (CSLC), reducing self-renewal and cell proliferation, while combined treatment with radiation can significantly enhance it. |
| In vivo study | LY2109761 (50 mg/kg) alone or in combination with Gemcitabine (25 mg/kg) in the L3.6pl/GLT xenograft mouse model significantly reduced tumor volume, reduced by ~ 70% and ~ 90%, respectively, prolonged life, median survival of 45.0 and 77.5 days, respectively, and reduced spontaneous abdominal metastasis. Consistent with the in vitro effect, LY2109761 alone or in combination with radiation treatment of an in situ CSLC glioblastoma model significantly inhibited tumor growth by 43.4 and 76.3, respectively, reduced tumor invasion and tumor vessel density, and significantly enhanced radiation-induced tumor growth delay in a U87MG xenograft mouse model. |
N-CYCLOPENTYL-Β-ALANINE - Risk and Safety
| HS Code | 29349990 |
N-CYCLOPENTYL-Β-ALANINE - Introduction
LY2109761 is a novel, selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively, which negatively affects the phosphorylation of Smad2.
Last Update：2022-10-16 17:41:46
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Product Name: LY2109761 Visit Supplier Webpage Request for quotationCAS: 700874-71-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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