| Target |
IC50: 29 nM (Glutaminase C)[1] Kd: 27 nM (Glutaminase C)[1]
|
|---|
| In Vitro |
UPGL00004 inhibits MDA-MB-231, HS578T and TSE cells with IC50s of 70, 129, and 262 nM, respectively[1].
|
| In Vivo |
The combination of UPGL00004 (1 mg/kg body weight) and Bevacizumab
(2.5 mg/kg body weight) via intraperitoneal injection completely
prevent any detectable increase in tumor size in a triple-negative
breast cancer patient-derived tumor graft model[1].
|
| References |
[1]. Characterization of the interactions of potent allosteric
inhibitors with glutaminase C, a key enzyme in cancer cell glutamine
metabolism. J Biol Chem. 2018 Mar 9;293(10):3535-3545 |
