Terevalefim

Names

[ CAS No. ]:
1070881-42-3

[ Name ]:
Terevalefim

[Synonym ]:
Pyrazolidine, 3-[(E)-2-(2-thienyl)ethenyl]-
3-[(E)-2-(2-Thienyl)vinyl]pyrazolidine

Biological Activity

[Description]:

Terevalefim (ANG-3777), an hepatocyte growth factor (HGF) mimetic, selectively activates the c-Met receptor[1][2].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

[In Vitro]

Terevalefim (ANG-3777) (0-10 μM) significantly inhibited cancer cells proliferation in HUVECs[2]. Cell Viability Assay[2] Cell Line: Human Umbilical Vein Epithelial Cells (HUVECs). Concentration: 0.44, 1.78, and 7.1 μM. Incubation Time: 24 to 48 hours. Result: Dose-dependently inhibited cell proliferation.

[In Vivo]

Terevalefim (ANG-3777) decreases apoptosis, increases proliferation, and promotes organ repair and function in animal models[1]. Terevalefim (ANG-3777, 40 mg/kg, IP) phosphorylates the c-Met receptor in rats[2]. Animal Model: SD rats[2]. Dosage: 40 mg/kg. Administration: IP injection, once. Result: Selectively phosphorylated the c-Met receptor and not other growth factor receptors.

[References]

[1]. Jonathan S Bromberg, et al. Renal Function Improvement Following ANG-3777 Treatment in Patients at High Risk for Delayed Graft Function After Kidney Transplantation. Transplantation. 2021 Feb 1;105(2):443-450.

[2]. Latha Paka, et al. The Effect of ANG-3777 on Hepatocyte Growth Factor Receptor, c-MET Signaling. American Transplant Society.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
288.0±29.0 °C at 760 mmHg

[ Molecular Formula ]:
C₉H₈N₂S

[ Molecular Weight ]:
176.24

[ Flash Point ]:
128.0±24.3 °C

[ Exact Mass ]:
180.072113

[ LogP ]:
1.31

[ Vapour Pressure ]:
0.0±0.6 mmHg at 25°C

[ Index of Refraction ]:
1.681

Related Compounds

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